Oral composition

Abstract

The present invention addresses the problem of providing a composition for oral cavity, said composition being capable of reducing the stimulating feeling of a stimulating component such as a component for suppressing stain adhesion to teeth, while enabling the stimulating component to exhibit the desired original effect thereof. The present invention provides: a composition for oral cavity, said composition containing component (A) which is composed of one or more substances selected from among a condensed phosphoric acid, phytic acid and salts of these acids, and component (B) which is (N-(2-(2-pyridinyl)ethyl)-2-isopropyl-5-methylcyclohexane carboxamide); a stimulation relaxing agent for a stimulating component of a composition for oral cavity, said stimulation relaxing agent containing (N-(2-(2-pyridinyl)ethyl)-2-isopropyl-5-methylcyclohexane carboxamide); and a composition for oral cavity, said composition containing a stimulating component and (N-(2-(2-pyridinyl)ethyl)-2-isopropyl-5-methylcyclohexane carboxamide).

Description

[Technical field]

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

[0002] Condensed phosphates are known to have an effect of suppressing stain adhesion to teeth, but have the problem of being highly irritating to the oral mucosa, which is particularly noticeable in liquid preparations such as mouthwashes. Patent Document 1 discloses the use of specific flavoring ingredients to reduce the irritation caused by pyrophosphate and polyphosphates. Patent Document 2 proposes preparations that incorporate hydroxyalkyl cellulose to suppress the irritation through viscosity, and mask the irritation with flavoring ingredients. [Prior art documents] [Patent documents]

[0003] [Patent Document 1] JP 2011-98917 A [Patent Document 2] Patent No. 6217628 Summary of the Invention [Problem to be solved by the invention]

[0004] However, the technology of Patent Document 1 does not provide sufficient effects for oral compositions, especially liquid preparations, and there are problems with the persistence of irritation relief, particularly with preparations that are not rinsed with water, such as mouthwashes and mouth sprays, and with the technology of Patent Document 2, there are problems with reduced palatability and inability to provide long-term masking.

[0005] An object of the present invention is to provide an oral composition which can reduce the irritating sensation caused by irritating ingredients such as ingredients that inhibit stain adhesion to teeth, while still allowing the irritating ingredients to exert their inherent effects. [Means for solving the problem]

[0006] The present invention provides the following [1] to

[11] . [1] An oral composition comprising component (A): one or more selected from condensed phosphoric acid, phytic acid, and salts thereof, and component (B): (N-(2-(2-pyridinyl)ethyl)-2-isopropyl-5-methylcyclohexanecarboxamide). [2] The oral composition according to [1], wherein the component (A) is one or more selected from the group consisting of pyrophosphoric acid, tripolyphosphoric acid, hexametaphosphoric acid, ultraphosphoric acid, phytic acid, and salts thereof. [3] The oral composition according to [1] or [2], wherein the amount of component (A) is 0.05 to 2 mass %. [4] The oral composition according to any one of [1] to [3], wherein the amount of component (B) is 0.00001 to 0.01% by mass. [5] The oral composition according to any one of [1] to [4], further comprising a component (C): one or more selected from organic acids having 3 to 6 carbon atoms and salts thereof. [6] The oral composition according to [5], wherein the component (C) is one or more selected from malic acid, tartaric acid, citric acid, lactic acid, succinic acid, fumaric acid, and salts thereof. [7] The oral composition according to [5] or [6], wherein the amount of component (C) is 0.05 to 3 mass %. [8] The oral composition described in any one of [1] to [7], which is a liquid oral composition. [9] An agent for reducing irritation of irritating components in an oral composition, comprising (N-(2-(2-pyridinyl)ethyl)-2-isopropyl-5-methylcyclohexanecarboxamide).

[10] The irritation-relieving agent according to [9], wherein the irritating component is one or more selected from condensed phosphoric acid, phytic acid, and salts thereof.

[11] An oral composition containing a stimulating ingredient and (N-(2-(2-pyridinyl)ethyl)-2-isopropyl-5-methylcyclohexanecarboxamide). Effect of the Invention

[0007] According to the present invention, there is provided an oral composition which can inhibit stain adhesion to teeth, inhibit the sensation of irritation and maintain the inhibiting effect, and which exhibits good flavor and improved appearance stability of the formulation, thereby enabling these effects to be felt. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

[0008] Hereinafter, the present invention will be described in detail with reference to preferred embodiments thereof. In the present specification, the content of each component is based on the amount of each component charged when preparing the composition.

