Oral composition

Abstract

To provide an oral composition which has a cooling sensation at the start of use, is capable of suppressing bitterness from a bactericide from the start of use to a certain time after use, and further capable of continuing the suppressing effect. An oral composition which contains (A) a bactericide, and (B) one or more selected from the group consisting of N-(ethoxycarbonylmethyl)-p-menthane-3-carboxamide and N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide.

Description

Technical Field

[0001] This invention relates to a composition for oral use. Background Technology

[0002] Oral hygiene products such as dental floss contain bactericides, which are important ingredients that effectively reduce the number of pathogenic bacteria in the mouth, suppress halitosis, prevent tooth decay, and prevent periodontal disease. However, bactericides have a characteristic bitter taste. Due to this bitterness, even when combined with cooling agents such as menthol, no cooling sensation is felt at the beginning of use, and the bitterness persists for a certain period after use, thus significantly impairing the user experience. Therefore, various studies have been conducted to date to mask the bitterness from bactericides.

[0003] Patent Document 1 relates to an oral composition containing a bactericide (isopropylmethylphenol), polyvinylpyrrolidone, a fragrance ingredient (selected from at least one of 3-octanol, 3-octyl acetate, and 3-octanone), and a surfactant. Patent Document 1 discloses that by containing polyvinylpyrrolidone in a specific proportion, it is possible to mask the odor from the bactericide during brushing. Patent Document 2 relates to a dental cleaning composition containing ingredients effective in preventing periodontal disease (glucanase, tranexamic acid, and isopropylmethylphenol), alkyl sulfates, and fragrance ingredients (menthol, anethole, eugenol, and / or thyme oil). Patent Document 2 discloses that by containing a fragrance ingredient in a specific proportion, it is possible to mask complex odors after brushing. Patent Document 3 relates to an oral composition containing a bactericide (cationic bactericide), a moisturizing and antibacterial agent (alkyldiol), and a cooling agent (3-1-methoxypropane-1,2-diol and / or N-substituted-p-menthane-3-carboxamide). Patent Document 3 discloses a method for masking the odor from a bactericide shortly after applying an oral composition to the mouth by using a moisturizing / antibacterial agent and a cooling agent. Patent Document 4 relates to an oral composition containing a bactericide, a fragrance (Japanese peppermint oil and N-(2-(2-pyridyl)ethyl)-2-isopropyl-5-methylcyclohexaneformamide). Patent Document 4 discloses a method for masking the bitter taste from a bactericide after rinsing by using peppermint oil and N-(2-(2-pyridyl)ethyl)-2-isopropyl-5-methylcyclohexaneformamide. [Existing Technical Documents] [Patent Literature]

[0004] Patent Document 1: Japanese Patent No. 5493732 Patent Document 2: Japanese Patent Application Publication No. 2019-167297 Patent Document 3: Japanese Patent No. 6740901 Patent Document 4: Japanese Patent Application Publication No. 2018-203645 Summary of the Invention [The problem the invention aims to solve]

[0005] In oral compositions, if not only is bitterness suppressed, but also a suitable sensation of coolness from the cooling agent is continuously felt at the beginning of use, then the oral composition can be used continuously, and an improved bactericidal effect in the oral cavity can be expected. However, Patent Documents 1-4 do not disclose oral compositions from the viewpoint of the continuity of the cooling sensation at the beginning of use and the suppression of bitterness. The present invention was made in view of the above circumstances, and its object is to provide an oral composition that has a cooling sensation at the beginning of use and can suppress the bitterness from the bactericide after a certain period of time from the beginning of use to the end of use (for example, in the case of a dental floss, from the beginning of brushing to the end of brushing). [Methods used to solve problems]

[0006] That is, the present invention provides the following [1] to

[12] . [1] An oral composition, characterized in that the oral composition contains (A) a bactericide and (B) one or more selected from the group consisting of N-(ethoxycarbonylmethyl)-p-menthane-3-carboxamide and N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide. [2] The oral composition according to [1], wherein component (A) is one or more bactericides selected from the group consisting of cationic bactericides, nonionic bactericides and anionic bactericides. [3] The oral composition according to [1] or [2], wherein component (A) is one or more bactericides selected from the group consisting of quaternary ammonium salts, biguanide bactericides, phenolic bactericides, eucalyptol and acylsarcosinate salts. [4] An oral composition according to any one of [1] to [3], wherein the content of component (A) is 0.001% to 0.5% by mass relative to 100% by mass of the oral composition. [5] The oral composition described in any of [1] to [4], wherein the content of component (B) is 0.00001% to 0.1% by mass relative to 100% by mass of the oral composition. [6] An oral composition according to any one of [1] to [5], wherein the oral composition further comprises (C) a nonionic surfactant. [7] The oral composition according to [6], wherein component (C) is one or more nonionic surfactants selected from the group consisting of polyoxyethylene hydrogenated castor oil, polyoxyethylene alkyl ether, polyglycerol fatty acid ester and polyoxyethylene polyoxypropylene copolymer. [8] The oral composition according to [6] or [7], wherein the content of component (C) is 0.1% to 2% by mass relative to 100% by mass of the oral composition. [9] An oral composition according to any one of [1] to [8], wherein the oral composition further comprises (D) a cooling agent.

