BRPI0921830B1 - "COMPOSITIONS FOR ORAL TREATMENT UNDERSTANDING FOAMED SILICA OF THE BALL". - Google Patents

Description

Report of the Invention Patent for "COMPOSITIONS FOR ORAL TREATMENT UNDERSTANDING SPHERIC FUSED SILICA".

FIELD OF THE INVENTION The present invention relates to buccal treatment compositions. comprising fused silica, with at least 25% of fused silica particles being spherical.

BACKGROUND OF THE INVENTION

An effective oral composition can maintain and preserve the appearance of teeth by removing dental stains and polishing teeth. It can also clean and remove external debris, which can help in preventing tooth decay and promoting gengi-goes health.

Abrasives in buccal compositions assist in the removal of the tightly adhering biological film to which the dental stains are attached. Generally, the biological film comprises an acellular glycoprotein-mucoprotein coating which adheres to enamel within minutes of teeth cleaning. The presence of various food pigments housed in the biological film is responsible for most instances of tooth staining. An abrasive can remove biological film with minimal abrasive damage to oral tissues such as dentin and enamel.

In addition to cleaning, it may be desirable for abrasive systems to provide polishing of dental surfaces, as polished surfaces may be more resistant to ectopic deposition of undesirable components. The appearance of the teeth can be optimized by giving them a polished feature, since surface roughness, ie, their degree of polish, affects the refiectance and light scattering, which is integrally related to the visual appearance of the teeth. . Surface roughness also affects the tactile feel of the tooth. For example, polished teeth have a clean, smooth and slippery tactile feel.

Numerous toothpaste compositions use precipitated silicas as abrasives. Precipitated silicas are observed, and described in US Patent No. 4,340,583 of July 20, 1982, issued to Wason, in EP Patent No. 535,943A1 of April 7, 1993, issued to McKeown et al., In PCT application WO 92/02454 of February 20, 1992, issued to McKeown et al., In US Patent Nos. 5,603,920 of February 18, 1997 and US Patent R $ 5,716,601 of February 1: 1998, both issued Rice, and US Patent No. 6,740,311 to May 25, 2004, issued to. White et al.

There is a need for an abrasive system that has good active compatibility for oral care and important dentifrice components while providing safe and effective cleaning and polishing of dental tissue. In addition, there is a continuing need for abrasives that can produce higher levels of. cleaning, and polishing a. reduced costs. The fused silicas of the present invention may provide one or more of these advantages. Fused silicas in which the particles are spherical may particularly provide these advantages. Accordingly, the present invention relates to oral care compositions comprising fused silica, with at least about 25% of the fused silica particles being spherical.

SUMMARY OF THE INVENTION The present invention relates to oral care compositions comprising fused silica, with at least about 25% of the fused silica particles being spherical.

BRIEF DESCRIPTION OF THE DRAWINGS Figure 1. is a table of material properties of various fused silicas, e.g. precipitated. Figure 2 is a compatibility data table for fused and precipitated silicas. Figure 3 (a) is a table of sodium fluoride-based formulations for use in oral care compositions. Figure 3 (b) is a table of PCR and RDA values for the compositions of figure 3 (a). Figure 4 (a) is a table of stannous straight fluid based formulas for use in buccal treatment compositions. Figure 4 (b) is. a table of PCR and RDA values for the compositions of figure 4 (a). Figure 5 is a table of the cleaning and abrasion capabilities of fused silica.

Figures 6 (a) to 6 (i) are SEM (scanning electron microscopy) micrographs of the precipitated, fused silica images. Figure 7 (a) is a formula table of the composition. Figure 7 (b) is a tin, zinc and fluorine compatibility chart for the compositions of figure 7 (a). Figure 8 is a tin compatibility chart as a function of silica filler. The figure. 9 (a) is a table of formula compositions comprising fused and precipitated silica peroxide.

Figure 9 (b) is a peroxide compatibility table for the compositions of Figure 9 (a). Figure 10 (a) is a table of compositions of formulas comprising fused silica. Fig. 10 (b) is a cleaning and bleaching performance table for the compositions of Fig. 10 (a). Figure 11 (a) is a table of formula compositions containing fused and precipitated silicas. Figure 1 t (b) is a table of data on consumer perception of the compositions of Figure 11 (a). Figure 12 is a table of examples of additional formulas. Figure 13 (a) is a table of example formulas. Figure 13 (b) is a table of PCR and RDA values for the sodium fluoride-based compositions of Figure 13 (a). The figure. 1.3 (c) is a table of formula examples. Figure 13 (d) is a table of RDA values for. the compositions based on. stannous fluoride of. Figure 13 (c).

DETAILED DESCRIPTION OF THE INVENTION

While the disclosure report ends with claims that particularly point to and distinctly claim the invention, it is believed that it will be better understood from the following description. Definitions For use in the present invention, the term "buccal acceptable carrier" means a suitable carrier or ingredient which may be used to safely and effectively form, apply and / or apply present compositions to the buccal cavity. Such a carrier may include materials such as fluoride ion sources, bactericidal agents, anti-calculating agents, buffers, other abrasive materials, peroxide sources, alkali metal bicarbonate salts, materials, thickeners, humectants, water, surfactants, titanium dioxide, system flavors, sweetening agents, cooling agents, xylitol, coloring agents, other suitable materials and mixtures thereof.

For use in the present invention, the term "comprising" means that steps and ingredients may be added in addition to those specifically mentioned. This term encompasses the terms "consisting of" and "consisting essentially of". The compositions of the present invention may comprise, consist of, and consist essentially of, essential elements and limitations of the invention described herein, as well as any of the additional or optional ingredients, components, steps or limitations described herein.

For use in the present invention, the term "effective amount" means one. amount of a compound or composition that is sufficient to induce a positive benefit, an oral health benefit, and / or an amount low enough to avoid serious side effects, i.e. to provide an adequate benefit / risk ratio, within the good judgment of one skilled in the art.

For use in the present invention, the term "buccal composition" means a product which, in its normal course of use, is retained in the buccal cavity for a time sufficient to come into contact with some or all dental surfaces and / or buccal tissues. , for purposes of. buccal activity. The buccal composition of the present invention may be in various forms, including toothpaste, toothpaste, dental gel, dental powders, tablets, rinses, subgingival gel, foam, mousse, chewing gum, lipstick, sponge, dental floss, prophylactic paste, petrolatum gel or denture product. The buccal composition may also be incorporated into tapes or films for application or direct attachment to buccal surfaces, or may be incorporated into the dental floss.

For use in the present invention, the term "dentifrice" means formulations in the form of paste, gel, powder, tablets or liquids, unless otherwise specified, which are used to clean oral cavity surfaces.

For use in the present invention, the term "teeth" refers to both .a. natural teeth such as artificial teeth or dental prostheses.

For use in the present invention, the term "polymer" encompasses both materials produced by polymerization of one type of monomer and those produced from two (i.e. copolymers) or more types of monomers.

For use in the present invention, the term "water soluble" means that the material is water soluble in the present composition. In general, the material needs to be soluble a. 25 * 0, to one. 0.1% by weight concentration of the water solvent, preferably 1%, more preferably a. 5% and more preferably 15% by weight.

For use in the present invention, the term "phase" means a homogeneous and mechanically separated part of a heterogeneous system.

For use in the present invention, the term "substantially unhydrated" means that the material has a low number of surface hydroxyl groups or is substantially free of surface hydroxyl groups. This may also mean that the material contains less than about 0.5% of total water (free or / and bound). For use in the present invention, the term "majority" means the largest or most or more than half of the total.

For use in the present invention, the term "mean number" means the mean value in a distribution above and below which there is an equal number of values.

All percentages, parts and ratios are based on the total weight of the compositions of the present invention, except where otherwise indicated. All such weights, as they relate to ingredients listed herein, are based on the active content and therefore do not include solvents or by-products that may be included in commercially available materials unless otherwise indicated. The term "weight percent" may be referred to as "weight percent" in this document.

All molecular weights for use in the present invention are weight average molecular weights expressed in grams / mol, except where indicated in. contrary. Fused Silica Fused silica is a high purity amorphous silicon dioxide. Sometimes it is called fused quartz, vitreous silica, silica glass or quartz glass. Molten silica is a type of glass, which, as is typical of glass, has no far-reaching order in its atomic structure. The optical and thermal properties of fused silica, however, are unique to those of other glass since fused silica typically has more resistance, thermal stability and transparency to ultraviolet. For these reasons, fused silica is known to be used in situations such as semiconductor manufacturing and laboratory equipment. The present invention uses fused silica in bueal compositions, particularly in dentifrice compositions. Although many current dentifrice compositions use silica as a thickening agent and as an abrasive, the typically used silicas are precipitated silicas. Precipitated silicas are produced by an aqueous precipitation or drying process. Fused silica, by contrast, is typically produced by melting high purity silica sand at very high temperatures of about 2,000 ° C. Figure 1 is a table of material properties of various types of fused silica. For comparison, the same physical properties are also shown for some precipitated silicas. Some of the important material properties that distinguish fused silica from precipitated silica are shown, including BET surface area, drying loss, ignition loss, silanol density, bulk density, compaction density, oil absorption and particle size distribution. Each of these material properties is discussed in more detail below. Heating the silica to such high temperatures destroys the porosity and surface functionality of the silica. This produces a silica that is extremely hard and inert to most substances. The fusion process also results in a low BET surface area smaller than that of the precipitated silica. The BET surface area of the fused silica is in the range from about 1 m2 / g to about 50 m2 / g, from about 2 m2 / g to about 20 m2 / g, from about 2 m2 / g to about 9 m2 / g. g, and from about 2 m2 / g to about 5 m2 / g. In comparison, precipitated silicas typically have a BET surface area in the range of 30 m 2 / g to 80 m 2 / g. BET surface area is determined by the BET nitrogen absorption method of Brunaur et al., J, Am. Chem. Soc 60, 309 (1938). See also US Patent No. 7,255,852, issued August 14, 2007 to Gallis. Molten silica typically has, relative to other types of silica, a low amount of free and / or bound water. The amount of bound and free water in the fused silica is typically less than about 10%. The amount of bound and free water in the fused silica may be less than about 5%, or less than about 3%. Silicas with less than about 5% free bound water may be considered substantially unhydrated. Total free and bound water can be calculated by the sum of two measurements; loss on drying (LOD) and loss on ignition (LGI). For the first loss on drying, a sample may be dried at 105 ° C for two hours, the weight loss being free water. For the ignition loss, the dried sample may then be heated for one hour at 1,00 ° C, the weight loss corresponding to the bound water. The sum of LOD and LOI represents the total free bound water present in the original sample. For example, following the test method described, fused silica (Teco-Sil 44CSS) has a drying loss of 0.1% and a loss of ignition of 2.2% for a sum of 2.3% of water in total. In comparison, a typical precipitated silica, Z-119, has a drying loss of 6.1% and an ignition loss of 5.1% for a total of 11.2% of water. (For another test method, see United States Pharmacopoeia - National Form, or USP-NF), General Chapter 731, "Loss on Drying", and USP-NF, General Chapter 733 , "Loss on Ignition".) Relative to precipitated silica, fused silica has a low number of surface hydroxy groups or silanol. Surface hydroxy group counts can be found using nuclear magnetic resonance spectroscopy (NMR) to measure the silanol density of a specific silica. Silanols are compounds that contain silicon atoms to which hydroxy substituents directly bond. When NMR solids analysis is performed on multiple silicas, the silicon signal is enhanced by energy transfer from neighboring protons. The amount of signal intensification depends on the proximity of the silicon atom to the protons found on or near the hydroxy groups. Accordingly, silanol density, established as the normalized silanol signal strength (intensity / g), is a measure of surface hydroxy concentration. The density of silanol for fused silicas may be less than 3,000 intensity / g, in some embodiments less than 2,000 intensity / g and generally less than about 900 intensity / g. Fused silicas may contain an intensity / g of from about 10 to about 800 and typically from about 300 to about 700. For example, a sample of fused silica (Teco-Sil 44CSS) has a silanol density of 574 intensity. / g. A typical precipitated silica has a maximum measurement of 3,000 intensity / g and typically above 3,500 intensity / g. For example, silica Z-119 available from Huber measures 3716 intensity / g. The test method for silanol density used cross-polarized solid state NMR with rotation around the magic angle (5 kHz), high power controlled proton decoupling and Varian llníty Plus-200 spectrophotometer with a channel probe. supersonic 7 mm double, available from Doty Sdentífic. Relaxation delay was 4 seconds and contact time was 3 ms. The number of scans was between 8,000 and 14,000, and the experimental time interval was 10 to 14 hours per sample. Samples were weighed to within 0.1 mg for the normalization procedure. The spectra were plotted in. absolute intensity mode and integrals were obtained in absolute intensity mode. The density of silanol is measured by delineating and integrating the spectra in absolute intensity mode. The surface reactivity of silica, a reflection of the relative number of hydroxyls on the surface, can be measured by the ability of silica to absorb methyl red from a solution. This measures the relative number of sianols. The test is based on the fact that methyl red will be selectively absorbed at the reactive silanol sites on a silica surface. In some embodiments, upon exposure to fused silica the methyl red solution may have a higher absorbance than that of a solution exposed to a typical precipitated silica. This is because fused silica does not react as much with methyl red solution as precipitated silica. Typically, the fused silica will have an absorbance to the methyl red solution that is 10% higher than that of a conventional precipitated silica, since the precipitated silica reacts more readily with the methyl red solution. Absorbance can be measured at 470 nm. Ten grams of 0.001% methyl red in benzene is added to 0.1 gram of each of the two silica samples, and mixed for five minutes on a magnetic stirrer. The resulting fluid pastes are centrifuged for five minutes at 12,000 rpm and then the percent transmission at 470 nm for each sample is determined and averaged. See "Improving the Cationic Compatibility of Abrasive Silica Through the Use of Topochemical Reactions" by Gary Kelm, November 1, 1974, in Iter, Ralph K., The Golloid Chemistry of Silica and Silicates, Gomeli University Press, Ithaca, NY, USA , 1955.

Without sticking to the theory, fused silica, with its low specific surface area BET, low porosity and low number of surface hydroxyl groups, is believed to be less reactive than precipitated silica. As a result, fused silica may absorb less of other components, such as flavorings, actives or cations, leading to better availability of these other components. For example, dentifrices incorporating fused silica have superior stability and bioavailability for tin, fluorine, zinc, other cationic bactericides and hydrogen peroxide. Molten silica formulated in a dentifrice composition can result in at least about 50%, 60%, 70%, 80% or 90% compatibility with cations or other components. In some embodiments, cation may be stannous.

Figure 2 shows the stannous and fluoride compatibility of various types of fused and precipitated silicas. Stannous and fluoride compatibility was determined by adding 15% silica in a sorbitol / water mixture containing 0.6% sodium glyconate and 0.454% stannous fluoride, and mixing well. Each sample of silica slurry was then stored at 40 ° C for 14 days and then analyzed for the presence of tin and fluorine. A measure of the concentration of soluble tin and zinc under normal tooth brushing conditions may be as follows. Prepare a slurry at a ratio of 3: 1 between water and dentifrice (silica), and centrifuge it to isolate a clear layer of supernatant. Dilute the supernatant in acidic solution (nitric or hydrochloric acid) and analyze by inductively coupled plasma optical emission spectrometry. The compatibility percentage is calculated by subtracting from the initial values the result of the analysis. A measure of the concentration of soluble tin and fluorine under normal tooth brushing conditions can be as follows: Prepare a slurry at a ratio of 3: 1 between water and dentifrice (silica), and centrifuge it to isolate a layer. transparent.of supernatant. The supernatant is analyzed for the presence of fluoride by means of a fluorine electrode (after mixing at a 1: 1 ratio with a TISAB buffer) or by dilution with a hydroxide solution followed by tonic chromatography analysis. .with conductivity detection. The compatibility percentage is calculated by subtracting the initial values, the result of the analysis. In general, the compatibility between cations can be determined by the "Percent PCC Compatibility Test" disclosed in US Patent No. 7,255,852.

