Oral components

By combining specific enzymes with cooling agents, the bitterness issue in dentifrice compositions due to high-temperature storage is addressed, ensuring a pleasant taste and improved usability.

JP7779709B2Active Publication Date: 2025-12-03LION CORP
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Patent Information

Application Number
JP2021192407
Authority / Receiving Office
JP · JP
Patent Type
Patents
Current Assignee / Owner
Filing Date
2021-11-26
Publication Date
2025-12-03
Estimated Expiration
2041-11-26

AI Technical Summary

Technical Problem

Conventional dentifrice compositions containing enzymes for plaque breakdown develop a bitter taste after high-temperature storage due to the volatility of flavoring ingredients and enzyme sensitivity to temperature changes, necessitating improved bitterness reduction during storage.

Method used

Incorporation of specific polysaccharide-degrading and protease enzymes with cooling agents like N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide to stabilize enzyme activity and reduce bitterness perception during high-temperature storage.

Benefits of technology

The solution effectively suppresses bitterness and maintains a pleasant taste sensation even after prolonged high-temperature storage, enhancing usability and reducing the need for temperature control during logistics and storage.

✦ Generated by Eureka AI based on patent content.

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Abstract

To provide an oral composition comprising an enzyme, making it possible to inhibit a peculiar acridity derived from the enzyme after high temperature storage, and also capable of keeping the inhibitory effect.SOLUTION: An oral composition comprises a component (A): at least one enzyme selected from the group consisting of polysaccharide-degrading enzymes and proteases, and a component (B): at least one selected from N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide, N-(4-cyanomethylphenyl)-2-isopropyl-5-methylcyclohexane carboxamide, and N-(2-(2-pyridinyl)ethyl)-2-isopropyl-5-methylcyclohexane carboxamide.SELECTED DRAWING: None
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Description

[Technical Field]

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

[0002] Conventional dentifrice compositions have a pleasant taste and a refreshing feeling when used, which encourages continued use and can be expected to improve effectiveness, but they are easily affected by the ingredients they contain. Enzymes, in particular, that have the function of breaking down plaque are effective in preventing dental caries by breaking down plaque, and are therefore incorporated as active ingredients in oral compositions. However, when enzyme-containing toothpaste is used after being stored at high temperatures, there is a drawback in that, although there is no problem with the caries prevention effect, a distinctive bitter taste is felt, which significantly impairs the feeling of use, and improvement in this area has been desired.

[0003] Several methods for masking the harshness of enzymes using flavorings or base ingredients have been reported. Patent Document 1 describes that the combined harshness of dextranase, tranexamic acid, isopropylmethylphenol, and alkyl sulfates can be reduced by adding menthol, anethole, eugenol, and / or thyme oil to a dentifrice composition in specific ratios. Patent Document 2 also reports that the unpleasant taste of nonionic surfactants can be reduced while improving the stability of dextranase by adding sodium lauryl sulfate, polyoxyethylene hydrogenated castor oil, polyoxyethylene alkyl ether, and sodium bicarbonate in specific ratios to an oral composition containing dextranase. [Prior art documents] [Patent documents]

[0004] [Patent Document 1] Japanese Patent Application Publication No. 2019-167297 [Patent Document 2] Patent No. 5228380 Summary of the Invention [Problem to be solved by the invention]

[0005] However, the typical flavoring ingredients used in Patent Document 1 are highly volatile, and when the dentifrice composition is stored at high temperatures, the flavoring ingredients volatilize, which can result in insufficient bitterness reduction. Enzymes such as dextranase are particularly susceptible to temperature changes, and are prone to exhibiting a strong bitterness after high-temperature storage. Therefore, the oral composition of Patent Document 1 has the problem of insufficient bitterness reduction after high-temperature storage. Furthermore, Patent Document 2 also exhibits a strong bitterness derived from dextranase after high-temperature storage, necessitating a need for an improved usability. In recent years, with the progress of global warming, temperatures often rise in warehouses during distribution, retail warehouses, and even during storage at home, even near the sink, creating a need for an improved usability during high-temperature storage.

