Oral composition

Abstract

To ensure the stability of an amino acid with time and to suppress the deterioration of appearance with time such as the deterioration of kneaded skin.SOLUTION: An oral composition comprising (A) amino acids, (B) silicic anhydride, and (C) a fluorine-containing compound, wherein the content of (C) the fluorine-containing compound is an amount corresponding to 3000ppm to 20000ppm in terms of fluoride ion concentration.SELECTED DRAWING: None

Description

[Technical Field]

[0001] The present invention relates to an oral composition. [Background technology]

[0002] Oral compositions may contain amino acids with anti-inflammatory properties, such as tranexamic acid and epsilon-aminocaproic acid (ε-aminocaproic acid), for the purpose of preventing and inhibiting the progression of periodontal disease.

[0003] Specifically, for example, even when cetylpyridinium chloride and tranexamic acid are combined, a known embodiment is to combine tranexamic acid or a salt thereof, a cationic disinfectant, a disinfectant that is an anionic surfactant, and a fluorine-containing compound in order to improve the refreshing aftertaste (see Patent Document 1).

[0004] Furthermore, even when an aluminum compound and epsilon-aminocaproic acid and / or its salt are used in combination, an embodiment is known in which an α-amino acid and / or its salt is incorporated into an oral composition in order to stabilize the epsilon-aminocaproic acid and / or its salt (see Patent Document 2).

[0005] Furthermore, when limonene and tranexamic acid are used in combination, an embodiment is known in which a predetermined amount of thickening silica is blended into an oral composition in order to prevent the remaining amount of tranexamic acid from decreasing over time (see Patent Document 3). [Prior art documents] [Patent documents]

[0006] [Patent Document 1] JP 2019-52110 A [Patent Document 2] Japanese Patent Application Laid-Open No. 2016-69331 [Patent Document 3] Japanese Patent Publication No. 2022-39864 Summary of the Invention [Problem to be solved by the invention]

[0007] Even when amino acids such as tranexamic acid and epsilon-aminocaproic acid are combined with silicic anhydride in an oral composition, there is a risk that the amino acids will be adsorbed onto the silicic anhydride, resulting in a decrease in the amino acid content over time.

[0008] Therefore, the object of the present invention is to provide an oral composition that can effectively suppress the decrease in amino acid content over time, increase the stability of the amino acid, and suppress deterioration of appearance even after storage for a specified period of time, even when amino acids such as tranexamic acid and epsilon-aminocaproic acid are used in combination with silicic anhydride in the oral composition. [Means for solving the problem]

[0009] That is, the present invention provides the following [1] to [4]. [1] (A) an amino acid; (B) silicic anhydride, (C) fluorine-containing compounds and It contains (C) An oral composition in which the content of the fluorine-containing compound is 3000 ppm to 20000 ppm when converted into a fluoride ion concentration. [2] The oral composition according to [1], wherein the amino acid (A) is one or both of tranexamic acid and epsilon-aminocaproic acid. [3] The oral composition according to [1] or [2], wherein the content of the fluorine-containing compound (C) is an amount that is 4000 ppm to 15000 ppm when converted into a fluoride ion concentration. [4] The oral composition according to any one of [1] to [3], which is a dentifrice. [Effects of the Invention]

[0010] According to the present invention, even when an amino acid such as tranexamic acid and epsilon-aminocaproic acid is used in combination with silicic anhydride in an oral composition, it is possible to provide an oral composition that effectively suppresses a decrease in the amino acid content over time, thereby increasing the stability of the amino acid, and that suppresses deterioration of the appearance, such as a pasted skin, when the composition is exposed from a storage container even after a predetermined period of storage. DETAILED DESCRIPTION OF THE INVENTION

[0011] The present invention will be described in detail below. The oral composition of the present invention contains (A) an amino acid, (B) silicic anhydride, and (C) a fluorine-containing compound, and the content of (C) the fluorine-containing compound is an amount, when converted into a fluorine ion concentration, of 3000 ppm to 20000 ppm.

[0012] First, we will explain the (A) amino acid (sometimes referred to as component (A)), (B) silicic anhydride (sometimes referred to as component (B)), and (C) fluorine-containing compound (sometimes referred to as component (C)) contained in the oral composition of this embodiment.

[0013] [(A) Amino acid] In this embodiment, the amino acid (A) is a component that imparts an anti-inflammatory effect to the oral composition. In this embodiment, the amino acid (A) is not particularly limited, provided that the effect of the present invention is not impaired.

