JP7558059B2 - Oral Composition - Google Patents

Description

The present invention relates to an oral composition.

Bactericides contained in oral compositions such as dentifrices are important ingredients that reduce the number of pathogenic bacteria in the oral cavity and are effective in suppressing bad breath, preventing dental caries, and preventing periodontal disease. However, bactericides have a unique bitter taste. Due to this bitter taste, even if a cooling agent such as menthol is added, the cooling sensation is not felt when the oral composition is first used, and the bitter taste persists for a certain period of time after the start of use, which can significantly impair the feeling of use. For this reason, various efforts have been made to mask the bitter taste derived from bactericides.

Patent Document 1 relates to an oral composition containing a bactericide (isopropylmethylphenol), polyvinylpyrrolidone, a flavoring component (at least one selected from 3-octanol, 3-octyl acetate, and 3-octanone), and a surfactant, and discloses that the inclusion of polyvinylpyrrolidone in a specific ratio masks the unpleasant taste caused by the bactericide during tooth brushing. Patent Document 2 relates to a dentifrice composition containing ingredients effective in preventing periodontal disease (dextranase, tranexamic acid, and isopropylmethylphenol), an alkyl sulfate, and a flavoring component (menthol, anethole, and eugenol and/or thyme oil), and discloses that the inclusion of the flavoring component in a specific ratio masks the complex unpleasant taste after tooth brushing. Patent Document 3 relates to an oral composition containing a bactericide (cationic bactericide), a moisturizing/antibacterial agent (alkanediol), and a cooling agent (3-1-methoxypropane-1,2-diol and/or N-substituted-p-menthane-3-carboxamide), and discloses that the combined use of the moisturizing/antibacterial agent and the cooling agent masks the unpleasant taste derived from the bactericide immediately after application of the oral composition to the oral cavity. Patent Document 4 relates to an oral composition containing a bactericide and a flavoring (Japanese peppermint oil and N-(2-(2-pyridinyl)ethyl)-2-isopropyl-5-methylcyclohexanecarboxamide), and discloses that the combined use of peppermint oil and N-(2-(2-pyridinyl)ethyl)-2-isopropyl-5-methylcyclohexanecarboxamide masks the bitter taste derived from the bactericide after mouthwashing.

Patent No. 5493732 JP 2019-167297 A Patent No. 6740901 JP 2018-203645 A

In an oral composition, if the bitterness is suppressed and a suitable feeling of use such as a refreshing sensation due to a cooling agent at the start of use can be continuously realized, it will lead to continuous use of the oral composition, and as a result, it is expected that the bactericidal effect in the oral cavity will be improved. However, Patent Documents 1 to 4 do not disclose anything about the oral composition from the viewpoint of the sustainability of the refreshing sensation at the start of use and the effect of suppressing the bitterness.
The present invention has been made in consideration of the above circumstances, and has an objective to provide an oral composition which has a refreshing feeling when first used and can suppress and maintain the bitterness derived from the bactericide for a certain period of time from the start of use to after use (for example, in the case of dentifrice, from the start of tooth brushing to after tooth brushing).

That is, the present invention provides the following [1] to [12].
[1] A composition for the oral cavity comprising (A) a bactericide and (B) one or more members selected from the group consisting of ethyl-3-(p-menthane-3-carboxamide) acetate and N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide.
[2] The oral composition according to [1], wherein the component (A) is one or more bactericides selected from the group consisting of cationic bactericides, nonionic bactericides and anionic bactericides.
[3] The oral composition according to [1] or [2], wherein the component (A) is one or more bactericides selected from the group consisting of quaternary ammonium salts, biguanide bactericides, phenolic bactericides, cineole and acylsarcosine salts.
[4] The oral composition according to any one of [1] to [3], wherein the content of the (A) component is 0.001 to 0.5% by mass relative to 100% by mass of the oral composition.
[5] The oral composition according to any one of [1] to [4], wherein the content of the (B) component is 0.00001 to 0.1 mass% relative to 100 mass% of the oral composition.
[6] The oral composition described in any one of [1] to [5], further containing (C) a nonionic surfactant.
[7] The oral composition described in [6], wherein the (C) component is one or more nonionic surfactants selected from the group consisting of polyoxyethylene hydrogenated castor oil, polyoxyethylene alkyl ether, polyglycerin fatty acid ester, and polyoxyethylene polyoxypropylene copolymer.
[8] The oral composition according to [6] or [7], wherein the content of component (C) is 0.1 to 2 mass% relative to 100 mass% of the oral composition.
[9] The oral composition according to any one of [1] to [8], further comprising (D) a cooling agent.
[10] The oral composition according to [9], wherein the component (D) is menthol and/or carvone or an essential oil containing these.
[11] The oral composition according to [9] or [10], wherein the content of the (D) component is 0.001 to 1.5 mass% as the content of menthol and/or carvone relative to 100 mass% of the oral composition.
[12] The oral composition according to any one of [1] to [11], which is a dentifrice, a mouthwash, a spray, a topical agent, a patch, or an oral dissolving agent.