[0009] [1. Oral composition] The oral cavity composition of the present invention contains components (A) and (B), and may further contain component (C). Components (A) to (C) will be described below.

[0010] <Component (A)> The component (A) is at least one selected from condensed phosphoric acid, phytic acid, and salts thereof. The component (A) enables the oral composition to exhibit a stain adhesion inhibitory effect.

[0011] Examples of condensed phosphoric acid include linear polyphosphoric acid such as pyrophosphoric acid, tripolyphosphoric acid, and tetrapolyphosphoric acid; cyclic polyphosphoric acid such as trimetaphosphoric acid, tetrametaphosphoric acid, and hexametaphosphoric acid; and mesh-like polyphosphoric acid such as ultraphosphoric acid. As linear polyphosphoric acid, pyrophosphoric acid and tripolyphosphoric acid are preferred, and as cyclic polyphosphoric acid, hexametaphosphoric acid is preferred. As condensed phosphoric acid, linear polyphosphoric acid is preferred. Condensed phosphoric acid and phytic acid may be in the form of a salt, and examples of the salt include inorganic base salts such as alkali metal salts (e.g., sodium salt, potassium salt), alkaline earth metal salts (e.g., calcium salt, magnesium salt), copper salt, zinc salt, aluminum salt, and ammonium salt; and organic base salts such as triethylammonium salt, triethanolammonium salt, pyridinium salt, and diisopropylammonium salt. Preferable are alkali metal salts and alkaline earth metal salts, more preferably sodium salt, potassium salt, and calcium salt, and even more preferably sodium salt or potassium salt. The component (A) preferably contains one or more selected from linear polyphosphoric acid and phytic acid, and more preferably contains one or more selected from pyrophosphoric acid, sodium tripolyphosphate, and phytic acid.

[0012] The component (A) may be one selected from condensed phosphoric acid, phytic acid, and salts thereof, or may be a combination of two or more. The combination of two or more is preferably two or more selected from polyphosphoric acid and salts thereof, and preferably includes one or more linear polyphosphoric acid and salts thereof. Such combinations include a combination of one or more selected from linear polyphosphoric acid and salts thereof with one or more selected from cyclic polyphosphoric acid, network polyphosphoric acid, and salts thereof; and a combination of two or more selected from linear polyphosphoric acid and salts thereof. The condensed phosphoric acid, phytic acid, and salts thereof as the component (A) may be mixed with other phosphoric acid or phosphate salts in the oral composition.

[0013] The amount of the (A) component is usually 0.05% by mass or more, preferably 0.1% by mass or more, based on the total amount of the oral cavity composition. This allows for a better effect of inhibiting stain adhesion to be exhibited. The upper limit is usually 2% by mass or less, preferably 1% by mass or less. This allows for the oral cavity composition to suppress the irritation felt by the oral mucosa, and to suppress the deterioration of flavor expression and appearance stability. Therefore, the amount of the (A) component is usually 0.05 to 2% by mass, preferably 0.1 to 1% by mass.

[0014] <(B) component> The component (B) is (N-(2-(2-pyridinyl)ethyl)-2-isopropyl-5-methylcyclohexanecarboxamide). By including the component (B), the occurrence of irritation in the oral composition can be suppressed, and the suppression of irritation can be further sustained.

[0015] The amount of the (B) component is not particularly limited, but is usually 0.00001% by mass or more, preferably 0.0001% by mass or more, based on the total amount of the oral composition. This can suppress the irritating sensation of the oral composition, and the suppressing effect can be sustained. The upper limit is usually 0.01% by mass or less, preferably 0.005% by mass or less. This can suppress the development of a strong irritating sensation, and suppress the decline in flavor development. Therefore, the amount of the (B) component is usually 0.00001 to 0.01% by mass, preferably 0.0001 to 0.005% by mass.

