Oral components

Abstract

To suppress the disproportionation of cetylpyridinium chloride hydrate (CPC) even with a relatively high level of the CPC.SOLUTION: An oral composition contains cetylpyridinium chloride hydrate of 0.1 mass% or more, and further contains carboxylate ester.SELECTED DRAWING: None

Description

Technical Field

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

Background Art

[0002] Conventionally, oral compositions aimed at preventing or treating periodontitis and stomatitis are known. Patent Document 1 discloses an oral composition containing cetylpyridinium chloride, which is also called cetylpyridinium chloride hydrate.

Prior Art Literature

Patent Literature

[0003]

Patent Document 1

Summary of the Invention

Problem to be Solved by the Invention

[0004] Meanwhile, in an oral composition containing cetylpyridinium chloride hydrate (hereinafter also referred to as CPC), CPC becomes non-uniform as the concentration of CPC increases. When CPC becomes non-uniform, variation in CPC concentration occurs in the oral composition, which may lead to variation in the bactericidal action of CPC.

Means for Solving the Problem

[0005] An oral composition for solving the above problem contains 0.1% by mass or more of cetylpyridinium chloride hydrate, and further contains a carboxylic acid ester. In the above oral composition, it is preferable that the carboxylic acid ester is an ester of sebacic acid.

[0006] In the above oral composition, it is preferable that the carboxylic acid ester is diethyl sebacate. In the above oral composition, it is preferable that the content of the carboxylic acid ester is 0.1% by mass or more and 3% by mass or less.

[0007] In the above oral composition, it is preferable that the content of hydroxyethylcellulose is 1% by mass or more and 3% by mass or less, and the content of crystalline cellulose is 5% by mass or more and 20% by mass or less.

[0008] In the above oral composition, it is preferable that the content of the cetylpyridinium chloride hydrate is 0.3% by mass or more. [Effects of the Invention]

[0009] According to the oral composition of the present invention, even when the concentration of CPC is relatively high, the non-uniformity of CPC can be suppressed. [Modes for carrying out the invention]

[0010] Embodiments of the oral composition according to the present invention will be described. The oral composition contains 0.1% by mass or more of CPC, and further contains a carboxylic acid ester.

[0011] By containing CPC at a relatively high concentration of 0.1% by mass or more in the oral composition, the bactericidal effect of CPC can be suitably expressed. Furthermore, the inclusion of carboxylic acid esters can suppress the heterogeneity of CPC.

[0012] The following describes each component that makes up the oral composition. <cpc> CPC is generally used as a disinfectant. There are no particular restrictions on the type of CPC used; any known CPC can be used.

[0013] The CPC content is preferably 0.3% by mass or more. When the CPC content is 0.3% by mass or more, the concentration of CPC is higher, which allows the bactericidal effect of CPC to be expressed more favorably.

[0014] <Carboxylic acid esters> The carboxylic acid ester is not particularly limited, and known carboxylic acid esters obtained by the condensation reaction of a carboxylic acid and an alcohol can be used.

[0015] The carboxylic acid used as a raw material for carboxylic acid esters is not particularly limited and may be a saturated carboxylic acid or an unsaturated carboxylic acid. It may be a linear carboxylic acid or a branched carboxylic acid. It may be a monovalent carboxylic acid or a polyvalent carboxylic acid.

[0016] The alcohol used as a raw material for carboxylic acid esters is not particularly limited and may be a saturated alcohol or an unsaturated alcohol. It may be a linear alcohol or a branched alcohol. It may be a monohydric alcohol or a polyhydric alcohol.

[0017] Specific examples of carboxylic acid esters include isoamyl acetate, isoamyl butyrate, amyl formate, isoamyl propionate, ethyl butyrate, isopropyl myristate, polyoxyl 40 stearate, decyl oleate, isopropyl adipate, dibutyloctyl sebacate, diethyl sebacate, diisopropyl sebacate, and diethylhexyl sebacate.

[0018] The above carboxylic acid esters may be used individually or in combination of two or more. Among these, an ester of sebacic acid is preferred, and diethyl sebacate is more preferred.

[0019] The content of the carboxylic acid ester is not particularly limited, but is preferably 0.1% by mass or more and 3% by mass or less. When the content of the carboxylic acid ester falls within the above numerical range, the heterogeneity of CPC can be more suitably suppressed.

[0020] <Other Components> The oral composition may contain, in accordance with the application purpose, form, use, etc., other components besides the aforementioned components, for example, bactericides, antibacterial agents, surfactants, humectants, thickeners, stabilizers, preservatives, sweeteners, pH adjusters, antioxidants, flavoring agents, coloring agents, and the like. For each of these components, known components that are commonly formulated in oral compositions can be used. One of these components may be used alone, or two or more thereof may be used in combination.