[10] The oral composition according to [9], wherein component (D) is either or both of menthol and carvone, or is an essential oil containing either or both of menthol and carvone.

[11] The oral composition according to [9] or

[10] , wherein the content of component (D) relative to 100% by mass of the oral composition is 0.001% to 1.5% by mass, based on the content of either or both of menthol and carvone.

[12] An oral composition according to any one of [1] to

[11] , wherein the oral composition is a dental cleaning agent, mouthwash, spray, coating, patch or oral solvent. [Invention Effects]

[0007] According to the present invention, an oral composition is provided that has a cooling sensation at the beginning of use and can suppress the bitterness from the bactericide after a certain period of time from the beginning of use to the end of use. Detailed Implementation

[0008] The present invention will now be described in detail.

[0009] The oral composition of the present invention contains components (A) and (B) below, and preferably further contains any one or both of components (C) and (D). It should be noted that, in this specification, the content of each component is based on the amount of each component added during the manufacture of the composition.

[0010] [(A) ingredient] Component (A) is a bactericide. By including component (A) in the oral composition, a bactericidal effect can be achieved.

[0011] Examples of components (A) include cationic, nonionic, and anionic bactericides. Component (A) is preferably a bactericide selected from one or more of the cationic, nonionic, and anionic bactericides. As a cationic bactericide, quaternary ammonium salts and biguanide bactericides are preferred, such as quaternary ammonium salts like alkylpyridinium salts, benzyl long-chain alkyl short-chain dialkylammonium salts, and long-chain alkyl short-chain trialkylammonium salts; and biguanide bactericides like chlorhexidine salts. As component (A), more specifically, examples include benzyl chloride, benzalkonium chloride, dequalinium chloride, hexadecylpyridinium chloride, stearyl dimethyl benzyl chloride, lauryl trimethyl ammonium chloride, myristyl trimethyl ammonium chloride, cetyl trimethyl ammonium chloride, stearyl trimethyl ammonium chloride, chlorhexidine, chlorhexidine hydrochloride, chlorhexidine gluconate, and chlorhexidine acetate. Among these, benzyl chloride, benzalkonium chloride, and hexadecylpyridinium chloride are particularly preferred. As a nonionic fungicide, phenolic fungicides and eucalyptol are preferred, such as isopropyl methylphenol, physalisol, triclosan, thymol, thyme oil, 1,8-cineole, and eucalyptus oil. Among these, isopropyl methylphenol and physalisol are preferred as nonionic fungicides. As an anionic bactericide, an acyl sarcosine salt (e.g., an alkali metal salt such as a sodium salt) having an acyl group (e.g., an acyl group with 10 to 18 carbon atoms) is preferred, with sodium lauroyl sarcosine being the most preferred. Therefore, component (A) is preferably a bactericide selected from one or more of quaternary ammonium salts, biguanide bactericides, phenolic bactericides, eucalyptol, and acyl sarcosine salts. These can be used alone or in combination of two or more.

[0012] From the viewpoint of achieving a bactericidal effect without strongly expressing the bitterness (hereinafter simply referred to as bitterness) from the bactericide, the lower limit of the content of component (A) relative to the total oral composition (100% by mass) is preferably 0.001% by mass or more, more preferably 0.005% by mass or more. This allows for a good bactericidal effect. The upper limit is preferably 0.5% by mass or less. This suppresses the expression of bitterness. Therefore, the content of component (A) is preferably 0.001% by mass to 0.5% by mass, more preferably 0.005% by mass to 0.5% by mass. Within the above range, when component (A) contains a cationic bactericide, the content of the cationic bactericide relative to the total oral composition (100% by mass) is preferably 0.001% by mass to 0.5% by mass, more preferably 0.005% by mass to 0.2% by mass. When component (A) contains a nonionic bactericide, the content of the nonionic bactericide is preferably 0.005% to 0.2% by mass relative to the total oral composition (100% by mass). When component (A) contains an anionic bactericide, the content of the anionic bactericide is preferably 0.05% to 0.5% by mass relative to the total oral composition (100% by mass).