[0006] An object of the present invention is to suppress the occurrence of unpleasant sensations specific to enzymes after storage at high temperatures in an oral composition containing enzymes, and to achieve a sustained suppression effect. [Means for solving the problem]

[0007] The present inventors provide the following [1] to

[11] . [1] Component (A): one or more enzymes selected from the group consisting of polysaccharide-degrading enzymes and protease enzymes, and Component (B): one or more selected from N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide, N-(4-cyanomethylphenyl)-2-isopropyl-5-methylcyclohexanecarboxamide, and N-(2-(2-pyridinyl)ethyl)-2-isopropyl-5-methylcyclohexanecarboxamide An oral composition comprising: [2] The oral composition according to [1], wherein the polysaccharide-degrading enzyme is one or more enzymes selected from the group consisting of dextranase and mutanase. [3] The oral composition according to [1] or [2], wherein the protease is one or more enzymes selected from the group consisting of papain, actinidin, and bromelain. [4] The dentifrice composition according to any one of [1] to [3], wherein the amount of component (A) is 0.01 to 5.0% by mass. [5] The oral composition according to any one of [1] to [4], wherein the amount of component (B) is 0.00001 to 0.1% by mass. [6] The oral composition according to any one of [2] to [5], wherein the enzymatic activity of dextranase is 10,000 to 14,000 units / g. [7] The oral composition according to any one of [2] to [6], wherein the mutanase enzyme activity is 4,000 to 70,000 U / g. [8] The oral composition according to any one of [3] to [7], wherein the papain has an enzymatic activity of 200,000 to 2,500,000 units / g. [9] The oral composition according to any one of [3] to [8], wherein the enzymatic activity of actinidin is 9,000 to 210,000 units / g.

[10] The oral composition according to any one of [3] to [9], wherein the enzyme activity of bromelain is 300,000 to 500,000 units / g.

[11] The oral composition according to any one of [1] to

[10] , which is a dentifrice. [Effects of the Invention]

[0008] According to the present invention, the occurrence of unpleasant sensations such as bitterness can be suppressed even after high-temperature storage (for example, storage at 30 to 40°C for 1 to 6 months), and the suppression effect can be sustained, thereby reducing the effort required for temperature control during logistics and storage and improving the feel when used. DETAILED DESCRIPTION OF THE INVENTION

[0009] [1. Oral composition] The composition contains the following components (A) and (B):

[0010] [1.1 (A) Component: Enzyme] Component (A) is one or more enzymes selected from the group consisting of polysaccharide-degrading enzymes and proteases. By including component (A), the composition can be endowed with enzyme-derived functions.

[0011] -Polysaccharide degrading enzyme- Polysaccharide-degrading enzymes hydrolyze the glycosidic bonds of polysaccharides to produce their constituent monosaccharides, oligosaccharides, or derivatives thereof. Examples of polysaccharides include dextran, mucin, cellulose, starch, chitin, agarose, carrageenan, heparin, alginic acid, hyaluronic acid, pectin, xylan, glucomannan, levan, glycogen, β-1,6-glucan, β-1,3-glucan, β-1,2-glucan, α-1,3-glucan, and α-1,2-glucan. Among these, polysaccharides involved in oral diseases (e.g., dental caries) are preferred, and polysaccharides contained in oral biofilms (e.g., dental plaque), such as dextran and mucin, are more preferred. Examples of polysaccharide-degrading enzymes include dextranase, mutanase, α-amylase, β-amylase, pullulanase, glucoamylase, α-glucosidase, isoamylase, cellulase (including β-glucanase), and hemicellulase, with dextranase and mutanase being preferred. These enzymes degrade polysaccharides such as dextran and mutan contained in oral biofilms (e.g., dental plaque), thereby inhibiting and preventing the progression of dental caries in the oral cavity. The origin of the enzyme is not particularly limited, and it may be naturally derived from microorganisms, plants, animals, etc., or may be artificially prepared by genetic recombination, chemical synthesis, etc. When the polysaccharide-degrading enzyme is dextranase, it may be derived from bacteria capable of producing dextranase (e.g., bacteria of the genera Chaetomium, Penicillium, Aspergillus, Spicaria, Lactobacillus, and Cellvibrio). When the polysaccharide-degrading enzyme is mutanase, it may be a mutanase derived from a bacterium capable of producing mutanase (for example, the genus Probetella or Paenibacillus). One type of polysaccharide-degrading enzyme may be used alone, or two or more types may be used in combination.