[0016] The ratio (A / B) of the amount of component (A) to the amount of component (B) is usually at least 20, preferably at least 50, and more preferably at least 80. The upper limit is usually at most 30,000, preferably at most 20,000, and more preferably at most 10,000.

[0017] <(C) component> Component (C) is at least one selected from organic acids having 3 to 6 carbon atoms and salts thereof. By containing component (C), the oral composition can exhibit a better effect of inhibiting stain adhesion.

[0018] Examples of organic acids having 3 to 6 carbon atoms include monocarboxylic acids, dicarboxylic acids, tricarboxylic acids, and oxycarboxylic acids, and malic acid, tartaric acid, citric acid, lactic acid, succinic acid, and fumaric acid are preferred. Examples of salts include inorganic base salts such as alkali metal salts (e.g., sodium salt, potassium salt), alkaline earth metal salts (e.g., calcium salt, magnesium salt), and ammonium salts; and organic base salts such as triethylammonium salt, triethanolammonium salt, pyridinium salt, and diisopropylammonium salt, and are preferably alkali metal salts and alkaline earth metal salts, more preferably sodium salt, potassium salt, and calcium salt, and even more preferably sodium salt or potassium salt.

[0019] The amount of component (C) is usually 0.05% by mass or more, preferably 0.1% by mass or more, based on the total amount of the oral cavity composition. This can further improve the effect of inhibiting stain adhesion. The upper limit is usually 3.0% by mass or less, preferably 1.5% by mass or less. If it exceeds 3.0% by mass, the appearance stability and flavor expression may decrease. Therefore, the amount of component (C) is usually 0.05 to 3% by mass, preferably 0.1 to 1.5% by mass.

[0020] <Dosage form> The dosage form of the oral composition is not particularly limited, but may be, for example, solid, paste, or liquid, with liquid being preferred. In this specification, an oral composition in a liquid dosage form is referred to as a liquid oral composition. The liquid oral composition can be prepared as a liquid such as a mouthwash (e.g., gargle, mouthwash), liquid toothpaste, or mouth freshener, and may be of a concentrated type as necessary. The oral composition may be any of a medicine, a quasi-drug, a cosmetic, or a food.

[0021] <Optional ingredients> In addition to the above components, the oral composition of the present invention may contain optional components other than the above components as necessary. The optional components can be appropriately selected depending on the application and formulation of the oral composition. For example, when the oral composition is a liquid, the optional components include surfactants, humectants, pH adjusters, preservatives, sweeteners, flavorings, active ingredients, and solvents. When the oral composition is in a formulation other than a liquid, the optional components other than the above-mentioned optional components include, for example, binders and abrasives. The content of the optional components is not particularly limited, and can be set to the amount used in a normal oral composition as long as it does not impair the effects of the present invention.

[0022] (Surfactant) Examples of the surfactant include anionic surfactants, nonionic surfactants, cationic surfactants, and amphoteric surfactants, and it is preferable to include at least one of anionic surfactants and nonionic surfactants. By including an anionic surfactant in the oral composition, the effect of inhibiting stain adhesion can be further improved. By including a nonionic surfactant in the oral composition, the effect of solubilizing oil-soluble components can be obtained.

[0023] Examples of anionic surfactants include alkyl sulfates, N-acyl amino acid salts, α-olefin sulfonates, N-acylsulfonates, N-acyltaurine salts, and sulfates of glycerol fatty acid esters, with alkyl sulfates and N-acyltaurine salts being preferred. Examples of alkyl sulfates include alkyl sulfates having 12 to 14 carbon atoms (e.g., alkali metal salts of lauryl sulfate, myristyl sulfate). Examples of N-acyl amino acid salts include acyl amino acid salts such as acyl glutamate and acyl sarcosine salts having a saturated or unsaturated hydrocarbon group (e.g., having 8 to 18 carbon atoms, preferably 12 to 16 carbon atoms; may be either linear or branched). Examples of acyltaurine salts include N-acyl methyl taurine salts having a saturated or unsaturated hydrocarbon group (e.g., having 8 to 18 carbon atoms, preferably 12 to 16 carbon atoms; may be either linear or branched). Examples of the α-olefin sulfonate include α-olefin sulfonate having 10 to 16 carbon atoms, such as tetradecene sulfonate, etc. As these salts, alkali metal salts such as sodium salts and potassium salts are preferred.