[0014] Examples of the (A) amino acid of this embodiment include tranexamic acid, epsilon-aminocaproic acid, arginine, lysine, glutamine, cysteine, and glycine.

[0015] In this embodiment, the amino acid (A) may be of the L-form or the D-form, and may contain both optical isomers in any ratio. In this embodiment, (A) amino acid includes "salt of amino acid".

[0016] In this embodiment, the amino acid (A) is preferably tranexamic acid and / or epsilon-aminocaproic acid, from the viewpoints of imparting an anti-inflammatory effect, further increasing the stability of the amino acid, and suppressing deterioration of the appearance of the skin, such as a smooth texture, after storage for a predetermined period of time.

[0017] In this embodiment, the content of (A) amino acid is preferably 0.025% by mass or more, more preferably 0.03% by mass or more, preferably 0.2% by mass or less, more preferably 0.1% by mass or less, preferably 0.025% by mass to 0.2% by mass, and more preferably 0.03% by mass to 0.1% by mass, when the total amount of the oral composition is taken as 100% by mass, in order to ensure the stability of the amino acid over time and to suppress deterioration of appearance over time, such as deterioration and discoloration of the paste surface.

[0018] [B) Silica anhydride] Component (B) is silicic anhydride (SiO2). By including silicic anhydride (B) in the oral composition of this embodiment, stains and plaque can be effectively removed by physical action, improving the feeling of cleaning, and the feeling of use can be improved by adjusting the viscosity and improving shape retention.

[0019] Examples of (B) silicic anhydride include precipitated silica, silica gel, and pyrogenic silica. In this embodiment, (B) silicic anhydride also includes compounds whose main component is a silicate, such as aluminosilicate, zirconosilicate, and titanium-bonded silica. As (B) silicic anhydride, one or more of these can be used in combination as desired. As (B) silicic anhydride, precipitated silica and / or silica gel are preferably used.

[0020] In this embodiment, the amount of (B) silicic anhydride is, from the viewpoint of ensuring the stability of amino acids over time and suppressing deterioration of appearance over time, such as deterioration and discoloration of the kneaded surface, preferably 1% by mass or more, more preferably 3% by mass or more, preferably 30% by mass or less, more preferably 25% by mass or less, preferably 1% by mass to 30% by mass, and more preferably 3% by mass to 25% by mass, when the total amount of the oral composition is 100% by mass.

[0021] In this embodiment, the average particle size of (B) silicic anhydride is preferably 2 μm or more, more preferably 5 μm or more, preferably 300 μm or less, more preferably 100 μm or less, preferably 2 μm or more and 300 μm or less, and more preferably 5 μm or more and 100 μm or less.

[0022] Here, the "average particle size" refers to the volume-based median diameter (D50) measured by a laser diffraction / scattering method. The average particle size can be measured by a conventionally known method, specifically, for example, using a particle size distribution analyzer (Microtrac particle size distribution analyzer Model MT3000II manufactured by Nikkiso Co., Ltd.) with water as the dispersion medium.

[0023] In this embodiment, the BET specific surface area of ​​(B) silicic anhydride is 15 cm 2 / g or more, and 2 / g or more is more preferable, and 2 / g or less, and 2 / g or less is more preferable, and 15cm 2 / g~500cm 2 / g, and 20cm 2 / g~450cm 2 / g is more preferred.

[0024] Specifically, the BET specific surface area can be measured using a specific surface area measuring device (Nikkiso Co., Ltd., automatic specific surface area meter) by the BET multipoint method at 25°C using nitrogen gas as the measurement gas.

[0025] In this embodiment, (B) silicic anhydride may be abrasive silica and / or thickening silica. Here, abrasive silica is a component that can remove stains and plaque by physical action. On the other hand, thickening silica is a component that has almost no abrasive properties but can improve the feel in use by adjusting the viscosity of the oral composition to improve its shape retention.

[0026] [(C) Fluorine-containing compounds] Component (C) according to an embodiment of this embodiment is a fluorine-containing compound. (C) fluorine-containing compound is a component that supplies fluoride ions to the oral composition. In this embodiment, the fluorine-containing compound that can be used is not particularly limited. (C) fluorine-containing compound includes, for example, sodium fluoride, sodium monofluorophosphate, and stannous fluoride.

[0027] In this embodiment, the (C) fluorine-containing compound may be used alone or in combination of two or more. In this embodiment, the (C) fluorine-containing compound is preferably sodium fluoride and / or sodium monofluorophosphate, from the viewpoint of ensuring stability of the amino acid over time and suppressing deterioration over time of appearance, such as deterioration of the kneaded surface and discoloration.