The present invention provides an oral composition that has a refreshing sensation when first used and can suppress the bitter taste of the bactericide for a certain period of time after use.

The present invention will be described in detail below.

The oral composition of the present invention contains the following components (A) and (B), and preferably further contains either or both of components (C) and (D). Note that in this specification, the content of each component is based on the amount of each component charged when the composition is produced.

[Component (A)]
The component (A) is a bactericide. By including the component (A), a bactericidal effect can be exhibited.

Examples of the (A) component include cationic disinfectants, nonionic disinfectants, and anionic disinfectants. As cationic disinfectants, quaternary ammonium salts and biguanide disinfectants are preferred, such as quaternary ammonium salts such as alkylpyridinium salts, benzyl long-chain alkyl short-chain dialkyl ammonium salts, and long-chain alkyl short-chain trialkyl ammonium salts; and biguanide disinfectants such as chlorhexidine salts. More specifically, examples include benzethonium chloride, benzalkonium chloride, depotassium chloride, cetylpyridinium chloride, stearyldimethylbenzylammonium chloride, lauryltrimethylammonium chloride, myristyltrimethylammonium chloride, cetyltrimethylammonium chloride, stearyltrimethylammonium chloride, chlorhexidine, chlorhexidine hydrochloride, chlorhexidine gluconate, and chlorhexidine acetate. Among these, benzethonium chloride, benzalkonium chloride, and cetylpyridinium chloride are particularly preferred. As nonionic bactericides, phenolic bactericides and cineole are preferred, for example, isopropylmethylphenol, hinokitiol, triclosan, thymol, thyme oil, 1,8-cineole, and eucalyptus oil. Of these, isopropylmethylphenol and hinokitiol are preferred as nonionic bactericides. As anionic bactericides, acyl sarcosine salts (e.g., alkali metal salts such as sodium salts) having an acyl group (e.g., an acyl group having 10 to 18 carbon atoms) are preferred, and sodium lauroyl sarcosine is preferred. These may be used alone or in combination of two or more.

From the viewpoint of exerting a bactericidal effect without strongly expressing the bitterness derived from the bactericide (hereinafter simply referred to as bitterness), the content of the (A) component is preferably 0.001% by mass or more, more preferably 0.005% by mass or more, based on the entire oral composition (100% by mass). This allows a good bactericidal effect to be obtained. The upper limit is preferably 0.5% by mass or less. This allows the expression of bitterness to be suppressed. Therefore, it is preferably 0.001 to 0.5% by mass, more preferably 0.005 to 0.5% by mass. Within the above range, when the (A) component contains a cationic bactericide, the content of the cationic bactericide is preferably 0.001 to 0.5% by mass, more preferably 0.005 to 0.2% by mass, based on the entire oral composition (100% by mass). When the (A) component contains a nonionic bactericide, the content of the nonionic bactericide is preferably 0.005 to 0.2% by mass, based on the entire oral composition (100% by mass). When component (A) contains an anionic bactericide, the content of the anionic bactericide is preferably 0.05 to 0.5% by mass relative to the entire oral composition (100% by mass).

[Component (B)]
The component (B) is one or more selected from the group consisting of ethyl-3-(p-menthane-3-carboxamide) acetate and N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide. By including the component (B), even if a bactericide is included, a refreshing sensation can be felt upon use, and bitterness can be suppressed and maintained for a certain period of time from the start of use to after use. In this specification, the term "refreshing sensation" refers to a sensation that is favorable for an oral composition, and does not refer only to a cold sensation, but also refers to a complex sensation including a refreshing feeling and a clean feeling.

The (B) component may be one type alone or a combination of two types, but it is preferable to include N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide. This can further improve the sustained bitterness suppression effect over a certain period of time from the start of use until after use.