There are several other characteristic differences between fused silica and precipitated silica in addition to the compatibility and concentration of surface hydroxyls. For example, fused silica is denser and less porous. The apparent density of fused silica is typically greater than 0.45 g / mL, and may be from about 0.45 g / mL to about 0.80 g / mL, while the apparent density of precipitated silicas is at most about 0.40 g / mL. The compaction density of fused silica is typically greater than 0.6 g / mL, and may be from about 0.8 g / mL to about 1.30 g / mL, while the compaction density of precipitated silicas is maximum 0.55 g / mL. Bulk density and compaction density can be measured by following the methods discussed in USP-NF, General Chapter 616, Bulk Density and Tapped Density. For bulk density, method 1, "Measuring in a graduated cylinder" may be used, and for bulk density, method 2 may be used. a mechanical compactor. Bulk density and compacted density represent the particle mass to volume ratios (multiple particles confined in a given space), and reflect the captured air, the porosity. and the manner in which the particles fit together into a given space. The true or intrinsic density of a particle (mass to volume ratio of a single particle) to fused silica is about 2.1 g / cm3 to 2.2 g / cm3, while true or intrinsic density of the precipitated silicas is at most about 2.0 g / cm3. Similarly, the specific gravity of the fused silica can be from about 2.1 to 2.2, while the specific gravity of the precipitated silicas can be at most about 2.0. The difference in densities can have a significant effect during the manufacture of a dentifrice, for example where the higher density of the fused silica reduces or removes the deaeration processing step it may. result in shorter cycle times per batch. The fused silica has comparatively low absorption. water and oil, measurements that correlate well with the specific surface area BET. The absorption of water to the fused silica, which means the amount of water it can absorb while maintaining a powder consistency, is less than about 80 g / 100 g, optionally less than about 7.0 g / 100 g. , 6.0 g / 100 g, or about 50 g / 100 g. Water absorption for molten silica may be even lower, in the range of less than about 40 g / 100 g, optionally less than about 30 g / 100 g, and may be about 2 g / 100 g and about 30 g. g / 100 g. For precipitated silicas, water absorption is typically about 90 g / 100 g. Water absorption is measured using the standard J.M Huber Corp. evaluation method (S.E.M No. 5,140, August 10, 2004). Oil absorption by the fused silica is less than about 75 ml dibutyl phthalate / 100 g fused silica, and may be less than about 60 ml dibutyl phthalate / 100 g fused silica. Oil absorption may range from about 10 mL dibutyl phthalate / 100 g fused silica to about 50 mL dibutyl phthalate / 100 g fused silica, and may be desirable to be about 15 mL. dibutyl phthalate / 100 g silica. melted to about 45 mL of dibutyl phthalate / 100 g of. fused silica. For precipitated silicas, the oil absorption is typically about 100 ml of dibutyl phthalate / 100 g of precipitated silica. (Oil absorption is measured according to the method described in US Patent Application 2007 / 0001037A1, published January 4, 2007.

Due to this relatively low water absorption, the fused silica can be made into a slurry during processing, basically allowing for faster processing and faster batch times. In general, the creation of a precipitated silica slurry would typically require at least about 50% water. Accordingly, it would not be practical to use a precipitated silica slurry in the manufacture of buccal compositions. However, because the fused silica is inert, or the lack of porosity of the fused silica, which is reflected in its relatively low absorption of water, silica slurries can be made. water in which water comprises less than about 30% in some embodiments or less than 40% in some embodiments. Some embodiments may consist of a method for manufacturing. an. buccal treatment composition comprising the addition of a molten silica slurry. In some embodiments, the molten silica slurry comprises a binder. This can help keep molten silica suspended in the slurry, especially if there is a lot of water. This may also allow the binder to take longer to hydrate. In some embodiments, the binder is selected from the group consisting of carboxyvinyl, carrageenan, hydroxy ethyl cellulose polymers, water soluble salts of cellulose ethers such as sodium carboxy methyl cellulose, cross-linked carboxy methyl cellulose, sodium hydroxy ethyl cellulose, cross-linked starch , natural gums such as caraia gum, xanthan gum, arabic gum and tragacanth gum, aluminum magnesium silicate, silica, alkylated polyacrylates, alkylated cross-linked polyacrylates and mixtures thereof. The molten silica slurry may be premixed. In some embodiments, the molten silica slurry may be flowable or pumpable. In some embodiments, the molten silica slurry may further contain a preservative, such as benzoic acid, sodium benzoate, sorbic acid or parabens, at a content of less than about 1%. Fused silica typically has much less conductivity than precipitated silica. Conductivity is an indirect measure of dissolved electrolytes, and precipitated silica cannot be made without. produce soluble electrolytes. Thus, although precipitated silica is in the range of about 900 to 1,600 microsiemens / cm (based on a 5% dispersion in deionized water), the fused silica measures less than about 10 microsiemens / cm (measurements made using Orion 3 Star Benchtop conductivity meter available from Thermo Electron Corporation). The pH of the fused silica may be in the range of from about 5 to about 8, while the pH of the precipitated silicas is typically in the range of from about 7 to about 8. The pH is determined according to the application. US 2007 / 0001037A1, published January 4, 2007. The refractive index, a measure of light transmission, is typically higher for fused silica than for precipitated silica. Put in one. The sorbitol / water mixture, the fused silica has a refractive index of at least about 1.45, while the precipitated silicas have measurements from 1.44 to 1.448. A higher refractive index may allow for easier production of transparent gels. The refractive index is determined using the method disclosed in US Patent Application No. 2006 / 01103Q7A1, published May 25, 2006. The fused silica typically has a Mohs hardness greater than about 6, greater than about 6.5, and greater than about 7. Precipitated silicas are not hard, typically having a Mohs hardness of 5.5 to 6.

Another distinction between fused and precipitated silica is purity, with fused silica having a higher purity than that of precipitated silica. The percentage of silica by weight in fused silica may be greater than about 97%, about 97.5%, about 98%, about 98.5%, in some embodiments greater than about 99%, and in some modalities, greater than about 99.5%. For precipitated silica, the percentage by weight of silica is typically only about 90%. These purity measurements include water as an impurity, and can be calculated using the LOD and LOI methods described above.

Depending on the supplier, impurities other than water may include metal ions and salts, among other materials. In general, for precipitated silicas, impurities other than water mostly consist of sodium sulfate. Precipitated silicas will typically have from about 0.5% to 2.0% sodium sulfate. Fused silica typically contains no sodium sulfate, or is less than 0.4% of it. Purity levels other than water may be determined by reference to "USP-NF Dental Silica Silicon Monograph" as follows: Purity consists of the combined results of the Assay (silicon dioxide) and Sodium Sulphate tests. For the essay. - Transfer about 1 g of gel. silica to a tared platinum plate, ignite at 1,000 ° C for 1 hour, cool in a desiccator and weigh. Carefully wet with water and add about 10 mL of hydrofluoric acid in small increments. Evaporate on a steam bath until dry and then cool. Add about 10 ml of hydrofluoric acid and about 0.5 ml of sulfuric acid, e.g. evaporate to dryness. Slowly raise the temperature until all acids have been volatilized, and ignite at 1,000 ° C. Cool in a desiccator and weigh. The difference between the final weight and the weight of the initially ignited portion represents the weight of Si02. Sodium Sulphate - Transfer to a platinum plate about 1 g of accurately weighed tooth-like silica, wet with a few drops of water, add 15 mL of perchloric acid and place the plate on a hot plate. Add 10 mL of hydrofluoric acid. Heat until copious amounts of steam are released. Add 5 mL of hydrofluoric acid and again heat to copious amounts of steam. Add about 5 mL of boric acid solution (1 in 25), and heat to vapors. Cool and transfer the residue to a 400-mL beaker with the aid of 10 mL of hydrochloric acid. Adjust the volume with water to about 300 mL, and bring to a boil on a hot plate. Add 20 mL of TS hot barium chloride. Keep the beaker on the hot plate for 2 hours, keeping the volume above 200 mL. After cooling, transfer the precipitate and solution to a filter pan with a pore size of 0.8 μπη, tared and dried. Wash the filter and precipitate 8 times with hot water, dry the crucible at 105 ° C for 1 hour and weigh. The weight, multiplied by 0.6085, is the sodium sulphate content of the amount of sample taken. No more than 4.0% is obtained. Purity may also be determined by the use of conventional analytical techniques such as atomic absorption spectroscopy or by elemental analysis. Unique surface morphology of fused silica may result in more favorable ratios between PCR / RDA. The Pellicle Cleaning Ratio (PGR) of the fused silica of the present invention is a measure of the cleaning characteristics of a dentifrice, and is in the range of from about 70 to about 200, preferably about 100 to about 200. about 80 to about 200. The Radioactive Dentine Abrasion (RDA) of the silica of the invention is a measure of the abrasive capacity of fused silica when incorporated into a dentifrice, and is less than about 250, and may range from about 100 to about 230. Figure 3 (a) shows compositions of sodium fluoride-based formulas comprising various fused and precipitated silicas Figure 3 (b) shows the corresponding PCR and RDA values. Figure 4 (a) shows compositions of stannous fluoride-based formulas comprising various fused and precipitated silicas Figure 4 (b) shows the corresponding PCR and RDA values PGR values are determined by the method discussed in "In Vitro Removal of Stain with Dentifriee," G.K. Stookey, et al., J. Dental Res., 61, 1236-9, 1982. RDA values are determined according to the method established by Hefferren, Journal of Dental Research, July-August 1976, pages 563-573, and described in U.S. Patent Nos. 4,340,583, 4,420,312 and 4,421,527 to Was.cn. Osvalores.de. RDA may also be determined by means of. ADA recommended procedure for determining the abrasive capacity of dentifrices. The PCR / RDA to fused silica ratio, when incorporated into a dentifrice, may be greater than 1, indicating that the dentifrice is providing effective cleaning of the biological film without excessive abrasiveness. The PCR / RDA ratio may also be at least about 0.5. The PCR / RDA ratio is a function of particle size, shape, texture, hardness and concentration. Figure 5 is a table of PGR and RDA data for various amounts of both fused and precipitated silica. This demonstrates that fused silica (TS10 and TS44CSS) may have superior cleanability (PCR) compared to precipitated silicas (Z119 and Z109). The data show that a 5% molten silica buccal composition can better clean than a 10% precipitated silica buccal composition. In addition .., the data show that a. Fused silica can provide this cleaning while still being in the. Acceptable abrasive capacity levels (RDA). The shape of fused silica particles can be classified as angular or spherical, or a combination of shapes, depending on the type of manufacturing process. Additionally, fused silica can also be ground to reduce the. particle size. Spherical particles include any particle that as a whole has a predominantly round or elliptical shape. Angular particles include any non-spherical particles, including those with polyhedral shapes. The angular particles may have some rounded edges, some or all sharp edges, some or all serrated edges, or a combination of these shapes. The particle shape of fused silica can impact its abrasive capacity. For example, at the same particle size, a spherical fused silica may have a minor radioactive dentin (RDA) abrasion than that of an angular fused silica. Consequently, it would be possible to optimize the cleaning capacity without increasing the abrasive capacity. Or, as another example, a prophylactic paste or a weekly paste could comprise an angular fused silica with a large particle size.

Compositions comprising spherical fused silica, that is, in which at least 25% of the fused silica particles are spherical, have certain advantages. Due to the rounded edges, spherical fused silica may be less abrasive. This means that the ratio of PCR to RDA can be improved and yet provide good cleaning.

In addition, spherical fused silica can be used at higher contents without being too abrasive. Spherical fused silica may also be used in combination with angular fused silica, or silica in which at least about 25% of the particles are angular. This could help lower costs while still providing good cleaning with acceptable abrasiveness. In embodiments having both angular and spherical fused silicas, the amount of angular fused silica may be from about 1% to about 10% by weight of the composition.

In some embodiments where at least 25% of the fused silica particles are spherical, the RDA may be less than 150, in other embodiments less than 120. In some embodiments where at least 25% of the fused silica particles are spherical, the RDA may be less than 150. The ratio of PCR to RDA may be at least about 0.7, at least about 0.8, at least about 0.9 or at least about 1.0. In some embodiments, the amount of fused silica may be from about 20% to about 50% by weight of the composition, and in such embodiments the composition may have an RDA value of less than 170. In some of those same embodiments, the size The average fused silica particle size may be from about 3.0 microns to about 15.0 microns.

Examples of spherical fused silicas include Spheron P1500 and Spheron N-2000R, produced by the Japanese Glass Company, and Sun-Sil 130NP. It is important to note that fused silica particles generally do not form as much aggregate clusters as precipitated silicas and typically do not form clusters as easily as precipitated silicas. In some embodiments, most fused silica particles do not form aggregate clusters. In contrast, precipitated silicas generally form aggregate clusters of primary particles with. irregular shape, with dimensions in the submicron scale. A silica. Precipitate may be treated or coated which may increase or decrease the amount of aggregation. The particle shape of both fused and precipitated silica can be determined using a scanning electron microscope (SEM).

Figures 6, from (a) to (i) are precipitated fused SEM SEM micrographs with an increase of 3.0. The samples were coated with gold by ion bombardment using the EMSS75X spray coating device cooled by a Peítier system. SEM surface images of the sample were obtained using a JEOL JSM-6100 equipment. The SEM was operated at 20 kV, 14 mmD, and increased by 1,500x and 3-OOOx.

The micrographs (a) and (b) of precipitated silicas Z-109 and Z-119 show irregularly shaped agglomerated particles. The particles appear to be made of smaller agglomerated particles loosely bonded together. The micrographs (c) and (d), which are the fused silica Spheron P15QG and Spheron N-2000R, show regular shaped spheroid particles. That is, each particle has a predominantly spherical shape. And micrographs (e), (f), (g), (h) and (i), which are fused silicas 325F, RG5, RST 2500 DSO, Teco-Sil 44C and Teco-Sil 44CSS, show dense particles of irregular shape. Some particles may be agglomerated and tightly packed, while others appear to consist of a single mass. In general, this latter group of fused silicas have irregularly shaped particles with sharp and / or sharp edges, and could be considered angular.

In general, buccal compositions, for example dentifrices, comprising fused silica can be distinguished from buccal compositions comprising only precipitated silica by reducing both compositions to ashes by heating to about 500 ° C and then comparing them. samples. Heating at about 500 ° C leaves only the abrasive, but is not hot enough to remove the hydroxyl groups. Fused silica and precipitated silica can be distinguished by surface area ΒΈΤ either by SEM analysis as described above or by XRD (X-ray scattering technique) analysis. The average particle size of the fused silicas of the present invention may range from about 1 micron to about 20 microns, from about 1 micron to about 15 microns, from about 2 microns to about 12 microns, or about 10 microns. 3 microns to about 10 microns as measured by laser light scattering particle sizing on a Malvern equipment. Angle-shaped particles can have a size (average D50) of about. 5 'to about 10 microns. It is preferred that D90 (average particle size 90%) is less than about 50 microns, less than about. 40 microns, less than about. 30 microns or less than about .25 microns. Small size fused silica particles can provide a sensitivity benefit since the particles can block the opening of the tubules. Particle size is determined using the methods disclosed in US Patent Application No. 2007 / 0001Q37A1, published January 4, 2007. The size of the fused silica particles can be controlled by processing the material. The size of the precipitated silica particles depends on the precipitation method. Although the particle size of some precipitated silicas overlaps with those of fused silicas, typically precipitated silicas will have a larger particle size. For example, precipitated silicas Z-109 and Z-119 range from about 6 microns to about 12 microns and from about 6 microns to about 14 microns, respectively. However, it is important to note that if, for example, fused silica and precipitated silica are the same particle size, the BET surface area of the fused silica will typically still be much smaller than the BET surface area of the precipitated silica due to lack of porosity. of fused silica particles. Thus, fused silica with particle size similar to that of a precipitated silica will be distinguishable from the precipitated silica and will offer optimum cleanliness and / or compatibility compared to the precipitated silica.