[0024] The amount of the anionic surfactant is usually 0.01% by mass or more based on the total amount of the oral cavity composition. This allows for a better effect of inhibiting stain adhesion to be exhibited. The upper limit is usually 3% by mass or less, preferably 0.5% by mass or less, and more preferably 0.3% by mass or less. This allows for the suppression of the occurrence of a strong irritating sensation. Therefore, the amount of the anionic surfactant is usually 0.01 to 3% by mass, preferably 0.01 to 0.5% by mass, and preferably 0.01 to 0.3% by mass.

[0025] Examples of nonionic surfactants include polyoxyethylene fatty acid esters such as polyoxyethylene hydrogenated castor oil, polyoxyethylene glycerin fatty acid esters, and polyoxyethylene sorbitan fatty acid esters; polyoxyethylene higher alcohol ethers such as polyoxyethylene alkyl ethers; sugar alcohol fatty acid esters; sorbitan fatty acid esters; polyglycerin fatty acid esters; and polyoxyethylene sorbitan fatty acid esters. The average number of moles of ethylene oxide added to the polyoxyethylene hydrogenated castor oil is usually 20 to 150 moles, preferably 20 to 130 moles, and more preferably 40 to 110 moles.

[0026] The amount of the nonionic surfactant is usually 0.1% by mass or more, preferably 0.3% by mass or more, based on the total amount of the oral cavity composition. The upper limit is usually 1% by mass or less, preferably 0.8% by mass or less. By being within these ranges, a better solubilizing effect of the oil-soluble components can be obtained. Therefore, the amount of the nonionic surfactant is preferably 0.1 to 1% by mass, preferably 0.3 to 0.8% by mass.

[0027] Examples of cationic surfactants include quaternary ammonium compounds such as alkyl ammonium compounds and alkyl benzyl ammonium compounds. Examples of amphoteric surfactants include alkyl amide betaine type amphoteric surfactants; acetic acid betaine type amphoteric surfactants such as alkyl dimethyl amino acetic acid betaine and fatty acid amido propyl dimethyl amino acetic acid betaine; and imidazoline type amphoteric surfactants such as N-fatty acid acyl-N-carboxymethyl-N-hydroxyethyl ethylenediamine salts.

[0028] (Wetting agent) The oral composition contains a humectant, which can improve the feeling of use. Examples of humectants include sugar alcohols such as sorbitol, erythritol, maltitol, lactitol, and xylitol; and polyhydric alcohols such as glycerin, propylene glycol, ethylene glycol, and polyethylene glycol. The polyhydric alcohols are preferably glycerin and propylene glycol, and the sugar alcohols are preferably sorbitol and xylitol.

[0029] The amount of the humectant is usually 3% by mass or more, preferably 5% by mass or more, based on the total amount of the oral cavity composition. The upper limit is usually 40% by mass or less, preferably 30% by mass or less, more preferably 15% by mass or less. By being within these ranges, a better effect of improving the feeling of use can be obtained. Therefore, the amount of the humectant is usually 3 to 40% by mass, preferably 3 to 30% by mass, more preferably 5 to 15% by mass.

[0030] (pH adjuster) The pH stability of the formulation can be ensured by including a pH adjuster in the oral composition. The components (A) and (C) of the present invention act as pH adjusters in the composition, but any other pH adjuster can be further used as necessary. Examples of the optional pH adjuster include phthalic acid, orthophosphoric acid, acetic acid, carbonic acid, ribonucleic acid, and salts thereof (preferable examples are the same as those of the component (A), preferably potassium salts, sodium salts, and ammonium salts), sodium hydroxide, and hydrochloric acid, and are preferably orthophosphoric acid or a salt thereof, and more preferably sodium dihydrogen phosphate, sodium monohydrogen phosphate, potassium dihydrogen phosphate, and potassium monohydrogen phosphate. When any pH adjuster is used, the amount can be adjusted to a pH of 5.5 to 8.5, preferably 6 to 8, at 25°C. For pH adjustment, citric acid or a salt thereof is preferably used, and further an orthophosphate is preferably used in combination. The pH can be measured immediately after preparation of the oral composition at 25°C and after 3 minutes using a pH meter (model number HM-25R) manufactured by DKK-TOA Corporation. By adjusting the pH of the oral composition of the present invention to fall within the above range, demineralization of tooth enamel can be inhibited, and efficacy and stability can be maintained.

