JP2577558B2 - Oral composition - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION [Industrial Application Field] The present invention relates to an oral composition, and more specifically, one or more selected from fluorides selected from the group consisting of pyridoxine and derivatives thereof. The present invention relates to a composition for oral cavity in which the effect of preventing dental caries is improved by one or more by combining one or more of the above-mentioned compounds.

[Prior Art] The effect of fluoride on caries prevention is widely recognized. Dental caries is a phenomenon in which the dentifrice is demineralized by organic acids such as lactic acid, which are produced by the oral bacteria, mainly Streptococcus mutans, which degrade sugars such as sucrose. is there. The main constituent of enamel is hydroxyapatite, but fluoride ions are easily incorporated into the crystal lattice of hydroxyapatite to improve its crystallinity. As a result, the tooth substance is strengthened, and the enamel is not easily demineralized even by the organic acid produced by the bacteria resident in the oral cavity, thereby preventing dental caries. It is also said that fluoride ions are more easily incorporated into early caries lesions where demineralization has progressed than in healthy enamel, promoting remineralization and inhibiting the progress of caries. .

Currently, fluoride such as sodium fluoride, sodium monofluorophosphate, stannous fluoride, etc.
It is used in methods such as fluoride addition to waterworks, fluoride tooth surface application method, fluoride mouthwash method, fluoride-added dentifrice and the like.

[Problems to be Solved by the Invention] However, at present, dental caries is still widespread, and the effect of preventing dental caries is not always satisfactory with conventional fluoride alone. It is the present situation that has been eagerly awaited.

In view of the above circumstances, the present inventors have conducted intensive studies in pursuit of a further caries prevention effect, and as a result, added one or more selected from the group consisting of pyridoxine and its derivatives to conventional fluoride. Then, it has been found that fluoride ions are efficiently taken in by hydroxyapatite, and it has been found that the dentin strengthening action of fluoride is enhanced, and the present invention has been completed.

[Means for Solving the Problems] That is, the present invention comprises one or more selected from fluoride and one or more selected from the group consisting of pyridoxine and its derivatives, One or two or more kinds selected from the group consisting of pyridoxine and derivatives thereof are mixed with one or more kinds selected from fluoride in a ratio of 1/50 to 10 times (molar ratio). And a composition for oral cavity.

 Hereinafter, the configuration of the present invention will be described in detail.

The fluoride used in the present invention is a compound containing fluorine (F), which is an element very common in the living world,
Sodium fluoride, potassium fluoride, lithium fluoride,
Cesium fluoride, zirconium fluoride, ammonium fluoride, stannous fluoride, sodium monofluorophosphate,
Inorganic fluorides such as potassium monofluorophosphate, sodium titanium fluoride, potassium potassium titanium fluoride, hexylamine hydrofluoride, laurylamine hydrofluoride, cetylamine hydrofluoride, glycine hydrofluoride, lysine hydrofluoride, alanine One or more of organic fluorides such as hydrofluoride and fluorosilane are used, but sodium fluoride, potassium fluoride, ammonium fluoride, stannous fluoride, and monofluorocarbon are used in the oral cavity. Sodium phosphate and potassium monofluorophosphate are preferred.

The compounding amount of these fluorides is 50 to 10,000 ppm (μg / g, the same applies hereinafter), preferably 200 to 10,000 ppm, as the total fluorine concentration in the oral composition. If it is less than 50 ppm, the effect of adding one or more selected from the group consisting of pyridoxine and its derivatives cannot be expected, and if it exceeds 10,000 ppm, the effect does not increase much and is uneconomical.
In the case of manufacturing dentifrice, the total fluorine concentration is
It is desirable that the content be 1000 ppm or less.

Pyridoxine used in the present invention is a substance represented by the following formula.

In general is said that vitamin B _6, anti-dermatitis factor, but there is a growth-promoting factor of microorganisms, nothing is known about the effect of the combination with fluoride.

Examples of the pyridoxine derivative include pyridoxal having an aldehyde group at the 4-position, pyridoxamine having an ethylamine group at the 4-position, and various salts thereof such as phosphate esters and hydrochlorides thereof. Particularly, pyridoxine hydrochloride is preferred.

In the composition for oral cavity of the present invention, one or more kinds are appropriately selected and used from the group consisting of the above pyridoxine and its derivatives.

The compounding amount is 1/50 to 10 times, preferably 1/20 to 5 times, more preferably 1/10 to 3 times the molar ratio of fluoride. If it is less than 1/50 times, the effect of enhancing the action of the fluoride used in combination cannot be expected, and if it exceeds 10 times, the effect does not increase so much and is uneconomical.