In some embodiments, the particle size of the fused silica may be optimized for cleaning. In some embodiments, the average fused daylene particle size may be from about 3 microns to about 15 microns, with 90% of the particles having a size of about 50 microns or less. In other embodiments, the average particle size may be from about 5 microns to about 10 microns, with 90% of the particles having a particle size of about 30 microns or less. In other embodiments, the average particle size may be from about 5 microns to 10 microns, with 90% of the particles having a particle size of about 15 microns or less. The fact that fused silica is harder than precipitated silica contributes to its better cleaning ability. This means that a fused silica of the same particle size and amount as a precipitated silica will have comparatively better cleanability. For example, the PGR for a fused silica composition may be at least about 10% greater than the PGR for a precipitated silica composition when the average particle size and silica contents are equal. The improved cleanability of fused silica leads to different formulation possibilities, some maximizing cleanliness, some optimizing cleanliness without increasing abrasive capacity, some optimizing cleanliness and reducing abrasive capacity, and some formulations simply cost more. low because a smaller amount of abrasive is required to provide acceptable cleaning. In. In some embodiments, a buccal treatment composition comprising a fused silica abrasive may have a PGR of at least about 80, at least about 100, or at least about 120. In some embodiments, the ratio between PGR and RDA may be at least about 0.8, at least about 0.7, at least about 0.8, or at least about 0.9. In some embodiments, the composition may comprise less than about 20% molten silica by weight of the composition. In some embodiments, the composition may comprise less than about 15% molten silica by weight of the composition, and have a PGR of at least about 100, or may comprise less than about 10% molten silica by weight of the composition. composition, and have a PCR of at least about 100.

In some embodiments optimized for better cleanliness, at least about 80% of the fused silica particles may be angular. In other embodiments, the composition may further comprise precipitated silica. In still other embodiments, the composition may comprise a gel network. In some embodiments, the composition may comprise one or more of the following: anti-caking agent, anti-erosion agent, bactericidal agent, anti-calculating agent, anti-hypersensitivity agent, antiinflammatory agent, antiplaque agent, anti-gingivating agent, odorant agent unpleasant, and / or an anti-stain agent. In some embodiments, the composition may comprise an additional abrasive material, including, but not limited to, precipitated silica, calcium carbonate, dicalcium phosphate dihydrate, calcium phosphate, perlite, pumice, calcium pyrophosphate, nanodiamonds, silica precipitated surface treated and dehydrated, and mixtures thereof. Some embodiments may consist of a method for cleaning the individual's teeth and oral cavity by using a buccal treatment composition comprising a fused silica abrasive in a buccal acceptable carrier, the fused silica abrasive having an average particle size of about 3 microns to about 15 microns, and 90% of the particles have a size of about 50 microns or less.

In some embodiments, the particle size of the fused silica may be reduced to favor the benefits of polishing and anti-sensitivity. In some embodiments, the fused silica may have an average particle size of from about 0.25 microns to about 5.0 microns, from about 2.0 microns to about 4.0 microns, or from about 1, 0 microns to about 2.5 microns. In some embodiments, 10% of the fused silica particles may have a particle size of about 2.0 microns or less. In some embodiments, 90% of the fused silica particles may have a particle size of about 4.0 microns or less. In some embodiments, the particles may have an average particle size that is no larger than the average diameter of a mammalian dentin tubule, so that one or more particles are capable of being housed within the tubule, thereby obtaining a reduction or elimination of perceived sensitivity in the teeth. Dental tubules are structures that run the full thickness of the dentin, and form as a result of the mechanism of dentin formation. From the outer surface of the dentin to the area closest to the pulp, these tubules follow an S-shaped path. The diameter and density of the tubules are larger near the pulp. Tapering from the inner to the outer surface, they have a diameter of 2.5 microns close to the pulp, 1.2 microns in the middle of the dentin, and 0.9 microns in the dentin-enamel junction. Their density is 59,000 to 76,000 per square millimeter near the pulp, only half of it near the enamel.

To enhance the antisensitivity benefit provided by a small particle size, the compositions may further comprise additional antisensitivity agents such as tubule blocking agents and / or desensitizing agents. Tubule blocking agents may be selected from the group consisting of stannous ion source, strontium ion source, calcium ion source, phosphorus ion source, aluminum ion source, magnesium ion source, amino acids, bivasses, nanoparticides, polycarboxyates, Gantrez and mixtures thereof. Amino acids can be basic amino acids, and a basic amino acid can be arginine. The nanoparticles may be selected from the group consisting of apatite nanohydroxy, titanium nano-dioxide, metal nano-oxides and mixtures thereof. The desensitizing agent may be a potassium salt selected from the group consisting of potassium fluoride, potassium citrate, potassium nitrate, potassium chloride and mixtures thereof. Some embodiments may consist of a method for reducing tooth hypersensitivity by administering to an individual in need a buccal treatment composition comprising fused silica which has an average particle size of about 0.25 microns to about 5.0 microns. Some embodiments may consist of a method for polishing teeth by administering to an individual an oral treatment composition comprising fused silica which has an average particle size of 0.25 microns to about 5.0 µm. microns.

In other embodiments, the particle size may be relatively large to be part of a prophylactic paste or some other non-daily paste. In some embodiments, the fused silica may have an average particle size of at least about 7 microns, and the composition has a PGR of at least about 100. In other embodiments, the average particle size it can be from about 7 microns to about 20 microns. In some embodiments with an average particle size of at least about 7 microns, an additional abrasive selected from the group consisting of pumice, perlite, precipitated silica, calcium carbonate, rice husk silica, silica gels may be used. aluminas, phosphates including orthophosphates, polymetaphosphates and pyrophos facts, other inorganic particles and mixtures thereof. In embodiments with a larger particle size, the fused silica may comprise from about 1% to about 10% by weight of the composition. Some embodiments may be essentially free of surfactant, fluoride or any active oral treatment. Some embodiments may have a flavoring agent. Some embodiments consist of methods for cleaning and polishing dental enamel, comprising a buccal treatment composition in which the average particle size is at least about 7 microns and the PCR is at least about 100. The fused silica may be produced by melting silica (quartz or sand) at 2,000 ° C. After cooling in ingots or pellets, the material is ground. Grinding techniques vary, but some examples include jet milling, hammer milling, or ball milling. Ball milling may result in particles with rounder edges, while jet milling may result in sharper or more angular edges. Fused silica can be produced by the process disclosed in US Patent No. 5,004,488 to Mehrotra and Barker 1991. Fused silica can also be produced from a silicon rich chemical precursor, generally using a process. of continuous flame hydrolysis involving the chemical gasification of silicon, the oxidation of this gas to silicon dioxide, and the thermal fusion of the resulting dust. This process may produce spherical fused silica, but may be more expensive. While the production of precipitated silica is a chemical process, the production of fused silica is a natural process. Production of fused silica generates less waste and offers better sustainability benefits In some embodiments of the present invention there may be multiple types of fused silica. For example, a. Fused silica can be made by melting the silica at even higher temperatures, such as 4,000 ° C. These fused silicas may have a different particle size or surface morphology, but still maintain the benefits discussed above, including low reactivity, due to the relatively low concentration of surface hydroxyl and / or smaller specific surface area. . BET

Precipitated or hydrated silicas may be made by dissolving the silica (sand) using sodium hydroxide and causing precipitation by the addition of sulfuric acid. Once washed and dried the material is then ground. Such precipitated silicas can be produced by the process disclosed in US Patent No. 6,740,311, White, 2004. Precipitated silica and other silicas are described in more detail in "Handbook of Porous Solids", edited by Ferdi Schuth, Kenneth SW Sing and Jens Weitkamp, Chapter 4.7.1.1.1, entitled "Formation of Silica Soils, Gels, and Powders", and in "Cosmetic Properties and Structure of Fine-Particle Synthetic Precipitated Silicas", by SK Wason, Journal of Soc. Cosmetic Chem. , volume 29, (1078), pages 497-521. The amount of fused silica used in the present invention may be about 1%, 2%, 5%, 7%, 10%, 12%, 15%, 20%, 25%, 30%, 35%, 40%, 45% or 50% to about 5%, 7%, 10%, 12%, 15%, 20%, 25%, 30%, 35%, 40% ·, 45%, 50%, 55%, 60% , 65% or 70%, or any combination thereof. The fused silicas of the present invention may be used alone or with other abrasives. A composition may comprise more than one type of fused silica. One type of abrasive that can be used with fused silica is a precipitated silica. Total abrasives in the buccal compositions described herein are generally present in contents of from about 5% to about 70% by weight of the composition. Preferably the total abrasives in the toothpaste compositions represent from about 5% to about 50% by weight of the composition. For combinations of fused silica with precipitated silicas, fused silica may represent from about 1% to about 99% by weight of the total abrasive. The precipitated silica or silicas may comprise from about 1% to about 99% by weight of the total abrasive. In some embodiments, small amounts of fused silica may be used, from about 1% to about 10%, or from about 2% to about 5%. The fused silica may be used in combination with inorganic particles which have been treated with nonionic surfactants such as ethoxylated and non-ethoxylated fatty alcohols, as well as acids and esters. An example of such a nonionic surfactant is PEG 40 hydrogenated castor oil. In general, the buccal treatment compositions of the present invention may be used with additional abrasive material, such as one or more substances selected from the group consisting of precipitated silica, calcium carbonate, rice husk silica, silica gels, aluminum, aluminum silicates, phosphates, including orthophosphates, polymetaphosphates and pyrophosphates, other inorganic particulates, dicalcium phosphate dihydrate, calcium phosphate, perlite, pumice pyrophosphate calcium, nanodiamonds, surface treated dehydrated precipitated silica, and mixtures thereof.

In some embodiments, the ratio of other abrasives to fused silica is greater than about 2 to 1, in some embodiments greater than about 10 to 1. In some embodiments, the ratio is about 1 to 1. In some embodiments In both embodiments, the amount of fused silica is from about 1% to about 10% by weight of the composition. In some embodiments, the amount of fused silica is from about 2% to about 25% by weight of the abrasive combination. In one embodiment, the other abrasive is calcium carbonate. In some embodiments, the amount of calcium carbonate by weight of the composition is from about 20% to about 60%. In some embodiments, the amount of calcium carbonate by weight of the composition is from about 20% to about 60%. In another embodiment, an additional abrasive may comprise at least one precipitated silica. The precipitated silica abrasive may comprise from about 5% to about 40% by weight of the combination. The amount of fused silica in the abrasive combination may comprise from about 1% to about 10% by weight of the composition. In some embodiments, the composition comprising an abrasive combination may have a PCR of at least about 80, about 100, or about 120, or an RDA less than about 150, or less than about 200.

To further increase the availability of cations in the compositions, the fused silicas of the present invention may be used in combination with treated precipitated silicas, such as modified surface precipitated silica, dehydrated precipitated silica, or reduced porosity precipitated silicas, reduced surface hydroxyl groups or small surface areas that have lower cation compatibility compared to regular precipitated silicas. However, it is emphasized that although these specific precipitated silicas receive a surface treatment in an attempt to reduce surface hydroxyls and optimize properties such as low porosity or cationic compatibility, they will still be considered precipitated silicas. (See, for example, US 7,255,852, US 7,438,895, WO 9323007 and WO 9406868). That is, they are silicas produced by a wet track process. Water is added during the manufacturing process and then removed. This remains true even for precipitated silica that can be heated to very high temperatures in an attempt to remove hydroxyl groups. In contrast, fused silica, although it may receive a surface treatment, does not need this or any other treatment. Molten silica is manufactured without any water, only by heating. This heating process can more effectively reduce surface hydroxyls than most precipitated processes can.

Other abrasive polishing materials may include silica gels, rice husk silica, alumina, phosphates including orthophosphates, polymetaphosphates and pyrophosphate, and mixtures thereof. Specific examples include dicalcium dihydrate orthophosphate, calcium pyrophosphate, tricalcium phosphate, calcium polymetaphosphate, insoluble sodium polymetaphosphate, hydrated alumina, beta calcium pyrophosphate, calcium carbonate and resinous abrasive materials such as urea condensate particulate products, and others such as those disclosed by Cooley et al in US Patent No. 3,070,510, issued December 25, 1962. The abrasive may be precipitated silica or silica gels such as silica xerogels described in US Patent No. 3,538,230. of Pader et al., issued March 2, 1970, and US Patent No. 3,862,307 to DiGiuIio, issued January 21, 1975. Examples are silica xerogels available under the trade name "Syloid" from WR Grace & Company, Davison Chemical Division. There are also precipitated silica materials, such as those marketed by J. M. Huber Corporation under the tradename "Zeodent", particularly silicas under the designation "Zeodent 109" (Z-109) and "Zeodent 119" (Z-119). Other commercially available precipitated silicas comparable to Z-109 and Z-119 include, for example, Toxosil 63, Tixosil 73 and Tixosil 103, all available from Rhodia, Huber silicas Z-103, Z-113 and Z-124, OSC DA available from OSC in Taiwan, and ABSiL-200 and ABSIL-HC available from Madhu Siiica. Among these commercially available precipitated silicas, Tixosil 73 is the most similar to Z-119. The present precipitated silica abrasives may be used in combination with fused silica and other abrasives.

The types of precipitated silica-based dental abrasives that can be mixed with the fused silica of the present invention are described in more detail in US Patent No. 4,340,583, issued to Wason on July 29, 1982. Silica-based abrasives Precipitated precipitates are also described in Rice U.S. Patent Nos. 5,589,160, 5,603,920, 5,651,958, 5,658,553 and 5,716,601.

A suitable type of fused silica is Teco-Sil 44CSS, which is available from CE Minerals Products. Also available from CE Minerals are fused silicas under the names Teco-Sil 44C, Teco-Sil T10 and TecoSpere A. Other Silicas Suitable castings include R610G0, available from Jiangsu Kaída Silica and Spheron N-2000R and Spheron P1500, available from JGC, Japanese Glass Company, Others include RST 2500, RG 1500 and RG 5, available from Líanyungang Ristar Electronic Materials, SO- C5 and SO-C4, available from Adamatech, Fuserex AS-1, available from Tatsumori, FS 30 and FS-2DC, available from Denki Kagaku Kogyou, Min-Sil 325F, available from Minco, and SunsiUSONP, available from Sunjin as well as a fused silica available from Shin-Etsu. The CAS number for some types of fused silica is 60676-86-0. The CAS number for hydrated silica is 7631-86-9. The INCl name for fused silica is "fused silica", while the INCl name for precipitated silica is "hydrated silica". The silicas of the present invention do not include silicates, and the fused silicas of the present invention do not include fused silicates.

Acceptable buccal carrier The carrier for the components of the present compositions may be any buccal acceptable carrier suitable for use in the buccal cavity. The carrier may comprise suitable cosmetic and / or therapeutic actives. These assets include any material that is generally considered safe for use in the oral cavity, and which provides changes in the overall appearance and / or health of the oral cavity including, but not limited to, anti-calculus agents, fluoride ion sources, stannous ion sources. , whitening agents, antimicrobial agents, unpleasant odor agents, antisensitivity agents, anti-erosion agents, anti-caries agents, anti-plaque agents, anti-inflammatory agents, nutrients, antioxidants, antiviral agents, analgesic and anesthetic agents, antagonists H-2 and mixtures thereof. The content of cosmetic actives and / or therapeutic actives, when present in the oral care composition, corresponds in one embodiment from about 0.001% to about 90%, in another embodiment from about 0.01% to about 90%. 50% and, in another embodiment, from about 0.1% to about 30% by weight of the oral care composition.

Assets One of the advantages of fused silica is its compatibility with other materials, particularly those that are reactive and may lose their effectiveness, such as actives. Since fused silica does not react as much to the active as precipitated silica and other traditional abrasives, less active can be used to achieve the same effectiveness. If the asset has any potential negative aesthetic aspect, such as unpleasant or strong taste, astringency, staining or other negative aesthetic aspect, a smaller amount of active may be preferable. Additionally, using less active for equal or similar effectiveness represents savings. Alternatively, if the same amount of asset is used as is traditionally used, the asset will be more effective as a larger amount will be available to provide the benefit. Because fused silica is slightly harder than traditional abrasives such as precipitated silica, it can also remove more stains and / or clean better.

