WO2023277084A1 - Composition for oral cavity - Google Patents

Abstract

The purpose of the present invention is to provide a composition for oral cavity, the composition containing a compound that releases metal ions but still capable of suppressing not only metallic taste during use but also metallic taste after use. The present invention provides a composition for oral cavity, the composition containing: (A-i) a compound such as copper gluconate, copper citrate, copper sulfate, zinc chloride, zinc citrate, zinc gluconate, zinc acetate, zinc salicylate, zinc sulfate, tin fluoride and aluminum lactate, the compound releasing one or more kinds of metal ions that are selected from among copper ions, zinc ions, tin ions and aluminum ions, and/or (A-ii) a compound such as potassium nitrate, potassium hydroxide, potassium citrate, potassium chloride and potassium sulfate, the compound releasing potassium ions; and (B) N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide.

Description

oral composition

The present invention relates to an oral composition.

Conventionally, compounds that release metal ions such as copper, zinc, aluminum, iron, tin, aluminum and potassium have been incorporated into oral compositions such as dentifrices. For example, a copper salt has an effect of suppressing bad breath (Patent Document 1), a zinc salt has an effect of suppressing dental plaque (Patent Document 2), a tin salt has an anti-caries effect as tin fluoride (Patent Document 3), and potassium salts are potassium nitrate and potassium chloride. As an aluminum salt, aluminum lactate is known to have an effect of suppressing hypersensitivity (Patent Document 8). However, compounds that release metal ions sometimes exhibit a metallic taste, which has been a factor in reducing the usability of oral compositions.

As a means of improving metallic taste, L-menthol derivatives and/or N-ethyl-p-menthane-3-carboxamide are added to oral compositions containing compounds that release metal ions (Patent Document 4). (1R,2S,5R)-N-(4-(cyanomethyl)phenyl)menthyl carboxamide and organic acid having 10 or less carbon atoms, polyphosphoric acid, α-amino acid, and them to oral composition containing ionic copper compound (Patent Document 5). Pyrrolidone carboxylic acid (Patent Document 6) or blending of anethole and polyhydric alcohol in a predetermined ratio (Patent Document 7) has been proposed as means for masking the metallic taste of zinc compounds.

JP-A-1-153622 JP-A-47-20351 JP-A-47-19045 JP-A-2003-137755 JP 2019-116442 A JP 2019-108276 A JP-A-2004-203894 JP 2022-007409 A

However, although the techniques of Patent Documents 1 to 8 can improve the metallic taste during use of oral compositions, they are insufficient to mask the metallic taste after use. For example, during the daytime, when a beverage is consumed after use of the oral composition (eg, within about 30 minutes after use), a strong metallic taste may be perceived, which may detract from the taste of the beverage. As a result, there is a possibility that the intention to use dentifrice during the daytime may decline, and a technique for masking the metallic taste after use is required to improve QOL.

The present invention has been made in view of the above, and provides an oral composition that contains a compound that releases metal ions and that can suppress not only the metallic taste during use but also the metallic taste after use.

The present invention provides the following [1] to [8].
[1] (A) one or more selected from the following (Ai) and (A-ii):
(Ai) a compound that releases one or more metal ions selected from the group consisting of copper, zinc, tin, and aluminum;
(A-ii) a compound that releases potassium ions; and (B) N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide.
[2] The composition for oral cavity according to [1], wherein (B)/(A) is 0.00001 or more as a mass ratio.
[3] The composition for oral cavity according to [1] or [2], wherein the amount of component (Ai) is 5% by mass or less.
[4] The oral composition according to any one of [1] to [3], wherein the amount of component (A-ii) is 10% by mass or less.
[5] The composition for oral cavity according to any one of [1] to [4], wherein the amount of component (B) is 0.000005 to 0.1% by mass.
[6] component (Ai) from the group consisting of copper gluconate, copper citrate, copper sulfate, zinc chloride, zinc citrate, zinc gluconate, zinc acetate, zinc sulfate, tin fluoride, and aluminum lactate One or two or more selected,
The oral composition according to any one of [1] to [5].
[7] component (A-ii) is one or more selected from potassium nitrate, potassium hydroxide, potassium citrate, potassium chloride, and potassium sulfate;
The oral composition according to any one of [1] to [6].
[8] The oral composition according to any one of [1] to [7], which is a dentifrice, mouthwash or spray.

According to the present invention, there is provided an oral composition capable of suppressing a metallic taste during and after use despite containing a compound that releases metal ions. Therefore, the oral composition of the present invention can exhibit various effects of the compound that releases metal ions, can achieve a good feeling of use, can be used comfortably throughout the day, and can improve the QOL of the user. is.

The oral composition contains (A) and (B) components.

[(A): Compound that releases metal ions]
Component (A) is a compound that releases metal ions. By containing the component (A), it is possible to impart product performance such as bad breath control effect, dental plaque control effect, caries preventive effect, hypersensitivity control effect and the like.

As used herein, a compound that releases metal ions means a compound that can be ionized in an aqueous solution to release (ionize) metal ions (for example, a metal salt). Metal ions include, for example, polyvalent metal ions such as copper ions, zinc ions, tin ions, aluminum ions, and potassium ions, and may be one selected from these ions or a combination of two or more thereof. Component (A) is one or more selected from (Ai) a compound that releases polyvalent metal ions and (A-ii) a compound that releases potassium ions, and (Ai), (A-ii) or a combination thereof.