[0031] (Preservatives) The oral composition contains a preservative, which can ensure the preservative power of the preparation. Examples of the preservative include paraoxybenzoic acid esters such as methyl paraoxybenzoate and ethyl paraoxybenzoate, sodium benzoate, alkyldiaminoethylglycine hydrochloride, and potassium sorbate.

[0032] (Sweetener) The oral composition contains a sweetener, which can improve the feeling of use. Examples of the sweetener include sugar alcohols such as xylitol, maltitol, erythritol, and sorbitol; and high-intensity sweeteners such as saccharin, aspartame, sucralose, acesulfame potassium, stevia, neohesperidin hydrochalcone, glycyrrhizin, perillartine, p-methoxycinnamic aldehyde, and thaumatin.

[0033] (fragrance) The oral composition contains a fragrance, which can improve the feeling of use and suppress the initial irritation after use. For example, the fragrance can be a fragrance containing menthol and carvone, but any fragrance used in oral compositions can be used without any particular limitation. The content of menthol and carvone in the fragrance containing menthol and carvone is preferably 10 to 80% by mass. Essential oils containing these, such as peppermint oil, Japanese peppermint oil, and spearmint oil, can also be used. The amount of the fragrance is usually 0.00001% by mass or more relative to the total amount of the oral composition, and the upper limit is usually 3% by mass or less, but is not particularly limited.

[0034] (Active ingredient) Examples of the active ingredient include anti-inflammatory agents such as tranexamic acid and epsilon-aminocaproic acid; enzymes such as dextranase, amylase, protease, mutanase, lysozyme, and Liteque enzyme; fluorine-containing compounds such as sodium fluoride, sodium monofluorophosphate, and stannous fluoride; allantoin or its derivatives such as aluminum chlorohydroxyallantoin and allantoin; vitamin C such as ascorbic acid; plant extracts such as thyme, Scutellaria baicalensis, clove, and witch hazel; dentin hypersensitivity inhibitors such as strontium chloride, potassium nitrate, and aluminum lactate; azulene, lysozyme chloride, dihydrocholesterol, glycyrrhetin salts, glycyrrhetinic acids, hydrocholesterol, chlorophyll, copper chlorophyllin sodium, copper gluconate, caropeptide, water-soluble inorganic phosphate compounds, polyethylene glycol, polyvinylpyrrolidone, sodium lauroyl sarcosine, anti-tartar agents, and anti-plaque agents, but are not particularly limited as long as they are active ingredients used in oral compositions. The content of the above-mentioned active ingredient can be appropriately determined to be an effective amount according to a conventional method.

[0035] (solvent) When the oral composition is in a liquid formulation, it usually contains a solvent. Examples of the solvent include water (e.g., purified water) and alcohol (e.g., lower monohydric alcohol such as ethanol). Usually, it is water, and alcohol can be added as necessary. However, any solvent that can be used in oral compositions in a liquid formulation is acceptable, and is not particularly limited. When ethanol is added as a solvent, the amount is usually 30% by mass or less, preferably 20% by mass or less, based on the total amount of the oral composition, but it is not necessary to add it. By being in this range, it is possible to improve the feeling of suppressing bad breath during use.

[0036] (Binding agent) Examples of the binder include any suitable organic binder known in the art, such as polysaccharides, cellulose-based binders (e.g., carboxymethylcellulose (CMC), hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, methylcellulose, cationic cellulose, etc.), other polysaccharide-based thickeners (e.g., xanthan gum, guar gum, gellan gum, tragacanth gum, karaya gum, arabic gum, 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 thickening silica and aluminum silicate can also be included. The content of the binder when blended is usually 0.01 to 10% by mass based on the total amount of the oral composition.