The actives include, but are not limited to, bactericidal actives, antipiaca agents, anti-caries agents, antisensitivity agents, anti-erosion agents, oxidizing agents, anti-inflammatory agents, anti-calculus agents, nutrients, antioxidants, analgesic agents, anesthetics, H-1 and H-2 antagonists, antiviral actives and combinations thereof. A material or ingredient may be classified under more than one type of material. For example, an antioxidant may also be an antipiaca and bactericidal active. Examples of suitable actives include stannous fluoride, sodium fluoride, essential oils, mono alkyl phosphates, hydrogen peroxide, PCC, chlorhexidine, triclosan and combinations thereof. The following is a non-limiting list of assets that may be used in the present invention: Fluoride ion The present invention may comprise a safe and effective amount of a fluoride compound. The fluoride ion may be present in an amount sufficient to result in a fluoride ion concentration in the composition at 25 ° C, and / or, in one embodiment, may be used in contents of from about 0.0025% to about 5%. 0% by weight and in another embodiment from about 0.005% to about 2.0% by weight to provide anti-caries efficacy. A wide variety of fluoride ion producing materials can be employed as a source of soluble fluoride in the present compositions. Examples of suitable fluoride ion producing materials are disclosed in US Patent Nos. 3,535,421 and 3,678,154. Representative sources of fluoride ion include: stannous fluoride, sodium fluoride, potassium fluoride, amine fluoride, sodium monofluoro phosphate, zinc fluoride and many others. In one embodiment, the dentifrice composition comprises stannous fluoride or sodium fluoride, as well as mixtures thereof. The pH of the buccal composition may be from about 3 to about 10. The pH is typically measured as a slurry pH by methods known in the industry. Depending on the actives used in the buccal composition, a different pH may be desired. For fluoride containing formulations, it may be desirable to have a slightly lower pH than typical dentifrices. Typical buccal compositions with precipitated silica and fluoride have a pH high enough that the fluoride in the formula does not form fluorosilicate and then reacts with the hydroxyl groups present in the precipitated silica. Since the number of hydroxyl groups in fused silica is less than the number of hydroxyl groups in precipitated silica, this is not a problem and the pH of the fused silica buccal composition may be lower.

Compositions containing fused silica and fluoride may have a pH of less than about 6.0 or less than about 5.5. The pH may be less than about 5.2 or about 5.0. It may be desirable to have a pH of from about 3.5 to about 5 or from about 2.4 to about 4.8. The pH may be below 5.5 to allow for greater fluoride absorption as a larger amount of fluoride will be available. The low pH may help in conditioning the dental surface to accept more fluoride. For formulations containing peroxide and fused silica, the pH may be less than 5.5 or less than 4.5. For a peroxide and fused silica formulation, it may be from about 3.5 to about 4.0. For formulations comprising fused silica, tin and fluorine, it may be desirable to have a pH of less than 5.0. A pH lower than 5.0 may allow a larger amount of SnF3 stannous species to form.

Anti-Calculating Agent The toothpaste compositions of the present invention may also comprise an anti-calculating agent, which in one embodiment may be present in from about 0.05% to about 50%, in another embodiment from about 0.05% to about 50%. about 25% and in another embodiment is from about 0.1% to about 15% by weight of the oral care composition. The anti-calculating agent may be selected from the group consisting of polyphosphates (including pyrophosphates) and their salts, polyamino propane sulfonic acid (AMPS) and its salts, polyioiefine sulfonate and its salts, polyvinyl phosphates and their salts, polyoxyphine phosphates and their salts , diphosphonates and their salts, phosphonoalkane carboxylic acid and its salts, polyphosphonates and their salts, polyvinyl phosphonates and their salts, polyhydine phosphonates and their salts, polypeptides and combinations thereof, polycarboxylates and salts thereof, carboxy substituted polymers and mixtures of the same. In one embodiment, the polymeric polycarboxylates used in the present invention include those described in US Patent 5032386. An example of such commercially available polymers is Gantrez of International Specialty Products (ISP). In one embodiment, the salts are alkali metal or ammonium salts. Polyphosphates are generally used in the form of their fully or partially neutralized water-soluble alkali metal salts, such as potassium, sodium, ammonium salt and mixtures thereof. Inorganic polyphosphate salts include alkali metal tripolyphosphate or tetrapolyphosphate (eg sodium), diaiquyl metal diacid (eg disodium), trialkyl metal monacid (eg trisodium), potassium hydrogen phosphate, sodium hydrogen phosphate, hexahyaphosphate. alkali metal (e.g. sodium), and mixtures thereof. Polyphosphates larger than tetrapolyphosphate usually occur as amorphous glassy materials. In one embodiment, the polyphosphates are those produced by FMC Corporation, which are available under the trade names Sodaphos (# 6), Hexaphos (# 13), and Glass H (# 21, Sodium Hexametate). mixtures thereof. Pyrophosphate salts useful in the present invention include: alkali metal pyrophosphates, di, tri and monopotassium or sodium pyrophosphates, di-alkali metal pyrophosphate salts, tetraalkaline metal pyrophosphate salts and mixtures thereof. In one embodiment, the pyrophosphate salt is selected from the group consisting of trisodium pyrophosphate, dihydrogen disodium pyrophosphate (Na2H2P207), pyrophosphate, dipotassium, tetrasodium pyrophosphate (Na4P207), tetrapotassium pyrophosphate (K4P2O) and the same. Polyiefine sulfonates include those wherein the olefin group contains 2 or more carbon atoms, as well as their salts. Polyiefine phosphonates include those wherein the olefin group contains 2 or more carbon atoms. Polyvinyl phosphonates include polyvinyl phosphonic acid. Diphosphonates and their salts include azocycloalkane-2,2-diphosphonic acids and salts thereof, azocycloalkane-2,2-diphosphonic acid ions and salts thereof, azacyclohexane-2,2-diphosphonic acid, azacyclopentane ~ 2, 2-diphosphonic acid, N-methyl azacidopentane-2,3-diphosphonic acid, EHDP (ethane-1-hydroxy-1,1, diphosphonic acid), AHP (azacycloeptane-2,2-diphosphonic acid), ethane 1-amino-1,1-diphosphonate, dichloromethane diphosphonate, etc. Phosphonoalkane carboxylic acid or alkali metal salts thereof include PPTA (tricarboxylic phosphonopropane acid) and PBTA (~ 1,2,4-tricarboxylic acid phosphonobutane), each of which is acid or alkali metal salts. Polyiefine phosphates include those wherein the olefin group contains 2 or more carbon atoms. Polypeptides include polyaspartic and polyglutamic acids. Stannous ion The buccal compositions of the present invention may include a stannous ion source. As stated above, one of the advantages of fused silica is its compatibility with other materials, particularly those that are reactive and may lose effectiveness. Stannous ions are considered reactive, so using them with fused silica can have some important benefits. Since fused silica does not react with both tin and precipitated silica and other traditional abrasives, a smaller amount can be used just as effectively. Tin has been reported to have potential negative aesthetic aspects, such as unpleasant or strong taste, astringency, staining, or other negative aesthetic aspects that make the oral compositions containing it less desirable to consumers. Accordingly, it may be preferable to use a smaller amount of tin. Additionally, the use of less tin for the same or similar effectiveness represents an economy. Alternatively, if the same amount of tin is used as is traditionally used, the tin will be more effective as a larger amount of tin will be available to provide the benefit. Because fused silica is slightly harder than traditional abrasives such as precipitated silica, it can also remove more stains and / or clean better. It has also been disclosed that tin-containing formulations may increase tooth strength. Consequently, tin-containing formulations may have lower RDA scores than comparable formulations which do not contain it. Lower RDA scores may provide a better ratio of PCR to RDA as fused silica is a good cleaning abrasive and tin provides stronger teeth. The synergy achieved by combining fused silica and tin offers consumers a highly effective and highly clean formula.

Stannous ions may be obtained from stannous fluoride and / or other stannous salts. Stannous fluoride has been found to aid in the reduction of gingivitis, plaque, tenderness and erosion, as well as the benefit of breath improvement. The stannous ions contained in a toothpaste composition will provide efficacy to an individual using the toothpaste composition. While efficacy may include benefits that go beyond reducing gingivitis, it is defined as a noticeable amount of reduction in plaque metabolism in situ. Formulations providing such efficacy typically include tin contents from stannous fluoride and / or other stannous salts, in the range of from about 50 ppm to about 15,000 ppm of stannous ions in the total composition. The stannous ion is present in an amount from about 1,000 ppm to about 10,000 ppm and, in one embodiment, from about 3,000 ppm to about 7,500 ppm. Other stannous salts include stannous organic carboxylates such as stannous acetate, stannous gluconate, stannous oxalate, stannous malonate, stannous citrate, stannous ethylene glyoxide, stannous formate, stannous lactate, stannous tartrate and the like. Other sources of stannous ion include stannous halides such as stannous chlorides, stannous bromide, stannous iodide and stannous dihydride chloride. In one embodiment, the stannous ion source is stannous fluoride, in another embodiment dehydrated or trihydrate stannous chloride, or stannous gluconate. The combined stannous salts may be present in an amount from about 0.001% to about 11% by weight of the oral care compositions. The stannous salts may, in one embodiment, be present in an amount of from about 0.01% to about 7%, in another embodiment, from about 0.1% to about 5%, and in another embodiment. about 1.5% to about 3% by weight of the oral care composition.

Whitening Agent A whitening agent may be included as an active in the present toothpaste compositions. Suitable bleaching actives are selected from the group consisting of alkali metal and alkaline earth metal peroxides, metal chlorites, perborates including mono and tetrahydrates, perphosphates, percarbonates, peroxyacids and persulphates such as ammonium, potassium, sodium and lithium, and combinations thereof. Suitable peroxide compounds include hydrogen peroxide, ur peroxide, calcium peroxide, carbamide peroxide, magnesium peroxide, zinc peroxide, strontium peroxide and combinations thereof. In one embodiment, the peroxide compound is carbamide peroxide. Suitable metal chlorites include calcium chlorite, barium chlorite, magnesium chlorite, lithium chlorite, sodium chlorite and potassium chlorite. Additional bleaching assets may be hypochlorite and chlorine dioxide. In one embodiment, the chlorite is sodium chlorite. In another embodiment, the percarbonate is sodium percarbonate. In one embodiment, the persulfates are oxones. The content of these substances depends on the available oxygen or chlorine, respectively, that the molecule is able to provide to target the stain. In one embodiment, the bleaching agents may be present in contents ranging from about 0.01% to about 40%, in another embodiment from about 0.1% to about 20%, in another embodiment of about 0%. From 5% to about 10% and, in another embodiment, from about 4% to about 7% by weight of the oral care composition.

Oxidizing Agent The compositions of the invention may contain an oxidizing agent, such as a peroxide source. A peroxide source may comprise hydrogen peroxide, calcium peroxide, carbamide peroxide, or mixtures thereof. In some embodiments, the source of peroxide is hydrogen peroxide. Other peroxide actives may include those that produce hydrogen peroxide when mixed with water, such as percarbonates, for example sodium percarbonates. In certain embodiments, the peroxide source may be in the same phase as a stannous ion source. In some embodiments, the composition comprises from about 0.01% to about 20% of a peroxide source, in other embodiments from about 0.1% to about 5%, in certain embodiments from about 0.2 % to about 3%, and in another embodiment from about 0.3% to about 2.0% of a peroxide source by weight of the buccal composition. The peroxide source may be provided as free ions, salts, complexed or encapsulated. It is desirable that the peroxide in the composition be stable. Peroxide may provide a reduction in staining as measured by the Cyclic Stain Test or other relevant methods.

In addition to the optional ingredients detailed below, certain thickeners and flavorings offer better compatibility with oxidizing agents such as peroxide. For example, in some embodiments, preferred thickening agents may be cross-linked polyvinyl pyrrolidone, polyacrylates, alkylated polyacrylates, alkylated cross-linked polyacrylates, polymeric alkylated polyethers, carbomers, alkylated carbomers, gel networks, nonionic polymeric thickeners, Sepinov EMT 10 (Seppic, sodium hydroxyl acrylate / acryloyl dimethyl taurate copolymer), Thix Pure 1450, 1442, HH (PEG 180 lauret-50 / ΤΜΜΡ or polyether 1, Rockwood Specialties), Structure 2001 (Akzo, Acriate / Itaconate Copolymer) stearet-20), Structure 3001 (Akzo, acetate / ketet-20 itaconate copolymer), Aculin 28 (Dow Chemical / Rohm and Haas, beenet-25 acrylate / methacrylate copolymer), Genopur 350QD (Ciariant), Aculin 33 (Dow Chemical / Rohm and Haas, acrylate copolymer), Aculin 22 (Dow Chemical / Rohm and Haas acrylate copolymer / stearet-20 methacrylate), Aculin 46 (Dow Chemical / Rohm and Haas, PEG-150 / copolymer) stearyl alcohol / SMDI), A500 (cross-linked carboxy methyl cellulose, Hercules), Structure XL (hydroxy propyl starch phosphate, National Starch), and mixtures thereof.

Other suitable thickening agents may include polymeric sulfonic acids such as Aristoflex AVC, AVS, BLV and HMB (Ciariant, polymers, copolymers and cross-polymers of acryl dimethyl taurate), Diaformer (Ciariant, amide and methacrylate oxide copolymer), Genapol ( Ciariant, polyglycol ether of fatty alcohol and alkylated polyglycol ethoxylated fatty alcohol), fatty alcohols, ethoxylated fatty alcohols, high molecular weight nonionic surfactants such as BRIJ 721 (Croda), and mixtures thereof.

Suitable flavor systems particularly compatible with peroxide include those discussed in US 2007/0231278. In one embodiment, the taste system comprises menthol in combination with at least one secondary refrigerant, together with selected traditional taste components that have been found to be relatively stable in the presence of peroxide. For use in the present invention, the term "stable" means that the character or flavor profile is not significantly altered or consistent over the life of the product. The present composition may comprise from about 0.04% to 1.5% total cooling agents (menthol + secondary cooling agent) with at least about 0.015% by weight menthol. Typically, the menthol content in the final composition ranges from about 0.015% to about 1.0% and the content of secondary refrigerants ranges from about 0.01% to about 0.5%. Preferably, the content of the total refrigerant is in the range of from about 0.03% to about 0.8%.

Suitable secondary refrigerants for use with menthol include a wide variety of materials such as carboxamides, ketals, diols, menthyl esters and mixtures thereof. Examples of secondary refrigerants in the present compositions are carboxamide paramentan based agents, such as N-ethyl-p-menthane-3-carboxamide, commercially known as "WS-3", N, 2,3-trimethyl-2-one. iso-propyl butanamide, known as "WS-23", and others in this series such as WS-5, WS-11, WS-14 and WS-30. Additional suitable refrigerants include 3-1-menthoxy propane-1,2-dioxy! known as TK-10 and produced by Takasago, mentona glycerol acetal known as MGA, menthyl esters such as menthyl acetate, menthyl acetoacetate, menthol lactate known as Frescolat® and available from Haarmann and Reimer, and monomentine succinate available under the trade name Physcool with V. Mane. For use in the present invention, the terms menthol and menthyl include dextrogyr and levogyr isomers of such compounds, as well as racemic mixtures thereof. TK-10 is described in US Patent No. 4,459,425 to Am et al, issued July 10, 1984. WS-3 and other agents are described in Watson US Patent No. 4,136,163 , et al., issued January 23, 1979.

Traditional flavor components that have been found to be relatively stable in the presence of peroxide include methyl methalylate, ethyl salicylate, methyl cinnamate, butyl cinnamate, ethyl butyrate, ethyl acetate, methyl anthranilate, methyl acetate. isoamyl, isoamyl butyrate, allyl caproate, eugenol, eucaiiptol, thymol, cinnamic alcohol, cinnamic aldehyde, octanol, octanal, decanol, decanal, phenyl alcohol, benzyl alcohol, benzaldehyde, alpha-terpinol, linalol, limonene, citral, vanillin , ethyl vaniiine, propenyl guaetol, maltol, ethyl maltol, heliotropin, anethole, dihydroanetol, carvone, oxanone, mentone, β-damascenone, ionone, decalactone range, nonalactone range, undecalactone range, 4-hydroxy-2,5-dimethyl-3 (2H) -furanone and mixtures thereof. Generally suitable flavoring agents are those having structural characteristics and functional groups that are less prone to peroxide oxidation. These include derivatives of flavoring chemicals that are saturated, or that contain aromatic rings or stable ester groups. Also suitable are flavoring chemicals which may undergo some oxidation or degradation without resulting in a significant change in flavor character or profile. Flavoring agents are generally used in the compositions in contents of from about 0.001% to about 5% by weight of the composition.