[0028] In this embodiment, the content of the (C) fluorine-containing compound is, in terms of fluorine ion concentration, preferably 3000 ppm or more, more preferably 4000 ppm or more, and preferably 20000 ppm or less, more preferably 15000 ppm or less, and preferably 3000 ppm to 20000 ppm, and more preferably 4000 ppm to 15000 ppm, from the viewpoint of ensuring stability of the amino acid over time and suppressing deterioration of appearance over time, such as deterioration and discoloration of the kneaded surface, particularly by suppressing adsorption of the (A) amino acid to the (B) silicic anhydride.

[0029] The content of (C) fluorine-containing compound varies depending on the selected fluorine-containing compound. Specifically, for example, when component (C) is sodium fluoride, the content of sodium fluoride is preferably 0.6% by mass or more, more preferably 0.8% by mass or more, preferably 4.5% by mass or less, more preferably 3.4% by mass or less, preferably 0.6% by mass to 4.5% by mass, and more preferably 0.8% by mass to 3.4% by mass, based on 100% by mass of the total amount of the oral composition, in order to ensure stability of the amino acid over time, particularly by suppressing adsorption of the amino acid (A) to the anhydrous silicic acid (B), and to suppress deterioration of appearance over time, such as deterioration of the polished surface and discoloration.

[0030] Furthermore, for example, when component (C) is sodium monofluorophosphate, the content of sodium monofluorophosphate is preferably 2.2% by mass or more, more preferably 3.0% by mass or more, preferably 15.2% by mass or less, more preferably 11.4% by mass or less, preferably 2.2 to 15.2% by mass, and more preferably 3.0 to 11.4% by mass, when the total amount of the oral composition is taken as 100% by mass, in order to ensure the stability of the amino acid over time and to prevent deterioration of the appearance over time, such as deterioration and discoloration of the polished surface, particularly by suppressing adsorption of the amino acid (A) to the anhydrous silicic acid (B).

[0031] Furthermore, for example, when component (C) is stannous fluoride, the content of stannous fluoride is preferably 1.2% by mass or more, more preferably 1.6% by mass or more, preferably 8.3% by mass or less, more preferably 6.2% by mass or less, preferably 1.2 to 8.3% by mass, and more preferably 1.6 to 6.2% by mass, when the total amount of the oral composition is taken as 100% by mass, in order to ensure the stability of the amino acid over time, particularly by suppressing adsorption of the amino acid (A) to the anhydrous silicic acid (B), and to suppress deterioration of the appearance over time, such as deterioration and discoloration of the polished surface.

[0032] [Content ratio] -Component (C) (fluoride ion concentration) / Component (A) - The ratio of the fluoride ion concentration corresponding to the content of component (C) to the content of component (A) (component (C) (fluoride ion concentration) / component (A)) is preferably 20,000 or more, more preferably 80,000 or more, and preferably 400,000 or less, more preferably 120,000 or less, preferably 20,000 to 400,000, and more preferably 80,000 to 120,000, particularly from the viewpoint of suppressing adsorption of the amino acid (A) to the silicic anhydride (B) thereby ensuring stability of the amino acid over time and suppressing deterioration over time of appearance such as deterioration of the kneaded surface and discoloration.

[0033] [Optional ingredients] The oral composition of this embodiment may contain any optional components other than the components (A) to (C) already described, provided that the effects of the present invention are not impaired. These will be specifically described below.

[0034] When the oral composition is a dentifrice composition (liquid dentifrice, gel dentifrice, or toothpaste), examples of optional components include solvents, surfactants, sweeteners, flavorings, medicinal ingredients, oily ingredients, preservatives, humectants, abrasives, binders, pH adjusters, and colorants (pigments).When the oral composition is a mouthwash, examples of optional components include solvents, humectants, surfactants, sweeteners, preservatives, pH adjusters, and flavorings.These are described in detail below.

[0035] In this specification, the content of each component is based on the amount of each component charged when producing the oral composition.

[0036] -solvent- The oral composition of the present embodiment may further contain a solvent, preferably water (purified water) or ethanol.

[0037] -Surfactants- The oral composition of the present embodiment may further contain a surfactant. Examples of surfactants that can be used in the oral composition include anionic surfactants, nonionic surfactants, and amphoteric surfactants.