-(Ai) a compound that releases polyvalent metal ions-
Polyvalent metal ions include, for example, copper ions, zinc, tin, and aluminum.

Compounds that release copper ions include, for example, copper chloride, copper fluoride, copper fluorosilicate, copper sulfate, copper nitrate, copper hydroxide, copper oxide, copper bromate, copper iodate, copper fluorophosphate, acetic acid Copper, copper formate, copper benzoate, copper citrate, copper tartrate, copper lactate, copper malate, copper mandelate, copper sorbate, copper pyrophosphate, copper pantothenate, copper gluconate, copper phytate, copper glycerophosphate , copper cinnamate, copper butyrate, copper propionate, copper laurate, copper oxalate, copper salicylate, copper glycinate, copper aspartate, copper glutamate, copper chlorophyll.

Examples of compounds that release zinc ions include zinc chloride, zinc fluoride, zinc fluorosilicate, zinc sulfate, zinc nitrate, zinc hydroxide, zinc oxide, zinc bromate, zinc iodate, zinc fluorophosphate, and acetic acid. Zinc, zinc formate, zinc benzoate, zinc citrate, zinc tartrate, zinc lactate, zinc malate, zinc mandelate, zinc pyrophosphate, zinc sorbate, zinc pantothenate, zinc gluconate, zinc phytate, zinc glycerophosphate , zinc cinnamate, zinc butyrate, zinc propionate, zinc laurate, zinc oxalate, zinc salicylate, zinc glycinate, zinc aspartate, zinc glutamate.

Examples of compounds that release tin ions include tin chloride, tin fluoride, tin acetate, tin oxide, tin gluconate, tin oxalate, tin sulfate, tin lactate, tin tartrate, tin citrate, tin malate, stannic acid Sodium, tin phosphate.

Examples of compounds that release aluminum ions include aluminum acetate, aluminum borate, aluminum lactate, aluminum chloride, aluminum hydroxide, aluminum laurate, aluminum oxalate, aluminum oxide, aluminum oleate, aluminum phosphate and aluminum sulfate. mentioned.

Component (Ai) is preferably copper gluconate, copper citrate, copper sulfate, zinc chloride, zinc citrate, zinc gluconate, zinc acetate, zinc sulfate, tin fluoride, and aluminum lactate. It is preferable to include at least Component (Ai) may be used alone or in combination of two or more.

-(A-ii) a compound that releases potassium ions-
Compounds that release potassium ions include, for example, potassium nitrate, potassium hydroxide, potassium citrate, potassium chloride, and potassium sulfate, with potassium nitrate being preferred. Component (A-ii) may be used alone or in combination of two or more.

The compound that releases metal ions may be a chemically synthesized component or a natural product. Examples of natural products include plants such as tea, microorganisms such as yeast, animals, polyvalent metals such as copper, zinc, tin and aluminum as trace metals, and natural products containing potassium.

The component (A) preferably contains either or both of (Ai) and (A-ii), more preferably either one.

The (A) component may be a compound that releases metal ions alone, or may be a combination of two or more.

The content of component (A) can be adjusted as appropriate depending on the type of metal compound used and the intended effect of the composition, but an example is as follows.

The content of component (Ai) is preferably 5% by mass or less, more preferably 2% by mass or less, and even more preferably 1% by mass or less, relative to the entire oral composition (100% by mass). Thereby, the metallic taste can be sufficiently masked by the component (B), and the feeling of use can be improved. Generally, the lower limit of the content of component (Ai) is preferably 0.001% by mass or more, more preferably 0.01% by mass or more, and even more preferably 0.1% by mass or more. As a result, the product performance attributed to the component (Ai), such as halitosis control effect, dental plaque control effect, caries prevention effect, etc., can be exhibited satisfactorily. Therefore, the content of component (Ai) is preferably 0.001 to 5% by mass, more preferably 0.01 to 2% by mass, even more preferably 0.1 to 1% by mass.

The content of component (A-ii) is preferably 0.5% by mass or more, more preferably 1% by mass or more, 2% by mass or more, or 3% by mass or more, relative to the entire oral composition (100% by mass). is more preferred. As a result, the effect of suppressing hypersensitivity can be satisfactorily exhibited. The upper limit is preferably 10% by mass or less, more preferably 8% by mass or less, and even more preferably 7% by mass or less or 6% by mass or less. Therefore, the content of component (A-ii) is preferably 0.5 to 10% by mass, more preferably 1 to 8% by mass, and more preferably 2 to 7% by mass or 3 to 8% by mass.

The content of component (A) may be adjusted depending on whether one or both of components (Ai) and (A-ii) are included. , more preferably 0.005 to 13% by mass, and even more preferably 0.01 to 10% by mass.

[(B): N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide]
Component (B) is N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide. By containing the component (B), the metallic taste can be improved not only during use but also after use.