[0012] -Proteolytic enzymes- Proteases are enzymes that catalyze the hydrolysis of peptide bonds in proteins. Proteases may be either endopeptidases or exopeptidases (aminopeptidases, carboxypeptidases), with endopeptidases being preferred. Examples of endoproteases include cysteine ​​proteases such as papain, bromelain, and actinidin, and serine proteases such as nattokinase. Cysteine ​​proteases are preferred, with papain, bromelain, and actinidin being more preferred, and papain being even more preferred. This allows the enzyme to decompose proteins present in oral biofilms (e.g., tongue coating) and exhibit oral biofilm removal effects. The origin of the enzyme is not particularly limited, and it may be naturally derived from microorganisms, plants, animals, etc., or artificially prepared by genetic recombination, chemical synthesis, etc. Papain can be derived from papaya (Carica papaya) fruit, actinidin from kiwi (Actinidia deliciosa) fruit, bromelain from pineapple (Ananas comosus) fruit or rhizome, and nattokinase from Bacillus natto. Examples of protease include proteases produced by bacteria belonging to the genera Aspergillus and Bacillus. Proteases may be used singly or in combination.

[0013] -Enzyme activity- The enzymatic activity (enzyme titer) of the polysaccharide-degrading enzyme and the protease is not particularly limited and can be appropriately selected depending on the type of enzyme. Examples are as follows: The enzymatic activity of dextranase (per 1 g of enzyme, hereinafter the same) is preferably 10,000 to 14,000 U / g, more preferably 11,000 to 13,000 U / g, even more preferably 11,500 to 12,500 U / g, and even more preferably about 12,000 U / g.The enzymatic activity of mutanase is preferably 4,000 to 70,000 U / g, more preferably 5,000 to 10,000 U / g, even more preferably 5,500 to 8,000 U / g, and even more preferably about 6,000 U / g. The enzymatic activity of papain is preferably 200,000 to 2,500,000 U / g, more preferably 500,000 to 1,000,000 U / g, even more preferably 600,000 to 900,000 U / g, and even more preferably about 800,000 U / g.The enzymatic activity of actinidin is preferably 9,000 to 210,000 U / g, more preferably 50,000 to 200,000 U / g, even more preferably 100,000 to 190,000 U / g, and even more preferably about 180,000 U / g. The enzymatic activity of bromelain is preferably 300,000 to 500,000 U / g, more preferably 350,000 to 450,000 U / g, even more preferably 380,000 to 420,000 U / g, and even more preferably about 400,000 U / g. By setting the enzymatic activity of each enzyme within the above numerical range, the desired function of the enzyme can be exhibited well, and the unpleasant feeling (e.g., bitterness) of the oral composition caused by the enzyme-derived component (A) after high-temperature storage can be reduced by the component (B).

[0014] In terms of enzyme activity, one unit is defined as "the amount of enzyme that can convert 1 μmol of substrate in 1 minute at 30°C in 1 L of sample under optimal conditions," based on the 1964 definition of "international units" by the International Union of Biochemistry (see https: / / www.jslm.org / committees / standard / standard_Q&A.pdf).

[0015] The enzymatic activity of each enzyme can be defined according to standard methods. For example, one unit of enzymatic activity for dextranase or mutanase can be defined as the amount of each enzyme that produces free reducing sugars equivalent to 1 μmol of glucose per minute when reacted at 40°C and pH 5 using dextran or mutan, respectively, as substrates. One unit of enzymatic activity for papain, actinidin, and bromelain can be measured according to the Japanese Food Additives Standards. Specifically, it is the amount of each enzyme that produces amino acids equivalent to 1 μg of tyrosine per minute using casein as a substrate. In the above measurement methods, the amount of enzyme can also be measured according to standard methods, such as absorbance. One unit of enzymatic activity for nattokinase can be defined as the amount of enzyme that increases the absorbance (275 nm) of fibrin degradation products by 0.01 per minute using fibrin as a substrate.

[0016] The component (A) may be any of a polysaccharidase, a protease, or a combination thereof, with a polysaccharidase being preferred and a dextranase being more preferred.

