Oral components

Abstract

To improve retentivity of cetylpyridinium chloride hydrate (A) on a tooth surface.SOLUTION: An oral composition contains cetylpyridinium chloride hydrate (A), an anionic polymer (B), and hydroxyethyl cellulose (C). The content of the anionic polymer (B) is 0.1 mass% or more and 4 mass% or less, and the content of the hydroxyethyl cellulose (C) is 0.1 mass% or more and 5 mass% or less. The mass ratio of the anionic polymer (B) to the hydroxyethyl cellulose (C), (B / C), is 0.25 or more and 2 or less.SELECTED DRAWING: None

Description

[Technical Field]

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

[0002] Conventionally, oral compositions intended for the prevention or treatment of periodontitis and stomatitis are known. Patent Document 1 discloses an oral composition containing 0.05 to 0.3% by mass of cetylpyridinium chloride, which is a cationic bactericide, and a surfactant containing β-cyclodextrin and a betaine skeleton. [Prior Art Documents] [Patent Documents]

[0003] [Patent Document 1] Japanese Unexamined Patent Publication No. 2021-147343 [Summary of the Invention] [Problems to be Solved by the Invention]

[0004] Cetylpyridinium chloride hydrate, also called cetylpyridinium chloride, is known to exhibit antibacterial activity when retained on the tooth surface. However, since cetylpyridinium chloride hydrate is a cationic bactericide, electrostatic interaction easily occurs between it and ionic components in the oral cavity. When electrostatic interaction occurs between the compound and ionic components in the oral cavity, there is a risk that the retention of the compound on the tooth surface may decrease.

[0005] Therefore, in order to allow the antibacterial activity of cetylpyridinium chloride hydrate to be expressed for a longer time, improvement of the retention of cetylpyridinium chloride hydrate on the tooth surface is demanded in oral compositions such as those disclosed in Patent Document 1. [Means for Solving the Problems]

[0006] The oral composition for solving the above problems is an oral composition containing cetylpyridinium chloride hydrate (A), an anionic polymer (B), and hydroxyethylcellulose (C), wherein the anionic polymer (B) is contained in an amount of 0.1% to 4% by mass, and the hydroxyethylcellulose (C) is contained in an amount of 0.1% to 5% by mass, and the mass ratio of the anionic polymer (B) to the hydroxyethylcellulose (C) (B / C) is 0.25 to 2.

[0007] In the oral composition described above, it is preferable that the anionic polymer (B) is at least one selected from sodium polyacrylate and carboxyvinyl polymer.

[0008] In the above oral composition, it is preferable that the cetylpyridinium chloride hydrate (A) is contained in an amount of 0.01% by mass or more and 0.5% by mass or less. [Effects of the Invention]

[0009] According to the oral composition of the present invention, the retention of cetylpyridinium chloride hydrate (A) on the tooth surface can be improved. [Modes for carrying out the invention]

[0010] Embodiments of the oral composition according to the present invention will be described. The oral composition contains cetylpyridinium chloride hydrate (hereinafter also referred to as CPC) (A), an anionic polymer (B), and hydroxyethylcellulose (hereinafter also referred to as HEC) (C).

[0011] The oral composition contains an anionic polymer (B) in an amount of 0.1% to 4% by mass and HEC (C) in an amount of 0.1% to 5% by mass. The mass ratio of anionic polymer (B) to HEC (C) (B / C) is 0.25 to 2.

[0012] The oral composition contains anionic polymer (B) and HEC (C) in the above proportions, and furthermore, the mass ratio of the two is within the above numerical range, thereby improving the retention of CPC (A) on the tooth surface.

[0013] The following describes each component that makes up the oral composition. <CPC(A)> CPC(A) is generally used as a cationic disinfectant. There are no particular restrictions on the CPC(A) used; any known CPC(A) can be used.

[0014] The content of CPC(A) is not particularly limited. The lower limit of the CPC(A) content is preferably 0.01% by mass, more preferably 0.05% by mass. The upper limit of the CPC(A) content is preferably 0.5% by mass, more preferably 0.3% by mass. Furthermore, the upper or lower limit within this range may be, for example, 0.02, 0.03, 0.04, 0.05, 0.06, 0.07, 0.08, 0.09, 0.1, 0.15, 0.2, 0.25, 0.3, 0.35, 0.4, or 0.45% by mass.