The lower limit of the content of component (B) is preferably 0.000005% by mass or more, more preferably 0.00001% by mass or more, and 0.00005% by mass or more, relative to the entire oral composition (100% by mass). More preferred. Thereby, the effect of suppressing the metallic taste can be exhibited. The upper limit is preferably 0.1% or less, more preferably 0.05% by mass or less, and even more preferably 0.01% by mass or less. As a result, the irritation caused by the component (B) can be moderately suppressed, and the deterioration of the aftertaste can be suppressed. Therefore, the content of component (B) is preferably 0.000005 to 0.1% by mass, more preferably 0.00001 to 0.05% by mass, and even more preferably 0.00005 to 0.01% by mass.

[Content ratio of (B)/(A)]
The lower limit of the ratio of the content of component (B) to the content of component (A) ((B)/(A)) is preferably 0.00001 or more, or 0.00002 or more, 0.00005 or more, and 0.00005 or more. 00007 or more, 0.0001 or more, or 0.0002 or more is more preferable, and 0.0004 or more, 0.0005 or more, or 0.001 or more is still more preferable. Thereby, the metallic taste of the composition for oral cavity can be suppressed sufficiently. The upper limit is not particularly limited, and may exceed 1000, for example, 100 or less, 10 or less, or 0.1 or less. As a result, product performance such as halitosis control effect, dental plaque control effect, tooth decay prevention effect, hypersensitivity control effect, etc. can be exhibited.

[Optional component]
The oral composition of the present invention may contain optional components other than the components (A) and (B) within the range that does not impair the effects of the present invention.

Optional components other than components (A) and (B) may be used, and examples include abrasives, surfactants, wetting agents, medicinal ingredients, flavors, sweeteners, oily components, preservatives, binders, and pH. Adjustment agents, colorants (pigments), and solvents are included. A specific description will be given below.

-Abrasive-
The abrasive may be either an inorganic abrasive or an organic abrasive. Examples of inorganic abrasives include abrasive silica such as silicic anhydride, zeolite, precipitated silica, aluminosilicate, zirconosilicate, crystalline zirconium silicate, titanium-bonded silica, silica gel; dicalcium phosphate dihydrate. Or calcium phosphate compounds such as anhydrous, monocalcium phosphate, dicalcium phosphate dihydrate or anhydrate, insoluble calcium metaphosphate, tricalcium phosphate, tetracalcium phosphate, octacalcium phosphate, calcium pyrophosphate; calcium carbonate (light Calcium carbonate-based abrasives such as calcium hydroxide, calcium sulfate, calcium oxide; Silicic acid-based abrasives such as silicic anhydride, zeolite, and zirconium silicate; magnesium-based abrasives such as magnesium phosphate; apatite-based abrasives such as hydroxyapatite, fluoroapatite and calcium-deficient apatite; titanium-based 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. The abrasive is preferably an inorganic abrasive, more preferably abrasive silica, and still more preferably abrasive silica.

The abrasive silica is preferably abrasive particles with an average particle diameter of 1 to 40 μm, and the BET specific surface area of the abrasive silica is preferably 80 to 250 square meters per 1 g. Here, the average particle diameter of abrasive silica is the volume-based median diameter (D50) measured by a laser diffraction/scattering method.

The preferred RDA value (Radioactive Dentine Abrasion Value) of the abrasive is not particularly limited, but usually 50 or more, especially 50 to 200 is preferred. The abrasive may be granulated. Examples of such granules include particles obtained by granulating a water-insoluble powder (eg, silica gel) into granules. When granulating into granules, any suitable conventionally known binder may be used.

The abrasive may be used singly or in combination of two or more.

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

-Surfactant-
Examples of surfactants include anionic surfactants, nonionic surfactants, amphoteric surfactants, and cationic surfactants.

Examples of anionic surfactants include alkyl sulfates, acyl amino acid salts, acyl taurine salts, α-olefin sulfonates, hydrogenated coconut fatty acid monoglyceride monosulfate, and lauryl sulfoacetate. Alkyl groups and acyl groups may be linear or branched, saturated or unsaturated, and usually have 10 to 20 carbon atoms. Salts may be selected from pharmacologically acceptable salts. Pharmaceutically acceptable salts include base addition salts and amino acid salts. Specific examples include inorganic base salts such as sodium salts, calcium salts, magnesium salts and ammonium salts; organic base salts such as triethylammonium salts, triethanolammonium salts, pyridinium salts and diisopropylammonium salts; basic salts such as arginine salts. Amino acid salts are included. Among them, inorganic base salts are preferred, alkali metal salts (for example, sodium salts) or ammonium salts are more preferred, and sodium salts are even more preferred.