[0017] -(A) Component Content- The content of component (A) may be appropriately determined within the range of the effective amount of the enzyme, but from the viewpoint of the effects of the present invention, it is as follows. The lower limit is usually 0.01% by mass or more, preferably 0.05% by mass or more, and more preferably 0.07% by mass or more. This allows the oral composition to contain an effective amount of the enzyme, allowing the desired function of the enzyme to be satisfactorily exhibited. The upper limit of the content of component (A) is usually 5.0% by mass or less, preferably 3.0% by mass or less, and more preferably 1.0% by mass or less. This allows component (B) to reduce the unpleasant sensation (e.g., bitterness) of the oral composition caused by the enzyme from component (A) after high-temperature storage. Therefore, the content of component (A) is preferably 0.01 to 5.0% by mass of the total composition, preferably 0.05 to 3.0% by mass, and more preferably 0.07 to 1.0% by mass. The content of component (A) refers to the content of each enzyme constituting component (A). When component (A) is dextranase (12,000 units / g) and mutanase (6,000 units / g), if the content of each enzyme in component (A) is within the above range, a good plaque decomposition effect can be achieved.

[0018] [1.2 (B) Ingredient: Cooling agent] Component (B) is one or more selected from N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide (molecular weight 316), N-(4-cyanomethylphenyl)-2-isopropyl-5-methylcyclohexanecarboxamide (molecular weight 298), and N-(2-(2-pyridinyl)ethyl)-2-isopropyl-5-methylcyclohexanecarboxamide (molecular weight 288). These cooling agents have larger molecular weights than typical fragrance ingredients, and therefore volatilize less from the composition even during high-temperature storage. Therefore, by including component (B), the discomfort caused by component (A) after high-temperature storage can be suppressed, and the suppression effect can be maintained.

[0019] Component (B) may be a single compound or a combination of two or more compounds, but preferably contains N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide, and more preferably consists of only N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide, which can suppress irritation to the oral cavity.

[0020] -(B) Component content- The content of component (B) is typically 0.000001% by mass or more of the total composition, preferably 0.00001% by mass or more, and more preferably 0.00005% by mass or more. This suppresses the discomfort caused by component (A) after high-temperature storage, and the suppressive effect can be maintained even after use. The upper limit is typically 0.5% by mass or less of the total composition, preferably 0.1% by mass or less, and more preferably 0.05% by mass or less. This suppresses irritation to the oral cavity caused by component (B). Therefore, the content of component (B) is typically 0.000001 to 0.5% by mass of the total composition, preferably 0.00001 to 0.1% by mass, and more preferably 0.00005 to 0.05% by mass.

[0021] [1.3 Optional components] The oral composition may contain components other than the components (A) and (B) to the extent that the effects of the present invention are not impaired.

[0022] Examples of optional components include components that are commonly used in oral compositions, such as abrasives, medicinal components, surfactants, binders, humectants, thickeners, sweeteners, preservatives, pH adjusters, solvents, oily components, colorants (pigments), and flavors. These will be explained in detail below.

[0023] -Abrasives- The abrasive may be either inorganic or organic. Examples of inorganic abrasives include abrasive silicas such as precipitated silica, aluminosilicate, zirconosilicate, crystalline zirconium silicate, and titanium-bonded silica; calcium phosphate compounds such as dibasic calcium phosphate dihydrate or anhydrate, monobasic calcium phosphate, tribasic calcium phosphate, and calcium pyrophosphate; calcium carbonate abrasives such as calcium carbonate; calcium abrasives other than carbonates or phosphates such as calcium hydroxide and calcium sulfate; aluminum-based materials such as aluminum oxide, aluminum hydroxide, and alumina; silicate-based materials such as anhydrous silicic acid, zeolite, and zirconium silicate; magnesium-based materials such as magnesium carbonate and tribasic magnesium phosphate; apatite-based materials 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-based abrasives. Of these, silica-based abrasives are preferred.

[0024] The content of the abrasive is generally 70% by mass or less, preferably 50% by mass or less, and more preferably 8 to 50% by mass, based on the entire oral composition (100% by mass).