[0013] [(B) Component] (B) Component (B) is selected from one or more of N-(ethoxycarbonylmethyl)-p-menthane-3-carboxamide and N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide. By including component (B) in the oral composition, a cooling sensation can be felt during use even if the oral composition contains a bactericide, and bitterness can be continuously suppressed from the start of use until a certain period of time after use. In this specification, "cooling sensation" refers to the sensation of the oral composition working well, and includes not only a cooling sensation but also a complex sensation including a refreshing sensation and a comfortable sensation.

[0014] (B) The ingredient can be a single component or a combination of two or more, preferably containing N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide. This enhances the sustained bitterness-suppressing effect from the start of use until a certain period after use.

[0015] The lower limit of the content of component (B) relative to the total oral composition (100% by mass) is preferably 0.00001% by mass or more, more preferably 0.00005% by mass or more. This allows for a sustained effect of suppressing bitterness after a certain period of time from the start of use to after use. The upper limit of the content of component (B) relative to the total oral composition (100% by mass) is preferably 0.1% by mass or less, more preferably 0.01% by mass or less, and particularly preferably 0.005% by mass or less. This allows for suppression of irritation in the oral cavity and reduction of the aroma manifestation of fragrances (other than cooling agents). That is, the content of component (B) relative to the total oral composition (100% by mass) is preferably 0.00001% by mass to 0.1% by mass, more preferably 0.00005% by mass to 0.005% by mass.

[0016] [(C) Component] (C) is a nonionic surfactant. By including (C) in the oral composition, the reduction of the cooling sensation at the beginning of use can be suppressed, and a sustained effect of suppressing bitterness can be provided from the beginning of use until a certain period of time after use.

[0017] Examples of components (C) include, for example, polyoxyethylene alkyl ethers, polyoxyethylene hydrogenated castor oil, sorbitan fatty acid esters, polyoxyethylene sorbitan fatty acid esters (e.g., polyoxyethylene sorbitan monostearate), alkanolamides, polyoxyethylene fatty acid esters, polyoxyethylene alkenyl ethers, polyglycerol 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 diethanolamides), 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 molar addition of ethylene oxide is typically 5 to 30 moles. The average molar addition of ethylene oxide in the polyoxyethylene hydrogenated castor oil is typically 20 to 100 moles, preferably 20 to 60 moles. The fatty acids in sorbitan fatty acid esters typically have 12 to 18 carbon atoms. The fatty acids in polyoxyethylene sorbitan fatty acid esters typically have 16 to 18 carbon atoms, and the average molar number of ethylene oxide additions is typically 10 to 40 moles. The alkyl chains in alkanolamides typically have 12 to 14 carbon atoms. As nonionic surfactants, one or more nonionic surfactants selected from polyoxyethylene hydrogenated castor oil, polyoxyethylene alkyl ethers, polyglycerol fatty acid esters, and polyoxyethylene-polyoxypropylene copolymers are preferred. These can be used individually or in combination of two or more.

[0018] The lower limit of the content of component (C) relative to the total oral composition (100% by mass) is preferably 0.1% by mass or more, more preferably 0.3% by mass or more. This allows for a good suppression effect on bitterness. The upper limit of the content of component (C) relative to the total oral composition (100% by mass) is preferably 2% by mass or less, more preferably 1% by mass or less, and particularly preferably 0.8% by mass or less. This allows for suppression of the decrease in cooling sensation at the start of use, and provides a sustained suppression effect on bitterness from the start of use until a certain period of time after use. Therefore, the content of component (C) relative to the total oral composition (100% by mass) is preferably 0.1% to 2% by mass, more preferably 0.3% to 1% by mass, and even more preferably 0.3% to 0.8% by mass.

[0019] [(D) component] (D) is a cooling agent. By including (D) in the oral composition, a cooling sensation can be imparted, thus improving the user experience.

[0020] Examples of ingredients (D), i.e., cooling agents, include menthol and carvone. Both menthol and carvone can be used as compounds. Alternatively, essential oils containing either or both of menthol and carvone can be used. Examples of essential oils include peppermint oil, Japanese peppermint oil, and spearmint oil. Ingredient (D) can be a single ingredient or a combination of two or more. From the viewpoint of providing a more refreshing sensation, ingredients containing menthol and either or both of menthol-containing essential oils are preferred.