[0015] By keeping the CPC(A) content within the above numerical range, the dispersibility of CPC(A) in the oral composition can be improved while allowing the bactericidal action of CPC(A) to be suitably expressed.

[0016] <Anionic polymer (B)> Anionic polymer (B) is a polyelectrolyte that carries a negative charge in solution. Anionic polymer (B) is generally used as a thickener. There are no particular limitations on anionic polymer (B), and known anionic polymers (B) can be used.

[0017] Specific examples of anionic polymers (B) include, for example, polyacrylic acid, polyacrylates, polysulfates, polysulfons, alginates, xanthan gum, carrageenan, carboxyvinyl polymers, and carboxymethylcellulose (hereinafter also referred to as CMC). Specific examples of the above polyacrylates include, for example, sodium polyacrylate (hereinafter also referred to as polyacrylate Sodium), methyl polyacrylate, and ethyl polyacrylate. Furthermore, the above carboxyvinyl polymer is a polymer of acrylic acid crosslinked with pentaerythristyl ether, sucrose allyl ether, or propylene allyl ether.

[0018] Among these, the anionic polymer (B) is preferably at least one selected from sodium polyacrylate and carboxyvinyl polymer. When it is at least one selected from sodium polyacrylate and carboxyvinyl polymer, the retention of CPC (A) on the tooth surface can be suitably improved.

[0019] The above-mentioned anionic polymer (B) may be used alone or in combination of two or more types. Anionic polymers are also referred to as anionic polymers.

[0020] The content of the anionic polymer (B) is 0.1% by mass or more and 4% by mass or less. The lower limit of the content of the anionic polymer (B) is preferably 0.3% by mass. The upper limit of the content of the anionic polymer (B) is preferably 2% by mass, and more preferably 1% by mass. Furthermore, the upper or lower limit within this range may be, for example, 0.2, 0.3, 0.4, 0.5, 0.6, 0.7, 0.8, 0.9, 1, 1.5, 2, 2.5, 3, or 3.5% by mass.

[0021] <HEC(C)> HEC(C) is a nonionic, water-soluble polymer obtained by adding ethylene oxide to cellulose, and is generally used as a thickening agent. There are no particular restrictions on the HEC(C) used; any known HEC(C) can be used.

[0022] The content of HEC (C) is 0.1% by mass or more and 5% by mass or less. The lower limit of the content of HEC (C) is preferably 0.5% by mass. The upper limit of the content of HEC (C) is preferably 3% by mass, more preferably 2% by mass, and still more preferably 1.5% by mass. In addition, the upper limit or lower limit of the range may be, for example, 0.2, 0.3, 0.4, 0.5, 0.6, 0.7, 0.8, 0.9, 1, 1.5, 2, 2.5, 3, 3.5, 4, or 4.5% by mass.

[0023] The lower limit of the mass ratio (B / C) of the anionic polymer (B) to HEC (C) is preferably 0.3, and more preferably 0.4. The upper limit of the mass ratio (B / C) is preferably 1.0, and more preferably 0.5. In addition, the upper limit or lower limit of the range may be, for example, 0.35, 0.4, 0.45, 0.5, 0.55, 0.6, 0.65, 0.7, 0.75, 0.8, 0.85, 0.9, 0.95, 1.0, 1.1, 1.2, 1.3, 1.4, 1.5, 1.6, 1.7, 1.8, or 1.9% by mass.

[0024] <Other Components> The oral composition may optionally be formulated with other components in addition to the components described above, for example, medicinal ingredients, surfactants, abrasives, humectants, thickeners, stabilizers, preservatives, sweeteners, pH adjusters, antioxidants, flavors, colorants, and the like, depending on the application purpose, form, use and the like. Any of these components that are known to be formulated in oral compositions may be used. Each of these components may be used alone singly, or two or more kinds may be used in combination.

[0025] Specific examples of medicinal ingredients include, for example, cationic disinfectants such as benzethonium chloride, benzalkonium chloride, chlorhexidine gluconate, and chlorhexidine hydrochloride; amphoteric disinfectants such as dodecyldiaminoethylglycine; halogenated diphenyl ethers such as triclosan (2',4,4'-trichloro-2-hydroxy-diphenyl ether); phenolic disinfectants such as isopropylmethylphenol; and hinokitiol.

[0026] Examples of blood circulation promoters include vitamin E derivatives such as dl-α-tocopherol acetate, tocopherol succinate, and tocopherol nicotinate, as well as enzymes such as dextranase, amylase, protease, mutanase, lysozyme, and lytic enzymes (Litec enzyme).