[0038] Examples of anionic surfactants include alkyl sulfates, acylamino acid salts, acyltaurine salts, α-olefin sulfonates, hydrogenated coconut fatty acid monoglyceride monosulfates, and lauryl sulfoacetates. The alkyl and acyl groups may be linear or branched, saturated or unsaturated, and typically have 10 to 20 carbon atoms, preferably 12 to 18, and more preferably 12 to 14. The salts may be selected from pharmacologically acceptable salts. Examples of pharmacologically acceptable salts include base addition salts and amino acid salts. Specific examples 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, with alkali metal salts (e.g., sodium salts and potassium salts) and ammonium salts being more preferred, and sodium salts being even more preferred.

[0039] Examples of alkyl sulfates include lauryl sulfate (sodium lauryl sulfate) and myristoyl sulfate. Examples of acylamino acid salts include acyl sarcosine salts such as lauroyl sarcosine salt and myristoyl sarcosine salt; 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 acyltaurates include lauroyl methyl taurine, N-methyl-N-acyltaurate, and N-cocoyl methyl taurine. Examples of α-olefin sulfonates include 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 and sodium lauryl sulfoacetate.

[0040] In terms of foaming and foam quality, the anionic surfactant preferably contains a sulfonic acid group, and alkyl sulfates and α-olefin sulfonates are more preferred. For example, when the oral composition is a dentifrice, 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 0.8 to 2.5% by mass, of the entire composition. When the oral composition is a mouthwash, the content of the anionic surfactant is preferably 0% by mass to 1.0% by mass, and more preferably 0% by mass to 0.3% by mass, when the total amount of the oral composition is taken as 100% by mass.

[0041] Examples of nonionic surfactants 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, glycerin 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 alkyl chain of the polyoxyethylene alkyl ether typically has 14 to 18 carbon atoms, and the average number of moles of ethylene oxide added is typically 5 to 30 moles. The average number of moles of ethylene oxide added in polyoxyethylene hydrogenated castor oil is typically 20 to 100 moles, preferably 20 to 60 moles. The fatty acid of the sorbitan fatty acid ester typically has 12 to 18 carbon atoms. 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. The number of carbon atoms in the alkyl chain of the alkylolamide is usually 12 to 14. Preferred nonionic surfactants are polyoxyethylene hydrogenated castor oil, polyoxyethylene sorbitan fatty acid ester, and polyoxyethylene alkyl ether.

[0042] Examples of amphoteric surfactants include betaine-type amphoteric surfactants such as alkyl dimethylamino acetic acid betaine (e.g., lauryl dimethylamino acetic acid betaine) and fatty acid amidopropyl dimethylamino acetic acid 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 oil fatty acid acyl-N-carboxymethyl-N-hydroxyethyl imidazolinium betaine), coconut oil fatty acid imidazolinium betaine, and 2-alkyl-N-carboxymethyl-N-hydroxyethyl imidazolinium betaine; and alkyl betaines such as lauryl dimethylamino acetic acid betaine.

[0043] The content of the surfactant is typically 0.05% by mass or more, preferably 0.1% by mass or more, and more preferably 0.5% by mass or more, and typically 10% by mass or less, preferably 5% by mass or less, and more preferably 3% by mass or less, and typically 0.05% by mass to 10% by mass, preferably 0.1% by mass to 5% by mass, and more preferably 0.5% by mass to 3% by mass, when the total amount of the oral composition is 100% by mass.

[0044] -Sweetener- The oral composition of the present embodiment may contain any suitable conventionally known sweetener in any suitable amount. By including a sweetener in the oral composition, the feeling of use can be further improved.

[0045] Examples of sweeteners include saccharin, saccharin sodium, aspartame, stevioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidin dihydrochalcone, perillartine, thaumatin, aspartyl phenylalanine methyl ester, etc. As the sweetener, one of the above-exemplified sweeteners may be used alone, or two or more may be used in combination.

[0046] -Fragrance- The oral composition of the present embodiment may contain any suitable conventionally known flavor in any suitable amount. By including a flavor in the oral composition, the feeling of use can be further improved.