[0021] Relative to the total oral composition (100% by mass), the content of component (D) is preferably 0.001% by mass or more, more preferably 0.01% by mass or more, based on the content of either or both of menthol and carvone (in the case of using essential oils, the amount of menthol and carvone in the essential oil is also included). The upper limit is generally 1.5% by mass or less, preferably 1.2% by mass or less, more preferably 0.8% by mass or less. Therefore, it is preferably 0.001% by mass to 1.5% by mass, more preferably 0.001% by mass to 1.2% by mass, and even more preferably 0.01% by mass to 0.8% by mass.

[0022] [Any ingredients] The oral composition of this embodiment may contain any ingredients other than those already described (A) to (D) without impairing the effects of the present invention.

[0023] Examples of any ingredient include abrasives, pharmaceutical ingredients, surfactants other than ingredient (C), humectants, binders, sweeteners, preservatives, pH adjusters, solvents, oily ingredients, colorants (pigments), and flavorings other than ingredient (D). These will be explained in detail below.

[0024] -Abrasive- Abrasives can be either inorganic or organic. Examples of inorganic abrasives include abrasive silica such as precipitated silica, aluminum silicate, zirconium silicate, crystalline zirconium silicate, and titanium-bonded silica; calcium phosphate compounds such as dicalcium phosphate dihydrate or non-hydrated dicalcium phosphate, calcium dihydrogen phosphate, tricalcium phosphate, and calcium pyrophosphate; calcium carbonate abrasives such as calcium carbonate; calcium hydroxide and calcium sulfate, calcium-based abrasives other than carbonate / phosphate; aluminum-based materials such as alumina, aluminum hydroxide, and alumina; silica-based materials such as anhydrous silicic acid, zeolite, and zirconium silicate; magnesium-based materials such as magnesium carbonate and trimagnesium phosphate; apatite-based materials such as hydroxyapatite, fluorapatite, and calcium-deficient apatite; titanium-based materials such as titanium dioxide, mica titanium, and titanium oxide; and minerals such as bentonite. Examples of organic abrasives include polymethyl methacrylate and synthetic resin abrasives. Among them, silica-based abrasives are preferred.

[0025] The content of abrasive is typically 70% by mass or less, preferably 50% by mass or less, and more preferably 8% by mass to 50% by mass, relative to the total oral composition (100% by mass).

[0026] -Medicinal ingredients- Examples of pharmaceutical ingredients include enzymes such as dextranase, polysaccharidase, amylase, protease, and LeTech enzyme; fluorides such as sodium fluoride, sodium monofluorophosphate, and tin fluoride; anti-inflammatory agents such as ε-aminocaproic acid, allantoin, tranexamic acid, glycyrrhizic acid salts (e.g., dipotassium glycyrrhizate), glycyrrhetinic acid, glycyrrhetinic acid derivatives (e.g., stearyl glycyrrhetinic acid), allantoin, aluminum chlorohydroxyl, azulene, and dihydrocholesterol; metal salts such as zinc salts, copper salts, and tin salts; polyphosphates and ethane hydroxybisphosphonates. The active ingredients include: tartar prevention agents; blood flow promoters such as vitamin E (e.g., tocopherol acetate); sensory hypersensitivity inhibitors such as potassium nitrate, aluminum lactate, and strontium chloride; application agents such as hydroxyethyl cellulose and dimethyl diallyl ammonium 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 chlorophyllin and copper gluconate; tartar prevention agents; amino acids such as alanine, glycine, and proline; plant extracts such as thyme, scutellaria baicalensis, clove, and witch hazel; seal peptides; and polyvinylpyrrolidone. These can be used alone or in combination of two or more. The effective dosage of the above-mentioned active ingredients can be appropriately determined using conventional methods.

[0027] -surfactant- Any surfactant is a surfactant other than component (C), and is anionic surfactant or amphoteric surfactant.

[0028] Examples of anionic surfactants include alkyl sulfates, acyl amino acid salts, acyl taurates, α-olefin sulfonates, hydrogenated coconut oil fatty acid monoglyceride monosulfates, and lauryl sulfoacetates. The alkyl and acyl groups can be either straight-chain or branched, and either saturated or unsaturated, and typically have 10 to 20 carbon atoms, preferably 12 to 18, and more preferably 12 to 14. The salt can be selected from pharmacologically permissible salts. Examples of pharmacologically permissible salts include, for example, base addition salts and amino acid salts. Specific examples include inorganic base salts such as sodium, potassium, calcium, magnesium, and ammonium salts; organic base salts such as triethylammonium, triethanolamine, pyridinium, and diisopropylammonium salts; and basic amino acid salts such as arginine salts. Inorganic base salts are preferred, alkali metal salts (e.g., sodium and potassium salts) or ammonium salts are more preferred, and sodium salts are even more preferred.