[0025] -Medicinal ingredients- Examples of medicinal ingredients include bactericidal or antibacterial agents such as cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride, isopropylmethylphenol, zinc gluconate, zinc citrate, triclosan, thymol, hinokitiol, and lysozyme chloride; enzymes other than component (A) such as amylase and Liteque Enzyme; fluorides such as sodium fluoride, sodium monofluorophosphate, and stannous fluoride; ε-aminocaproic acid, allantoin, tranexamic acid, glycyrrhizinate (e.g., dipotassium glycyrrhizinate), glycyrrhetinic acid, glycyrrhetinic acid derivatives (e.g., stearyl glycyrrhetinate), allantoin chlorohydroxyaluminum, azulene, and dihydrocholesterol. Examples of suitable medicinal ingredients include anti-inflammatory agents such as benzoyl benzoate, zinc salts, copper salts, and tin salts; metal salts such as zinc salts, copper salts, and tin salts; anti-tartar agents such as condensed phosphates and ethanehydroxydiphosphonate; blood flow promoters such as vitamin E (e.g., tocopherol acetate); dentin hypersensitivity inhibitors such as potassium nitrate, aluminum lactate, and strontium chloride; coating agents such as hydroxyethylcellulose dimethyldiallylammonium chloride; astringents such as vitamin C (e.g., ascorbic acid or its salts), lysozyme chloride, and sodium chloride; water-soluble copper compounds such as copper chlorophyll and copper gluconate; amino acids such as alanine, glycine, and proline; plant extracts such as thyme, Scutellaria Root, 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 determined in an effective amount according to conventional methods.

[0026] -Surfactants- The optional surfactants are anionic surfactants, nonionic surfactants, and amphoteric surfactants.

[0027] 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 contain 10 to 20 carbon atoms, preferably 12 to 18, and more preferably 12 to 14 carbon atoms. 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.

[0028] Examples of alkyl sulfates include lauryl sulfate (e.g., 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 sulfonate. Other examples of anionic surfactants include hydrogenated coconut fatty acid monoglyceride sodium monosulfate and sodium lauryl sulfoacetate.

[0029] From the viewpoint of foaming ability and foam quality, the anionic surfactant preferably contains a sulfonic acid group, and α-olefin sulfonate, alkyl sulfate, lauryl sulfate, and tradecene sulfonate are more preferred. 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.

[0030] 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.

[0031] Examples of amphoteric surfactants include betaine-type amphoteric surfactants such as alkyldimethylaminoacetic acid betaine (e.g., lauryldimethylaminoacetic acid betaine) and fatty acid amidopropyldimethylaminoacetic acid betaine (e.g., cocamidopropyl betaine); imidazoline-type amphoteric surfactants such as N-fatty acid acyl-N-carboxymethyl-N-hydroxyethylethylenediamine salts (e.g., N-coconut fatty acid acyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine), coconut fatty acid imidazolinium betaine, and 2-alkyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine; and alkyl betaines such as lauryldimethylaminoacetic acid betaine. Examples of cationic surfactants include alkylammonium salts and alkylbenzylammonium 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 total oral composition.

[0032] The content of the surfactant is generally 3% by mass or less, preferably 2% by mass or less, more preferably 0.1 to 3% by mass, and even more preferably 0.3 to 2% by mass, based on the entire oral composition (100% by mass).

[0033] -Wetting agent- Examples of humectants include sugar alcohols and polyhydric alcohols other than sugar alcohols. Examples of sugar alcohols include sorbitol (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 include, for example, polyethylene glycols having an average molecular weight of 150 to 6,000, and polyethylene glycols having an average molecular weight of 190 to 630 (PEG200, PEG300, PEG400, and PEG600). The average molecular weight is the average molecular weight specified in the Quasi-drug Raw Materials Standards 2006. The content of the humectant is typically 40% by mass or less, preferably 1 to 35% by mass, based on the total oral composition (100% by mass).

[0034] The content of the humectant is usually 40% by mass or less, and preferably 1 to 30% by mass, based on the entire oral composition (100% by mass).

[0035] -Binder- Examples of binders include any suitable conventionally known organic binders, such as polysaccharides, cellulose-based binders (e.g., carboxymethyl cellulose (CMC), hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropylmethyl cellulose, methyl cellulose, and cationized cellulose), other polysaccharide thickeners (e.g., xanthan gum, guar gum, gellan gum, tragacanth gum, karaya gum, gum arabic, locust bean gum, carrageenan, and sodium alginate), and synthetic water-soluble polymers (e.g., sodium polyacrylate, carboxyvinyl polymer, polyvinylpyrrolidone, polyvinyl alcohol, and propylene glycol alginate). Furthermore, inorganic binders such as thickening silica and aluminum silicate may also be added.