Examples of anionic surfactants include alkyl sulfates, acyl amino acid salts, acyl taurine salts, α-olefin sulfonates, hydrogenated coconut fatty acid monoglyceride monosulfate, and lauryl sulfoacetate. Alkyl groups and acyl groups may be linear or branched, saturated or unsaturated, and usually have 10 to 20 carbon atoms, preferably 12 to 18 carbon atoms, more preferably 12 to 14. Salts may be selected from pharmacologically acceptable salts. Pharmaceutically acceptable salts include, for example, base addition salts and amino acid salts. Specific examples thereof include inorganic base salts such as sodium salts, calcium salts, magnesium salts and ammonium salts; organic base salts such as triethylammonium salts, triethanolammonium salts, pyridinium salts and diisopropylammonium salts; basic salts such as arginine salts. Amino acid salts are included. Among them, inorganic base salts are preferred, alkali metal salts (eg, sodium 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 myristoyl sulfate. Acyl amino acid salts include, for example, acyl sarcosine salts such as lauroyl sarcosine salt and myristoyl sarcosine salt; acyl glutamates such as lauroyl glutamate, myristoyl glutamate and palmitoyl glutamate; N-lauroyl-N-methylglycinate and cocoylglycine. Acylglycine salts such as salts; N-lauroyl-β-alanine salt, N-myristyl-β-alanine salt, N-cocoyl-β-alanine salt, N-lauroyl-N-methyl-β-alanine salt, N-myristoyl acylalanine salts such as -N-methyl-β-alanine salts and N-methyl-N-acylalanine salts; and acyl aspartates such as lauroyl aspartate. Acyl taurate salts include, for example, lauroyl methyl taurate, N-methyl-N-acyl taurate, N-cocoyl methyl taurate, and lauroyl methyl taurate. The α-olefin sulfonate includes α-olefin sulfonates having 12 to 18 carbon atoms such as tetradecene sulfonate. Other examples of anionic surfactants include hydrogenated coconut fatty acid monoglyceride sodium monosulfate, sodium lauryl sulfoacetate.　

The anionic surfactant preferably contains a sulfonic acid group, more preferably an alkyl sulfate or an α-olefin sulfonate, in terms of foaming and good foam quality.

Examples of nonionic surfactants include polyoxyethylene alkyl ethers (e.g., polyoxyethylene stearyl ether), polyoxyethylene hydrogenated castor oil, sorbitan fatty acid esters, polyoxyethylene sorbitan fatty acid esters (e.g., polyoxyethylene sorbitan monosterate). rate), alkylolamide, polyoxyethylene fatty acid ester, polyoxyethylene alkenyl ether, (poly)glycerin fatty acid ester (e.g., polyglyceryl monolaurate), sucrose fatty acid ester (e.g., maltose fatty acid ester), sugar alcohol fatty acid ester ( Examples include maltitol fatty acid esters, lactitol fatty acid esters), fatty acid diethanolamides (eg, 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 generally 14-18, and the average number of moles of ethylene oxide added is generally 5-30 mol. The average mole number of ethylene oxide added to the polyoxyethylene hydrogenated castor oil is generally 20 to 100 mol, preferably 20 to 60 mol. The number of carbon atoms in the fatty acid of the sorbitan fatty acid ester is usually 12-18. The number of carbon atoms in the fatty acid of the polyoxyethylene sorbitan fatty acid ester is generally 16-18, and the average number of moles of ethylene oxide added is generally 10-40 mol. The alkyl chain of the alkylolamide usually has 12-14 carbon atoms. Preferred nonionic surfactants are polyoxyethylene hydrogenated castor oil, polyoxyethylene sorbitan fatty acid ester, and polyoxyethylene alkyl ether.

Examples of amphoteric surfactants include betaine-type amphoteric surfactants such as alkyldimethylaminoacetic acid betaine (eg, lauryldimethylaminoacetic acid betaine), fatty acid amidopropyldimethylaminoacetic acid betaine (eg, cocamidopropyl betaine); Fatty acid acyl-N-carboxymethyl-N-hydroxyethylethylenediamine salts (e.g., N-cocoate acyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine), cocoate imidazolinium betaine, 2-alkyl imidazoline type amphoteric surfactants such as -N-carboxymethyl-N-hydroxyethylimidazolinium betaine; and alkylbetaines such as lauryldimethylaminoacetate betaine.

Examples of cationic surfactants include alkylammonium salts and alkylbenzylammonium salts.

The surfactants may be used singly or in combination of two or more. The content of the surfactant is preferably 10% by mass or less, more preferably 0.1 to 9% by mass, still more preferably 0.5 to 8% by mass, relative to the entire oral composition (100% by mass), Even more preferably, it is 1 to 7% by mass.

-wetting agent-
Preferred humectants are sugar alcohols and polyhydric alcohols other than sugar alcohols. Examples of sugar alcohols include sugar alcohols such as sorbitol, erythritol, maltitol, lactitol, xylitol, and reduced starch saccharification products; glycerin; and polyhydric alcohols such as ethylene glycol, propylene glycol, dipropylene glycol, butylene glycol, and polyethylene glycol. mentioned. Among these, sorbitol is preferred as the sugar alcohol, and propylene glycol is preferred as the polyhydric alcohol. Wetting agents may be used singly or in combination of two or more.

The content of the humectant is usually 50% by mass or less, preferably 40% by mass or less, more preferably 1 to 35% by mass or 1 to 30% by mass, relative to the entire oral composition (100% by mass). .