In the oral composition of the present invention, depending on the type of the oral composition in addition to the above essential components, dicalcium phosphate.
Dihydrate and anhydride, monobasic calcium phosphate, tribasic calcium phosphate, calcium carbonate, calcium pyrophosphate, titanium oxide, aluminum hydroxide, aluminum oxide, amorphous silica, crystalline silica, anhydrous alkali metal silicate complex salt, etc. Silica-based abrasive, aluminum silicate,
Abrasives such as insoluble sodium metaphosphate, insoluble potassium metaphosphate, insoluble calcium polyphosphate, tertiary magnesium phosphate, magnesium carbonate, magnesium sulfate, calcium sulfate, polymethyl methacrylate, bentonite, zirconium silicate, hydroxyapatite, synthetic resin, etc. Wetting agents such as glycerin, sorbitol, propylene glycol, polyethylene glycol, ethylene glycol, 1,3-butylene glycol, xylitol, maltitol, lactitol, carboxymethylcellulose, methylcellulose, hydroxyethylcellulose, sodium carboxymethylhydroxyethylcellulose, sodium alginate, carrageenan, Sodium polyacrylate, gum arabic, xanthan gum, gum tragacanth, Thickeners such as aya gum, polyvinyl alcohol, carboxyvinyl polymer, and polyvinylpyrrolidone; water-soluble salts of alkyl sulfates having 8 to 18 carbon atoms such as sodium lauryl sulfate and sodium myristyl sulfate; sodium lauryl monoglyceride sulfate; coconut oil fatty acid monoglyceride Sodium sulfate, water-soluble higher fatty acid monoglyceride sulfate having 10 to 18 carbon atoms in the fatty acid group such as sodium fatty acid monoglyceride sulfate, α-olefin sulfate, paraffin sulfate, N-methyl-N-palmitoyl tauride Anionic activators such as sodium salt, sodium N-lauroyl sarcosinate, sodium N-lauroyl-β-alanine, fatty acid alkanolamides such as lauric acid diethanolamide, sucrose mono and dilaurate Sucrose fatty acid esters such as sucrose, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene fatty acid esters, polyoxyethylene hydrogenated castor oil derivatives, lactose fatty acid esters, lactitol fatty acid esters, maltitol fatty acid esters, polyoxyethylene polyoxypropylene block copolymers Nonionic surfactants such as nonionic surfactants, surfactants such as cationic surfactants and amphoteric surfactants, oils such as higher alcohols and waxes, lower alcohols, sodium saccharin, stepioside, neohesperidin dihydrochalcone, glycyrrhizin, perillartin, p-methoxy Sweetening agents such as cinnamaldehyde, essential oils such as peppermint, spearmint, fennel oil, and flavors such as 1-menthol, carvone, eugenol, and anethole Ingredients such as fragrances, dyes, preservatives and fungicides, anti-drugs, water, etc., dextranase, protease, ricinzyme, mutanase, mutastain, sorbic acid, alexidine, β-glycyrrhetinic acid, hinokitiol, dihydrocholesterin, epidihydro Cholesterin, alkyl glycine, alkyl diaminoethyl glycine salt, allantoin, ε-aminocaproic acid, tranexamic acid, azulene, other vitamins, water-soluble primary or secondary phosphates, quaternary ammonium compounds such as cetylpyridinium chloride Ingredients usually used in oral compositions, such as sodium chloride, active ingredients such as crude drug extracts, etc., can be blended.

Further, the dosage form of the oral composition of the present invention is also optional, and toothpastes such as toothpaste, powdered toothpaste, lubricating dentifrice, and water dentifrice, oral cleansing agents such as oral pasta and mouthwash, mouthwashes, topical It can be used as a coating agent, mouth freshener, chewing gum, dental floss, gargle such as troche and the like.

Although the pH of the oral composition of the present invention is not necessarily limited, it is preferably pH 3 to 10, more preferably pH 4 to 9, and particularly preferably pH 5 to 7.

[Effects of the Invention] Example 1 A predetermined amount of sodium fluoride and pyridoxine hydrochloride were added, and a composition adjusted to pH 4.5 with dilute hydrochloric acid or dilute sodium hydroxide was prepared. Synthetic hydroxyapatite powder was immersed in these compositions at 37 ° C for 5 minutes, then immersed in a calcification solution at 37 ° C for 60 minutes, filtered through a filter and dried. With respect to the synthetic hydroxyapatite powder thus treated, the fluorine concentration in the powder is measured by a micro-diffusion method, and the amount of calcium eluted by immersion in an acetate buffer at 37 ° C for 60 minutes is measured. The ash suppression rate was calculated to evaluate the acid resistance.

The results are shown in Table 1.

From the above results, when pyridoxine hydrochloride was used in combination with sodium fluoride, the amount of fluorine uptake and acid resistance of synthetic hydroxyapatite were significantly increased as compared with sodium fluoride alone, and pyridoxine hydrochloride was found to have an effect of enhancing the effect of sodium fluoride.

Example 2 A composition was prepared by adding a predetermined amount of fluoride and pyridoxine hydrochloride. In these compositions, bovine teeth whose surface is removed by polishing 200 μm to expose the enamel surface are immersed at 37 ° C. for 5 minutes, then immersed in a calcifying solution at 37 ° C. for 60 minutes, and then washed with tap water. And dried. The bovine teeth thus treated are measured for the fluorine concentration in the enamel by acidity detection method, and an acidic gelatin gel prepared by the method of Silverstone (Leon M. Silverstone (Leon M) .Silverstone); Caries Res .: 1: 261-274,1967｝ for 4 weeks, 8 weeks, and 15 weeks, then observed the state of demineralization by microradiography. Was scored to evaluate acid resistance.