[0047] Examples of fragrances include natural essential oils such as 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, 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, paracles oil, vanilla oil, cinnamon oil, pimento oil, cinnamon leaf oil, perilla oil, and wintergreen oil; menthol, carvone, cinnamic aldehyde, anethole, 1,8-cineole, methyl salicylate, eugenol, thymol, linalool, limonene, menthone, and menthyl acetate. , citral, decanal, camphor, borneol, pinene, spilanthol, n-decyl alcohol, citronellol, α-terpineol, citronellyl acetate, ethyl linalool, vanillin, and other fragrance components contained in the above-mentioned natural essential oils; ethyl acetate, ethyl butyrate, isoamyl acetate, hexanal, hexenal, methyl anthranilate, ethyl methylphenylglycidate, benzaldehyde, vanillin, ethyl vanillin, furaneol, N-ethyl-p-menthane-3-carboxamide, menthyl lactate, ethylene glycol-l-menthyl carbonate, and other fragrance components; and various blended flavors such as mint, fruit, and herb flavors that are made by combining several fragrance components and natural essential oils. Examples of fragrances that can also function as cooling agents include N-ethyl-p-menthane-3-carboxamide, menthyl lactate, menthyl monosuccinate, isopulegol, menthone glycerol ketal, N-(4-cyanomethylphenyl)-p-menthanecarboxamide, 3-l-menthoxypropane-1,2-diol, 5-methyl-2-propan-2-yl-N-(2-pyridin-2-ylethyl)cyclohexane-1-carboxamide, ethyl 3-(p-menthane-3carboxamide)acetate, and 2-isopropyl-N,2,3-trimethylbutyramide. The fragrances exemplified above may be used alone or in combination of two or more.When the oral composition contains a flavoring, the content thereof is usually 0.000001% by mass to 1% by mass, and preferably 0.01% by mass to 1% by mass, when the total amount of the oral composition is taken as 100% by mass. When the oral composition contains a flavoring that can also function as a cooling agent, the content thereof is preferably 0.00001% by mass to 0.01% by mass, when the total amount of the oral composition is taken as 100% by mass.

[0048] -Medicinal ingredients- Examples of medicinal ingredients include anti-inflammatory agents such as allantoin, allantoin chlorhydroxyaluminum, azulene, glycyrrhizinic acid or a salt thereof (e.g., dipotassium glycyrrhizinate), and glycyrrhetinic acid or a salt thereof (e.g., stearyl glycyrrhetinate); cell activators such as sodium chloride and vitamins; isopropylmethylphenol, cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride, hinokitiol, thymol, lysozyme chloride, chlorhexidine, triclosan, zinc gluconate, and chlorhexidine. Examples of suitable oral compositions include bactericidal or antibacterial agents such as zinc enoate; water-soluble copper compounds such as copper chlorophyll and copper gluconate; anti-tartar agents such as zeolite, ethanehydroxydiphosphonate, and polyphosphates; vitamins such as vitamin C (e.g., ascorbic acid), vitamin E (e.g., tocopherol acetate, tocopherol nicotinate, and tocopherol) and pyridoxine; astringents such as sodium chloride, alum, and lysozyme chloride; anti-dentin hypersensitivity agents such as potassium nitrate, aluminum lactate, and strontium chloride; and peptides such as callopeptides. When the oral composition contains a medicinal ingredient, the amount contained therein can be an effective amount within a range that does not interfere with the effects of the present invention (a pharmacologically acceptable range).

[0049] -Oil-based ingredients- Examples of oily components include hydrocarbons such as squalane, (light) 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.

[0050] -Preservatives- The oral composition of the present embodiment may contain any suitable preservative known in the art in any suitable amount. By including a preservative in the oral composition, the oral composition can ensure its preservative power.

[0051] Examples of preservatives that may be contained in the oral cavity composition include parahydroxybenzoic acid esters (e.g., methyl parahydroxybenzoate, ethyl parahydroxybenzoate, butyl parahydroxybenzoate), sodium benzoate, etc. The preservatives may be used alone or in combination of two or more.

[0052] -Wetting agent- The oral composition of the present embodiment may contain any suitable conventionally known humectant in any suitable amount. By including any suitable humectant in the oral composition, the feeling of use can be further improved.

[0053] 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. Examples of polyethylene glycols include polyethylene glycols having an average molecular weight of 150 to 6,000, preferably polyethylene glycols having an average molecular weight of 190 to 630. Specific examples include PEG200, PEG300, PEG400, and PEG600. The average molecular weight is the average molecular weight specified in the Quasi-drug Raw Materials Standards 2021. When the oral composition contains a humectant, the content of the humectant is typically 1% to 70% by mass, preferably 1% to 65% by mass, more preferably 1% to 60% by mass, and even more preferably 3% to 60% by mass, based on 100% by mass of the total amount of the oral composition.

[0054] -Abrasives- Abrasives other than the abrasive silica, which is component (B), can be suitably used when the oral composition of this embodiment is a dentifrice composition (liquid dentifrice, gel dentifrice, toothpaste).