-Medicinal Ingredients-
Medicinal ingredients other than components (A) and (B) include, for example, cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride, isopropylmethylphenol, triclosan, thymol, hinokitiol, bactericidal or antibacterial agents such as lysozyme chloride; Enzymes such as stranase, mutanase, amylase, protease, and litek enzyme; fluorides such as sodium fluoride and sodium monofluorophosphate; ε-aminocaproic acid, allantoin, tranexamic acid, glycyrrhizinate, glycyrrhetinic acid, glycyrrhetinate ( anti-inflammatory agents such as stearyl glycyrrhetinate), azulene and dihydrocholesterol; anticalculus agents such as condensed phosphate and ethanehydroxydiphosphonate; blood flow promoters such as vitamin E (e.g. tocopherol acetate); Hypersensitivity inhibitors such as strontium; coating agents such as hydroxyethylcellulose dimethyldiallylammonium chloride; astringents such as vitamin C (e.g., ascorbic acid or its salts) and lysozyme chloride; anticalculus agents, alanine, glycine, proline, pyrrolidone carvone Amino acids such as acids (salts), plant extracts such as Phellodendron bark, thyme, Scutellaria root, clove, and hamamelis; calopeptide, and polyvinylpyrrolidone. Of these, sodium fluoride is preferred. A medicinal ingredient may be used individually by 1 type, and may be used in combination of 2 or more type. The content of the medicinal ingredient can be appropriately set to an effective amount according to a conventional method.

-Perfume-
When the composition contains a fragrance, the feeling of use can be further improved. Examples of fragrances include peppermint oil, spearmint oil, Japanese peppermint oil, anise oil, cassia oil, eucalyptus oil, wintergreen oil, mastic oil, neroli oil (orange flower oil), lemongrass oil, jasmine oil, and rose oil. , iris oil, clove oil, thyme oil, sage oil, cardamom oil, rosemary oil, laurel oil, chamomile oil, caraway oil, basil oil, marjoram oil, lemon oil, orange oil, lime oil, yuzu oil, nutmeg oil , lavender oil, paracress oil, vanilla oil, cinnamon oil, pimento oil, cinnamon leaf oil, perilla oil, wintergreen oil; menthol, carvone, cinnamic aldehyde, anethole, 1,8-cineole, methyl salicylate, eugenol , thymol, linalool, limonene, menthone, menthyl acetate, citral, decanal, camphor, borneol, pinene, spiranthol, n-decyl alcohol, citronellol, α-terpineol, citronellyl acetate, cineole, ethyl linalool, vanillin, etc. Fragrant ingredients contained therein: Ethyl acetate, ethyl butyrate, isoamyl acetate, hexanal, hexenal, methyl anthranilate, ethyl methylphenylglycidate, benzaldehyde, vanillin, ethyl vanillin, furaneol, etc.; N-ethyl-p - menthane-3-carboxamide, menthyl lactate, menthyl monosuccinate, isopulegol, menthone glycerol ketal, N-(4-cyanomethylphenyl)-p-menthane carboxamide, 3-l-menthoxypropane-1,2-diol, 5-methyl-2-propan-2-yl-N-(2-pyridin-2-ylethyl)cyclohexane-1-carboxamide, 3-(p-menthane-3carboxamido)ethyl acetate, 2-isopropyl-N, 2, Cooling agents such as 3-trimethylbutyramide, (1R,2S,5R)-N-(4-(cyanomethyl)phenyl)menthylcarboxamide, and mint-based and fruit-based combinations of some fragrance ingredients and natural essential oils , herb-based and the like. As the perfume, one of the above-exemplified perfumes may be used alone, or two or more thereof may be used in combination.

-sweetener-
By including a sweetener in the composition, the feeling of use can be further improved. Sweetening agents include, for example, saccharin, saccharin sodium, aspartame, stevioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidin dihydrochalcone, perillartine, glycyrrhizin, thaumatin, asparatylphenylalanine methyl ester and the like. Of these, saccharin sodium is preferred. As the sweetener, the above-exemplified sweeteners may be used singly or in combination of two or more.

- Oily component -
Examples of oily components include hydrocarbons such as squalane, liquid paraffin, petrolatum, and microcrystalline wax; higher alcohols (such as lauryl alcohol, cetyl alcohol, cetostearyl alcohol, oleyl alcohol, -22 alcohols); higher fatty acids (e.g., fatty acids with 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; fatty acid esters. As the oily component, one of the above-exemplified oily components may be used alone, or two or more thereof may be used in combination.

-Preservative-
By including a preservative in the composition, the antiseptic power of the formulation can be ensured. Examples of antiseptics include paraoxybenzoic acid esters (eg, methyl parahydroxybenzoate, ethyl parahydroxybenzoate, butyl parahydroxybenzoate), sodium benzoate, and the like. The preservatives may be used singly or in combination of two or more.

-Binder-
By including an optional binder in the composition, the viscosity can be optimized, and the shape retention and feel during use can be further improved. As the binding agent, any suitable conventionally known organic binding agent such as polysaccharides, cellulose-based binding agents (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), synthetic water-soluble polymers (e.g., sodium polyacrylate, carboxyvinyl polymer, polyvinylpyrrolidone, polyvinyl alcohol, propylene glycol alginate) and salts thereof. Furthermore, inorganic binders such as thickening silica, silicates, and silicic anhydride can also be blended. Among these, carboxymethylcellulose (eg, sodium carboxymethylcellulose) and thickening silica are preferred. A caking agent may be used individually by 1 type, and may be used in combination of 2 or more type.