[0037] (Abrasive) The abrasive may be either an inorganic abrasive or an organic abrasive. Examples of inorganic abrasives include abrasive silica such as precipitated silica, aluminosilicate, zirconosilicate, crystalline zirconium silicate, and titanium-bonded silica; calcium phosphate compounds such as dibasic calcium phosphate dihydrate or anhydrous, monobasic calcium phosphate, tribasic calcium phosphate, and calcium pyrophosphate; calcium carbonate abrasives such as calcium carbonate; calcium abrasives other than carbonate / phosphate such as calcium hydroxide and calcium sulfate; aluminum materials such as aluminum oxide, aluminum hydroxide, and alumina; silicic acid materials such as anhydrous silicic acid, zeolite, and zirconium silicate; magnesium materials such as magnesium carbonate and tribasic magnesium phosphate; apatite materials such as hydroxyapatite, fluoroapatite, and calcium-deficient apatite; titanium materials such as titanium dioxide, titanium mica, and titanium oxide; and minerals such as bentonite. Examples of organic abrasives include polymethyl methacrylate and synthetic resin abrasives. Among these, silica abrasives are preferred. When an abrasive is included, the content is usually 70% by mass or less, preferably 50% by mass or less, and more preferably 8 to 50% by mass, based on the total amount of the oral cavity composition.

[0038] The method of using the oral composition of the present invention is not particularly specified. In the case of a liquid oral composition, for example, a method of putting an appropriate amount in the mouth and rinsing the mouth for several tens of seconds can be mentioned. In addition, teeth can be brushed after rinsing.

[0039] <Application> The oral composition is useful as a stain adhesion improver because stain adhesion can be suppressed by applying the oral composition to teeth. The target subjects are not particularly limited. For example, subjects who wish to improve stain adhesion caused by food and beverages such as black tea, green tea, and coffee, and subjects who have not developed these symptoms but wish to prevent them, etc. can be mentioned.

[0040] <Method for producing oral composition> The oral composition of the present invention can be produced by mixing the above-mentioned components. The order in which the components are mixed is not particularly limited, but it is preferable to mix the components uniformly.

[0041] [2. Irritation reliever] The above component (B), (N-(2-(2-pyridinyl)ethyl)-2-isopropyl-5-methylcyclohexanecarboxamide), is useful as an irritation reducer for the irritating component contained in the oral composition. Examples of the irritating component include one or more selected from the above component (A), condensed phosphoric acid, phytic acid, and salts thereof, as well as irritating components having a structure similar to these, but are not particularly limited as long as they are components that can be contained in the oral composition and cause irritation during use. The amount of the irritation reducer used may be an amount that suppresses irritation caused by the irritating component in the oral composition, and may be an amount exemplified as the amount of the above component (B). In addition, the oral composition may be an oral composition containing an irritating component, and when the irritating component is component (A), an oral composition containing the amount exemplified as the amount of the above component (A) is preferred. The dosage form of the oral composition and optional components that may be contained as necessary are not particularly limited.

[0042] [3. Oral cavity composition containing stimulating ingredients] The above component (B), (N-(2-(2-pyridinyl)ethyl)-2-isopropyl-5-methylcyclohexanecarboxamide), is useful as an irritation-relieving agent, and can therefore be an essential component of the oral composition together with the irritating component as an irritation-relieving component. The amount of the irritating component may be as exemplified in the description of the irritation-relieving agent. EXAMPLES

[0043] The present invention will be described in detail below with reference to examples. The following examples are provided to suitably explain the present invention, and are not intended to limit the present invention. Note that "%" means "% by mass" unless otherwise specified. The blending amount of each component shown in the following table is the value converted to pure content (AI). The amount of water (balance) includes the amount of water carried over by each component.