[0036] The content of the organic binder is preferably 0 to 3 mass %, more preferably 0.1 to 2 mass %, relative to the total oral composition (100 mass %), and the content of the inorganic binder is preferably 0 to 10 mass %, more preferably 1 to 8 mass %.

[0037] -Sweetener- Examples of sweeteners include xylitol, erythritol, maltitol, saccharin, saccharin sodium, aspartame, stevioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidin dihydrochalcone, perillartine, glycyrrhizin, thaumatin, and aspartylphenylalanine methyl ester. The sweeteners may be used singly or in combination of two or more of the above-listed sweeteners.

[0038] -Preservatives- Examples of preservatives include parahydroxybenzoic acid esters (e.g., methyl parahydroxybenzoate, ethyl parahydroxybenzoate, butyl parahydroxybenzoate) and sodium benzoate. The preservatives may be used singly or in combination of two or more.

[0039] - pH adjuster - 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.

[0040] The content of the pH adjuster is usually an amount such that the pH of the oral composition after addition is preferably 5 to 9, more preferably 6 to 8.5.

[0041] 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.

[0042] -solvent- Examples of the solvent include water (purified water) and ethanol, with water being preferred. The amount of the solvent is not particularly limited, but the water content of the solvent is preferably more than 2% by mass. The solvent may be used alone or in combination of two or more.

[0043] -Oil-based 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.

[0044] -Coloring agent- Examples of colorants include natural dyes such as safflower red, gardenia yellow, gardenia blue, perilla color, red koji color, red cabbage color, carrot color, hibiscus color, cacao color, spirulina blue, and tamarind color, as well as legally designated dyes 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 of the entire oral composition.

[0045] -Fragrance- By including a fragrance in the composition, the feeling during use can be further improved. Examples of fragrances include natural fragrances such as eucalyptus oil, wintergreen oil, cassia oil, sage oil, lemon oil, orange oil, cardamom oil, coriander oil, mandarin oil, lime oil, lavender oil, rosemary oil, laurel oil, chamomile oil, caraway oil, marjoram oil, bay oil, lemongrass oil, origanum oil, pine needle oil, neroli oil, rose oil, jasmine oil, grapefruit oil, sweetie oil, yuzu oil, iris concrete, absolute rose, and orange flower; fragrances obtained by processing these natural fragrances (e.g., front-end cutting, back-end cutting, fractional distillation, liquid-liquid extraction, essence formation, powdered fragrance formation); and menthol, anethole, eugenol, carvone, cineole, methyl salicylate, cinnamic aldehyde, 3-l-menthoxypropane-1,2-diol, linalool, linalyl azalea, and the like. Examples of flavorings include single flavorings such as acetate, limonene, menthone, menthyl acetate, pinene, octyl aldehyde, citral, pulegone, carbeyl acetate, anisaldehyde, ethyl acetate, ethyl butyrate, allyl cyclohexane propionate, methyl anthranilate, ethyl methylphenylglycidate, vanillin, undecalactone, hexanal, butanol, isoamyl alcohol, hexenol, dimethyl sulfide, cyclotene, furfural, trimethylpyrazine, ethyl lactate, and ethyl thioacetate, as well as blended flavorings such as strawberry flavor, apple flavor, banana flavor, pineapple flavor, grape flavor, mango flavor, butter flavor, milk flavor, fruit mix flavor, and tropical fruit flavor. Among these, mint flavorings (e.g., menthol, anethole, eugenol, and blended flavorings containing these) are preferred. As the fragrance, the fragrances exemplified above may be used alone or in combination of two or more, as long as the effects of the present invention are not impaired. The above-mentioned fragrance materials are preferably used in an amount of 0.000001 to 2% in the composition, and fragrances using the above-mentioned fragrance materials are preferably used in an amount of 0.1 to 2% in the composition.

[0046] -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.

[0047] 2. Dosage Form and Use of Composition The oral composition can be prepared as an oral preparation such as a dentifrice, mouthwash, spray, liniment, patch, or oral dissolving agent. The dosage form of the oral composition can be appropriately selected depending on the form of use and is not particularly limited. For example, the dosage form may be a paste, liquid, or the like, and in the case of a dentifrice, it can be prepared as a toothpaste, gel toothpaste, liquid toothpaste, liquid toothpaste, or lubricant toothpaste.