The content of the optional organic binder is preferably 0 to 5% by mass, more preferably 0.1 to 4% by mass, relative to the entire oral composition (100% by mass). The content of the inorganic binder is preferably 0 to 10% by mass, more preferably 1 to 8% by mass.

-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, salts thereof (sodium citrate), and inorganic acids such as phosphoric acid (orthophosphoric acid). Acids or salts thereof (eg, sodium salts and ammonium salts), and hydroxides such as sodium hydroxide. Examples of inorganic acid salts include disodium hydrogen phosphate and sodium dihydrogen phosphate.

The content of the pH adjuster can usually be 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 after 3 minutes at 25°C from 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.

-coloring agent-
Examples of coloring agents include natural pigments such as safflower red pigment, gardenia yellow pigment, gardenia blue pigment, perilla pigment, monascus pigment, red cabbage pigment, carrot pigment, hibiscus pigment, cocoa pigment, spirulina blue pigment, and tamarind pigment, and red. Legal pigments such as 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, and Blue No. 1, riboflavin, and titanium dioxide. . The colorants may be used singly or in combination of two or more.

When the oral composition contains a coloring agent, the content thereof is preferably 0.00001 to 3% by mass based on the total oral composition.

-solvent-
Examples of the solvent include water (purified water), ethanol and the like, with water being preferred. A solvent may be used individually by 1 type, or may be used in combination of 2 or more type.

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

[Dosage form and use of oral composition]
The oral composition of the present invention can be an oral preparation such as a dentifrice, a mouthwash, a spray, a coating, 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. As for the dosage form, for example, it can be prepared in the form of a paste, a liquid, or the like, and if it is a dentifrice, it can be prepared as a toothpaste, a liquid dentifrice, a liquid dentifrice, or a wet dentifrice.

[Method for producing composition]
The method for producing the oral composition is not particularly limited, and it can be prepared by each usual method depending on the dosage form. For example, when it is used as a toothpaste, there is a method of preparing components that dissolve in a solvent, mixing other insoluble components, and defoaming (for example, reducing pressure) as necessary. The obtained toothpaste can be stored in a container to be used as a product. The shape and material of the container are not particularly limited, and any container commonly used for dentifrice compositions can be used. Examples include containers such as laminated tubes made of plastic such as polyethylene, polypropylene, polyethylene terephthalate, and nylon. be done.

The present invention will be specifically described below with reference to examples and comparative examples, but the present invention is not limited to the following examples. Note that % in each example is mass percentage.

Examples 1-22 and Comparative Examples 1-5
Dentifrice compositions (toothpaste) having compositions shown in Tables 1 to 5 and 7 were each prepared by a conventional method and housed in a conventional oral formulation container (toothpaste: laminated tube). In addition, a spray composition having the composition shown in Table 6 was prepared according to the information and contained in a conventional mouth spray container. These were used as samples and evaluated by the methods described below. The results are also shown in Tables 1-6.

<Raw materials used>
-(A) component-
A1: Copper gluconate (trade name: copper gluconate, manufacturer: Fujifilm Wako Pure Chemical Industries, Ltd.)
A2: Copper citrate (trade name: copper citrate, manufacturer: Kanto Chemical Co., Ltd.)
A3: Copper sulfate (trade name: copper sulfate, manufacturer: Kanto Chemical Co., Ltd.)
A4: Zinc chloride (trade name: zinc chloride, manufacturer: Fujifilm Wako Pure Chemical Industries, Ltd.)
A5: Zinc citrate (trade name: zinc citrate, manufacturer: Kanto Chemical Co., Ltd.)
A6: Zinc gluconate (trade name: zinc gluconate, manufacturer: Fujifilm Wako Pure Chemical Industries, Ltd.)
A7: Zinc acetate (trade name: zinc acetate, manufacturer: Fujifilm Wako Pure Chemical Industries, Ltd.)
A8: Zinc sulfate (trade name: zinc sulfate, manufacturer: Fujifilm Wako Pure Chemical Industries, Ltd.)
A9: Tin fluoride (trade name: tin fluoride, manufacturer: Fujifilm Wako Pure Chemical Industries, Ltd.)
A10: Aluminum lactate (trade name: aluminum lactate, manufacturer: Fujifilm Wako Pure Chemical Industries, Ltd.)
A11: Potassium nitrate (trade name: potassium nitrate, manufacturer: Otsuka Chemical Co., Ltd.)
A12: Potassium hydroxide A13: Potassium citrate A14: Potassium chloride A15: Potassium sulfate

-Component (B) and its alternative component-
B: N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide (trade name: CA370, manufacturer: Takasago International Corporation)
N-ethyl-p-menthane-3-carboxamide (trade name: WS-3, manufacturer: Simrise Japan)
3-L-menthoxypropane-1,2-diol (manufacturer: Takasago International Corporation)
(1R,2S,5R)-N-(4-(cyanomethyl)phenyl)menthylcarboxamide (trade name: Evercool180, manufacturer: Givaudan)