[0044] The main raw materials used are listed below: Sodium pyrophosphate (manufactured by Taihei Chemical Industry Co., Ltd.) Evercool® 190 (N-(2-(2-pyridinyl)ethyl)-2-isopropyl-5-methylcyclohexanecarboxamide, manufactured by Givaudan Japan) Evercool® 180 ((1R,2S,5R)-N-(4-(cyanomethyl)phenyl)-2-isopropyl-5-methylcyclohexane-carboxamide, manufactured by Givaudan Japan) WS-3 (N-ethyl-p-menthane-3-carboxamide, manufactured by Symrise Japan Co., Ltd.) Sodium lauroyl sarcosine (Kawaken Fine Chemicals Co., Ltd.) Glycerin (manufactured by Sakamoto Pharmaceutical Co., Ltd.) Sorbitol solution (Mitsubishi Corporation Life Sciences Co., Ltd.) Ethanol (manufactured by Japan Alcohol Industry Co., Ltd.) Sodium saccharin (Aisan Chemical Industry Co., Ltd.) Polyoxyethylene hydrogenated castor oil 100 E.O. (manufactured by Nippon Emulsion Co., Ltd.) Polyoxyethylene hydrogenated castor oil 60 E.O. (manufactured by Nippon Emulsion Co., Ltd.) Sodium lauryl sulfate (PT BASF Indonesia) Citric acid (manufactured by Komatsuya Co., Ltd.) Sodium citrate (manufactured by Komatsuya Co., Ltd.)

[0045] ·Fragrance The fragrances used had the compositions shown in Table 1.

[0046] [Table 1]

[0047] Purified water (Kosakai Pharmaceutical Co., Ltd.) Other ingredients used were those that conformed to the 2006 Standards for Quasi-Drug Ingredients.

[0048] [Examples 1 to 20 and Comparative Examples 1 to 4] <How to prepare mouthwash> Mouthwash was prepared by uniformly mixing each component according to the composition shown in Tables 2 to 5 (the content of each component in the tables is in mass %). Specifically, POE hydrogenated castor oil was added to ethanol and stirred, and then an oil layer with the fragrance dissolved therein was prepared. The oil layer was added to a water layer in which the other components were dissolved in purified water, and the mixture was uniformly dissolved using a Three-One Motor (BL1200, manufactured by HEIDON) to prepare the mouthwash. The pH (25°C) of the prepared mouthwash was 6.5 to 8.0.

[0049] <Evaluation method> (1. Stain adhesion prevention effect) The surface of an untreated hydroxyapatite pellet (HAP) (HOYA Corporation, diameter 7 mm x thickness 3.5 mm) was treated with abrasive paper and washed with an ultrasonic cleaner, after which the initial color difference was measured with a colorimeter (UV-1800, Shimadzu Corporation). Next, the HAP was immersed in saliva supernatant at 37°C for 30 minutes, and then (1) to (4) were repeated 10 times under the following conditions: (1) 1% mucin artificial saliva solution (50°C for 10 minutes), (2) 1% albumin artificial saliva solution (50°C for 10 minutes), (3) sample (room temperature for 30 seconds), (4) stain solution (1% black tea powder aqueous solution) (50°C for 10 minutes). The color difference of the HAP after coloring was then measured after washing with water and drying. L * a * b * The stain adhesion inhibition rate was calculated from Δb of the color system using the following formula: Note that the control in the formula was purified water instead of the sample, and the same series of operations were carried out as above. The color difference of this HAP was measured and Δb was calculated in the same way.

[0050] A series of experimental procedures was carried out with N=3 for each Example and Comparative Example, the stain adhesion inhibition rate of each HAP was calculated using the formula below, the average value was calculated, and the stain adhesion inhibition effect was evaluated according to the following evaluation criteria.

[0051] (formula) Stain adhesion inhibition rate (%) = {1-(color difference change of sample Δb / color difference change of control Δb)} x 100

[0052] · Criteria for determining stain adhesion prevention effect +++: Stain adhesion prevention rate is 90% to 100% ++: Stain adhesion inhibition rate is 70% or more but less than 90% +: Stain adhesion inhibition rate is 50% or more but less than 70% ±: Stain adhesion inhibition rate is 30% or more but less than 50% -: Stain adhesion inhibition rate is less than 30%

[0053] (2. No irritation) Participants were asked to place 20 mL of the mouthwash in their mouths and rinse for 20 seconds, after which they rated the intensity of the irritation on a four-point scale as shown below. The average score of the 10 participants was expressed as ++, +, ±, or - according to the following criteria.