[0029] Examples of alkyl sulfates include lauryl sulfate (sodium lauryl sulfate) and myristoyl sulfate. Examples of acyl amino acid salts include lauroyl glutamate, myristoyl glutamate, palmitoyl glutamate, and other acyl glutamate salts; N-lauroyl-N-methylglycine, cocoyl glycine, and other acyl glycine salts; N-lauroyl-β-alanine, N-myristoyl-β-alanine, N-cocoyl-β-alanine, N-lauroyl-N-methyl-β-alanine, N-myristoyl-N-methyl-β-alanine, N-methyl-N-acylalanine, and other acylalanine salts; and lauroyl aspartate, and other acyl aspartate salts. Examples of acyl taurates include lauroyl methyl taurate, N-methyl-N-acyl taurate, and N-cocoyl methyl taurate. Examples of α-olefin sulfonates include tetradecene sulfonate and other α-olefin sulfonates with 12 to 18 carbon atoms. Other examples of anionic surfactants include sodium hydrogenated coconut oil fatty acid monoglyceride monosulfate and sodium lauryl sulfoacetate.

[0030] From the viewpoint of good foaming and foam quality, the anionic surfactant preferably contains a sulfonic acid group, more preferably lauryl sulfate and tetradecyl sulfonate. The content of the anionic surfactant is preferably 0.1% to 2.5% by mass of the total oral composition, more preferably 0.6% to 2.5% by mass, and even more preferably 1% to 2.5% by mass.

[0031] Examples of amphoteric surfactants include, for example, alkyl dimethylaminoacetic acid betaine (e.g., lauryl dimethylaminoacetic acid betaine) and fatty acid amamidopropyl dimethylaminoacetic acid betaine (e.g., cocamidopropyl betaine), which are betaine-type amphoteric surfactants; N-fatty acid acyl-N-carboxymethyl-N-hydroxyethyl ethylenediamine salts (e.g., N-cocoa fatty acid acyl-N-carboxymethyl-N-hydroxyethyl imidazoline betaine), cocoa fatty acid imidazoline betaine, 2-alkyl-N-carboxymethyl-N-hydroxyethyl imidazoline betaine, which are imidazoline-type amphoteric surfactants; and alkyl betaines such as lauryl dimethylaminoacetic acid betaine. Examples of cationic surfactants include alkyl ammonium salts and alkyl benzyl ammonium salts. The content of the amphoteric surfactant is preferably 0.1% to 2% by mass of the total oral composition, more preferably 0.2% to 1.5% by mass, and even more preferably 0.3% to 1% by mass.

[0032] The content of surfactant (other than component (C)) is preferably 3% by mass or less, more preferably 2% by mass or less, more preferably 0.1% to 3% by mass, and particularly preferably 0.3% to 2% by mass, relative to the total oral composition (100% by mass).

[0033] -Wetting agent- By including a humectant in the oral composition, the user experience can be further improved.

[0034] Examples of humectants include sugar alcohols and polyols other than sugar alcohols. Examples of sugar alcohols include sorbitol, erythritol, maltitol, lactitol, and xylitol. Examples of polyols other than sugar alcohols include glycerol; glycols such as ethylene glycol, propylene glycol, dipropylene glycol, butylene glycol, and polyethylene glycol (PEG); and reduced starch saccharides. For polyethylene glycol, polyethylene glycol with an average molecular weight of 150 to 6000 is preferred, and polyethylene glycol with an average molecular weight of 190 to 630 (PEG200, PEG300, PEG400, PEG600) is more preferred. The average molecular weight is the average molecular weight specified in the Pharmaceutical Raw Material Specification 2006.

[0035] The content of the humectant is typically 40% by mass or less, preferably 1% to 30% by mass, relative to the total oral composition (100% by mass).

[0036] -Adhesive- By incorporating a binder into the oral composition, the viscosity of the oral composition can be optimized, further improving its shape retention and user experience.

[0037] As a binder, any suitable organic binder known in the past can be cited, such as polysaccharides, cellulose-based binders (e.g., carboxymethyl cellulose (CMC), hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, methyl cellulose, cationic cellulose, etc.), other polysaccharide thickeners (e.g., xanthan gum, guar gum, gellan gum, tragacanth gum, ebony gum, gum arabic, locust bean gum, carrageenan, sodium alginate), and synthetic water-soluble polymers (e.g., sodium polyacrylate, carboxyvinyl polymers, polyvinylpyrrolidone, polyvinyl alcohol, propylene glycol alginate). Furthermore, oral compositions can also contain thickening inorganic binders such as silica and aluminum silicate.