In some embodiments, the pH of the composition may be from about 3.5 to about 5.5, which may provide additional stability for the oxidizing agent. In some embodiments the composition may further contain a stannous ion source. In some embodiments, the present invention may provide a method for reducing plaque occurrence, gingivitis, tenderness, unpleasant odor in the oral cavity, erosion, cavities, calculus and staining by administering to the oral cavity of an individual a composition. comprising fused silica and peroxide. In some embodiments, the present invention provides a method for reducing plaque, gingivitis, tenderness, unpleasant odor in the oral cavity, erosion, cavities, calculus and staining by first administering to the oral cavity a composition which does not comprise a peroxide, and then of a composition comprising a fused silica and a peroxide. In some embodiments, the composition may be in a single phase. In some embodiments, the composition may comprise an oxidizing agent and one or more of a fluoride ion source, zinc ion source, calcium ion source, phon phosphate source, potassium ion source, strontium ion source, aluminum ion, magnesium ion source, or combinations thereof. In some embodiments, the composition may comprise an oxidizing agent and chelating agent selected from the group consisting of polyphosphates, polycarboxylates, Dolivinyl pyrrolidone, polyvinyl alcohol, polymeric polyether, Dolimeric alkyl phosphate, polyvinyl ether copolymers and maleic anhydride, polyphosphonates and mixtures thereof. In some embodiments, the composition may comprise an oxidizing agent and an oral care active agent selected from the group consisting of bactericidal agents, antiplaque agents, anti-inflammatory agents, anti-caries agents, anti-calculating agents, anti-erosion agents, unpleasant odor agents, antisensitivity, nutrients, analgesic agents, anesthetic agents, H-1 and H-2 antagonists, antiviral actives and combinations thereof. In some embodiments, the bactericidal agent may be selected from the group consisting of cetylpyridinium chloride, chlorhexidine, hexithidine, triclosan, metal ions, essential oils and mixtures thereof.

Bactericidal Agent Microbicidal agents may be included in the dentifrice compositions of the present invention. Such agents may include, but are not limited to, cationic bactericides such as chlorhexidine, alexidine, hexetidine, benzalkonium chloride, domiphene bromide, cetylpyridinium chloride (OCR), tetradecylpyridinium chloride (CTP), N-tetradecyl-4 chloride -ethylpyridinium [CTDEP), octenidine, bisbiguanides, zinc or tin ion agents, grapefruit extract, and mixtures thereof. Other bactericidal and microbicidal agents include, but are not limited to: 5-chloro-2- (2,4-dieloro phenoxy) -phenol, commonly called triclosan, 8-hydroxy quinoline and its salts, copper II compounds including, but not limited to: limited to, copper chloride (ll), copper sulfate (ll), copper acetate (ll), copper fluoride (ll) and copper (II) hydroxide, phthalic acid and their salts including, but not limited to to those disclosed in US Patent No. 4,994,262, including magnesium monopotassium phthalate, sanguinarine, salicylanilide, iodine, sulfonamides, phenolics, delmopinol, octapinol and other piperidine derivatives, niacin, nystatin, apple extract, thyme oil, thymol preparations , antibiotics such as augmentin, amoxicillin, tetracycline, doxycycline, minocycline, metronidazole, neomycin, kanamycin, cetylpyridinium chloride and clindamycin, analogs and salts thereof, methyl salicylate, hydrogen peroxide, ciorite metal salts, ethyl cocoi l Pyrrolidone arginate, ethyl arginate lauroyl monochloride and mixtures of all of the above. In another embodiment, the composition comprises phenolic microbicidal compounds and mixtures thereof. The microbicidal components may be present in a content of from about 0.001% to about 20% by weight of the buccal treatment composition. In another embodiment, the microbicidal agents generally correspond to from about 0.1% to about 5% by weight of the oral care compositions of the present invention.

Other antimicrobial agents may be, but are not limited to, essential oils. Essential oils are volatile aromatic oils, which may be synthetic or derived from plants by distillation, expression or extraction, and which commonly carry the odor or taste and aroma of the plant from which they are obtained. Useful essential oils may provide antiseptic activity. Some of these essential oils also act as flavoring agents. Useful essential oils include, but are not limited to, citra, thymol, menthol, methyl salicylate (wintergreen oil), eucalyptol, carvacrol, camphor, anethole, carvone, eugenol, isoeugenol, limene, osimene, n-decyl alcohol , citronella, a-salpineoi, methyl acetate, citronellyl acetate, methyl eugenol, cineol, linalol, ethyl linalaol, safrola vaniilina, peppermint oil, mint oil, lemon oil, sage oil, Rosemary, Cinnamon Oil, Pepper Oil, Bay Oil, Cedar Leaf Oil, Gerianol, Verbenone, Anise Oil, Bay Oil, Benzaldehyde, Bergamot Oil, Bitter Almond, Chlorothymol, Cinnamic Aldehyde, Citronella Oil, clove oil, coal tar, eucalyptus oil, guaiacol, tropolone derivatives such as hyquinitiol, lavender oil, mustard oil, phenol, phenyl salicylate, pine oil, pine needle oil, sassafras oil, lavender, sturge, thyme oil, bals I love tolu, terpentine oil, clove oil and combinations thereof. In one embodiment, the essential oils are selected from thymol, methyl salicylate, eucalyptus !, menthol and combinations thereof.

In one embodiment of the present invention there are disclosed oral care compositions comprising a blend of naturally occurring flavoring ingredients or essential oils (EOs) containing such flavoring ingredients, the blend having excellent microbicidal activity and comprising at least two components, being a first component selected from acyclic or non-ring structures such as citral, nerai, geraniai, geraniol and nerol, and a second component selected from cyclic or ring-based structures such as eucalyptol, carvacrol and eugenol. The essential oils may be used to obtain the flavoring ingredients mentioned above, including oils of grass, citrus (orange, lemon, lime), citronella, geranium, rose, eucalyptus, oregano, laurel and clove. However, it may be preferable for the flavoring ingredients to be obtained as individual or purified chemicals rather than being supplied to the composition by the addition of natural oils or extracts, as these sources may contain other components which may be unstable in combination with other ingredients. other components of the composition, or may introduce flavoring notes that are incompatible with the desired taste profile, resulting in a less organoleptically acceptable product. Natural oils or extracts that have been purified or concentrated to contain primarily the one or more desired components are most preferred for use in the present invention.

Preferably, the blend comprises 3, 4, 5 or more of the above components. The greater the number of different components mixed together, the greater the synergy achieved in microbicidal efficacy, provided that the blend comprises at least one ringless structure and one ring structure. A preferred blend comprises at least two ring structures or at least two ring structures. For example, a blend comprising two ringless structures (neral and geranium from citrus) and eugenol as the ring structure will be highly preferred for its effectiveness against buccal bacteria. Another preferred blend comprises three ringless structures (geraniol, neral and geranial) and two ring structures (eugenol and eucalyptol). Examples of this type of blending are discussed in more detail in published application US 2008 / G253976A1.

Other bactericidal agents may be basic amino acids and salts. Other embodiments may comprise arginine.

Antiplaque Agent The dentifrice compositions of the present invention may include an anti-plaque agent such as stannous salts, copper salts, strontium salts, magnesium salts, carboxylated polymer copolymers such as Gantrez, or a dimethicone copolyol. Dimethicone copolyol is selected from C12 to C20 alkyl dimethicone copolyols, and combinations thereof. In one embodiment, dimethicone copolyol is cetyl dimethicone copolyol available under the tradename Abil EM90. In one embodiment, the dimethicone copolyol may be present in a content of from about 0.001% to about 25%, in another embodiment from about 0.01% to about 5%, and in another embodiment from about 0% to about 25%. 1% to about 1.5% by weight of the oral care composition.

Anti-Inflammatory Agent Anti-inflammatory agents may also be present in the dentifrice compositions of the present invention. Such agents may include, but are not limited to, non-steroidal antiinflammatory agents (NSAIDs), cranberries, salicylates, propionic acids, acetic acids, and starches. These NSAIDs include, but are not limited to, ketorolac, flurbipro-haem, ibuprofen, naproxen, indomethacin, diclofenac, etodolac, indome-tacin, sulindac, tolmetin, ketoprofen, phenoprofen, piroxicam, nabutometone, aspirin, mechatrofenisa mefenamic acid, oxifembutazone, phenyl butazone and acetaminophen. The use of NSAIDs as ketorolac is claimed in US Patent No. 5,626,838. This document presents methods for preventing and / or treating primary and recurrent squamous cell carcinoma of the oral cavity or oropharynx by topically administering to the oral cavity or oropharynx an effective amount of one um. Suitable steroidal anti-inflammatory agents include corticosteroids such as fiucinolone and hydrocortisone. Nutrients Nutrients may improve oral cavity conditions, and may be included in the dentifrice compositions of the present invention. These nutrients include minerals, vitamins, oral nutritional supplements, enteral nutritional supplements and mixtures thereof. Useful minerals include calcium, phosphorus, zinc, manganese, potassium and combinations thereof. Vitamins can be included with minerals or used independently. Suitable vitamins include vitamins C and D, thiamine, riboflavin, calcium pantothenate, niacin, folic acid, nicotinamide, pyridoxine, cyanocobalamin, para-amino benzoic acid, bioflavonoids and combinations thereof. Oral nutritional supplements include amino acids, lipotropics, fish oil and mixtures thereof. Amino acids include, but are not limited to, L-tryptophan, L-lysine, methionine, threonine, ievocarnitine or L-carnitine, and combinations thereof. Lipotropics include, but are not limited to, choline, inositol, betaine, linoleic acid, linolenic acid and mixtures thereof. Fish oil contains large amounts of omega-3 (N-3) polyunsaturated fatty acids, eicosapentaenoic acid and docosaexaenoic acid. Enteral nutritional supplements include, but are not limited to, protein products, glucose polymers, corn oil, turmeric oil, and medium chain triglycerides. Minerals, vitamins, oral nutritional supplements and enteral nutritional supplements are described in more detail in "Drug Facts and Comparisons", by Wolters Kluer Company, St. Louis, MO, USA , © 1997, pages 3 to 17 and 54 to 57.

Antioxidants Antioxidants are generally recognized as useful in toothpaste compositions. Antioxidants are presented in texts such as The Handbook of Antioxidants, by Cadenas and Packer, © 1996 by Marcei Dekker, Inc. Antioxidants useful in the present invention include, but are not limited to, vitamin E, ascorbic acid, uric acid, carotenoids, vitamin A, flavonoids and polyphenols, herbal antioxidants, melatonin, aminoindols, lipoic acids and mixtures thereof.

Analgesic and Anesthetic Agents Analgesic or desensitizing agents may also be present in the dentifrice compositions of the present invention. Painkillers are pain-relieving agents, acting centrally to raise the pain threshold without disturbing consciousness or altering other sensory modalities. Such agents may include, but are not limited to: strontium chloride, potassium nitrate, sodium fluoride, sodium nitrate, acetanilide, phenacetin, acetorphan, thiorphan, spiradoline, aspirin, codeine, thebaine, levorphenol, hydromorphone, oxymorphone, phenazocine , fentaniia, buprenorphine, butafanol, nalbuphine, pentazocine, natural herbs such as gall, walnut, cubebin, galangal, scutellar, Liangmianzhen (Zanthoxylum nitidum) and Baizhi (Radix Angelicae Dahuricae). Topical anesthetic or analgesic agents such as sodium acetaminophen salicylate, trolamine salicylate, lidocaine and benzocaine may also be present. These analgesic assets are described in detail in Kirk-Othmer's Encyclopedia of Chemical Technology, Fourth Edition, Volume 2, Wiley-Interscience Publishers (1992), pages 729 to 737.

H-1 and H-2 Antagonists and Antiviral Actives The present invention may also optionally comprise selective H-1 and H-2 antagonists, including compounds disclosed in US Patent No. 5,294,433. Antiviral actives useful in the present composition include any actives that are routinely used to treat viral infections. These antiviral actives are presented in Drug Facts and Comparisons, Wolters Kluer Company, © 1997, pages 402 (a) -407 (z). Specific examples include antiviral actives disclosed in US Patent No. 5,747,070, issued May 5, 1998. Said patent discloses the use of stannous salts for virus control. Stannous salts and other antiviral actives are described in detail in Kirk & Othmer's Encyclopedia of Chemical Technology, Third Edition, Volume 23, Wiley-Interscience Publishers (1982), pages 42-71. Stannous salts which may be used in the present invention would include organic stannous carboxylates and inorganic stannous halides. Although stannous fluoride may be used, it is typically used only in combination with another stannous halide or one or more stannous carboxylates or another therapeutic agent.

Chelating Agent The present compositions may optionally contain chelating agents, also called chelating or sequestering agents, many of which also have anti-calculus activity or tooth adhesion activity. The use of chelating agents in oral care products is advantageous for their ability to complex with calcium as found in bacterial cell walls. Chelating agents can also disrupt plaque development by removing calcium from calcium bridges that help keep this biomass intact. Chelating agents also have the ability to form complexes with metal ions and thus help to avoid their adverse effects on the stability or appearance of products. Chelation of ions, such as iron or copper, helps retard oxidation deterioration of end products.

In addition, chelators can in principle remove stains by bonding to tooth surfaces, thereby displacing color residues or chromogens. The retention of such chelators may also prevent staining due to disturbance of the color residue binding sites on the dental surfaces.

As a result, chelators can help mitigate blemish formation and optimize cleanliness. A chelator can help optimize cleaning as fused silica and abrasives clean mechanically, while chelating can help provide chemical cleaning. As fused silica is a good mechanical cleaner, more stain may be removed, so a chelator may be desired to maintain, suspend, or complex with the stain so that it is not able to re-lodge on the surface. dental. Additionally, the chelator can coat the tooth surface to help prevent the formation of new stains.

Chelators may be desired for addition to formulations containing cationic bactericidal agents. The addition of chelators to tin-containing formulations may be desirable. The chelator is able to help stabilize the tin and keep a greater amount of it bioavailable. The chelator may be used in tin-containing formulations that have a pH above about 4.0. In some formulations, tin may be stable without the use of a chelator as it is more stable with fused silica compared to precipitated silica.

Suitable chelating agents include soluble phosphate compounds such as phytates and linear polyphosphates having two or more phosphate groups, including tripolyphosphate, tetrapolyphosphate and hexametaphosphate, among others. Preferred polyphosphates are those having the number of phosphate groups n averaging from about 6 to about 21, such as those known commercially as Sodaphos (no. 6), Hexaphos (no. 13) and Glass H (no. 21). . Other polyphosphorylated compounds may be used in addition to or instead of polyphosphate, in particular polyphosphorylated inositol compounds such as phytic acid, myo-inositol pentaquis (dihydrogen phosphate), myo-inositol tetrakis (dihydrogen phosphate), myo-inositol trichis ( phosphate) and an alkali metal, alkaline earth metal or ammonium salt thereof. Preferred for use in the present invention is phytic acid, also known as myo-inositol 1,2,3,4,5,6-hexaquis (dihydrogen phosphate) or inositol hexaphosphoric acid, as well as its metal salts alkaline, alkaline earth metal or ammonium metal. In the present invention, the term "phytate" includes phytic acid and its salts, as well as other polyphosphorylated inositol compounds. The amount of chelating agent present in the compositions will depend on the chelating agent to be used and typically will be from at least about 0.1% to about 20%, preferably from about 0.5% to about 10%, and more preferably from about 1.0% to about 7%. Still other phosphate compounds which are useful in the present invention for the ability to bind, solubilize and transport calcium are the organophosphate-based surface active compounds described above. , useful as teeth adhering agents and including organic phosphate mono, di or triesters.

Other suitable agents with chelating properties for use in plaque, stone and spot control include polyphosphonates described in US Patent Nos. 3,678,154 to Widder et al., 5,338,537 to White, Jr., and 5,451 to Zerby. et al., carbonyl diphosphonates in US patent no. No. 3,737,533 to Francis, acrylic acid polymer or copolymer in US Patent No. 4,847,070, issued July 11, 1989 to Pyrz et al., And US Patent No. 4,661,341, issued April 28, 1987 to Benedict et al., Sodium alginate in US Patent No. 4,775,525, issued October 4, 1988 to Pera, polyvinyl pyrrolidone in GB 741,315, WO 99/12517 and US Patent No. 5,538,714 to Pink et al. and vinyl pyrrolidone-carboxylate copolymers in US Patent No. 5,670,138 to Venema et al. and in Lion Corporation publication JP No. 2000-0633250.