[0055] The abrasive other than the abrasive silica of component (B) may be either an inorganic abrasive or an organic abrasive. Examples of inorganic abrasives include calcium carbonate abrasives such as heavy calcium carbonate; calcium hydroxide, aluminum hydroxide, tribasic magnesium phosphate, magnesium carbonate, calcium sulfate, bentonite, and hydroxyapatite. Examples of organic abrasives include synthetic resin abrasives and polymethyl methacrylate.

[0056] In the oral composition of this embodiment, two or more of the above-exemplified abrasives can be blended as abrasives other than the abrasive silica of component (B). Among these, inorganic abrasives are preferred, and calcium carbonate-based abrasives are more preferred.

[0057] The blending amount of the abrasive other than the abrasive silica of component (B), when the total amount of the oral composition is taken as 100% by mass, is preferably 7% by mass or more, more preferably 10% by mass or more, including the content of the abrasive silica of component (B). This makes it possible to impart appropriate cleaning properties and realize a good usability. The upper limit is preferably 50% by mass or less, more preferably 30% by mass or less. This makes it possible to impart good cleaning properties and realize a good usability. Therefore, the content of the abrasive is preferably 7% by mass to 50% by mass, more preferably 10% by mass to 50% by mass, and even more preferably 10% by mass to 30% by mass.

[0058] -Binder- The oral composition of this embodiment may contain any suitable amount of a binder other than the conventionally known and suitable thickening silica component (B). By including a binder other than the optional component (B) thickening silica in the oral composition, the viscosity can be optimized, and the shape retention and usability can be further improved.

[0059] Examples of binders other than thickening silica, which is optional component (B) that may be contained in the oral composition, include any suitable organic binders known in the art, such as polysaccharides, cellulose-based binders (e.g., carboxymethylcellulose (CMC), hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropylmethylcellulose, methylcellulose, cationized cellulose, etc., and pharmacologically acceptable salts thereof, such as sodium salts), other polysaccharide-based 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). Furthermore, inorganic binders such as aluminum silicate may also be blended. In the oral composition of this embodiment, two or more of the above-exemplified binders may be blended as binders other than thickening silica, which is component (B).

[0060] The content of any organic binder other than the thickening silica (B), when the total amount of the oral composition is taken as 100% by mass, including the thickening silica (B), is preferably greater than 0%, more preferably 0.1% or more, preferably 12% or less, more preferably 10% or less, preferably greater than 0% but not greater than 12%, and more preferably 0.1% to 10% by mass. The content of any inorganic binder other than the thickening silica (B), when the total amount of the oral composition is taken as 100% by mass, including the thickening silica (B), is preferably greater than 0%, more preferably 1% or more, preferably 11% or less, more preferably 8% or less, preferably greater than 0% but not greater than 11%, and more preferably 1% to 8% by mass.

[0061] - pH adjuster - The oral composition of the present embodiment may contain any suitable conventionally known pH adjuster in any suitable amount. By including a pH adjuster in the oral composition, the pH stability of the oral composition can be ensured.

[0062] 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 (e.g., sodium citrate), inorganic acids such as phosphoric acid (e.g., 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.

[0063] The content of the pH adjuster can usually be an amount that will give a pH of the oral composition after addition of the pH adjuster of 5.0 to 9.0, preferably 6.0 to 8.5.

[0064] In this specification, the pH value generally refers to the value measured 3 minutes after the start of measurement at 25° C. The pH value can be measured, for example, using a pH meter (model number Hm-30S) manufactured by Toa Dempa Kogyo Co., Ltd.

[0065] -Coloring agent- The oral composition of the present embodiment may contain any suitable colorant known in the art in any suitable content.

[0066] Examples of colorants that the oral composition may contain 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, cocoa colorant, spirulina blue colorant, and tamarind colorant, as well as legally designated 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, and Blue No. 1, riboflavin, sodium copper chlorophyll, and titanium dioxide. When the oral composition contains a colorant, the content thereof is preferably 0.00001% to 3% by mass when the total amount of the oral composition is taken as 100% by mass.

[0067] -Other optional ingredients- The oral composition of the present embodiment may contain any suitable amount of optional components other than those described above.

[0068] In this embodiment, examples of other optional components that may be contained in the oral composition include inorganic compounds such as titanium mica, titanium oxide, zinc oxide, magnesium oxide, and zirconium oxide; natural polymer compounds such as agar, gelatin, starch, and glucomannan; synthetic polymer compounds or copolymers thereof such as polyvinyl acetate, acrylic resin, polyurethane, polyester, polyvinyl chloride, nylon powder, and polyethylene powder; waxes such as carnauba wax, rosin, rice wax, microcrystalline wax, beeswax, and paraffin wax; higher alcohols such as cetanol and stearyl alcohol; polyisobutylene, polybutadiene, urethane, silicone, and natural rubber. The content of these other optional components can be appropriately set within a range that does not interfere with the effects of the present invention.