[0038] The content of organic binder relative to the total oral composition (100% by mass) is preferably 0% to 3% by mass, more preferably 0.1% to 2% by mass. The content of inorganic binder is preferably 0% to 10% by mass, more preferably 1% to 8% by mass.

[0039] -Sweeteners- By including sweeteners in the oral composition, the user experience can be further improved. Examples of sweeteners include xylitol, erythritol, maltitol, saccharin, sodium saccharin, aspartame, stevia, stevia extract, p-methoxycinnamicaldehyde, neohesperidin dihydrochalcone, perilla stigma, glycyrrhizin, thaumatin, and aspartyl-phenylalanine methyl ester. One of the sweeteners mentioned above can be used alone, or two or more can be used in combination.

[0040] -preservative- By including preservatives in oral compositions, the preservative properties of the formulation can be ensured.

[0041] Examples of preservatives include parabens (e.g., methylparaben, ethylparaben, butylparaben), sodium benzoate, etc. A single preservative can be used alone, or two or more can be used in combination.

[0042] -pH adjuster- By including a pH adjuster in the oral composition, the pH stability of the formulation can be ensured.

[0043] 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, sodium, 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.

[0044] The content of the pH adjuster is usually set to an amount that enables the pH value of the added oral composition to be 5 to 9, preferably 6 to 8.5.

[0045] In this instruction manual, pH value generally refers to the value after 3 minutes at 25°C from the start of the measurement. pH value can be measured, for example, using a pH meter (model Hm-30S) manufactured by Toa Denpa Kogyo Co., Ltd.

[0046] -solvent- Examples of solvents include water (purified water) and ethanol, with water being the preferred choice. A single solvent may be used, or two or more may be used in combination.

[0047] -Oily ingredients- Examples of oily components include hydrocarbons such as squalane, liquid paraffin, petrolatum, and microcrystalline wax; higher alcohols (e.g., alcohols with 8 to 22 carbon atoms such as lauryl alcohol, cetearyl alcohol, oleyl alcohol, and isostearyl alcohol); 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; and fatty acid esters such as isopropyl myristate.

[0048] -Coloring agents- Examples of coloring agents include, for example, natural pigments such as safflower red pigment, gardenia yellow pigment, gardenia blue pigment, perilla pigment, red yeast rice pigment, red cabbage blue pigment, carotene pigment, hibiscus pigment, cocoa pigment, spirulina blue pigment, and tamarind pigment; or legally permitted pigments 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 coloring agent, its content relative to the total oral composition is preferably 0.00001% to 3% by mass.

[0049] -Fragrances other than (D) ingredients- By including flavorings other than ingredient (D) in the oral composition, the user experience can be further enhanced.

[0050] Other fragrance ingredients besides (D) include, for example, fennel oil, cinnamon oil, winter green oil, mastic oil, neroli oil, lemongrass oil, jasmine oil, rose oil, iris oil, clove oil, sage oil, cardamom oil, rosemary oil, laurel oil, chamomile oil, basil oil, marjoram oil, lemon oil, orange oil, lime oil, grapefruit oil, nutmeg oil, lavender oil, paracress oil, vanilla oil, cinnamon oil, pepper oil, bay leaf oil, perilla oil, wintergreen oil, and other natural essential oils; cinnamaldehyde, anethole, etc. The fragrance components found in the aforementioned natural essential oils include methyl salicylate, eugenol, linalool, limonene, menthone, menthyl acetate, citral, decanal, camphor, borneol, pinene, citronellol, n-decyl alcohol, citronellol, α-terpineol, citronellol acetate, ethyl linalool, and vanillin; fragrance components such as ethyl acetate, ethyl butyrate, isoamyl acetate, hexanal, hexenal, methyl anthranilate, ethyl methylphenylglycidate, benzaldehyde, vanillin, ethyl vanillin, and furanone; and various blended fragrances such as peppermint, fruit, and herbal fragrances composed of several fragrance components and natural essential oils. As fragrances, one of the above-mentioned examples can be used alone, or two or more can be used in combination.

[0051] -Any other ingredients- Examples of any other components besides those mentioned above include polyisobutylene, polybutadiene, urethane, silicone, and natural rubber. The content of these other components can be appropriately set within a range that does not impair the effects of the present invention.

[0052] [Dosage Forms and Uses of Oral Compositions] The oral composition of the present invention can be formulated into oral preparations such as toothwashes, mouthwashes, sprays, coatings, patches, or oral solvents. The dosage form of the oral composition can be appropriately selected according to the method of use and is not particularly limited. As a dosage form, for example, it can be in the form of paste, liquid, etc.; if it is a toothwash, it can be formulated as a paste-like toothwash, a gel-like toothwash, a liquid toothwash, a wettable toothwash.