Still other chelating agents suitable for use in the present invention are anionic polymeric polycarboxylates. Such materials are well known in the art and are employed in the form of their free acids, or partially or preferably fully neutralized water soluble alkaline metal (e.g. potassium and preferably sodium) or ammonium salts. Examples are 1: 4 to 4: 1 copolymers of anhydride or maleic acid with another polymerizable ethylenically unsaturated monomer, preferably methyl vinyl ether (methoxy ethylene) having a molecular weight (MW) of from about 30,000 to about 1,000. 000.

Such copolymers are available, for example, under the name Gantrez® AN 139 (PM 500,000), AN 119 (PM 250,000) and pharmaceutical grade S-97 (PM 70,000) from GAF Chemicals Corporation.

Other operational polymeric polycarboxylates include 1: 1 maleic anhydride copolymers with ethyl acrylate, ethyl hydroxy methacrylate, N-vinyl-2-pyrrolidone or ethylene, the latter being available, for example, under the name Monsanto EMA No. 1103, MW 10,000 and EMA Grade 61, and 1: 1 acrylic acid copolymers with methyl or hydroxy ethyl methacrylate, methyl or ethyl acrylate, isobutyl vinyl ether or N-vinyl-2-pyrrolidone.

Additional operating polymeric polycarboxylates are disclosed in U.S. Patent No. 4,138,477, issued to Gaffar on February 6, 1979, and U.S. Patent No. 4,183,914, issued to Gaffar et al. on January 15, 1980, and include styrene maleic anhydride copolymers with styrene, isobutylene or ethyl vinyl ether, polyacrylic, polytaconic and polyaminoic acids, and sulfoacrylic oligomers as low as 1,000, available under the name Uniroyal ND-2.

Other suitable chelators include polycarboxylic acids as well as salts of these substances described in Smitherman U.S. Patent Nos. 5,015,467, 5,849,271 and 5,622,689, both as tartaric acid, citric acid, gluconic acid, malic acid, succinic acid, disuccinic acid as well as salts thereof such as gluconate and sodium or potassium citrate, combination of citric acid / alkali metal citrate, disodium tartrate, dipotassium tartrate, sodium potassium tartrate, hydrogen tartrate hydrogen, potassium hydrogen tartrate, sodium monosuccinate tartrate acid or salt, potassium disuccinate tartrate and mixtures thereof. In some embodiments, there may be mixtures or combinations of chelating agents.

Teeth Bonding Agent The present invention may include a teeth bonding agent. For the purposes of this application, teeth adhering agents are also included as chelators. Suitable agents may be polymeric surface active agents (PMSAs), including polyelectrolytes, more specifically anionic polymers. PMSAs contain anionic groups, for example phosphate, phosphonate, carboxy or mixtures thereof, and thus have the ability to interact with cationic or positively charged entities. The "mineral" descriptor is intended to convey the idea that the surface activity or adhesion of the polymer is directed to mineral surfaces such as calcium phosphate minerals present in teeth.

PMSAs are useful in the present compositions because of their many benefits, such as stain prevention. PMSAs are believed to provide a stain prevention benefit due to their reactivity to, or adherence to, mineral or dental surfaces, resulting in the desorption of portions of unwanted adsorbed biological film proteins, in particular those associated with the binding of residues of teeth staining, the development of stones and the attraction of undesirable microbial species. Retention of these PMSAs on teeth may also prevent staining due to disturbance of the bonding sites of color residues on dental surfaces.

The ability of PMSAs to bind to stain-promoting ingredients in oral care products such as stannous ions and cationic microbicides is also believed to be useful. PMSA also provides dental surface conditioning effects, which produce desirable effects on the surface thermodynamic properties and surface biological film properties, which give an aesthetics of enhanced cleansing sensation, either during rinsing or drying. brushing like, which is of utmost importance then the same. Many of these polymeric agents are also known to provide tartar control benefits when included in oral compositions, thereby optimizing both tooth appearance and tactile impression for consumers.

PMSAs include any agents that have a strong affinity for the dental surface, which deposit a polymer layer or coating on the dental surface and produce the desired surface modification effects. Suitable examples of such polymers are polyelectrolytes such as condensed phosphorylated polymers, polyphosphonates, copolymers of phosphate or phosphonate-containing monomers or polymers with other monomers as ethylenically unsaturated and amino acid monomers, or with other polymers such as proteins, polypeptides, polysaccharides, poly (acrylates). ), poly (acrylamide), poly (methacrylate), poly (ethacrylate), poly (hydroxy alkyl methacrylate), poly (vinyl alcohol), poly (maleic anhydride), poly (maleate) poly (amide), poly (ethyl) amine), poly (ethylene glycol), poly (propylene glycol), poly (vinyl acetate) and poly (vinyl benzyl chloride), polycarboxylates and carboxy substituted polymers, as well as mixtures thereof. Suitable polymeric mineral surface active agents include the carboxy-substituted alcohol polymers described in U.S. Patent Nos. 5,292,501, 5,213,789, 5,093,170, 5,009,882 and 4,939,284, all issued to Degenhardt et al. and diphosphonate derivatized polymers in US Patent No. 5,011,913 to Benedict et al., the synthetic anionic polymers include polyacrylates and copolymers of anhydride or maleic acid and methyl vinyl ether (e.g., Gantrez®) as described herein by for example, in US Patent No. 4,627,977 to Gaffar et al. A preferred polymer is diphosphonate modified polyacrylic acid. Active polymers need to be sufficiently prone to surface bonding so that they desorb the proteins from the biological film and remain attached to the enamel surfaces. For dental surfaces, polymers with phosphate or phosphonate functions in the terminal or side chain are preferred, although other polymers with mineral binding activity may be effective depending on the affinity for adsorption. . Additional examples of phosphonate-containing polymeric mineral surface active agents include the gemine diphosphonate polymers disclosed as anti-calculation agents in US Patent 4,877,603 to Degenhardt et al, phosphonate group-containing copolymers disclosed in US 4,749,758 to Dursch et al. and GB 1,290,724 (both assigned to Hoechst) suitable for use in detergent and cleaning compositions, and copolymers and cotelomers presented as useful for applications including scale formation and corrosion inhibition, coatings, cements and resins tonic in US 5,980,776 to Zakikhani et al., and US 6,071,434 to Davis et al. Additional polymers include water-soluble copolymers of vinyl phosphonic acid and acrylic acid, as well as salts thereof set forth in GB 1,290,724, with the copolymers containing from about 10% to about 90% by weight of acid. phosphonic vinyl and from about 90% to about 10% by weight acrylic acid, and more particularly the copolymers have a ratio of the weight of vinyl phosphonic acid to the weight of acrylic acid of 70% vinyl phosphonic acid for 30% acrylic acid, 50% vinyl phosphonic acid to 50% acrylic acid, or 30% vinyl phosphonic acid and 70% acrylic acid. Other suitable polymers include the water-soluble polymers presented by Zakikhani and Davis, prepared by co-limiting diphosphonate or polyphosphonate monomers, having one or more unsaturated C = C bonds (e.g. vinylidene-1,1-diphosphonic acid and 2- (hydroxyphosphinyl) ethylidene-1,1-diphosphonic acid, with at least one other compound having unsaturated C = C bonds (e.g. acrylate and methacrylate monomers): Suitable polymers include the available diphosphonate / acrylate polymers Rhodía under the designation ITC 1087 (average MW 3,000 to 60,000) and Polymer 1154 (average MW 6,000 to 55,000).

A preferred PMSA will be stable in the presence of other components of the oral care composition such as ionic fluoride and metal ions. Also preferred are polymers which have limited hydrolysis in high water formulations, thus allowing a single and single phase formulation for the dentifrice or mouthwash. If PMSA does not have these stability properties, one option is to use a dual-phase formulation with the polymeric mineral surface active agent separate from fluoride or other incompatible components. Another option is to formulate non-aqueous, essentially non-aqueous or water-limited compositions to minimize the reaction between PMSA and the other components.

A preferred PMSA is a polyphosphate. A polyphosphate is generally understood to consist of two or more phosphate molecules arranged primarily in a linear configuration, although some cyclic derivatives may be present. Although the pyrophosphates (n = 2) are technically polyphosphates, the desired polyphosphates are those having about three or more phosphate groups, so that surface adsorption at effective concentrations produces sufficient unbound phosphate functions, which increases the anionic charge. surface as well as the hydrophilic character of the surfaces. Desired inorganic polyphosphate salts include tripolyphosphate, tetrapolyphosphate and bexametaphosphate, among others. Polyphosphates larger than tetrapolyphosphate usually occur as amorphous glassy materials. Preferred in the present compositions are linear polyphosphates having the formula; wherein X is sodium, potassium or ammonium and n has an average value of from about 3 to about 125. Preferred polyphosphates are those having n with an average of about 6 to about 21, such as those commercially known as Sodaphos (n = 6), Hexaphos (# 13), and Glass H (# 21), and produced by FMC Corporation and Astaris. These polyphosphates may be used alone or in combinations. Polyphosphates are susceptible to hydrolysis in high water formulations at acid pH, particularly at pH below 5. Thus, it is preferred for longer chain polyphosphates, in particular Glass H, with an average chain length of about 21. These longer chain polyphosphates, when hydrolyzed, are believed to produce shorter chain polyphosphates, which are still effective for deposition on the teeth, offering a benefit of stain prevention.

Also useful as teeth-bonding agents are non-polymeric phosphate compounds, in particular polyphosphorylated inositol compounds such as phytic acid, myo-inositol pentaquis (dihydrogen phosphate), myo-inosite! tetrakis (dihydrogen phosphate), myo-inositol triquis (dihydrogen phosphate) and an alkali metal, alkaline earth metal or ammonium salt thereof. Preferred for use in the present invention is phytic acid, also known as myo-inositol 1,2,3,4,5,6-hexaquis (dihydrogen phosphate) or inositol hexa-phosphoric acid, as well as metal salts thereof. alkaline, alkaline earth metal or ammonium metal. In the present invention, the term "phytate" includes phytic acid and its salts, as well as other polyphosphorylated inositol compounds.

Other phosphate-based surface active compounds useful as tooth adhering agents include organophosphates such as phosphate mono, di or triesters, as described in the same application and published in US20080247973A1. Examples include mono, di and trialkyl and alkyl (poly) alkoxy phosphates such as dodecyl phosphate, lauryl phosphate, lauret-1 phosphate, lauret-3 phosphate, lauret-9 phosphate, dilauret-10 phosphate trilauret-4 phosphate, 012-18 PEG-9 phosphate and salts thereof. Many are commercially available from suppliers including Croda, Rhodia, Nikkol Chemical, Sunjin, Alzo, Huntsman Chemical, Clariant and Cognis. Some preferred agents are polymeric, for example those containing repeating alkoxy groups as a polymer moiety, in particular 3 or more ethoxy, propoxy isopropoxy or butoxy groups.

Additional suitable polymeric organophosphate-based agents include dextran phosphate, polyglycoside phosphate, alkylpo-liglycoside phosphate, polyglyceryl phosphate, alkyl polyglyceride phosphate, polyether phosphates and alkoxylated polyol phosphates. Some specific examples are PEG phosphate, PPG phosphate, PPG alkyl phosphate, PEG / PPG phosphate, PEG / PPG alkyl phosphate, PEG / PPG / PEG phosphate, dipropylene glycol phosphate, glyceryl PEG phosphate, PBG (polybutylene glycol), PEG cyclodextrin phosphate, PEG sorbitan phosphate, alkyl sorbitan PEG phosphate and methyl glycoside PEG phosphate.

Additional suitable non-polymeric phosphates include alkyl monoglyceride phosphate, alkyl sorbitan phosphate, alkyl methyl glycoside phosphate and alkyl sucrose phosphate.

Other useful tooth adhering agents include carboxylic acid functionalized siloxane polymers as disclosed in US Patent Nos. 7,025,950 and 7,166,235, both of which are assigned to The Procter & Gamble Go. These polymers comprise a hydrophobic siloxane backbone. and pendant anionic moieties containing carboxy groups, and have the ability to deposit on surfaces from aqueous based or essentially non-aqueous based formulations, forming a substantially hydrophobic coating on the treated surface. Carboxy-functionalized siloxane polymers are believed to bind to and form a polar surface on them by electrostatic interaction, that is, complex formation between the pendant carboxy groups with calcium ions present in the teeth. Carboxy groups thus serve to anchor the siloxane polymer backbone to a surface, thereby modifying it to be hydrophobic, which then confers a variety of purpose benefits to that surface, such as ease of cleaning, removal and prevention of stains, bleaching, etc. The functionalized carboxy siloxane polymer further acts to accentuate the deposition of active agents on the surface, and to optimize the retention and effectiveness of these actives on the treated surface.

Water soluble or water dispersible polymeric agents prepared by copolymerizing a mixture of one or more vinyl pyrrolidone (VP) monomers with a mixture of one or more alkenyl carboxylate (AC) monomers are also useful as teeth-adhering agents. ), specifically C 2 -C 12 alkenyl esters of straight or branched chain saturated C 1 -C 19 alkyl carboxylic acids described in US Patent No. 6,682,722, assigned to the same applicant. Examples include vinyl pyrrolidone copolymers with a mixture of one or more of vinyl acetate, vinyl propionate or vinyl butyrate. Preferred polymers have an average molecular weight in the range of from about 1,000 to about 1,000,000, preferably from 10,000 to 200,000, and most preferably from 30,000 to 100,000. The amount of tooth-bonding agent will typically be in the range of from about 0.1% to about 35% by weight of the total buccal composition. In dentifrice formulations, the amount is preferably about 2% to about 30%, more preferably from about 5% to about 25%, and most preferably from about 6% to about 20%. In mouthwash compositions, the amount of tooth-bonding agent is preferably in the range of from about 0.1% to about 5% and more preferably from about 0.5% to about 3%. .

Additional Assets Additional actives suitable for use in the present invention may include, but are not limited to, insulin, steroids, herbal derivatives and other herbal derivatives. Additionally, antigenic or gum care agents known in the art may also be included. Components that give a clean feel to the teeth may optionally be included. Such components may include, for example, sodium bicarbonate or Glass H. In addition, it is recognized that in certain forms of therapy, combinations of these agents mentioned above may be useful for obtaining an optimal effect. Therefore, for example, an antimicrobial and an anti-inflammatory agent may be combined into a single dentifrice composition to provide combined effectiveness.

Optional agents to be used include materials known as synthetic anionic polymers, including polyacrylates and copolymers of anhydride or maleic acid and methyl vinyl ether (e.g., Gantrez), as described, for example, in US Patent No. 4,627,977, as well as, for example, polyamino propanesulfonic acid (AMPS), zinc citrate trihydrate, polyphosphates (eg tripolyphosphate, hexametaphosphate), diphosphonates (eg EHDP, AHP), polypeptides (such as polyaspartic and polyglutamic acids), and mixtures thereof. same. Additionally, the dentifrice composition may include a polymer-based carrier such as those described in US Patent Nos. 6,682,722 and US 6,589,512, and in US Patent Applications No. 10 / 424,640 and US No. 10 / 430,617.

Other Optional Ingredients Buffering agents The dentifrice compositions may contain a buffering agent. For use in the present invention, the term "buffering agents" refers to agents that may be used to adjust the pH of toothpaste compositions within a range of from about pH 3.0 to about pH 10. Buffering agents include hydroxides of toothpaste. alkali metal, ammonium hydroxide, organic ammonium compounds, carbonates, sesquicarbonates, borates, silicates, phosphates, imidazole and mixtures thereof. Specific buffering agents include monosodium phosphate, trisodium phosphate, sodium benzoate, benzoic acid, sodium hydroxide, potassium hydroxide, alkali metal carbonate salts, sodium carbonate, imidazole, pyrophosphate salts, sodium gluconate, ionic acid, sodium lactate, citric acid and sodium citrate. Buffering agents are used in a content of from about 0.1% to about 30%, preferably from about 0.1% to about 10%, and more preferably from about 0.3% to about 30%. 3% by weight of toothpaste compositions.

Coloring Agent Coloring agents may also be added to the present composition. The coloring agent may be in the form of an aqueous solution, preferably 1% coloring agent in a water solution. Pigments, pearlizing agents, fillers, talc, mica, magnesium carbonate, calcium carbonate, bismuth oxychloride, zinc oxide and other materials capable of creating a visual change in toothpaste compositions may also be used. Colored solutions and other agents generally comprise from about 0.01% to about 5% by weight of the composition. Titanium dioxide may also be added to the present composition. Titanium dioxide is a white powder that gives opacity to the compositions. Titanium dioxide generally comprises from about 0.25% to about 5% by weight of the composition.