[0027] Examples of anti-inflammatory agents include epsilon-aminocaproic acid and dipotassium glycyrrhizinate. Examples of bleeding-improving agents include tranexamic acid and ascorbic acid.

[0028] Examples of tissue repair agents include allantoin. Examples of remineralizing agents include fluorine compounds such as sodium fluoride. Other examples include plant extracts extracted with water-soluble solvents, chlorophyll, sodium chloride, zinc chloride, potassium nitrate, etc.

[0029] Specific examples of surfactants include nonionic surfactants, anionic surfactants, cationic surfactants, and amphoteric surfactants. (Nonionic surfactant) Specific examples of nonionic surfactants include sugar fatty acid esters such as sucrose fatty acid esters and maltose fatty acid esters, sugar alcohol fatty acid esters such as maltitol fatty acid esters, sorbitan fatty acid esters such as sorbitan stearate and sorbitan monolaurate, polyoxyethylene sorbitan fatty acid esters such as polyoxyethylene sorbitan laurate (also called polysorbate 20), polyoxyethylene sorbitan stearate (also called polysorbate 60), and polyoxyethylene sorbitan oleate (also called polysorbate 80), fatty acid alkanolamides such as lauric acid diethanolamide, and polyoxyethylene Examples include polyoxyethylene alkyl ethers such as lencheryl ether and polyoxyethylene oleyl ether, polyethylene glycol fatty acid esters such as polyethylene glycol monooleate and polyethylene glycol monolaurate, alkyl glycosides such as lauryl glycoside and decyl glycoside, polyglycerin fatty acid esters, polyoxyethylene glycerin fatty acid esters, polyoxyethylene fatty acid esters, alkyl glucosides, polyoxyethylene hydrogenated castor oil (with an average number of added moles of ethylene oxide of 10, 20, 40, and 60), glycerin fatty acid esters, and polyoxyethylene propylene block copolymers.

[0030] (Anionic surfactant) Specific examples of anionic surfactants include sulfate ester salts such as sodium lauryl sulfate and sodium polyoxyethylene lauryl ether sulfate, sulfosuccinates such as sodium lauryl sulfosuccinate and sodium polyoxyethylene lauryl ether sulfosuccinate, acyl amino acid salts such as sodium cocoyl sarcosinate and sodium lauroyl methylalanine, and sodium cocoyl methyl taurate.

[0031] (Cationic surfactant) Specific examples of cationic surfactants include quaternary alkylammonium salts such as cocoyl arginine ethyl PCA, cetyltrimethylammonium chloride, distearyldimethylammonium chloride, stearyldimethylbenzylammonium chloride, and stearyltrimethylammonium chloride, as well as chlorhexidine gluconate.

[0032] (Amphoteric surfactant) Specific examples of amphoteric surfactants include amino acid-type amphoteric surfactants such as N-lauryldiaminoethylglycine and N-myristyldiethylglycine, and betaine-based amphoteric surfactants such as alkyldimethylaminoacetic acid betaine, N-alkyl-N'-carboxymethyl-N'-hydroxyethylethylenediamine salt, and 2-alkyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine.

[0033] Specific examples of abrasives include calcium carbonate, calcium phosphate, discalcium phosphate, calcium pyrophosphate, insoluble sodium metaphosphate, titanium dioxide, amorphous silica, crystalline silica, abrasive silica, thickening silica, aluminosilicate, aluminum oxide, titanium dioxide, aluminum hydroxide, resin, and hydroxyapatite. The above silica is also called anhydrous silicic acid.

[0034] Specific examples of wetting agents include, for example, propylene glycol, glycerin, sorbitol, polyethylene glycol, 1,3-butylene glycol, water, and alcohol.

[0035] Specific examples of thickening agents include crystalline cellulose, hydroxypropyl methylcellulose, methylcellulose, and propylene glycol alginate. Thickening agents are also called binders.

[0036] Specific examples of stabilizers include sodium edetate, sodium thiosulfate, sodium sulfite, calcium lactate, lanolin, triacetin, castor oil, and magnesium sulfate.

[0037] Specific examples of preservatives include, for example, 1,2-dibromo-2,4-dicyabutane, photosensitizers, isothiazolone derivatives, hydantoin derivatives, parabens, sodium benzoate, and phenol.