[0053] Method for manufacturing oral compositions There are no particular limitations on the manufacturing method of oral compositions, and they can be manufactured using various conventional methods depending on the dosage form. For example, when used as toothpaste, a method can be mentioned where, after preparing the components dissolved in a solvent, other insoluble components are mixed in, and defoaming (e.g., decompression) is performed as needed. The resulting toothpaste can be contained in a container to form a product. There are no particular limitations on the shape or material of the container; containers commonly used in dental cleaning compositions (toothpaste) can be used, such as laminated tubes made of plastics like polyethylene, polypropylene, polyethylene terephthalate, and nylon. Example

[0054] The present invention will now be specifically described with reference to embodiments, comparative examples, and reference examples. The present invention is not limited to the embodiments described below. It should be noted that, unless otherwise specified, the values ​​in the tables below are pure quantities, representing mass percentages.

[0055] [Ingredients used in the Examples, Comparative Examples, and Reference Examples] -(A)Component- Cetylpyridinium chloride: (Manufactured by Fujifilm and Koko Pure Chemical Industries, Ltd.) Isopropylmethylphenol: (Manufactured by Osaka Chemical Co., Ltd.) Sodium lauroyl sarcosinate: (Manufactured by Nikko Chemical Co., Ltd.) 1,8-Cephalotaxine: (Manufactured by Eikodo Main Store, Co., Ltd.) -(B) Ingredients- N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide: (Manufactured by Takasago Fragrance Industry Co., Ltd., trade name: Coolact (registered trademark) 370) N-(ethoxycarbonylmethyl)-p-menthane-3-carboxamide: (WS-5, manufactured by Toyotama Fragrance Co., Ltd.) -Fragrance ingredient used in the comparative example instead of ingredient (B)- N-Ethyl-p-menthane-3-carboxamide: (WS-3, manufactured by Symrise Japan) -(C) Component- Polyoxyethylene (20) hydrogenated castor oil: (manufactured by Nippon Emulsion Co., Ltd.)

[0056] -(D) component- Menthol: (Manufactured by Takasago Flavoring & Scenting Co., Ltd.) Carvone: (Manufactured by Shiono Spices Co., Ltd.) Peppermint oil (manufactured by Takasago Flavoring & Perfume Industry Co., Ltd.) Japanese peppermint oil (manufactured by V.MANE FILS Fragrance Company) Spearmint oil (manufactured by V.MANE FILS Perfume Company)

[0057] -Any ingredient- Abrasive silica: (Solvay manufactures Tixosil (registered trademark) 73) Sodium fluoride: (Manufactured by Stella Chemifa Co., Ltd.) Sodium lauryl sulfate: (manufactured by BASF Japan Co., Ltd.) Sorbitol solution (70%): (manufactured by Mitsubishi Corporation Life Sciences Co., Ltd.) Propylene glycol: (manufactured by ADEKA Corporation) Thickening silica: Carplex (registered trademark) #67 (manufactured by DSL Japan Co., Ltd.) Sodium saccharin: (manufactured by Aisan Chemical Industry Co., Ltd.) Water (purified water) For ingredients other than those mentioned above, all raw materials conforming to the pharmaceutical raw material specification 2006 are used.

[0058] Examples 1-30, Comparative Examples 1-4 A toothpaste composition (toothpaste) having the composition shown in Tables 1 to 4 below is prepared by conventional methods containing the above-mentioned ingredients and stored in a laminated tube.

[0059] [Evaluation Method] The user experience of the toothpaste composition was evaluated by a panel of four participants. A 1g sample of the toothpaste composition was placed on a toothbrush (Clinica Advantage toothbrush, 4-row compact standard type, manufactured by Lion Corporation), and brushed for 3 minutes. The cooling sensation at the start of brushing, the absence of bitterness during brushing, and the persistence of the absence of bitterness after brushing were assessed according to the scoring criteria shown below. The average score of the four participants was calculated, and the evaluation was based on the following criteria.