Flavoring Agent Suitable flavoring components include wintergreen oil, clove bud oil, menthol, anethole, methyl salicylate, eucalyptol, cassia, menthyl 1-acetate, sage, eugenol, parsley oil, oxanone, alpha -irisone, marjoram, lemon, orange, guaetol propenyl, cinnamon, vanillin, ethyl vanillin, heliotropin, 4-cis-heptenyl, diacetyl, methyl-to-butyl phenyl acetate, cranberry, chocolate, green tea and mixtures thereof. Essential oils may also be included as flavoring agents, and are described above in the discussion of bactericidal agents. Refrigerants may also be part of the flavoizante composition. Suitable refrigerants for the present compositions include paramentan carboxy amide based agents such as N-ethyl-p-mint-3-carboxamide (commercially known as WS-3, WS-23, WS-5), MGA, TK- 10, Physcool, and mixtures thereof. Release agents, heating agents, desensitizing agents and other optional materials may be used to provide a signal while the buccal composition is used. Due to the interactivity of precipitated silicas, flavor components can become entrapped or emulsified, in effect disappearing to the point where they are not perceived by a user. In contrast, the lack of interactivity of fused silica can affect the amount of a flavor component that needs to be added for a noticeable effect. In some embodiments, the amount of flavoring agent present by weight of the composition may be about 10%, about 20% or about 50% less than comparable precipitated silica formulations, while obtaining the same. flavor impact.

A flavoring composition is generally used in oral care compositions in contents of from about 0.001% to about 5% by weight of the oral care composition. Preferably the flavoring composition will be present in an amount from about 0.01% to about 4%, more preferably from about 0.1% to about 3%, and more preferably from about 0.01% to about 4%. 0.5% to about 2% by weight.

Similarly, refrigerants may not be absorbed as much in the present compositions, meaning that they may have a longer duration, or may be used in smaller amounts. Essential oils may also be less absorbed, so that smaller amounts can be used to achieve the same effectiveness. Fused silica may not bind to the taste receptor as precipitated silica does, which means that the taste receptor may be more accessible to the flavoring agent.

Other aesthetic benefits may be apparent to users, such as a clean mouth sensation and an increased perception of sweetness or freshness, for example. The improved mouth feel of smoothness and cleanliness may contribute to a lower perception of dry mouth, and the improved cleanliness provided by fused silica can help remove muscine layers and increase the perception of hydration. A further aesthetic benefit to the consumer may be the optimization of rinse removal from the buccal composition due to the fact that inert fused silica particles do not form lumps, remaining dispersed while the user brushes their teeth. Yet another potential benefit is optimized foaming. Again, since fused silica is less reactive than precipitated silica, surfactants are more available and optimized foaming may result.

Some embodiments may comprise a TRPV1 activator, a vanilloid receptor 1 transient potential receptor activator, which is a non-selective ligand-controlled cation channel, preferably expressed in small diameter sensory neurons and which detects noxious substances as well as other substances. By adding a TRPV1 activator to a mouthwash composition with an unpleasant taste component, the composition user can experience an improvement in taste compared to a mouthwash composition without the TRPV1 activator. Thus, the TRPV1 activator functions to compensate for the unpleasant taste associated with many components used in oral care compositions. These activators can not only compensate for unpleasant tastes, but can also reduce the perception of dryness by limiting the mouth's ability to perceive such dryness. In one embodiment, the TRPV1 activator comprises vanyl butyl ether, zingerone, capsaicin, capsiato, chogaol, gingerol, piperine or a combination thereof. In one embodiment, a TRPV1 activator will be added in an amount from about 0.0001% to about 0.25% by weight of the oral care composition. Sweetener Sweetening agents may be added to the compositions. These include sweeteners such as saccharin, dextrose, sucrose, lactose, xylitol, maltose, levulose, aspartame, sodium cyclamate, D-tryptophan, dihydrocalconas, acuifam, sucralose, neotame and mixtures thereof. Various coloring agents may also be incorporated into the present invention. Sweetening agents are generally used in buccal compositions in contents of from about 0.005% to about 5% by weight of the composition.

Thickeners Additional thickeners, such as polymeric thickeners, may be used. Suitable thickening agents are polymers of carboxyvinyl, carrageenan, hydroxy ethyl cellulose, laponite and water soluble salts of cellulose ethers such as sodium carboxymethyl cellulose and sodium carboxy methyl hydroxy ethyl cellulose. Natural gums such as caraia, xanthan, arabic and tragacanth can also be used. Colloidal aluminum magnesium silicate or finely divided silica may also be used as part of the thickening agent to further enhance texture. Other thickeners may include alkylated polyacrylates, alkylated cross-linked polyacrylates or gel networks. The thickening agents may include polymeric polyether compounds such as polypropylene or polyethylene oxide (molecular weight 300 to 1,000,000), terminated with alkyl or acyl groups containing from 1 to about 18 carbon atoms.

A suitable class of thickening or gelling agents includes a class of acrylic acid homopolymers crosslinked with a pentaerythritol alkyl ether, a sucrose alkyl ether, or carbomers. Carbomers are commercially available from B.F. Goodrich under the serial name Carbopol®. In particular, they include Carbopol 934, 940, 941, 956, and combinations thereof.

Lactide and glycololfide monomer-based copolymers of molecular weight in the range of about 1,000 to about 120,000 (numerical average) are useful for application of assets into or around periodontal pockets as a "carrier". subgingival gel ". Such polymers are described in US Patent Nos. 5,198,220, 5,242,910 and 4,443,430.

Due to the interaction of precipitated silica with other formulation components, precipitated silica can affect the rheology of a composition over time. Fused silica, however, due to its lack of interaction with other formulation components, has little impact on rheology. This means that mouthwash formulations formulated with fused silica are more stable over time which, among other things, may allow better cleaning and better predictability. Thus, in some embodiments the thickening agents, their combinations and quantities, may be very different from those of traditional toothpastes. In the present invention, the thickening agents may be used in an amount from about 0% to about 15%, or from about 0.01% to about 10%, or in another embodiment from about 0.1% to about 15%. about 5% by weight of the total buccal composition.

In some embodiments of the present invention, the composition may comprise a thickening agent selected from natural and synthetic sources. In some embodiments, the thickening agent may be selected from the group consisting of clay, laponite and mixtures thereof. In some embodiments, the composition may further contain a thickening agent selected from the group consisting of carboxyvinyl polymers, carrageenan, hydroxy ethyl cellulose, water-soluble salts of cellulose ethers such as sodium carboxy methyl cellulose, cross-linked carboxy methyl cellulose, hydroxy sodium cellulose, cross-linked starch, natural gums such as caraia gum, xanthan gum, arabic gum and tragacanth gum, aluminum magnesium silicate, silica, alkylated polyacrylates, alkylated cross-linked polyacrylates and mixtures thereof.

Other possible thickeners include carbomers, hydrophobically modified carbomers, carboxy methyl cellulose, cetyl / stearyl alcohol, sodium alginate, gum gelana, acylated gelatin, sodium hydroxy propyl starch phosphate, microcrystalline cellulose, microfibrous cellulose, crosslinked pyrrolidone polyvinyl, cetyl ethyl cellulose, cross-linked acryloyl methyl propane, sulfonic acid and copolymers, as well as mixtures thereof. The viscosity of the composition at the time it is produced may remain as the viscosity of the composition or, in other words, the composition may have a stable viscosity. For viscosity to be considered stable, it typically changes no more than about 5% after 30 days. In some embodiments, the viscosity of the composition does not change by more than about 5% after about 30 days, by more than about 10% after about 30 days, by more than about 20% after about 30 days, or by more than about 50% after about 90 days. Because the unstable viscosity problem over time is more pronounced in low water formulations, in some embodiments, the compositions of the present invention may contain less than about 20% total water, or less than about 10% of total water.

Gel nets A gel net can be used in the oral composition. The gel mesh may be used to structure the buccal composition or to assist in the release of an active, flavoring or other reactive material. The gel mesh may be used to structure, i.e. thicken or provide the desired rheology to molten silica buccal compositions alone or in combination with another thickening or structuring agent. A gel mesh composition has a rheology that may be advantageous for fused silica since fused silica is denser than some other abrasives or materials present in the buccal composition. Because molten silica is heavier or denser, it may separate or leave the composition or solution more easily than other less dense materials. This can happen when the composition is diluted with water. For example, when a toothpaste is used for brushing, it is diluted with water when it is in the mouth. The dilution rheology for a dentifrice containing a gel network that aids in its structuring may be higher than that of dentures structured with more typical polymeric materials or thickeners. Higher dilution rheology is beneficial in keeping molten silica suspended and allowing it to participate more fully in the cleaning process. If a material such as abrasive is not suspended or retained in the composition after dilution, the cleaning efficiency, such as the cleaning ratio of the biological film, may decrease. Additionally, as a larger amount of abrasive or fused silica is suspended, the buccal composition may contain a smaller total of abrasives, since a larger amount of the abrasive is able to participate in cleaning. Figure 13 shows PCR and RDA data for gel mesh structured compositions, compared to compositions which are not gel mesh structured but thickened with typical polymeric binders. As shown, the PCR score increases from 92.5 to 127.56 and from 95.44 to 121.04 when a gel network is used in a formula containing 15% fused silica. This increase in PCR of greater than about 10%, about 15%, about 20%, or about 25% may be due to the ability of gel nets to suspend a larger amount of fused silica during cleaning. Although cleaning scores increase, abrasion remains within acceptable ranges.

The buccal compositions of the present invention may comprise a dispersed gel network. For use in the present invention, the term "gel network" refers to a lamellar or vesicular solid crystalline phase comprising at least one fatty amphiphile, at least one surfactant and a solvent. The lamellar or vesicular phase comprises bilayers formed by a first layer comprising fatty amphiphil and secondary surfactant, alternating with a second layer comprising solvent. For the lamellar crystalline phase to form, the fatty amphiphile and secondary surfactant must be dispersed within the solvent. The term "solid crystalline" for use in the present invention refers to the structure of the lamellar or vesicular phase that forms at a temperature below the melt temperature of the chain to the gel network layer comprising one or more amphiphils. Fatty. Gel nets suitable for use in the present invention are described in more detail in US 2008 / 0081023A1, which describes the materials, methods of preparation and uses of gel nets. Additionally, US 2009 / 0246151A1 also describes gel nets and a method for producing the gel nets containing compositions. The gel network present in the buccal composition may be used to structure the buccal composition. The structure provided by the gel network offers the desired rheology or viscosity by thickening the buccal composition. Structuring can be done without the need to use polymeric thickening agents, although polymeric thickeners or other agents than the gel network may be used to structure the buccal composition. Since molten silica produces little or no thickening compared to typical precipitated silica, thickening of the buccal composition can benefit more from a gel network used to structure the buccal composition. The small or no effect of fused silica on the viscosity or thickening of the buccal composition may also provide the benefit that a buccal composition may be formulated with a gel network or other thickening system and thus, as much molten silica may be added as much. if desired, without having to readjust the thickening level, as would be necessary if the amount of precipitated silica were adjusted. The gel mesh component of the present invention comprises at least one fatty amphiphile. For use in the present invention, the term "fatty amphiphile" refers to a compound that has a hydrophobic tail group and a hydrophobic polar group that does not make the compound water soluble (immiscible), the compound also having a neutral net charge at the pH of the buccal composition. Fatty amphiphile may be selected from the group consisting of fatty alcohols, alkoxylated fatty alcohols, fatty phenols, alkoxylated fatty phenols, fatty amides, alkoxylated fatty amides, fatty amines, alkylamido fatty alkylamines, alkoxy fatty amines, carbamate oxides grease, fatty acids, alkoxylated fatty acids, fatty diesters, sorbitan fatty esters, sugar fatty esters, methyl glycoside esters, glycol fatty esters, mono, di and triglycerides, polyglycerine fatty esters, alkyl glyceryl ethers, fatty acid esters propylene glycol fat, cholesterol, ceramides, silicone fatty waxes, glucose fatty amides, phospholipids and combinations thereof. Suitable fatty amphiphiles include a combination of cetyl alcohol and stearyl alcohol. The gel network also comprises a surfactant. One or more surfactants are combined with the fatty amphiphile and oral carrier to form the gel network of the present invention. The surfactant is typically water soluble or miscible in the solvent or oral vehicle. Suitable surfactants include anionic, zwiterionic, amphoteric, cationic and nonionic surfactants. In one embodiment, anionic surfactants such as sodium lauryl sulfate are preferred. Surfactants may consist of a combination of more than one type of surfactant, such as an anionic and nonionic surfactant. The gel network will probably also comprise solvents such as water or other suitable solvents. Together, the solvent and surfactant contribute to the expansion of fatty amphiphil. This in turn leads to the formation and stability of the gel network. In addition to forming the gel network, the solvent can help prevent the toothpaste from hardening after exposure to air, and can provide a moist mouthfeel. For use in the present invention, the term "solvent" refers to suitable solvents that may be used in place of, or combined with, water to form the gel network of the present invention. Suitable solvents for the present invention include water, edible polyhydric alcohols such as glycerine, diglycerine, triglycerine, sorbitol, xylitol, butylene glycol, erythritol, polyethylene glycol, propylene glycol and combinations thereof. Sorbitol, glycerine, water and combinations thereof are preferred solvents.

To form a gel network, the buccal compositions may comprise fatty amphiphil in an amount from about 0.05% to about 30%, preferably from about 0.1% to about 20%, and more preferably. from about 0.5% to about 10% by weight of the buccal composition. The amount of fatty amphiphile will be chosen based on the formation of the gel network and the composition of the buccal formulation. For example, a buccal composition containing smaller amounts of water may require about 1% of a fatty amphiphil while a buccal composition containing larger amounts of water may require 6% or more of a fatty amphiphile. The amount of surfactant and solvent required to form the gel network will also vary based on the materials chosen, the function of the gel network, and the amount of fatty amphiphile. The surfactant as part of the gel mesh phase is typically present in an amount of from about 0.01% to about 15%, preferably from about 0.1% to about 10%, and more preferably. about 0.3% to about 5% by weight of the buccal composition. In some embodiments, a water-diluted surfactant solution is used. In one embodiment, the amount of surfactant is chosen based on the desired foaming level in the buccal composition, and the irritation caused by the surfactant. The solvent may be present in an amount suitable to obtain a gel network when combined with the fatty amphiphile and the surfactant according to the present invention. The buccal compositions may comprise at least about 0.05% by weight of the buccal composition of a solvent. The solvent may be present in the buccal composition in an amount from about 0.1% to about 99%, from about 0.5% to about 95%, and from about 1% to about 90%.

Humectant Humectant can help prevent toothpaste from hardening after exposure to air, and can provide a moist mouthfeel. An additional humectant or solvent may be added to the oral carrier phase. Suitable humectants for the present invention include water, edible polyhydric alcohols such as glycerine, sorbitol, xylitol, butyl glycol, polyethylene glycol, propylene glycol, and combinations thereof. Sorbitol, glycerin, water and combinations thereof are preferred humectants. The humectant may be present in an amount from about 0.1% to about 99%, from about 0.5% to about 95%, and from about 1% to about 90%.

Surfactants A surfactant may be added to the toothpaste composition. Surfactants, also called foaming agents, may aid in cleaning or foaming the dentifrice composition. Suitable surfactants are those reasonably stable and foaming over a wide pH range. The surfactant may be anionic, nonionic, amphoteric, zwiterionic, cationic or mixtures thereof.

Examples of anionic surfactants useful in the present invention include water soluble alkyl sulfate salts having from 8 to 20 non-radical carbon atoms. alkyl (e.g. sodium alkyl sulfate) and the water soluble fatty acid sulfonated monoglyceride salts having from 8 to 20 carbon atoms. Sodium lauryl sulfate (SIS) and coco monoglyceride sodium sulfonates are examples of such anionic surfactants. Examples of other suitable anionic surfactants are sarcosinates, such as sodium lauroyl sarcosinate, taurates, sodium lauryl sulphoacetate, sodium lauroyl isethionate, sodium lauret carboxylate and sodium dodecyl benzene sulfonate. Anionic surfactant mixtures may also be employed. Many suitable anionic surfactants are disclosed in US Patent No. 3,959,458 to Agricola et al., Issued May 25, 1976. In some embodiments, the buccal treatment composition may comprise an anionic surfactant at a content of about 0.025%. to about 9%, from about 0.05% to about 5% in some embodiments, and from about 0.1% to about 1% in other embodiments.