The content of the (B) component is preferably 0.00001% by mass or more, more preferably 0.00005% by mass or more, based on the entire oral composition (100% by mass). This allows the bitterness suppression effect to be sustained for a certain period of time from the start of use. The content of the (B) component is preferably 0.1% by mass or less, more preferably 0.01% by mass or less, and particularly preferably 0.005% by mass or less, based on the entire oral composition (100% by mass). This allows the stimulation in the oral cavity and the decrease in the flavor expression of the flavoring (flavoring other than the cooling agent) to be suppressed. In other words, the content of the (B) component is preferably 0.00001 to 0.1% by mass, more preferably 0.00005 to 0.005% by mass, based on the entire oral composition (100% by mass).

[Component (C)]
The component (C) is a nonionic surfactant. By including the component (C), it is possible to suppress the decrease in the refreshing sensation at the start of use and to impart a sustained effect of suppressing bitterness over a certain period of time from the start of use to after use.

Examples of component (C) include polyoxyethylene alkyl ethers, polyoxyethylene hydrogenated castor oil, sorbitan fatty acid esters, polyoxyethylene sorbitan fatty acid esters (e.g., polyoxyethylene sorbitan monostearate), alkylolamides, polyoxyethylene fatty acid esters, polyoxyethylene alkenyl ethers, polyglycerin fatty acid esters, sucrose fatty acid esters (e.g., maltose fatty acid esters), sugar alcohol fatty acid esters (e.g., maltitol fatty acid esters, lactitol fatty acid esters), fatty acid diethanolamides (e.g., lauric acid mono- or diethanolamide), polyoxyethylene polyoxypropylene copolymers, and polyoxyethylene polyoxypropylene fatty acid esters. The number of carbon atoms in the alkyl chain of the polyoxyethylene alkyl ether is usually 14 to 18, and the average number of moles of ethylene oxide added is usually 5 to 30 moles. The average number of moles of ethylene oxide added in polyoxyethylene hydrogenated castor oil is usually 20 to 100 moles, preferably 20 to 60 moles. The number of carbon atoms in the fatty acid of the sorbitan fatty acid ester is usually 12 to 18. The number of carbon atoms in the fatty acid of the polyoxyethylene sorbitan fatty acid ester is usually 16 to 18, and the average number of moles of ethylene oxide added is usually 10 to 40 moles. The number of carbon atoms in the alkyl chain of the alkylolamide is usually 12 to 14. As a nonionic surfactant, polyoxyethylene hydrogenated castor oil is preferred. These may be used alone or in combination of two or more.

The lower limit of the content of the (C) component is preferably 0.1% by mass or more, more preferably 0.3% by mass or more, based on the entire oral composition (100% by mass). This allows the bitterness suppression effect to be well expressed. The upper limit is preferably 2% by mass or less, more preferably 1% by mass or less, and particularly preferably 0.8% by mass or less, based on the entire oral composition (100% by mass). This allows the decrease in the refreshing sensation at the start of use to be suppressed, and the bitterness suppression effect can be sustained for a certain period of time after use from the start of use. Therefore, the content of the (C) component is preferably 0.1 to 2% by mass, more preferably 0.3 to 1% by mass, and even more preferably 0.3 to 0.8% by mass, based on the entire oral composition (100% by mass).

[Component (D)]
The component (D) is a cooling agent. By including the component (D), a cooling sensation can be imparted and the feeling during use can be improved.

The cooling agent of component (D) is specifically menthol and/or carvone, and can be blended as a compound, but essential oils containing these can also be used. Examples of essential oils include peppermint essential oil, Japanese peppermint oil, and spearmint oil. Component (D) may be one type alone or two or more types may be combined. Of these, it is preferable to include either menthol or an essential oil containing menthol, or both, as this can impart a more refreshing feeling.

The content of component (D) is preferably 0.001% by mass or more, more preferably 0.01% by mass or more, as the content of menthol and/or carvone (including menthol and carvone in essential oils when essential oils are used), relative to the entire oral composition (100% by mass). The upper limit is usually 1.5% by mass or less, preferably 1.2% by mass or less, more preferably 0.8% by mass or less. Therefore, it is preferably 0.001 to 1.5% by mass, more preferably 0.001 to 1.2% by mass, and even more preferably 0.01 to 0.8% by mass.

[Optional ingredients]
The oral composition of the present embodiment may contain optional components other than the components (A) to (D) already described, as long as the effects of the present invention are not impaired.

Optional ingredients include, for example, abrasives, medicinal ingredients, surfactants other than component (C), binders, wetting agents, thickening agents, sweeteners, preservatives, pH adjusters, solvents, oily ingredients, colorants (pigments), and fragrances other than component (D). Specific details are explained below.