[0054] Evaluation criteria for non-irritation 4 points: No irritation felt 3 points: Almost no irritation felt 2 points: I felt a sense of irritation 1 point: Very strong sensation of irritation Criteria for determining lack of irritation ++: Average score 3.5 points or more and 4.0 points or less +: Average score 3.0 or more and less than 3.5 ±: Average score 2.0 points or more and less than 3.0 points -: Average score below 2.0 points

[0055] (3. No irritation sensation lasts After placing 20 mL of mouthwash in the mouth and rinsing for 20 seconds, the time during which no "irritation" was felt was evaluated on a four-point scale as shown below, and the average score of the 10 participants was expressed as ++, +, ±, or - according to the following criteria.

[0056] · Evaluation criteria for durability of non-irritation 4 points: 25 minutes or more (no stimulation 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

[0057] · Criteria for determining the durability of the lack of irritation ++: Average score 3.5 points or more and 4.0 points or less +: Average score 3.0 or more and less than 3.5 ±: Average score 2.0 points or more and less than 3.0 points -: Average score below 2.0 points

[0058] (4. Good flavor expression) Participants placed 20 mL of mouthwash in their mouths and rinsed for 20 seconds, after which they rated the flavor development during rinsing on the following four-point scale. The average score of the 10 participants was indicated as ++, +, ±, or - according to the following criteria. Evaluation criteria for flavor expression 4 points: Very good flavor development 3 points: Good flavor development 2 points: The flavor expression is not very good. 1 point: Poor flavor development

[0059] · Criteria for judging the quality of flavor expression ++: Average score is between 3.5 and 4.0 +: Average score is 3.0 or more and less than 3.5 points ±: Average score is between 2.0 and 3.0 points -: Average score is between 1.0 and 2.0

[0060] (5. Evaluation of the appearance stability of the formulation) The prepared formulation was filled into a container with a capacity of 80 mL and allowed to stand at −5° C. for one month, after which the appearance and properties were evaluated visually.

[0061] - Criteria for determining the appearance stability of the formulation ++: No precipitate or turbidity observed +: Almost no precipitate or turbidity is observed ±: Precipitates or turbidity are observed -: Significant deposits or turbidity are observed

[0062] [Table 2]

[0063] [Table 3]

[0064] [Table 4]

[0065] [Table 5]

[0066] In Comparative Examples 1 to 4, which do not contain either the A or B component, there were problems such as no stain adhesion inhibitory effect, irritation, or the lack of irritation was somewhat sustained, whereas in Examples 1 to 20, which contain the A and B components, good results were obtained in the evaluation of the stain adhesion inhibitory effect, lack of irritation, and the sustainability of the lack of irritation, and further good results were obtained in terms of flavor expression and appearance stability of the preparation. This shows that the oral composition of the present invention can inhibit stain adhesion to teeth, can suppress irritation, and can sustain the inhibitory effect.

[0067] As a formulation example, a toothpaste formulation example is shown in Table 6.

[0068] [Table 6]

Claims

1. Component (A): one or more selected from condensed phosphoric acid, phytic acid, and salts thereof; (B) component: (N-(2-(2-pyridinyl)ethyl)-2-isopropyl-5-methylcyclohexanecarboxamide), and Component (C): one or more selected from organic acids having 3 to 6 carbon atoms and their salts It contains The component (C) is at least one selected from malic acid, tartaric acid, citric acid, lactic acid, succinic acid, fumaric acid, and salts thereof, An oral composition, wherein the ratio (A / C) of the amount of component (A) to the amount of component (C) is 0.25 to 20.

2. 2. The oral composition according to claim 1, wherein component (A) is at least one selected from the group consisting of pyrophosphoric acid, tripolyphosphoric acid, hexametaphosphoric acid, ultraphosphoric acid, phytic acid, and salts thereof.

3. 3. The oral composition according to claim 1 or 2, wherein the amount of component (A) is 0.05 to 2% by mass.

4. The oral composition according to any one of claims 1 to 3, wherein the amount of component (B) is 0.00001 to 0.01 mass%.

5. The oral composition according to claim 1, wherein the amount of component (C) is 0.05 to 3 mass %.

6. An oral composition according to any one of claims 1 to 5, which is a liquid oral composition.

7. The oral composition of claim 1, wherein the ratio (A / C) of the amount of component (A) to the amount of component (C) is 0.25 to 1.

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