[0021] Specific examples of bactericides include, in addition to the aforementioned CPC, hinokitiol and the like, for example. Specific examples of antibacterial agents include parabens, sodium benzoate, triclosan, chlorhexidine hydrochloride, chlorhexidine gluconate, minocycline hydrochloride, isopropylmethylphenol, benzalkonium chloride, benzethonium chloride, and the like.

[0022] Specific examples of surfactants include nonionic surfactants, anionic 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.

[0023] (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.

[0024] (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.

[0025] The surfactant content is not particularly limited, but is preferably 1.5% by mass or less, and more preferably 1% by mass or less. By having a surfactant content of 1.5% by mass or less, solid-liquid separation of each component in the oral composition can be effectively suppressed.

[0026] Specific examples of wetting agents include, for example, propylene glycol, glycerin, sorbitol, polyethylene glycol, 1,3-butylene glycol, water, and alcohol.

[0027] Among these, it is preferable that the product contains at least one of propylene glycol and glycerin. The content of the wetting agent is not particularly limited, but is preferably 35% by mass or more, more preferably 40% by mass or more, and even more preferably 45% by mass or more. Furthermore, it is preferably 90% by mass or less, more preferably 85% by mass or less, and even more preferably 80% by mass or less.

[0028] The propylene glycol content is not particularly limited, but is preferably 5% by mass or more, more preferably 10% by mass or more, and even more preferably 15% by mass or more. Furthermore, it is preferably 35% by mass or less, more preferably 30% by mass or less, and even more preferably 25% by mass or less.

[0029] The glycerin content is not particularly limited, but is preferably 15% by mass or more, more preferably 20% by mass or more, and even more preferably 25% by mass or more. Furthermore, it is preferably 45% by mass or less, more preferably 40% by mass or less, and even more preferably 35% by mass or less.

[0030] Specific examples of thickening agents include sodium polyacrylate, carrageenan, sodium carboxymethylcellulose, sodium alginate, xanthan gum, hydroxyethylcellulose, crystalline cellulose, hydroxypropyl methylcellulose, methylcellulose, and propylene glycol alginate. Thickening agents are also called binders.

[0031] Among these, it is preferable that the product contains hydroxyethylcellulose and crystalline cellulose. The content of hydroxyethylcellulose is not particularly limited, but it is preferably 1% by mass or more and 3% by mass or less.

[0032] The crystalline cellulose content is not particularly limited, but is preferably 5% by mass or more, more preferably 8% by mass or more, and even more preferably 10% by mass or more. Furthermore, it is preferably 20% by mass or less, more preferably 18% by mass or less, and even more preferably 15% by mass or less.

[0033] When the content of hydroxyethylcellulose and crystalline cellulose is within the above numerical range, it becomes easy to adjust the viscosity of the oral composition to make it into a paste or gel. Specific examples of stabilizers include sodium edetate, sodium thiosulfate, sodium sulfite, calcium lactate, lanolin, triacetin, castor oil, and magnesium sulfate.

[0034] Specific examples of preservatives include, for example, 1,2-dibromo-2,4-dicyabutane, photosensitizers, isothiazolone derivatives, hydantoin derivatives, parabens, sodium benzoate, and phenol.

[0035] Specific examples of sweeteners include saccharin, sodium saccharin, acesulfame potassium, stevia extract, palatinose, palatinose, erythritol, maltitol, xylitol, and lactitol.

[0036] 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.

[0037] 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.

[0038] 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.

[0039] 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.

[0040] <Application forms, dosage forms, and uses of oral compositions> The application forms of the oral composition are not particularly limited, and it can be used, for example, as a pharmaceutical product, a designated quasi-drug, a quasi-drug, or a cosmetic product.

[0041] The dosage form of the oral composition is not particularly limited, but it can be used as a paste, ointment, or gel. Applications of oral compositions include, for example, oral application agents including those for the tongue, gingival anti-inflammatory agents, periodontal disease treatment agents, denture fitting agents, and implant care agents.

[0042] <Mechanism and Effects> The action of the oral composition of this embodiment will now be described. In oral compositions, if the CPC content is 0.1% by mass or more, the CPC tends to become non-uniform. In other words, the CPC tends to become non-uniform in the oral composition. If the CPC content is 0.3% by mass or more, the CPC tends to become even more non-uniform. If the oral composition contains a carboxylic acid ester, the non-uniformity of CPC can be suppressed. The mechanism by which the non-uniformity of CPC is suppressed is presumed to be that the polarity of the CPC is suitably mitigated by the carboxylic acid ester, thereby suppressing aggregation between the CPCs.

[0043] Another possible method to suppress CPC non-uniformity is to include a surfactant. However, increasing the surfactant content makes the oral composition more susceptible to solid-liquid separation. Therefore, simply increasing the surfactant content may reduce the handling properties of the oral composition.

[0044] The effects of the oral composition of this embodiment will now be described. (1) Contains 0.1% by mass or more of cetylpyridinium chloride hydrate, and further contains a carboxylic acid ester.