- Abrasives -
The abrasive may be either inorganic or organic. Examples of inorganic abrasives include abrasive silica such as precipitated silica, aluminosilicate, zirconosilicate, crystalline zirconium silicate, and titanium-bonded silica; calcium phosphate compounds such as calcium diphosphate dihydrate or anhydrous, calcium monophosphate, calcium triphosphate, and calcium pyrophosphate; calcium carbonate abrasives such as calcium carbonate; calcium abrasives other than carbonate/phosphate such as calcium hydroxide and calcium sulfate; aluminum materials such as aluminum oxide, aluminum hydroxide, and alumina; silicic acid materials such as anhydrous silicic acid, zeolite, and zirconium silicate; magnesium materials such as magnesium carbonate and magnesium triphosphate; apatite materials such as hydroxyapatite, fluoroapatite, and calcium-deficient apatite; titanium materials such as titanium dioxide, titanium mica, and titanium oxide; and minerals such as bentonite. Examples of organic abrasives include polymethyl methacrylate and synthetic resin abrasives. Among these, silica abrasives are preferred.

The content of the abrasive is usually 70% by mass or less, preferably 50% by mass or less, and more preferably 8 to 50% by mass, based on the total oral composition (100% by mass).

-Medicinal ingredients-
Examples of medicinal ingredients include enzymes such as dextranase, mutanase, amylase, protease, and Liteque enzyme; fluorides such as sodium fluoride, sodium monofluorophosphate, and tin fluoride; anti-inflammatory agents such as ε-aminocaproic acid, allantoin, tranexamic acid, glycyrrhizinate (e.g., dipotassium glycyrrhizinate), glycyrrhetinic acid, glycyrrhetinic acid derivatives (e.g., stearyl glycyrrhetinate), aluminum allantoin chlorhydroxyl, azulene, and dihydrocholesterol; metal salts such as zinc salts, copper salts, and tin salts; condensed phosphates, ethanehydroxydiphosphonate, and the like. Examples of the medicinal ingredients include tartar preventive agents such as glycerol, vitamin E (e.g., tocopherol acetate), blood flow promoters such as potassium nitrate, aluminum lactate, strontium chloride, and other dentin hypersensitivity inhibitors; coating agents such as hydroxyethylcellulose dimethyl diallyl ammonium chloride; astringents such as vitamin C (e.g., ascorbic acid or its salt), lysozyme chloride, and sodium chloride; water-soluble copper compounds such as copper chlorophyll and copper gluconate; tartar preventive agents; amino acids such as alanine, glycine, and proline; plant extracts such as thyme, Scutellaria baicalensis, clove, and witch hazel; callopeptides; and polyvinylpyrrolidone. These may be used alone or in combination of two or more. The content of the medicinal ingredients can be appropriately set to an effective amount according to a conventional method.

-Surfactants-
The optional surfactants are anionic surfactants and amphoteric surfactants.

Examples of anionic surfactants include alkyl sulfates, acyl amino acid salts, acyltaurine salts, α-olefin sulfonates, hydrogenated coconut fatty acid monoglyceride monosulfates, and lauryl sulfoacetates. The alkyl and acyl groups may be either linear or branched, and may be either saturated or unsaturated, and the number of carbon atoms is usually 10 to 20, preferably 12 to 18, and more preferably 12 to 14. The salt may be selected from pharmacologically acceptable salts. Examples of pharmacologically acceptable salts include base addition salts and amino acid salts. Specific examples of such salts include inorganic base salts such as sodium salts, potassium salts, calcium salts, magnesium salts, and ammonium salts; organic base salts such as triethylammonium salts, triethanolammonium salts, pyridinium salts, and diisopropylammonium salts; and basic amino acid salts such as arginine salts. Among these, inorganic base salts are preferred, alkali metal salts (e.g., sodium salts, potassium salts) or ammonium salts are more preferred, and sodium salts are even more preferred.

