Composition for oral cavity

Abstract

To provide a composition for an oral cavity which can impart an impregnation experience even immediately after manufacture and after storage, and by which irritation on a tongue is suppressed.SOLUTION: A composition for an oral cavity having pH 6.0 to 8.5 contains (A) chlorobutanol, (B) a compound having Na or K: 0.25 to 8 mass% in terms of Na and K, and (C) water: 20 to 80 mass%.SELECTED DRAWING: None

Description

Technical Field

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

Background Art

[0002] Chlorobutanol is a base having a unique sense of use and contributes to the sense of penetration of oral products. For example, in oral products, in addition to the effects and efficacy, formulation design that gives a sense of effect during product use is also important. In oral compositions, l-menthol is used for the purpose of imparting a cooling sensation and enhancing user satisfaction. Patent Document 1 (Japanese Patent Application Laid-Open No. 2012-77032) discloses a technique for suppressing bitterness and irritation to the tongue and maintaining a cooling sensation by combining with chlorobutanol against the bitterness of l-menthol itself and irritation to the tongue.

[0003] On the other hand, chlorobutanol is easily decomposed over time by heat, light, and in a pH range from neutral to basic, and the sense of penetration decreases. However, in order to prevent demineralization of dental dentin, the pH of the oral composition is preferably 6 or more, and a technique for stabilizing chlorobutanol in a neutral to basic pH range has been demanded.

[0004] As a technique for stabilizing chlorobutanol, Patent Document 2 (Japanese Patent Application Laid-Open No. 2011-105764) discloses a technique in which trometamol is applied in an external preparation composition. However, in oral compositions such as dentifrices, the stabilizing effect of chlorobutanol was not sufficient.

Prior Art Documents

Patent Documents

[0005]

Patent Document 1

Patent Document 2

Summary of the Invention

Problems to be Solved by the Invention

[0006] The present invention has been made in view of the above circumstances, and an object thereof is to provide an oral composition that can impart a feeling of penetration immediately after production and after storage, and suppresses irritation to the tongue.

Means for Solving the Problems

[0007] As a result of intensive studies to achieve the above object, the present inventors have found that by adding a compound having Na or K in a certain amount in terms of Na and K to an oral composition having a pH of 6.0 to 8.5 containing chlorobutanol, not only excellent penetration feeling can be obtained immediately after production but also after storage, and irritation to the tongue is suppressed, and thus the present invention has been completed.

[0008] Therefore, the present invention provides the following oral composition. 1. An oral composition having a pH of 6.0 to 8.5 containing: (A) Chlorobutanol (B) A compound having Na or K: 0.25 to 8% by mass in terms of Na and K, and (C) Water: 20 to 80% by mass 2. The oral composition according to 1, wherein the content of the component (A) is 0.001 to 0.2% by mass. 3. The oral composition according to 1 or 2, wherein the component (B) is at least one selected from sodium chloride, sodium sulfate, potassium chloride, potassium nitrate, xanthan gum, and sodium carboxymethyl cellulose. 4. The oral composition according to any one of 1 to 3, wherein the content of the component (B) is 0.3 to 8.0% by mass in terms of Na and K. 5. The oral composition according to any one of 1 to 4, wherein the content mass ratio represented by (B) in terms of Na and K / (A) is 3 to 500.

Effects of the Invention

[0009] According to the present invention, it is possible to provide an oral composition that can impart an excellent feeling of penetration by chlorobutanol immediately after production and after storage, and suppresses irritation to the tongue.

Modes for Carrying Out the Invention

[0010] Hereinafter, the present invention will be described in detail. [Component (A)] Component (A) of the present invention is chlorobutanol and has an effect of imparting a sense of penetration. It is liable to decompose over time in the pH range from heat, light, neutral to basic. As chlorobutanol, commercially available products can be used.

[0011] From the viewpoint of the sense of penetration, the content of component (A) is preferably 0.001% by mass or more in the oral composition. By setting it to 0.001% by mass or more, a sense of penetration can be obtained more effectively. Also, from the viewpoint of suppressing irritation to the tongue, it is preferably 0.2% by mass or less. More preferably, it is 0.005 to 0.05% by mass, and even more preferably, it is 0.01 to 0.1% by mass.

[0012] [Component (B)] Component (B) of the present invention is a compound having Na or K, and may have both Na and K. By blending a certain amount of the compound having Na or K, a sense of penetration can be obtained even after storage.

[0013] Examples of the compound having Na or K include the following. B-1 Potassium alum (12-hydrate), sodium pyrrolidone carboxylate, sodium fluoride, sodium monofluorophosphate, sodium citrate, sodium hydroxide, sodium saccharin, sodium benzoate, sodium lauryl sulfate, sodium lauroyl methyl taurate, sodium tetradecene sulfonate, sodium lauroyl sarcosinate, coconut oil fatty acid amide propyl betaine, sodium chloride, sodium sulfate (including anhydrous), sodium pyrophosphate (including anhydrous), sodium polyphosphate, sodium metaphosphate, trisodium phosphate, sodium hydrogen phosphate, sodium dihydrogen phosphate, sodium hydrogen carbonate, potassium dihydrogen phosphate, potassium chloride, potassium nitrate, dipotassium edetate dihydrate, potassium dihydrogen phosphate

[0014] B-2 Sodium carboxymethyl cellulose, sodium alginate, xanthan gum, sodium polyacrylate

[0015] As the component (B), at least one selected from sodium chloride, sodium sulfate, potassium chloride, potassium nitrate, xanthan gum, and sodium carboxymethyl cellulose is preferable.