[0038] Specific examples of sweeteners include saccharin, sodium saccharin, acesulfame potassium, stevia extract, palatinose, palatinose, erythritol, maltitol, xylitol, and lactitol.

[0039] Specific examples of pH adjusters include, for example, citric acid, phosphoric acid, malic acid, pyrophosphate, lactic acid, tartaric acid, glycerophosphate, acetic acid, nitric acid, or chemically possible salts thereof, sodium hydroxide, etc.

[0040] Specific examples of antioxidants include tocopherols, dibutylhydroxytoluene, butylhydroxyanisole, and gallic acid esters. The fragrance may be natural or synthetic. It may also be a single fragrance or a blended fragrance.

[0041] Specific examples of fragrances include l-menthol, d-carvone, anethole, eugenol, methyl salicylate, limonene, ocimene, n-decyl alcohol, citronellol, α-terpineol, methyl acetate, citronellyl acetate, methyl eugenol, cineole, linalool, ethyl linalool, thymol, spearmint oil, peppermint oil, lemon oil, orange oil, sage oil, rosemary oil, perilla oil, wintergreen oil, clove oil, eucalyptus oil, pimento oil, d-camphor, d-borneol, fennel oil, cinnamon oil, cinnamaldehyde, peppermint oil, vanillin, and others.

[0042] Specific examples of colorants include legally approved pigments such as Green No. 1, Green No. 3, Blue No. 1, Yellow No. 4, Yellow No. 5, Red No. 102, and Red No. 3, as well as sodium copper chlorophyll and titanium dioxide.

[0043] <Application forms, dosage forms, and uses of oral compositions> The application forms of the oral composition are not particularly limited and can be used, for example, as a pharmaceutical product, a designated quasi-drug, a quasi-drug, or a cosmetic product.

[0044] The dosage form of the oral composition is not particularly limited and can be prepared as appropriate in solid, semi-solid, or liquid form. Examples of solid or semi-solid forms include powder, paste, or liquid, which are similar to the dosage forms of toothpaste specified by the Japan Toothpaste Manufacturers Association.

[0045] The uses of oral compositions are not particularly limited, and known compositions can be used as appropriate. Examples of uses for oral compositions include oral application agents including those for the tongue, gingival anti-inflammatory agents, periodontal disease treatment agents, denture fitting agents, implant care agents, toothpaste, powder toothpaste, liquid toothpaste, moisturizing toothpaste, and mouthwash.

[0046] <Mechanism and Effects> The action of the oral composition of this embodiment will now be described. The oral composition of the present invention contains CPC (A), an anionic polymer (B), and HEC (C). Furthermore, it contains the anionic polymer (B) and HEC (C) in predetermined proportions, and the mass ratio of the two is within a predetermined numerical range.

[0047] When an oral composition contains an anionic polymer (B), its viscosity can be increased due to the thickening effect of the anionic polymer (B). Increasing the viscosity of the oral composition makes it possible to improve the retention of CPC(A) on the tooth surface. However, since CPC(A) is prone to electrostatic interactions with the anionic polymer (B), there was a risk that the effect of improving retention would be canceled out. Furthermore, even if the oral composition contained HEC(C) without containing anionic polymer (B), it was not possible to sufficiently improve the retention of CPC(A).

[0048] The oral composition of the present invention contains a predetermined amount of anionic polymer (B) and a predetermined amount of HEC (C), with the mass ratio of the two being within a predetermined numerical range. This makes it possible to suppress electrostatic interactions between CPC (A) and anionic polymer (B). This makes it easier for CPC (A) to remain on the tooth surface, thereby improving the retention of CPC (A). The ionic components in the oral cavity are not particularly limited, but in addition to anionic polymer (B), examples include anhydrous silicic acid used as an abrasive and surfactants in toothpaste.

[0049] The effects of the oral composition of this embodiment will now be described. (1) An oral composition containing CPC (A), an anionic polymer (B), and HEC (C), wherein the anionic polymer (B) is contained in an amount of 0.1% to 4% by mass and HEC (C) is contained in an amount of 0.1% to 5% by mass. Furthermore, the mass ratio of the anionic polymer (B) to HEC (C) (B / C) is 0.25 to 2.

[0050] Therefore, the retention of CPC(A) on the tooth surface can be improved. Furthermore, it becomes possible to sustain the antibacterial activity of CPC(A) for a longer period. (2) The anionic polymer (B) is at least one selected from sodium polyacrylate and carboxyvinyl polymer. Therefore, the retention of CPC (A) on the tooth surface can be suitably improved.