[0069] [Dosage form and use of oral composition] The oral composition of this embodiment can be made into any suitable conventional dosage form by any suitable method according to conventional methods. Examples of dosage forms include liquids (liquids such as solutions, emulsions, suspensions, syrups, etc.), semi-solids (gels, creams, pastes, etc.), and solids (tablets, particulates, capsules, films, kneaded materials, molten solids, waxy solids, elastic solids, soft capsules, etc.). The dosage form of the oral composition is preferably a liquid or semi-solid.

[0070] The oral composition of the embodiment can be widely used in oral applications. Examples of applications in solid dosage forms include lozenges, gummies, chewing gum, and dentifrices. Examples of applications in semisolid dosage forms include toothpastes and gel dentifrices. Examples of applications in liquid dosage forms include mouthwashes, liquid dentifrices, and mouth fresheners (sprays, etc.).

[0071] Specifically, the oral composition of this embodiment is preferably made into a dentifrice (liquid dentifrice, toothpaste, gel dentifrice), for example.

[0072] In this embodiment, the oral composition preferably has a pH (25° C.) of 5.0 to 9.0. The pH can be adjusted by adding a pH adjuster, adjusting the component composition, and the like.

[0073] The viscosity of the oral composition of this embodiment can be adjusted appropriately depending on the dosage form, for example. When the oral composition is in paste or gel form, the viscosity at 25°C measured with a BH viscometer is preferably 30 Pa s to 150 Pa s.

[0074] In the case of an oral composition in a liquid dosage form, the viscosity at 25°C measured with a BH viscometer should be 30 mPa·s or less, and preferably 0.7 mPa·s to 30 mPa·s.

[0075] According to the oral composition of the present invention, by using a predetermined amount of fluorine-containing compound, it is possible to effectively suppress the adsorption of (A) amino acid to (B) silicic anhydride, thereby ensuring the stability of the amino acid over time and suppressing deterioration of the appearance over time, such as deterioration and discoloration of the kneaded surface.

[0076] [Method of manufacturing oral composition] The method for producing the oral composition of this embodiment is not particularly limited. The oral composition can be produced by any suitable method known in the art depending on the selected dosage form. Specific examples of the method for producing the oral composition include, for example, a method in which, when a toothpaste (composition) is produced, components that are soluble in a solvent are first prepared, and then other insoluble components are mixed in, and if necessary, degassing is further performed, for example, by reducing the pressure.

[0077] The toothpaste thus obtained can be placed in a designated container (laminated tube), or in the case of a mouthwash, the prepared liquid can be placed in a designated container (bottle) to make the final product.

[0078] The shape and material of the container in which the oral composition of the present invention can be stored are not particularly limited. Any suitable conventional container that is normally used for oral compositions can be used as the container. Examples of the container include plastic containers made of polyethylene, polypropylene, polyethylene terephthalate, and nylon. [Example]

[0079] The present invention will be specifically described below with reference to examples and comparative examples. The present invention is not limited to these examples. Numerical values ​​described in these examples (including the numerical values ​​in the following table) represent mass % unless otherwise specified.

[0080] [Components used in the Examples and Comparative Examples] First, the components used in the examples and comparative examples will be described. -Component (A) Amino Acids- (A1) ε-aminocaproic acid (manufactured by Daiichi Sankyo Co., Ltd.) (A2) Tranexamic acid (Kyowa Pharma Chemical Co., Ltd.)

[0081] -Component (B) Silica anhydride- (B1) Silica anhydride-1 (Zeodent 113: manufactured by Evonik Japan, abrasive) (B2) Silica anhydride-2 (Zeodent 165: manufactured by Evonik Japan, thickener)

[0082] -Component (C) Fluorine-containing compound- (C1) Sodium fluoride (manufactured by Stella Chemifa Co., Ltd.) (C2) Sodium monofluorophosphate (manufactured by CL Japan)

[0083] -Optional ingredients- (ingredients other than ingredients (A) to (C)) Sodium lauryl sulfate (BASF) Sorbitol solution (70%) (Mitsubishi Corporation Life Sciences) Xanthan gum (DSP Gokyo Food & Chemical Co., Ltd.) Sodium polyacrylate (manufactured by Toagosei Co., Ltd.) Propylene glycol (ADEKA) Saccharin sodium (Aisan Chemical Industry Co., Ltd.) Fragrance A purified water

[0084] The composition of fragrance A used in the examples and the compositions of fragrances B to P that can be used in place of fragrance A are shown in Tables 1 to 10 below.