[0048] 3. Method for producing the composition The method for producing the oral composition is not particularly limited, and it can be prepared by any conventional method depending on the dosage form. For example, when used as a toothpaste, a method can be used in which the components soluble in a solvent are prepared, and then the other insoluble components are mixed, and degassing (e.g., reduced pressure, etc.) is performed as necessary. The obtained toothpaste can be placed in a container to make a product. The shape and material of the container are not particularly limited, and containers used for conventional toothpaste compositions can be used, such as containers such as laminated tubes made of plastics such as polyethylene, polypropylene, polyethylene terephthalate, and nylon. [Example]

[0049] 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. In the tables, % indicates % by mass unless otherwise specified.

[0050] [Components used in Examples and Comparative Examples] -Component (A)- A-1: Dextranase (enzyme activity 12,000 U / g, manufacturer: Daiichi Sankyo Propharma Co., Ltd.) A-2: Mutanase (enzyme activity 6,000 U / g, manufacturer: Amano Enzyme Co., Ltd.) A-3: Actinidin (trade name: Actinase, enzyme activity 180,000 units / g, manufacturer: BHN Corporation) A-4: Papain (product name: purified papain, enzyme activity 800,000 U / g, manufacturer: Mitsubishi Chemical Foods Corporation) A-5: Bromelain (product name: Bromelain (enzyme activity 400,000 U / g), manufacturer: Godo Shusei Co., Ltd.)

[0051] -(B) Component and its substitutes- B-1: N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide (trade name: CA370, molecular weight 316, manufacturer: Takasago International Corporation) B-2: N-(4-cyanomethylphenyl)-2-isopropyl-5-methylcyclohexanecarboxamide (trade name: Evercool 180, molecular weight 298, manufacturer: Givaudan) B-3: N-(2-(2-pyridinyl)ethyl)-2-isopropyl-5-methylcyclohexanecarboxamide (trade name: Evercool 190, molecular weight 288, manufacturer: Givaudan) B-4 (alternative ingredient): N-ethyl-p-menthane-3-carboxamide (trade name: WS-3, molecular weight 211.35, manufacturer: Symrise Japan Co., Ltd.)

[0052] -Optional ingredients- Abrasive silica (trade name: Tixosil® 73, manufacturer: Solvay) Sodium fluoride (Manufacturer: Stella Chemifa Corporation) Sodium lauryl sulfate (manufacturer: BASF) Sorbitol solution (70%) (Manufacturer: Mitsubishi Corporation Life Sciences Co., Ltd.) Propylene glycol (manufacturer: ADEKA) Xanthan gum (product name: Monart Gum DA, manufacturer: CP Chemicals) Viscosity-increasing silica (product name: Carplex (registered trademark) #67, manufacturer: DSL Japan Co., Ltd.) Saccharin sodium (manufacturer: Aisan Chemical Industry Co., Ltd.) Mint flavor (contains 50% menthol)

[0053] Examples 1 to 19 and Comparative Examples 1 to 6 Dentifrice compositions having the compositions shown in Tables 1 to 5 were prepared by conventional methods. The resulting dentifrice compositions were used as samples and evaluated by the following methods. The results are also shown in the tables.

[0054] <Evaluation method> After storing each dentifrice composition at 40°C for one month, four expert flavor panelists evaluated the dentifrice composition's usability. One gram of sample dentifrice composition was placed on a toothbrush (Clinica Advantage Toothbrush, 4-row compact regular type, manufactured by Lion Corporation) and the patient brushed their teeth for three minutes. The refreshing sensation at the start of brushing, the lack of bitterness during use, and the persistence of the lack of bitterness after rinsing were each judged according to the rating scale shown below, and evaluated according to the following evaluation criteria. Furthermore, those rated as ◯ or better were judged to be dentifrice compositions with reduced bitterness, a good taste, and a refreshing, non-irritating feel when used.