◎ Demineralization is almost suppressed ○ Demineralization is suppressed to a certain extent △ Demineralization is considerable × No demineralization suppressing effect The results are shown in Table 2.

From the above results, when sodium fluoride and pyridoxine hydrochloride were used together, remarkable increase in fluorine uptake and remarkable suppression of demineralization of bovine enamel were observed compared to sodium fluoride alone, and the effect of sodium fluoride on pyridoxine hydrochloride was enhanced. An effect was observed.

As can be determined from Examples 1 and 2, the oral composition of the present invention can be used for preventing dental caries of a conventional fluoride by using one or more of pyridoxine and its derivatives in combination with fluoride. It is a very useful oral composition with enhanced effects.

[Examples] Next, the present invention will be specifically described with reference to Examples and Comparative Examples. The present invention is not limited to this. All amounts are% by weight.

Example 1 Toothpaste Dicalcium phosphate dihydrate 40.0 Glycerin 10.0 Sorbitol 10.0 Sodium carboxymethyl cellulose 1.5 Sodium lauryl sulfate 1.5 Saccharin sodium 0.1 Perfume 1.0 Sodium monofluorophosphate 0.76 Pyridoxine hydrochloride 1.0 Purified water Remainder The toothpaste was manufactured by the method.

Comparative Example 1 Toothpaste Comparative Example 1 was obtained in the same manner as in Example 1 except that pyridoxine hydrochloride was omitted from Example 1.

Comparative Example 2 Toothpaste Comparative Example 2 was obtained in the same manner as in Example 1 except that sodium monofluorophosphate and pyridoxine hydrochloride were omitted.

The toothpastes of Example 1, Comparative Example 1 and Comparative Example 2 were each diluted 1/10 with distilled water, and human extracted tooth enamel powder was immersed therein at 37 ° C. for 60 minutes and thoroughly washed. The mixture was filtered through a filter and dried. With respect to the human enamel powder thus treated, the fluorine concentration in the powder is measured by the microdiffusion method, and the amount of eluted calcium is measured by immersing the powder in an acetate buffer at 37 ° C. for 60 minutes. The ash suppression rate was calculated to evaluate the acid resistance.

The results are shown in Table 3.

As is clear from the above results, the toothpaste of the present invention was found to have extremely high fluorine uptake effect and demineralization inhibitory effect as compared with the comparative toothpaste.

Example 2 Toothpaste Silicic anhydride 20.0 Sorbitol 50.0 Carrageenan 0.5 Sodium carboxymethylcellulose 1.0 Sodium lauryl sulfate 1.8 Saccharin sodium 0.08 Methyl parahydroxybenzoate 0.2 Flavor 0.9 Sodium fluoride 0.2 Pyridoxine hydrochloride 0.2 Purified water Remaining Example 3 Toothpaste Sorbitol 20.0 Silicic anhydride 50.0 Sodium polyacrylate 0.7 Sodium lauryl sulfate 1.8 Triethanolamine 0.5 Sodium saccharin 0.1 Sodium parahydroxybenzoate 0.2 Flavor 0.9 Sodium monofluorophosphate 0.76 Pyridoxine hydrochloride 0.2 Allantoin 1.0 Purified water Remaining Example 4 Mouthwash Ethyl alcohol 10.0 Saccharin sodium 0.05 Flavor 0.8 Poly Oxyethylene (20 mol) Sorbitan laurate 1.0 Sodium fluoride 0.02 Pyridoxine hydrochloride 0.02 Purified water Remaining Example 5 Mouthwash Sodium fluoride 0.05 Pyridoxine hydrochloride 0.02 Disodium phosphate 0.3 Monosodium phosphate 0.7 Fragrance 0.5 Saccharin sodium 0.02 Purified water Remaining Example 6 Topical application sodium fluoride 2.0 Pyridoxine hydrochloride 1.0 Fragrance 0.5 Saccharin sodium 0.02 Purified water balance Example 7 Oral freshener (spray type) Ethyl alcohol 40.0 Saccharin sodium 0.1 Sorbitol 10.0 Perfume 1.0 Polyoxyethylene (60 mol) Hardened castor oil 0.7 Chlorhexidine hydrochloride 0.05 Sodium fluoride 0.05 Pyridoxine hydrochloride 0.5 Purified water Balance Example 8 Chewing gum Gum base 25.0 Calcium carbonate 2.0 Fragrance 1.0 Copper chlorophyll 0.05 Sodium fluoride 0.2 Pyridoxine hydrochloride 1.0 Sorbitol balance

Claims (1)

(57) [Claims] 1. One or more selected from fluorides containing one or more selected from fluorides and one or more selected from the group consisting of pyridoxine and derivatives thereof. In contrast, one or two or more selected from the group consisting of pyridoxine and its derivatives
An oral composition characterized by being blended at a ratio of 50 to 10 times (molar ratio).