[0045] Therefore, even if the concentration of CPC is relatively high, such as 0.1% by mass or more, the non-uniformity of CPC can be suppressed. Furthermore, since variations in the concentration of CPC in the oral composition can be suppressed, variations in the bactericidal effect can be suppressed.

[0046] (2) The carboxylic acid ester is an ester of sebacic acid. Therefore, heterogeneity of CPC can be effectively suppressed. (3) The carboxylic acid ester is diethyl sebacate. Therefore, the heterogeneity of CPC can be further suppressed.

[0047] (4) The carboxylic acid ester content is 0.1% by mass or more and 3% by mass or less. Therefore, the carboxylic acid ester content is suitable for suppressing the heterogeneity of CPC.

[0048] (5) The hydroxyethylcellulose content is 1% by mass or more and 3% by mass or less, and the crystalline cellulose content is 5% by mass or more and 20% by mass or less. Therefore, it becomes easy to adjust the viscosity of the oral composition to make it into a gel.

[0049] (6) The CPC content is 0.3% by mass or more. Therefore, the bactericidal effect of CPC can be more favorably expressed. Furthermore, even if the CPC content is 0.3% by mass or more, the heterogeneity of CPC can be suppressed.

[0050] (7) The surfactant content is 1% by mass or less. Therefore, solid-liquid separation of each component in the oral composition can be suppressed. [Examples]

[0051] 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. The oral compositions of Examples 1 and 2 and Comparative Examples 1 to 6 shown in Table 1 were prepared by mixing each component according to a conventional method. Diethyl sebacate was a commercially available product.

[0052] In Table 1, the numbers to the right of each component represent the content (mass%) of each component, and the mixture was formulated so that the total content with the remaining water was 100% by mass. The oral composition had a gel-like form.

[0053] In Table 1, POE hydrogenated castor oil 40 and POE hydrogenated castor oil 60 refer to polyoxyethylene hydrogenated castor oil with an average number of ethylene oxide additions of 40 and 60, respectively.

[0054] [Table 1] (Evaluation test) The oral compositions of Examples 1 and 2, and Comparative Examples 1 to 6 were evaluated for the presence or absence of heterogeneity and solid-liquid separation. The evaluation method and results are described below.

[0055] (Method for evaluating the presence or absence of heterogeneity) 25 g of each oral composition from Examples 1 and 2, and Comparative Examples 1 to 6, was taken and filled into 22 mm diameter aluminum laminate tubes. After sealing the laminate tubes with caps, they were left at a constant temperature of 55°C for one month. Subsequently, the oral compositions were squeezed out of the laminate tubes. The concentration of CPC in the squeezed oral compositions was measured at three points: 1 g from the tip, 2 g from the tip, and 3 g from the tip. A known high-performance liquid chromatography was used to measure the concentration of CPC. The coefficient of variation (hereinafter also referred to as CV value) of the concentrations at the three points was calculated, and if the CV value was 1.5 or less, it was considered uniform (○). If the CV value was greater than 1.5, it was considered non-uniform (×). The results are shown in Table 1.

[0056] (Method for evaluating whether solid-liquid separation is present or absent) In evaluating the presence or absence of heterogeneity, the oral composition was squeezed out of the laminate tube after being left at a constant temperature of 55°C for one month, and the presence or absence of solid-liquid separation was visually confirmed. If no solid-liquid separation was observed, it was marked as "no solid-liquid separation" (○). If solid-liquid separation was observed, it was marked as "solid-liquid separation present" (×). The results are shown in Table 1. Note that the above evaluation of the presence or absence of heterogeneity was not performed on oral compositions in which solid-liquid separation was observed.

[0057] (Evaluation results) Table 1 shows that Comparative Examples 1-6 all did not contain diethyl sebacate, and it was confirmed that the CPC was heterogeneous. In addition, in Comparative Example 3, solid-liquid separation occurred because the surfactant content was high at 1.9% by mass.

[0058] In contrast, in Examples 1 and 2, diethyl sebacate was contained, and the CPC was not heterogeneous. Furthermore, solid-liquid separation did not occur.< / cpc>

Claims

1. It contains 0.1% by mass or more of cetylpyridinium chloride hydrate, Furthermore, it contains carboxylic acid esters, An oral composition characterized in that the carboxylic acid ester is solely an ester of sebaic acid.

2. The oral composition according to claim 1, wherein the ester of sebaciac acid is diethyl sebaciate.

3. The oral composition according to claim 1, wherein the content of the carboxylic acid ester is 0.1% by mass or more and 3% by mass or less.

4. The oral composition according to claim 1, wherein the content of hydroxyethylcellulose is 1% by mass or more and 3% by mass or less, and the content of crystalline cellulose is 5% by mass or more and 20% by mass or less.

5. The oral composition according to any one of claims 1 to 4, wherein the content of the cetylpyridinium chloride hydrate is 0.3% by mass or more.

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