-Optional Ingredients-
Anethole (Product name: Anethole, Manufacturer: Nacalai Tesque Co., Ltd.)
Abrasive silica (trade name: Tixosil (registered trademark) 73, manufacturer: Solvay)
Sorbit liquid (70%) (manufacturer: Mitsubishi Corporation Life Sciences Corporation)
Propylene glycol (manufacturer: ADEKA)
Thickening silica (trade name: Carplex (registered trademark) #67, manufacturer: DSL Japan Co., Ltd.)
Carboxymethyl cellulose sodium (trade name: CMC1260, manufacturer: Daicel Finechem Co., Ltd.)
Sodium lauryl sulfate (manufacturer: BASF)
Sodium fluoride (manufacturer: Stella Chemifa Co., Ltd.)
Saccharin sodium (manufacturer: Aisan Chemical Industry Co., Ltd.)
For ingredients other than the above, raw materials conforming to the Standards for Quasi-drug Ingredients 2006 were used.

<Evaluation method>
It was evaluated by 4 subjects. In the case of a dentifrice, 1 g of the sample dentifrice composition was placed on a toothbrush (clinica advantage toothbrush, 4-row compact normal, manufactured by Lion Co., Ltd.), and after brushing the teeth for 3 minutes, 10 mL of water was once applied to the oral cavity. rinsed out. In the case of mouth spray, an appropriate amount was sprayed into the oral cavity. The metallic taste in the oral cavity immediately after use and the metallic taste when drinking water 30 minutes after use were evaluated according to the following scoring criteria.

<Metallic taste in the oral cavity>
Scoring criteria 5: Not felt at all 4: Hardly felt 3: Slightly felt but acceptable level 2: Feeled 1: Very felt Evaluation criteria ◎: 4 points or more ○: 3 points or more and less than 4 points ×: less than 3 points

[Table footnote]
* In Comparative Example 4, the stimulus derived from (1R,2S,5R)-N-(4-(cyanomethyl)phenyl)menthylcarboxamide was strong and could not be evaluated.
** The composition of the perfume is as follows.
Peppermint oil 50% by mass
Peppermint refined oil (20% cut in the upstream part) 5% by mass
Peppermint refined oil (15% cut in the front and back streams) 5% by mass
Spearmint oil 1% by mass
Spearmint refined oil (20% cut in the upstream part) 1% by mass
Japanese peppermint oil 1% by mass
Japanese peppermint refined oil (30% cut in the upstream part) 1% by mass
Menthol 10% by mass
Carvone 1% by mass
solvent balance
Total 100% by mass

In Comparative Examples 1 to 4 containing the A component and various other cooling agents instead of the B component, the metallic taste immediately after use could be suppressed, but the metallic taste could not be suppressed after 30 minutes of use, or both. could not be suppressed (Table 6). Moreover, even in Comparative Example 5, in which anethole was included as an alternative component and the ratio of anethole and sorbitol was 1:210, the metallic taste after 30 minutes of use could not be suppressed (Table 6). In contrast, all of Examples 1 to 22 containing the A and B components could suppress the metallic taste immediately after use and 30 minutes after use (Tables 1 to 5).
These results show that, according to the present invention, an oral composition containing a compound that releases metal ions can suppress metallic taste caused by the compound during and after use.

A prescription example is shown below. In the formulation examples, the perfumes are the same as those used in Examples 1-22.

Formulation Example 1: Mouthwash (A1): Copper gluconate 0.5% by mass
(B): N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide 0.0005% by mass
Ethanol 2.0% by mass
Citric acid 0.05% by mass
Sodium citrate 0.3% by mass
Polyoxyethylene (60) hydrogenated castor oil 0.5% by mass
Cetylpyridinium chloride 0.05% by mass
Methyl paraoxybenzoate 0.25% by mass
Perfume 1% by mass
Water Remaining total 100% by mass
(B)/(A) = 0.001

Formulation Example 2: Mouthwash (A1): Copper gluconate 0.5% by mass
(B): N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide 0.0005% by mass
Propylene glycol 3.0% by mass
Citric acid 0.05% by mass
Sodium citrate 0.3% by mass
Polyoxyethylene (60) hydrogenated castor oil 0.5% by mass
Cetylpyridinium chloride 0.05% by mass
Methyl paraoxybenzoate 0.25% by mass
Perfume 1% by mass
Water Remaining total 100% by mass
(B)/(A) = 0.001

Formulation Example 3: Toothpaste (A11): Potassium nitrate 5% by mass
(B): N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide 0.005% by mass
Propylene glycol 3.0% by mass
Sorbit liquid (70%) 42.0% by mass
Silicic anhydride 15.0% by mass
Sodium polyacrylate 0.7% by mass
Polyethylene glycol 400 0.3% by mass
Xanthan gum 1.6% by mass
Carrageenan 0.2% by mass
Coconut fatty acid amidopropyl betaine liquid 1.0% by mass
Sodium alginate 0.3% by mass
Sodium lauroyl sarcosinate 0.2% by mass
Sodium tetradecene sulfonate 0.4% by mass
Sodium lauroyl methyl taurate 0.5% by mass
Polyoxyethylene (60) hydrogenated castor oil 1.0% by mass
Polyoxyethylene (10) stearyl ether 1.5% by mass
Polyglyceryl monolaurate 0.1% by mass
Tocopherol acetate 0.2% by mass
Dextranase (13,000 units/g) 0.19 wt%
Sodium fluoride 0.21% by mass
Sodium monofluorophosphate 0.36% by mass
DL-alanine 0.5% by mass
Sodium DL-pyrrolidonecarboxylate liquid 7.0% by mass
Hydroxyethyl cellulose dimethyl diallyl ammonium chloride 0.02% by mass
Saccharin sodium 0.08% by mass
Titanium oxide 0.6% by mass
Perfume 1.2% by mass
Water Remaining total 100% by mass
(B)/(A) = 0.001