Examples of alkyl sulfates include lauryl sulfate (sodium lauryl sulfate) and myristyl sulfate. Examples of acylamino acid salts include acyl glutamates such as lauroyl glutamate, myristoyl glutamate, and palmitoyl glutamate; acyl glycine salts such as N-lauroyl-N-methyl glycine salt and cocoyl glycine salt; acyl alanine salts such as N-lauroyl-β-alanine salt, N-myristyl-β-alanine salt, N-cocoyl-β-alanine salt, N-lauroyl-N-methyl-β-alanine salt, N-myristoyl-N-methyl-β-alanine salt, and N-methyl-N-acylalanine salt; and acyl aspartates such as lauroyl aspartate. Examples of acyltaurine salts include lauroyl methyl taurine salt, N-methyl-N-acyltaurine salt, and N-cocoyl methyl taurine salt. Examples of α-olefin sulfonates include α-olefin sulfonates having 12 to 18 carbon atoms, such as tetradecene sulfonates. Other examples of anionic surfactants include sodium hydrogenated coconut fatty acid monoglyceride monosulfate and sodium lauryl sulfoacetate.

From the viewpoint of foaming and foam quality, the anionic surfactant preferably contains a sulfonic acid group, and lauryl sulfate and tradecene sulfonate are more preferable. The content of the anionic surfactant is preferably 0.1 to 2.5% by mass, more preferably 0.6 to 2.5% by mass, and even more preferably 1 to 2.5% by mass of the entire oral composition.

Examples of amphoteric surfactants include betaine-type amphoteric surfactants such as alkyl dimethyl amino acetate betaine (e.g., lauryl dimethyl amino acetate betaine) and fatty acid amidopropyl dimethyl amino acetate betaine (e.g., cocamidopropyl betaine); imidazoline-type amphoteric surfactants such as N-fatty acid acyl-N-carboxymethyl-N-hydroxyethyl ethylenediamine salts (e.g., N-coconut fatty acid acyl-N-carboxymethyl-N-hydroxyethyl imidazolinium betaine), coconut fatty acid imidazolinium betaine, and 2-alkyl-N-carboxymethyl-N-hydroxyethyl imidazolinium betaine; and alkyl betaines such as lauryl dimethyl amino acetate betaine. Examples of cationic surfactants include alkyl ammonium salts and alkyl benzyl ammonium salts. The content of the amphoteric surfactant is preferably 0.1 to 2% by mass, more preferably 0.2 to 1.5% by mass, and even more preferably 0.3 to 1% by mass of the entire oral composition.

The content of the surfactant (other than component (C)) is preferably 3% by mass or less, more preferably 2% by mass or less, and is preferably 0.1 to 3% by mass, and particularly preferably 0.3 to 2% by mass, based on the total oral composition (100% by mass).

- Wetting agent -
By including a wetting agent, the feeling during use can be further improved.

Examples of humectants include sugar alcohols and polyhydric alcohols other than sugar alcohols. Examples of sugar alcohols include sorbitol, erythritol, maltitol, lactitol, and xylitol. Examples of polyhydric alcohols other than sugar alcohols include glycerin; glycols such as ethylene glycol, propylene glycol, dipropylene glycol, butylene glycol, and polyethylene glycol (PEG); and reduced starch saccharification products. Examples of polyethylene glycols are, for example, polyethylene glycols with an average molecular weight of 150 to 6000, and polyethylene glycols with an average molecular weight of 190 to 630 (PEG 200, PEG 300, PEG 400, PEG 600). The average molecular weight is the average molecular weight described in the Quasi-Drug Raw Materials Standards 2006.

The content of the humectant is usually 40% by mass or less, and preferably 1 to 30% by mass, based on the total oral composition (100% by mass).

- Binding agent -
By including a binder, the viscosity of the oral composition can be optimized, and shape retention and usability can be further improved.

Examples of binders include any suitable organic binders known in the art, such as polysaccharides, cellulose-based binders (e.g., carboxymethylcellulose (CMC), hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, methylcellulose, cationic cellulose, etc.), other polysaccharide thickeners (e.g., xanthan gum, guar gum, gellan gum, tragacanth gum, karaya gum, gum arabic, locust bean gum, carrageenan, sodium alginate), and synthetic water-soluble polymers (e.g., sodium polyacrylate, carboxyvinyl polymer, polyvinylpyrrolidone, polyvinyl alcohol, propylene glycol alginate). Inorganic binders such as thickening silica and aluminum silicate can also be included.

The content of the organic binder is preferably 0 to 3% by mass, and more preferably 0.1 to 2% by mass, based on the total oral composition (100% by mass). The content of the inorganic binder is preferably 0 to 10% by mass, and more preferably 1 to 8% by mass.

-Sweetener-
The composition contains a sweetener, which can improve the feeling of use. Examples of sweeteners include xylitol, erythritol, maltitol, saccharin, saccharin sodium, aspartame, stevioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidin dihydrochalcone, perillartine, glycyrrhizin, thaumatin, and aspartyl phenylalanine methyl ester. The sweetener may be one of the above-listed sweeteners, or two or more of them may be used in combination.