Another suitable surfactant is selected from the group consisting of sarcosinate based surfactants, isethionate based surfactants and taurate based surfactants. Preferred for use in the present invention are alkali metal or ammonium salts of such surfactants such as the sodium and potassium salts of the following; lauroyl sarcosinate, myristoyl sarcosinate, palmitoyl sarcosinate, stearoyl sarcosinate and oleoyl sarcosinate. The sarcosinate surfactant may be present in the compositions of the present invention in contents of from about 0.1% to about 2.5%, or from about 0.5% to about 2.0%, by weight of the total amount. composition.

Cationic surfactants useful in the present invention include derivatives of aliphatic quaternary ammonium compounds with a long alkyl chain containing from about 8 to 18 carbon atoms, such as lauryl trimethyl ammonium chloride, cetylpyridinium chloride, cetyl trimethyl ammonium bromide, of diisobutyl phenoxy ethyl dimethyl benzii ammonium, coconut nityl trimethyl ammonium nitrite, cetylpyridinium fluoride, etc. Preferred compounds are quaternary ammonium fluorides described in US Patent No. 3,535,421 of October 20, 1970 to Briner et al., Wherein said quaternary ammonium fluorides have detergent properties. Certain cationic surfactants may also act as germicides in the compositions of the present invention.

Nonionic surfactants that may be used in the compositions of the present invention include compounds produced by the condensation of alkylene oxide groups (hydrophilic in nature) with an organic hydrophobic compound, which may be aliphatic or alkylaromatic in nature. Examples of other suitable nonionic surfactants include pluronics, polyethylene oxide condensates of ethyl phenols, products derived from ethylene oxide condensation with the ethylene oxide propylene oxide reaction product, ethylene oxide condensates from alcohols, acids and aliphatic esters, long chain tertiary amine oxides, long chain tertiary phosphine oxide, long chain diacyl sufoxides and mixtures thereof.

The zwitterionic synthetic surfactants useful in the present invention include aliphatic quaternary ammonium derivatives, phosphonium and sulfonium based compounds in which the aliphatic radicals may be straight chain or branched, and wherein one of the aliphatic substituents contains from about 8 to about 18 carbon atoms and one contains an anionic water solubilizing group, for example carboxy, sulfonate, sulfate, phosphate or phosphonate.

Suitable betaine surfactants are disclosed in US Patent No. 5,180,577 to Polefka et al. Issued January 19, 1993. Typical alkyl dimethyl betaines include decyl betaine or 2- (N-decii-N) acetate. , N-dimethyl ammonium), coconut betaine or 2- (N-coco-N, N-dimethyl ammonium) acetate, crystalline betaine, palmityl betaine, lauryl betaine, cetyl betaine, stearyl betaine, etc. Starch betaines are exemplified by cocoamido ethyl betaine, cocoamido propyl betaine, lauramido propyl betaine and the like. Preferred betaines are preferably cocoamido propyl betaine and more preferably lauramido propyl betaine. Precipitated silica tends to reduce foaming of an buccal composition. In contrast, fused silica, with its low reactivity, does not inhibit foaming, or does not inhibit it to a degree similar to that of precipitated silica. The absence of interference with surfactant components can impact the amount of surfactant used, which in turn may affect other variables. For example, if less surfactant is required to achieve consumer acceptable foaming, this may reduce irritation (a known negative point of SLS for the consumer), or may reduce the pH of the composition, which would allow better absorption of fluoride.

In some embodiments, polymeric mineral surface active agents are added to mitigate the negative aesthetic aspects of these compounds. The polymeric mineral surface active agents may be organophosphate polymers which, in some embodiments, are alkyl phosphate esters or salts thereof, ethoxylated alkyl phosphate esters and salts thereof, or mixtures of alkyl phosphate esters or salts thereof. In some embodiments, the polymeric mineral surface active agents may be polycarboxylates or polyphosphates or polymeric carboxylate copolymers such as Gantrez.

In some embodiments, the composition may comprise a fused silica and be essentially SLS free. Essentially free means that there is less than about 0.01% by weight of the composition. In some embodiments, the composition may further contain a surfactant in addition to SLS, selected from the group consisting of a nonionic surfactant, an anionic surfactant, a cationic surfactant, an amphoteric surfactant, a zwitterionic surfactant and mixtures thereof. In some embodiments, the composition may further contain a chelator. In some embodiments, the surfactant may be an amphoteric surfactant, such as betaine. In some embodiments, the composition may have a PCR of at least about 80. In some embodiments, the surfactant may be at least about 50% available. In some embodiments, the composition has less than 3% by weight of the composition of a surfactant. In some embodiments, the composition may further contain a source of peroxide and / or enzymes. Some embodiments may consist of a method for treating a dry mouth condition by administering to the buccal cavity of the subject a buccal composition comprising fused silica, the composition being essentially free of sodium lauryl sulfate. Method of Use The present invention also relates to methods for cleaning and polishing teeth. The method of use of the present invention comprises bringing the dental enamel surfaces and buccal mucosa of an individual into contact with the buccal compositions according to the present invention. The method of treatment may be brushing with a toothpaste, or rinsing with a toothpaste fluid paste or mouthwash. Other methods include contacting the individual's teeth and oral mucosa with a topical mouth gel, mouth spray, toothpaste, toothpaste, tooth gel, dental powders, tablets, subgingival gel, foam, mousse, chewing gum, lipstick, sponge, dental floss, petrolatum gel, or denture or other forms. Depending on the embodiment, the buccal composition may be used as often as a toothpaste, or may be used less frequently, for example weekly, or may be used by a practitioner in the form of a prophylactic paste or other intensive treatment.

Additional Data Figures 7 to 13 provide more detailed data on the material properties of fused silica, as well as its compatibility with other components of the oral care composition and its cleanability.

Figures 7 (a) and 7 (b) are compositions of the formula and their corresponding compatibility with tin, zinc and fluorine. Figure 7 (a) shows the compositions for buccal treatment, formula A comprising precipitated silicas, and formula B comprising fused silica. Figure 7 (b) shows the compatibility data for both formula A and formula B at 25 ° C and 40 ° C after 2 weeks, 1 month and 2 months, shown as a percentage of compatibility. The data in Figure 7 show that the fused silica composition offers superior stability and compatibility with tin, zinc and fluorine.

It may be desirable to have oral zinc salt compositions wherein the composition has a zinc availability greater than about 82%, 85%, 87 or 90% after two weeks of storage at 25 ° C. Availability of 82%, 85%, 87%, or 90% may be desirable to remain even before consumer use. Consequently, availability can be measured before use. The term "before use" may mean that the product was produced, packaged and distributed to a store or end customer, but before the end customer used the product. Storage conditions and temperatures during this time may vary.

It may be desirable to have straight-flowing buccal compositions, with the composition having a fluoride availability greater than about 88%, 90%, 91%, 92%, 93% or 94% after two weeks of storage at 25Â °. Ç. It may also be desirable for fluoride availability to remain greater than about 88%, 90%, 91%, 92%, 93% or 94% prior to use. For some formulations, fluoride availability may remain greater than 95% prior to use. It may be desirable to have mouthwash compositions which have a tin compatibility or availability greater than about 55%, 80%, 65%, 70%, 75%, 80%, 85% or 90% after two weeks. storage weeks at 25 ° C. In addition, it may be desirable for tin compatibility or availability to remain greater than about 55%, 60%, 65%, 70%, 75%, 80%, 85% or 90% prior to use. In some compositions, the availability or compatibility of tin may be at least about 92%. For tin-fused silica formulations, tin compatibility will typically be about 20% to about 50%, about 25% to about 45%, or about 30% to about 40% higher than that of formulations with comparable amounts of precipitated silica and tin. Figure 8 shows tin compatibility as a function of load. The greater the amount of precipitated silica, the less free or bioavailable tin. The table shows that the loss of tin for precipitated silica (Z-119) is 0.0081 g / g Z-119 (or 80 ppm / 1% Z-119 loading). In contrast, the tin loss for the fused silica is 0.001 g / g Tecosil 44CSS (or 10 ppm / 1 wt% Tecosil 44CSS). In some embodiments, depending on the surface area, the loss of tin for the fused silica is from about 5 to about 50 ppm / 1% load of fused silica, from about 7 to about 30 ppm / 1% load molten silica, from about 8 to about 20 ppm / 1% molten silica filler, or from about 10 to about 15 ppm / 1% molten silica filler.

Figures 9 (a) and 9 (b) are compositions containing peroxide and compatibility data. Figure 9 (a) shows peroxide containing compositions with various precipitated and fused silicas. Figure 9 (b) shows the peroxide compatibility of the compositions at 40 ° C, initially after 6 days, and after 13 days. The data show higher peroxide compatibility of fused silicas as compared to precipitated silicas. In some embodiments, peroxide compatibility is at least about 50%, at least about 60%, at least about 70%, at least about 80%, or at least about 85%, after about 13%. days at 40 ° C. In other words, in some embodiments, after about 13 days at 40 ° C, at least about 50%, 60%, 70% or 85% of the peroxide or oxidizing agent may remain. The method for sample preparation is as follows; Transfer 18 g of gel peroxide base to a plastic container, carefully mix 2 g of silica with a spatula, measure the pH of the mixture, divide the mixture into two equal parts and place one part at 25 ° C and the other at 40 ° C. ° C, place samples in the stability chamber at 25 ° C and 40 ° C. The analysis of the sample is as follows; take an initial sample for peroxide analysis, remove samples from the stability chambers at 5 and 12 days, allow to equilibrate for 1 day, remove 0.2 g of samples from each mixture and return the remaining samples to the stability chamber, perform peroxide analysis as set forth below; weigh 0.2000 g (+/- 0.0200 g) of the peroxide gel in a 250 ml plastic beaker, add the stir bar and 100 ml of 0.04 N H2SO4, cover with Parafilm, shake for at least 10 minutes, add 25 mL of 10% KCl solution and 3 drops of NH4-moibdate, and stir for an additional 3 to 20 minutes, analyze via autotitre with 0.1 N Na-thiosulfate. Compatibility is defined as the percentage of peroxide after 13 days at 40 ° C, divided by the initial peroxide percentage 'and then multiplied by 100. As is well known to those skilled in the art, a product placed at 40 ° C represents storage shelf extended. That is, for example, one month at 40 ° C would equal approximately eight months at room temperature. Figure 10 (a) shows formulas A through E which are buccal compositions comprising fused silica and peroxide. Figure 1G (b) shows the change in brightness (AL) of bovine enamel samples after a given number of brushing motions for two of the compositions in figure 10 (a) with fused silica and peroxide compared to a formula with silica. fused but without peroxide (formula F), and a formula without fused silica or peroxide (Crest Cavity Protection toothpaste). The data demonstrate that a combination of fused silica and peroxide provides superior cleaning and bleaching. In some embodiments, delta L may be greater than about 4.5 in 50 movements, greater than about 6.0 in 100 movements, greater than about 9.0 in 200 movements, or greater than about 15.0 movements. in 400 movements. In some embodiments, delta L may be about 50% to about 100% larger than Crest Cavity Protection toothpaste. The method is as follows: bovine enamel substrates are assembled and stained according to the conventional PCR protocol described by G.K. Stookey, et al., J. Dental Res., 61, 1236-9, 1982. Groups of 6 splinters are divided for each treatment step, with each group presenting approximately the same baseline level for the L value. 1: 3 fluids from the treatment paste, and stained bovine enamel substrates are brushed in 50, 100, 200 and 400 movements, and a calibrated force of 150 grams is exerted during brushing. After brushing with each number of movements, the substrates are captured and analyzed for L values. The change in L values is calculated as follows. Post-brush AL L ~ Pre-brush was statistically compared with the use of LSD. Figure 11 (a) shows formulas of dentifrice compositions comprising precipitated or fused silicas, and Figure 11 (b) shows the corresponding consumer perception data. The consumer perception test was performed with nine individuals who brushed twice with each product and provided through a written questionnaire information on the issues related to taste and aroma display and sensory impression in the mouth. Individuals were asked to provide information about their experiences during use, immediately after use and 15 minutes after use of the product. As shown in Figure 11 (b), in general, compositions comprising fused silica offer better flavor and aroma intensity, freshness, a feeling of smoothness in the teeth and a clean mouth compared to the precipitated silica used in Formula A. Figure 12 shows additional exemplary formulas of oral care compositions comprising fused silica. The formulas include compositions comprising a gel network, combinations of precipitated silica and calcium carbonate fused silica, compositions which are free of SLS, and compositions which may be used as a prophylactic paste or used on a non-daily basis. Figure 13 (a) shows sodium fluoride-based compositions in which formulas A and B comprise traditional thickener precipitated silicas, formulas C and D comprise traditional thickener fused silica, and formulas E and F comprise fused silica. with a gel network. Figure 13 (b) is a table of RDA and FCR values for the sodium fluoride-based compositions of Figure 13 (a), showing that the use of fused silica improves the cleanability of a composition, and that Using a gel mesh further enhances the cleanability of the composition, all with still acceptable abrasive capacity. Figure 13 (c) shows stannous fluoride-based compositions in embodiments similar to those of Figure 13 (a). Figure 13 (d) shows the corresponding RDA values for the compositions of figure 13 (c), indicating that the use of tin can decrease abrasion, and showing the possible strengthening of teeth by tin formulas.

Non-Limiting Examples The dentifrice compositions illustrated in the following examples show specific embodiments of the dentifrice compositions of the present invention, but are not intended to be a limitation thereto. Other modifications may be made by one skilled in the art without departing from the spirit and scope of this invention.

Example 1 Items A to D are typical buccal compositions comprising fused silica. Formula B shows a combination of fused and precipitated silicas, and Formula D a combination of fused silica and calcium carbonate: Example II. Items A to F are typical buccal compositions comprising fused silica with cationic microbicides. Continued The dimensions and values set forth in the present invention should not be understood to be strictly limited to the exact numerical values mentioned. Instead, unless otherwise specified, each of these dimensions is intended to mean both the mentioned value and a functionally equivalent range of values around that value. For example, a dimension displayed as "40 mm" is intended to mean "about 40 mm".

All documents cited in the Detailed Description of the Invention are, in their relevant part, incorporated herein by reference, and the citation of any document should not be construed as an admission that it represents prior art with respect to the present invention. If there is a conflict between the meanings or definitions of terms mentioned in this document and the meaning or definition of terms in a document incorporated by reference », the meaning or definition attributed to a specific term mentioned in this document shall take precedence.

While specific embodiments of the present invention have been illustrated and described, it will be apparent to those skilled in the art that various other changes and modifications may be made without departing from the character and scope of the invention. Therefore, it is intended to cover in the appended claims all such changes and modifications that are within the scope of the present invention.

Claims (10)

A buccal treatment composition comprising: (a) from about 20% to about 50% by weight of the composition of fused silica, wherein said fused silica has a particle size D90 of less than about 50 microns and wherein at least 25% of the fused silica particles are spherical; b) from about 0.0025% to about 5.0% by weight of the composition of stannous fluoride; c) from about 0.001% to about 20% by weight of the composition of an antimicrobial agent; and d) from about 0.1% to about 20% by weight of the composition of a chelating agent. Composition according to Claim 1, characterized in that it has an RDA of less than about 150 µm. Composition according to Claim 1, characterized in that it has an RDA of less than about 120 ° C. Composition according to Claim 1, characterized in that the ratio of PCR to RDA is at least about 0.7. Composition according to Claim 1, characterized in that the ratio of PCR to RDA is at least about 0.9. Composition according to Claim 1, characterized in that the ratio of PCR to RDA is at least about 1.0. Composition according to Claim 1, characterized in that it has an RDA of less than about 170. Composition according to Claim 1, characterized in that it further comprises fused silica, with at least 25% of the fused silica particles being angular. Composition according to Claim 8, characterized in that the amount of angular fused silica is from about 1% to about 10% by weight of the composition. Composition according to Claim 1, characterized in that the average particle size of the fused silica is from about 3.0 microns to about 15.0 microns.