[0016] The content of the component (B) is 0.25 to 8% by mass in the oral composition in terms of Na and K, preferably 0.3 to 8.0% by mass, more preferably 0.4 to 6% by mass, and even more preferably 0.5 to 5% by mass. If the component (B) in the oral composition is less than 0.25% by mass in terms of Na and K, the osmotic sensation after storage will be insufficient. On the other hand, if it exceeds 8% by mass, it is likely to cause irritation to the tongue.

[0017] The mass ratio represented by (B) Na, K conversion / (A) is preferably 3 to 500, more preferably 5 to 300, from the viewpoint of the osmotic sensation.

[0018] [Component (C)] The component (C) of the present invention is water and is not particularly limited such as purified water. The content of the component (C) is 20 to 80% by mass in the oral composition, preferably 30 to 70% by mass, more preferably 40 to 65% by mass, and even more preferably 40 to 60% by mass. If the content of the component (C) is less than 20% by mass, the extrudability from the container of the oral composition will decrease. On the other hand, if it exceeds 80% by mass, it is likely to cause irritation to the tongue.

[0019] The pH of the oral composition of the present invention is 6.0 to 8.5, preferably 6.0 to 8.0, more preferably 6.1 to 7.5. If the pH is too low, the teeth are likely to demineralize. If the pH is too high, there is a risk of irritation to the oral mucosa. The pH measurement is the value measured with a pH meter at 25 °C for a dispersion obtained by collecting the oral composition in a 5 g volumetric flask, adding water to adjust it to 50 mL and dispersing it. The details are the method described in the examples.

[0020] The dentifrice composition of the present invention can be prepared in forms such as solid, liquid, liquid-like, paste-like, gel-like, etc., and can be made into various dosage forms such as toothpaste, liquid dentifrice, liquid-like dentifrice, and moist dentifrice. The manufacturing method can also adopt conventional methods according to the dosage form. In this case, according to the purpose of the composition, dosage form, etc., appropriate known components can be blended in addition to the above-mentioned components. The oral composition of the present invention is preferably prepared as a dentifrice such as toothpaste. In addition to the above components, other known components can be blended as necessary within the range that does not interfere with the effects of the present invention. For example, in toothpaste, surfactants, abrasives, binders, thickeners (humectants), and further, if necessary, sweeteners, colorants, preservatives, fragrances, active ingredients, pH adjusters, wetting agents, solvents, etc. can be blended. The content may be a normal amount within the range that does not interfere with the effects of the present invention.

[0021] As the surfactant, anionic surfactants, nonionic surfactants, cationic surfactants, and amphoteric surfactants can be blended. Examples of anionic surfactants include alkyl sulfates having a hydrocarbon group with 8 to 20 carbon atoms, polyoxyethylene alkyl sulfate ester salts, α-sulfo fatty acid methyl ester salts, acyl amino acid salts, acyl taurine salts, higher fatty acid salts, etc. Examples of nonionic surfactants include sugar fatty acid esters such as sucrose fatty acid esters, sugar alcohol fatty acid esters, sorbitan fatty acid esters, glycerin fatty acid esters, polyglycerin fatty acid esters, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene fatty acid esters such as polyoxyethylene hydrogenated castor oil, polyoxyethylene higher alcohol ethers, fatty acid alkanolamides, etc. Examples of cationic surfactants include quaternary ammonium salt systems such as alkyl ammonium type and alkyl benzyl ammonium salts. Examples of amphoteric surfactants include betaine acetate types such as alkyl betaine and fatty acid amide propyl betaine, and imidazolinium betaine (alkyl imidazole) types such as alkyl imidazolinium betaine and 2-alkyl-N-carboxymethyl-N-hydroxyethyl imidazolinium betaine.

[0022] When a surfactant is blended, the amount is usually 0 to 10% by mass in the oral composition, and preferably 0.1 to 5% by mass.

[0023] Examples of the abrasive include silica-based abrasives such as anhydrous silicic acid, precipitated silica, aluminosilicate, and zirconosilicate; calcium phosphate-based compounds such as dicalcium phosphate dihydrate or anhydrate; calcium carbonate; and synthetic resin-based abrasives. When an abrasive is blended, the amount is usually 0 to 50% by mass, and preferably 10 to 40% by mass.