- Preservatives -
The composition may contain a preservative to ensure the preservative power of the formulation.

Examples of preservatives include paraoxybenzoic acid esters (e.g., methyl paraoxybenzoate, ethyl paraoxybenzoate, butyl paraoxybenzoate) and sodium benzoate. The preservatives may be used alone or in combination of two or more.

- pH adjuster -
By including a pH adjuster in the composition, the pH stability of the formulation can be ensured.

Examples of pH adjusters include organic acids such as phthalic acid, citric acid, succinic acid, acetic acid, fumaric acid, malic acid, and lactic acid, or their salts (sodium citrate), inorganic acids such as phosphoric acid (orthophosphoric acid), or their salts (e.g., potassium salts, sodium salts, and ammonium salts), and hydroxides such as sodium hydroxide and potassium hydroxide. Examples of inorganic acid salts include disodium hydrogen phosphate and sodium dihydrogen phosphate.

The content of the pH adjuster is usually an amount such that the pH of the oral composition after addition is 5 to 9, preferably 6 to 8.5.

In this specification, the pH value usually refers to the value measured at 25°C and 3 minutes after the start of measurement. The pH value can be measured, for example, using a pH meter (model number Hm-30S) manufactured by Toa Denpa Kogyo Co., Ltd.

-solvent-
Examples of the solvent include water (purified water), ethanol, etc., and water is preferred. The solvent may be used alone or in combination of two or more.

-Oily ingredients-
Examples of oily components include hydrocarbons such as squalane, liquid paraffin, petrolatum, and microcrystalline wax; higher alcohols (e.g., alcohols having 8 to 22 carbon atoms, such as lauryl alcohol, cetyl alcohol, cetostearyl alcohol, oleyl alcohol, and isostearyl alcohol); higher fatty acids (e.g., fatty acids having 8 to 22 carbon atoms, such as lauric acid, myristic acid, oleic acid, and isostearic acid), vegetable oils such as olive oil, castor oil, and coconut oil; and fatty acid esters such as isopropyl myristate.

- Coloring agent -
Examples of colorants include natural colorants such as safflower red colorant, gardenia yellow colorant, gardenia blue colorant, perilla colorant, red koji colorant, red cabbage colorant, carrot colorant, hibiscus colorant, cacao colorant, spirulina blue colorant, tamarind colorant, etc., legal colorants such as Red No. 2, Red No. 3, Red No. 104, Red No. 105, Red No. 106, Red No. 227, Yellow No. 4, Yellow No. 5, Green No. 3, Blue No. 1, etc., riboflavin, sodium copper chlorophyte, titanium dioxide, etc. When the oral composition contains a colorant, the content thereof is preferably 0.00001 to 3% by mass based on the total oral composition.

-Fragrances other than component (D)-
By including a fragrance other than the component (D) in the composition, the feeling during use can be further improved.

Fragrances other than component (D) include, for example, natural essential oils such as anise oil, cassia oil, wintergreen oil, mastic oil, neroli oil (orange flower oil), lemongrass oil, jasmine oil, rose oil, iris oil, clove oil, sage oil, cardamom oil, rosemary oil, laurel oil, chamomile oil, basil oil, marjoram oil, lemon oil, orange oil, lime oil, yuzu oil, nutmeg oil, lavender oil, paracles oil, vanilla oil, cinnamon oil, pimento oil, cassia leaf oil, perilla oil, and wintergreen oil; cinnamic aldehyde, anethole, methyl salicylate, eugenol, linalool, limonene, menthone, menthyl acetate, cinnamon, citron, linoleic acid ... These include fragrance components contained in the above natural essential oils, such as toral, decanal, camphor, borneol, pinene, spilanthol, n-decyl alcohol, citronellol, α-terpineol, citronellyl acetate, ethyl linalool, and vanillin; fragrance components, such as ethyl acetate, ethyl butyrate, isoamyl acetate, hexanal, hexenal, methyl anthranilate, ethyl methylphenyl glycidate, benzaldehyde, vanillin, ethyl vanillin, and furaneol; and various blended flavors, such as mint, fruit, and herb flavors, which are made by combining several fragrance components and natural essential oils. As the fragrance, the above-exemplified fragrances may be used alone or in combination of two or more.