[0051] (3) Contains CPC(A) in a proportion of 0.01% by mass or more and 0.5% by mass or less. Therefore, the dispersibility of CPC(A) is good, and the bactericidal effect of CPC(A) can be suitably expressed. [Examples]

[0052] The following are examples to illustrate the structure and effects of the present invention in more detail, but the present invention is not limited to these examples. In the following, Examples 1 and 3 shall be interpreted as Reference Examples 1 and 3. The oral compositions of Examples 1-6 and Comparative Examples 1 and 2 shown in Table 1 were prepared by mixing each component according to a conventional method. In Table 1, the numbers to the right of each component indicate the content (mass%) of each component, and the mixture was prepared so that the total amount with the remaining water was 100% by mass.

[0053] [Table 1] (Evaluation test) The retention of CPC(A) on tooth surfaces was evaluated for the oral compositions of Examples 1-6 and Comparative Examples 1 and 2. The evaluation method and results are described below.

[0054] (Method for evaluating the retention rate of CPC(A)) The following procedure was used to prepare a hydroxyapatite powder carrier (hereinafter also referred to as a HAP carrier) and to perform an adsorption test.

[0055] (Preparation of HAP carrier) 50 mg of hydroxyapatite powder (Bio-Gel HTP Gel; manufactured by BIO-RAD Lab.) was mixed with 2 mL of UV-sterilized human saliva and immersed at 37°C for approximately 15 hours to form an artificial pellicle on the apatite surface. Subsequently, the mixture was centrifuged at 3000 rpm for 5 minutes, and the supernatant was removed.

[0056] (Adsorption test) For each example, 4 g of a slurry prepared by diluting the oral composition four-fold with water was immersed in the above-mentioned HAP carrier at 37°C for 15 minutes. The supernatant was removed by centrifugation at 3000 rpm for 5 minutes, 2 mL of distilled water was added and stirred, and the supernatant was removed by centrifugation at 3000 rpm for 5 minutes. Another 2 mL of distilled water was added and stirred, and the supernatant was removed by centrifugation at 3000 rpm for 5 minutes.

[0057] Next, CPC(A) adsorbed onto the HAP carrier was extracted using an extraction solvent (a solution of 2.88 g of sodium lauryl sulfate dissolved in 1 L of 0.02 M citrate buffer at pH 3: acetonitrile = 1:3). The amount of CPC(A) retained on 50 mg of the HAP carrier was determined using a known quantitative method with liquid chromatography.

[0058] Furthermore, the retention rate (%) of CPC(A) in each example was calculated using the retention amount of CPC(A) in Comparative Example 1 as a baseline. The retention properties of CPC(A) were evaluated according to the following criteria. • Criteria for evaluating the retention rate of CPC(A) ◎◎ (Excellent): When the retention rate of CPC(A) is 180% or higher. ◎(Good): When the retention rate of CPC(A) is between 140% and 180%. ○(OK): When the retention rate of CPC(A) is 100% or more but less than 140%. × (Not allowed): When the retention rate of CPC(A) is less than 100% (Evaluation results) Table 1 shows that Comparative Example 2 had a lower retention rate of CPC(A) at 98% compared to Comparative Example 1. In contrast, Examples 1 to 6 all had a retention rate of CPC(A) of 106% or more compared to Comparative Example 1, confirming improved retention of CPC(A). This makes it possible to exert the antibacterial activity of CPC(A) for a longer period of time.

Claims

1. An oral composition containing cetylpyridinium chloride hydrate (A), an anionic polymer (B), and hydroxyethylcellulose (C), The anionic polymer (B) is contained in an amount of 0.1% by mass or more and 4% by mass or less, and the hydroxyethyl cellulose (C) is contained in an amount of 0.1% by mass or more and 5% by mass or less. The mass ratio (B / C) of the anionic polymer (B) to the hydroxyethyl cellulose (C) is 0.25 or more and 2 or less. An oral composition characterized in that the anionic polymer (B) is at least one selected from polyacrylates and polyacrylic acid.

2. The oral composition according to claim 1, wherein the anionic polymer (B) is sodium polyacrylate.

3. The oral composition according to claim 1 or 2, comprising the cetylpyridinium chloride hydrate (A) in an amount of 0.01% by mass or more and 0.5% by mass or less.

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