[0060] <The cooling sensation when you start brushing your teeth> Regarding the cooling sensation when you start brushing your teeth, evaluate the cooling sensation when you start brushing your teeth. Evaluation Criteria 4 / 5: It feels very refreshing. 3 points: I felt a cooling sensation. 2 points: I could hardly feel any cooling sensation. 1 point: I didn't feel any cooling sensation. Judgment Criteria Excellent: Average score of 3.5 or higher but less than 4.0. Good: Average score of 3.0 or above but less than 3.5 Pass: An average score of 2.0 or higher but less than 3.0. Unsatisfactory: Average score less than 2.0 points

[0061] <No bitter taste when brushing teeth> Regarding the absence of bitterness, the evaluation is based on the intensity of bitterness at the start of brushing. Scoring Criteria 4 points: No bitterness detected 3 points: Almost no bitterness can be detected. 2 points: I could taste the bitterness. 1 point: The bitterness was very strong. Judgment Criteria Excellent: Average score between 3.5 and 4.0 Good: Average score of 3.0 or above but less than 3.5 Pass: An average score of 2.0 or higher but less than 3.0. Unsatisfactory: Average score less than 2.0 points

[0062] No bitter taste when brushing teeth Regarding the absence of bitterness during brushing, the evaluation is based on the intensity of bitterness during a 3-minute brushing period. Evaluation Criteria 4 points: No bitterness detected 3 points: Almost no bitterness can be detected. 2 points: I could taste the bitterness. 1 point: The bitterness was very strong. Judgment Criteria Excellent: Average score of 3.8 or above and below 4.0 Excellent: Average score of 3.5 or higher but less than 3.8. Good: Average score of 3.0 or above but less than 3.5 Pass: An average score of 2.0 or higher but less than 3.0. Unsatisfactory: Average score less than 2.0 points

[0063] <Persistence of no bitter taste after brushing> Regarding the duration of no bitter taste after brushing, the evaluation was conducted after brushing for 3 minutes and rinsing for the time after which no bitter taste was felt. Evaluation Criteria 4 points: More than 25 minutes (no bitterness was detected) 3 points: 15 minutes or more but less than 25 minutes 2 points: 5 minutes or more but less than 15 minutes 1 minute: less than 5 minutes Judgment Criteria Excellent: Average score of 3.8 or above and below 4.0 Excellent: Average score of 3.5 or above but less than 3.8; Good: Average score of 3.0 or above but less than 3.5; Pass: Average score of 2.0 or above but less than 3.0; Unsatisfactory: Average score less than 2.0.

[0064] [Table 1] *Fragrances: Excludes menthol, carvone, and essential oils containing them.

[0065] [Table 2] *Fragrances: Excluding menthol, carvone, and essential oils containing them.

[0066] [Table 3] *Fragrances: Excludes menthol, carvone, and essential oils containing them.

[0067] [Table 4] *Fragrances: Excludes menthol, carvone, and essential oils containing them.

[0068] In Comparative Examples 1-3, which did not contain ingredient (B), almost no cooling sensation was felt at the start of brushing, but a very strong bitter taste was felt, which was also felt during brushing, resulting in a poor user experience. The duration of no bitterness after brushing was less than 5 minutes, which was not a satisfactory result. Similarly, the same result was obtained in Comparative Example 4, which used N-ethyl-p-menthane-3-carboxamide instead of ingredient (B). In contrast, Examples 1-30, which contained ingredients (A) and (B), achieved satisfactory results with an average score of 3.0 or higher in all evaluation items. Among them, Examples 21-30, which contained ingredient (C) in addition to ingredients (A) and (B), achieved excellent results with an average score of 3.8 or higher in the evaluation of no bitterness during and after brushing. These results indicate that the oral composition of the present invention provides a cooling sensation at the start of use and, after a certain period of time from the start of use to after use, can suppress the bitterness from the bactericide, thereby enabling a sustained inhibitory effect.

Claims

1. An oral composition, characterized in that, The oral composition contains: (A) Hexadecylpyridinium chloride, (B) N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide, and (C) Polyoxyethylene hydrogenated castor oil, Relative to 100% by mass of the oral composition, the content of component (A) is 0.001% to 0.5% by mass, the content of component (B) is 0.00001% to 0.1% by mass, and the content of component (C) is 0.1% to 0.8% by mass.

2. The oral composition according to claim 1, wherein, The oral composition also contains (D) a cooling agent.

3. The oral composition according to claim 2, wherein, (D) The component is either or both of menthol and carvone, or an essential oil containing either or both of menthol and carvone.

4. The oral composition according to any one of claims 1 to 3, wherein, The oral composition is a dental cleaning agent.

5. The oral composition according to any one of claims 1 to 3, wherein, The oral composition is a mouthwash.

6. The oral composition according to any one of claims 1 to 3, wherein, The oral composition is an intraoral solvent.

7. The oral composition according to any one of claims 1 to 3, wherein, The oral composition is a spray, a coating, or an adhesive.

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