[0085] [Table 1]

[0086] [Table 2]

[0087] [Table 3]

[0088] [Table 4]

[0089] [Table 5]

[0090] [Table 6]

[0091] [Table 7]

[0092] [Table 8]

[0093] [Table 9]

[0094] [Table 10]

[0095] Examples 1 to 10 and Comparative Examples 1 to 4 Using the above ingredients as raw materials, oral compositions having the formulations shown in Tables 11 to 13 below were prepared according to the preparation methods described below.

[0096] [Preparation of oral composition] The raw materials shown in Tables 1 and 2 were blended by a conventional method to obtain a dentifrice composition ((paste) dentifrice), which is an oral composition. The obtained oral composition was then placed in any suitable conventionally known oral preparation container (a laminated tube for a dentifrice composition).

[0097] The resulting dentifrice compositions (Examples 1 to 10 and Comparative Examples 1 to 4) were evaluated according to the following procedures. The evaluation results are shown in Tables 11 to 13 below.

[0098] [Evaluation method] (1) Evaluation of amino acid stability Three laminated tubes were filled with 50 g of each dentifrice composition and stored at 50°C for three months. After the storage treatment was completed, the laminated tubes were returned to room temperature, and the stability of the amino acids calculated from the quantitative values ​​of each amino acid before and after the storage treatment was evaluated according to the following formula and the following criteria. The amino acids were quantified by liquid chromatography according to conventional methods. The results are shown in Tables 11 to 13 below. Formula: Amino acid stability (%) = {(Amino acid quantification value after storage) / (Amino acid quantification value before storage)} x 100 (Evaluation criteria) ◎ (Excellent): Amino acid stability is 96% or more Good: Amino acid stability is 94% or more but less than 96% △ (Acceptable): Amino acid stability is 90% or more but less than 94% × (Not acceptable): Amino acid stability is less than 90%

[0099] (2) Evaluation of the kneaded surface The dentifrice composition was filled into three laminated tubes at 50 g each, and stored at -5°C for one month.

[0100] At -5°C, three 15cm long tubes of dentifrice composition were extruded from the laminated tube onto an evaluation sheet, and the evaluation sheet was folded and pinched to slightly crush the dentifrice composition. The sheet was then opened to its original state, and the texture of the dentifrice composition was evaluated using the following rating scale. Each of the three laminated tubes was evaluated in the same manner, and the average score of the three laminated tubes was evaluated using the following rating scale. The results are shown in Tables 1 to 3 below. (Grading criteria) 5 points: No wrinkles or grains, the surface is shiny 4 points: Some wrinkles and no shine 3 points: There are some wrinkles or grains 2 points: Wrinkles and grains are uniformly observed 1 point: Many wrinkles and grains are uniformly observed, and the dentifrice composition is not uniform (Evaluation criteria) ◎(Excellent): Average score 4.6 or higher ○ (Good): Average score 4.3 points or more and less than 4.6 points △ (Acceptable): Average score 4.0 or more and less than 4.3 points × (Fail): Average score below 4.0 points

[0101] [Table 11]

[0102] [Table 12]

[0103] [Table 13]

[0104] As is clear from the above, Examples 1 to 10, which contained components (A), (B), and (C) and also contained a predetermined amount of component (C), were good in both amino acid stability and evaluation of the texture, while Comparative Examples 1 to 4, which lacked component (B) or did not contain a predetermined amount of component (C), were extremely poor in evaluation of both the texture and the stability of the texture and amino acids. Note that similar effects were obtained when fragrance A used in Examples 1 to 10 was replaced with fragrance B to fragrance P, respectively.

Claims

1. (A) an amino acid; (B) silicic anhydride; (C) a fluorine-containing compound; It contains (C) An oral composition in which the content of the fluorine-containing compound is an amount, calculated as a fluorine ion concentration, of 3,000 ppm to 20,000 ppm.

2. 2. The oral composition of claim 1, wherein the amino acid (A) is one or both of tranexamic acid and epsilon-aminocaproic acid.

3. 3. The oral composition according to claim 1, wherein the content of the fluorine-containing compound (C) is in an amount equivalent to a fluoride ion concentration of 4,000 ppm to 15,000 ppm.

4. The oral composition according to claim 1 or 2, which is a dentifrice.