-Other optional ingredients-
Examples of optional components other than those mentioned above include polyisobutylene, polybutadiene, urethane, silicone, and natural rubber. The content of these optional components can be appropriately set within a range that does not impair the effects of the present invention.

[Formulation and Use of Oral Composition]
The oral composition of the present invention can be prepared as an oral preparation such as a dentifrice, a mouthwash, a spray, a coating agent, a patch, or an oral dissolving agent. The dosage form of the oral composition can be appropriately selected according to the form of use, and is not particularly limited. The dosage form can be, for example, a paste or liquid form, and in the case of a dentifrice, it can be prepared as a toothpaste, a gel dentifrice, a liquid dentifrice, a liquid dentifrice, or a lubricant dentifrice.

[Method of producing the composition]
The method of producing the oral composition is not particularly limited, and it can be prepared by a conventional method according to the dosage form. For example, when it is used as a toothpaste, it can be a method of preparing a component that dissolves in a solvent, mixing the other insoluble components, and degassing (e.g., reducing pressure, etc.) as necessary. The obtained toothpaste can be put into a container to make a product. The shape and material of the container are not particularly limited, and a container used for a conventional toothpaste composition can be used, for example, a container such as a laminated tube made of plastic such as polyethylene, polypropylene, polyethylene terephthalate, nylon, etc.

The present invention will be specifically described below with reference to examples, comparative examples, and reference examples. The present invention is not limited to the following examples. Note that the values in the following tables are pure amounts and represent mass % unless otherwise specified.

[Components used in the Examples, Comparative Examples and Reference Examples]
-Component (A)-
Cetylpyridinium chloride: (FUJIFILM Wako Pure Chemical Industries, Ltd.)
Isopropylmethylphenol: (Osaka Chemical Industry Co., Ltd.)
Sodium lauroyl sarcosine: (manufactured by Nikko Chemicals Co., Ltd.)
1,8-Cineole: (manufactured by Eikodo Honten Co., Ltd.)
-Component (B)-
N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide: (manufactured by Takasago International Corporation, product name: Coolact (registered trademark) 370)
Ethyl-3-(p-menthane-3-carboxamide) acetate: (WS-5, manufactured by Toyotama Fragrance Co., Ltd.)
-Fragrance component used in place of component (B) in the comparative examples-
N-ethyl-p-menthane-3-carboxamide: (WS-3, manufactured by Symrise Japan Co., Ltd.)
-Component (C)-
Polyoxyethylene (20) hydrogenated castor oil: (manufactured by Nippon Emulsion Co., Ltd.)

-Component (D)-
Menthol: (Takasago International Corporation)
Carvone: (Shiono Koryo Co., Ltd.)
Peppermint oil (Takasago International Corporation)
Japanese peppermint oil (Vemanfis Fragrance Company)
Spearmint oil (Vemanfis Fragrances)

-Optional components-
Abrasive Silica: (Tixosil® 73 from Solvay)
Sodium fluoride: (Stella Chemifa Corporation)
Sodium lauryl sulfate: (manufactured by BASF Japan Ltd.)
Sorbitol solution (70%): (Mitsubishi Corporation Life Sciences Co., Ltd.)
Propylene glycol: (manufactured by ADEKA Corporation)
Viscosifying silica: Carplex (registered trademark) #67 (manufactured by DSL Japan Co., Ltd.)
Sodium saccharin: (manufactured by Aisan Chemical Industry Co., Ltd.)
For ingredients other than those mentioned above, raw materials conforming to the Standards for Quasi-Drug Raw Materials 2006 were used.

Examples 1 to 30, Comparative Examples 1 to 4
The above components were mixed in a conventional manner to prepare toothpaste compositions having the compositions shown in Tables 1 to 4 below, and the compositions were packed in laminated tubes.

[Evaluation method]
The toothpaste composition was evaluated for usability by four panelists. 1 g of the sample toothpaste composition was placed on a toothbrush (Clinica Advantage Toothbrush, 4-row compact normal type, manufactured by Lion Corporation), and the toothbrush was brushed for 3 minutes. The refreshing sensation at the start of brushing, the lack of bitterness during brushing, and the persistence of the lack of bitterness after brushing were evaluated according to the following criteria. The scores of the four panelists were averaged and evaluated according to the following criteria.