[0055] <Lack of bitterness when using products stored at high temperatures> Regarding the lack of bitterness, we evaluated whether or not the subject felt any bitterness while brushing their teeth. (Grading criteria) 4 points: No bitterness felt 3 points: Almost no bitterness 2 points: I felt bitterness 1 point: Strong bitterness (Evaluation criteria) ◎: Out of 4 people, 3-4 people scored 4 points, 0-1 person scored 3 points, and 0 people scored 2 points or less ○: Out of 4 people, 0-2 people scored 4 points, 2-4 people scored 3 points, and 0 people scored 2 points or less △: 1 to 3 out of 4 people scored 2 points or less ×: If 4 out of 4 people score 2 points or less

[0056] <Maintains a lack of bitterness when stored at high temperatures> To assess the duration of the astringency, subjects brushed their teeth for 3 minutes, just as in the astringency test, and evaluated the time they were free from astringency after rinsing. (Grading criteria) 4 points: 25 minutes or more (no bitterness felt) 3 points: 15 minutes or more but less than 25 minutes 2 points: 5 minutes or more but less than 15 minutes 1 point: Less than 5 minutes (Evaluation criteria) ◎: Out of 4 people, 3-4 people scored 4 points, 0-1 person scored 3 points, and 0 people scored 2 points or less ○: Out of 4 people, 0-2 people scored 4 points, 2-4 people scored 3 points, and 0 people scored 2 points or less △: 1 to 3 out of 4 people scored 2 points or less ×: If 4 out of 4 people score 2 points or less

[0057] <Lack of stimulation> Regarding the lack of irritation, subjects brushed their teeth for three minutes, just as in the test for lack of astringency, and evaluated whether they felt any irritation while brushing their teeth. (Grading criteria) 4 points: No stimulation felt 3 points: Almost no stimulation was felt 2 points: I felt stimulated 1 point: I felt a strong stimulation (Evaluation criteria) ◎: Out of 4 people, 3-4 people scored 4 points, 0-1 person scored 3 points, and 0 people scored 2 points or less ○: Out of 4 people, 0-2 people scored 4 points, 2-4 people scored 3 points, and 0 people scored 2 points or less △: 1 to 3 out of 4 people scored 2 points or less ×: If 4 out of 4 people score 2 points or less

[0058] [Table 1]

[0059] [Table 2]

[0060] [Table 3]

[0061] [Table 4]

[0062] [Table 5]

[0063] Comparative Examples 1 to 5, which used high-temperature storage products containing component (A) but not component (B), and Comparative Example 6, which used a high-temperature storage product containing component (A) and comparative component (B-4), had a bitter taste that was felt even during use, whereas Examples 1 to 19, which used high-temperature storage products containing components (A) and (B), all fully exhibited the bitterness-suppressing effect and plaque-decomposing function, did not cause any irritation in the oral cavity, and had good bitterness-suppressing effect and sustained effect after spitting out.

Claims

1. Component (A): one or more enzymes selected from the group consisting of polysaccharide-degrading enzymes and proteases, and Component (B): one or more selected from N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide, N-(4-cyanomethylphenyl)-2-isopropyl-5-methylcyclohexanecarboxamide, and N-(2-(2-pyridinyl)ethyl)-2-isopropyl-5-methylcyclohexanecarboxamide Contains the polysaccharide-degrading enzyme is one or more selected from the group consisting of dextranase and mutanase; the protease is one or more selected from the group consisting of papain, actinidin, and bromelain; The amount of component (B) is 0.00001 to 0.005% by mass. Oral composition.

2. 2. The oral composition according to claim 1, wherein the amount of component (A) is 0.01 to 5.0% by mass.

3. The component (A) contains dextranase, 3. The oral composition according to claim 1, wherein the enzyme activity of dextranase is 10,000 to 14,000 units / g.

4. The component (A) contains mutanase, 3. The oral composition according to claim 1, wherein the mutanase has an enzyme activity of 4,000 to 70,000 U / g.

5. The component (A) contains papain, 3. The oral composition according to claim 1, wherein the papain has an enzyme activity of 200,000 to 2,500,000 units / g.

6. The component (A) contains actinidin, 3. The oral composition according to claim 1, wherein the enzyme activity of actinidin is 9,000 to 210,000 units / g.

7. The component (A) contains bromelain, 3. The oral composition according to claim 1, wherein the enzyme activity of bromelain is 300,000 to 500,000 units / g.

8. The oral composition according to any one of claims 1 to 7, which is a dentifrice.

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