Formulation Example 4: Toothpaste (A11): Potassium nitrate 5% by mass
(B): N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide 0.0005% by mass
Propylene glycol 5.0% by mass
Polyethylene glycol 400 1.0% by mass
Sorbit liquid (70%) 45.0% by mass
Silicic anhydride 13.0% by mass
Sodium polyacrylate 0.6% by mass
Xanthan gum 1.1% by mass
Carboxymethylcellulose sodium 0.1% by mass
Sodium alginate 0.6% by mass
Coconut fatty acid amidopropyl betaine liquid 2.0% by mass
Sodium lauroyl sarcosinate 0.1% by mass
Sodium lauroyl methyl taurate 0.3% by mass
Sodium tetradecene sulfonate 0.3% by mass
Polyoxyethylene (20) hydrogenated castor oil 2.0% by mass
Polyoxyethylene (5) stearyl ether 1.5% by mass
Polyglyceryl monolaurate 0.1% by mass
Phellodendron bark extract 0.02% by mass
Tocopherol acetate 0.1% by mass
Glycyrrhetinic acid 0.05% by mass
Dextranase (13,000 units/g) 0.15 wt%
Tranexamic acid 0.05% by mass
Sodium fluoride 0.32% by mass
DL-alanine 0.15% by mass
Sodium DL-pyrrolidonecarboxylate liquid 6.0% by mass
Hydroxyethyl cellulose dimethyl diallyl ammonium chloride 0.05% by mass
Saccharin sodium 0.11% by mass
Xylitol 0.09% by mass
Titanium oxide 0.4% by mass
Mica titanium 0.2% by mass
Perfume 1.3% by mass
Water Remaining total 100% by mass
(B)/(A) = 0.0001

Formulation Example 5: Toothpaste (A11): Potassium nitrate 5% by mass
(B): N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide 0.0001% by mass
Propylene glycol 8.0% by mass
Sorbit liquid (70%) 18.0% by mass
Glycerin 15.5% by mass
Silicic anhydride 18.0% by mass
Sodium polyacrylate 0.7% by mass
Xanthan gum 0.8% by mass
Carboxymethylcellulose sodium 0.1% by mass
Sodium alginate 0.7% by mass
Coconut fatty acid amidopropyl betaine liquid 1.5% by mass
Sodium lauroyl sarcosinate 0.1% by mass
Sodium tetradecene sulfonate 0.5% by mass
Polyoxyethylene (20) hydrogenated castor oil 3.0% by mass
Polyoxyethylene (5) stearyl ether 0.5% by mass
Polyglyceryl monolaurate 0.5% by mass
Tocopherol acetate 0.2% by mass
Isopropylmethylphenol 0.05% by mass
Dextranase (13,000 units/g) 0.13% by weight
Sodium fluoride 0.32% by mass
DL-alanine 0.3% by mass
Sodium DL-pyrrolidonecarboxylate liquid 8.0% by mass
Hydroxyethyl cellulose dimethyl diallyl ammonium chloride 0.1% by mass
Saccharin sodium 0.06% by mass
Stevia extract 0.01% by mass
Titanium oxide 1.0% by mass
Perfume 1.5% by mass
Water Remaining total 100% by mass
(B)/(A) = 0.00002

Claims (8)

1. (A) one or more selected from the following (Ai) and (A-ii):
   (Ai) a compound that releases one or more metal ions selected from the group consisting of copper, zinc, tin, and aluminum;
   (A-ii) a compound that releases potassium ions; and (B) N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide.
2. The composition for oral cavity according to claim 1, wherein (B)/(A) is 0.00001 or more as a mass ratio.　
3. The oral cavity composition according to claim 1 or 2, wherein the amount of component (Ai) is 5% by mass or less.　
4. The oral cavity composition according to any one of claims 1 to 3, wherein the amount of component (A-ii) is 10% by mass or less.　
5. The oral composition according to any one of claims 1 to 4, wherein the amount of component (B) is 0.000005 to 0.1% by mass.　
6. (Ai) component is selected from the group consisting of copper gluconate, copper citrate, copper sulfate, zinc chloride, zinc citrate, zinc gluconate, zinc acetate, zinc sulfate, tin fluoride, and aluminum lactate 1 species or two or more species,
   The oral composition according to any one of claims 1-5.
7. (A-ii) component is one or more selected from potassium nitrate, potassium hydroxide, potassium citrate, potassium chloride, and potassium sulfate;
   The oral composition according to any one of claims 1-6.
8. The oral composition according to any one of claims 1 to 7, which is a dentifrice, mouthwash, or spray.