<Refreshing feeling when you start brushing your teeth>
Regarding the cooling sensation at the start of tooth brushing, the cooling sensation at the start of tooth brushing was evaluated.
Evaluation criteria: 4 points: Very refreshing feeling 3 points: Refreshing feeling 2 points: Not much refreshing feeling 1 point: Not refreshing feeling Judgment criteria: ◎: Average score of 3.5 points or more and less than 4.0 points ○: Average score of 3.0 points or more and less than 3.5 points △: Average score of 2.0 points or more and less than 3.0 points ×: Average score of less than 2.0 points

<No bitter taste when you start brushing your teeth>
Regarding the lack of bitterness, the evaluation was based on the intensity of the bitterness when starting to brush teeth.
Rating criteria: 4 points: No bitterness was felt; 3 points: Almost no bitterness was felt; 2 points: Bitterness was felt; 1 point: Very strong bitterness was felt. Evaluation criteria: ◎: Average score of 3.5 to 4.0 points; ○: Average score of 3.0 to less than 3.5 points; △: Average score of 2.0 to less than 3.0 points; ×: Average score of less than 2.0 points.

<No bitterness while brushing teeth>
Regarding the lack of bitterness during tooth brushing, the intensity of bitterness was evaluated while brushing teeth for 3 minutes.
Evaluation criteria: 4 points: No bitterness was felt; 3 points: Almost no bitterness was felt; 2 points: Bitterness was felt; 1 point: Very strong bitterness was felt. Evaluation criteria: ☆: Average score of 3.8 to 4.0 points; ◎: Average score of 3.5 to less than 3.8 points; ○: Average score of 3.0 to less than 3.5 points; △: Average score of 2.0 to less than 3.0 points; ×: Average score of less than 2.0 points.

<Sustained lack of bitterness after brushing teeth>
The duration of the absence of bitterness after brushing was evaluated by brushing the teeth for 3 minutes and rinsing the teeth for a period during which no bitterness was felt.
Evaluation criteria: 4 points: 25 minutes or more (no bitterness felt)
3 points: 15 to less than 25 minutes 2 points: 5 to less than 15 minutes 1 point: Less than 5 minutes Evaluation criteria ☆: Average score of 3.8 to 4.0 points ◎: Average score of 3.5 to less than 3.8 points ○: Average score of 3.0 to less than 3.5 points △: Average score of 2.0 to less than 3.0 points ×: Average score of less than 2.0 points

In Comparative Examples 1 to 3, which do not contain component (B), the feeling of coolness was not very strong at the start of brushing, and the bitterness was very strong. Furthermore, the bitterness was felt even while brushing the teeth, so the feeling of use was not favorable. The lack of bitterness after brushing lasted less than 5 minutes, and no satisfactory results were obtained. The same results were obtained in Comparative Example 4, in which N-ethyl-p-menthane-3-carboxamide was used instead of component (B). In contrast, all of Examples 1 to 30, in which component (A) was mixed with component (B), achieved satisfactory results with an average score of 3.0 or more in all evaluation items. In particular, in Examples 21 to 30, in which component (C) was further added in addition to components (A) and (B), the evaluation of the lack of bitterness during brushing and the duration of the lack of bitterness after brushing improved to an average score of 3.8 or more, and excellent results were obtained. These results show that the oral composition of the present invention provides a refreshing sensation when use is started, and can suppress and sustain the bitter taste derived from the bactericide for a certain period of time from the start of use to after use.

Claims (9)

(A) a disinfectant which is a quaternary ammonium salt or an acylsarcosine salt ;
(B ) N- (2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1- carboxamide; and an oral composition which is a toothpaste . The oral composition according to claim 1 , wherein the content of component (A) is 0.001 to 0.5% by mass relative to 100% by mass of the oral composition. The oral composition according to claim 1 or 2 , wherein the content of component (B) is 0.00001 to 0.1 mass% relative to 100 mass% of the oral composition. The oral composition according to any one of claims 1 to 3 , further comprising (C) a nonionic surfactant. The oral composition of claim 4, wherein component (C) is one or more nonionic surfactants selected from the group consisting of polyoxyethylene hydrogenated castor oil, polyoxyethylene alkyl ether, polyglycerin fatty acid ester , and polyoxyethylene polyoxypropylene copolymer. The oral composition according to claim 4 or 5 , wherein the content of component (C) is 0.1 to 2 mass% relative to 100 mass% of the oral composition. The oral composition according to any one of claims 1 to 6 , further comprising (D) a cooling agent. 8. The oral composition according to claim 7 , wherein component (D) is menthol and/or carvone or an essential oil containing these. The oral composition according to claim 7 or 8 , wherein the content of the component (D) is 0.001 to 1.5% by mass as menthol and/or carvone per 100% by mass of the oral composition.