[0024] Examples of the organic binder or inorganic binder other than the component (B) include hydroxyethyl cellulose, povidone, hydroxyethyl cellulose, hydroxymethyl cellulose, hydroxypropyl methyl cellulose, methyl cellulose, ethyl cellulose, polyvinyl pyrrolidone, polyvinyl alcohol, carboxyvinyl polymer, etc. Examples of the inorganic binder include aluminum silicate and thickening silica. When a binder is blended, the amount is usually 0.1 to 10% by mass, and preferably 0.1 to 5% by mass.

[0025] Examples of the sweetener include sodium saccharin. Examples of the colorant include Food Blue No. 1, Food Blue No. 2, Food Green No. 3, Food Yellow No. 4, Food Yellow No. 5, Food Red No. 106, Food Red No. 227, caramel, titanium oxide, mica titanium, etc. Examples of the preservative include paraoxybenzoic acid esters such as methyl paraben (methyl paraoxybenzoate), and benzoic acid.

[0026] Examples of the fragrance include natural fragrances such as peppermint oil, spearmint oil, anise oil, eucalyptus oil, wintergreen oil, cassia oil, clove oil, thyme oil, sage oil, lemon oil, orange oil, perilla oil, cardamom oil, coriander oil, mandarin oil, lime oil, lavender oil, rosemary oil, laurel oil, chamomile oil, caraway oil, marjoram oil, bay oil, lemongrass oil, oregano oil, pine needle oil, neroli oil, rose oil, jasmine oil, grapefruit oil, sweety oil, pomelo oil, iris concrete, absolute peppermint, absolute rose, orange flower, and fragrances obtained by processing these natural fragrances (such as pre-run cut, tail cut, fractional distillation, liquid-liquid extraction, essence formation, powder fragrance formation, etc.), menthol, carvone, anethole, cineole, methyl salicylate, cinnamic aldehyde, borneol, camphor, eugenol, 3-l-menthoxypropane-1,2-diol, thymol, linalool, linalyl acetate, limonene, menthone, menthyl acetate, N-substituted-p-menthane-3-carboxamide, pinene, octyl aldehyde, citral, pregeone, carvyl acetate, anisaldehyde, ethyl acetate, ethyl butyrate, allyl cyclohexanepropionate, methyl anthranilate, ethyl methylphenylglycidate, vanillin, undecalactone, hexanal, butanol, isoamyl alcohol, hexenol, dimethyl sulfide, cyclotene, furfural, trimethylpyrazine, ethyl lactate, ethyl thioacetate, and other single-component fragrances, as well as compounded fragrances such as strawberry flavor, apple flavor, banana flavor, pineapple flavor, grape flavor, mango flavor, butter flavor, milk flavor, fruit mix flavor, tropical fruit flavor, etc. These can be used in combination with known fragrance materials used in oral compositions.

[0027] The amount of the fragrance when compounded is not particularly limited, but preferably 0.000001 to 1% by mass in the composition. The flavoring fragrance using the above fragrance materials is preferably used in an amount of 0.1 to 2% by mass in the oral composition.

[0028] As the active ingredient, an active ingredient acceptable for oral preparations can be used. For example, nonionic bactericides such as isopropylmethylphenol; cationic bactericides such as cetylpyridinium chloride; anti-inflammatory agents such as tranexamic acid, allantoin, glycyrrhetinic acid; enzymes such as dextranase; fluorine-containing compounds such as stannous fluoride; vitamin B5 or its derivatives such as pantothenic acid, panthenol; vitamin E or its derivatives such as ascorbic acid, tocopherol acetate, plant extracts, tartar inhibitors, and dental plaque inhibitors can be mentioned, but are not limited thereto. These active ingredients can be formulated in an effective amount within a range that does not interfere with the effects of the present invention.

[0029] Examples of the pH adjuster include acetic acid, hydrochloric acid, sulfuric acid, nitric acid, citric acid, phosphoric acid, malic acid, gluconic acid, maleic acid, succinic acid, glutamic acid, etc. The amount of the pH adjuster to be formulated is appropriately selected so as to achieve the target pH.

[0030] Examples of the humectant include sugar alcohols such as sorbitol, xylitol, erythritol, and polyhydric alcohols such as glycerin, propylene glycol, and polyethylene glycol (PEG).

[0031] Examples of the solvent include lower alcohols having 2 to 3 carbon atoms such as ethanol. In addition, when ethanol is formulated, the amount may be 25% by mass or less in the oral composition, or it may not be formulated.

[0032] The material of the container for accommodating the oral composition of the present invention is not particularly limited, and usually, a container used for oral compositions can be used. Specifically, plastic containers such as polyethylene, polypropylene, polyethylene terephthalate, and nylon can be used.

Examples

[0033] The following are examples and comparative examples to specifically illustrate the present invention, but the present invention is not limited to the following examples. In the following examples, unless otherwise specified, "%" of the composition refers to mass %, the ratio refers to the mass ratio, and the amount of each component in the table is the amount converted to pure components.

[0034] [Examples, Comparative Examples] Toothpaste compositions having the compositions shown in Tables 1 to 5 were prepared by a conventional method, and the evaluations shown in the following (1) to (3) were carried out. The results are also shown in the table.

[0035] (1) Penetration feeling: Immediately after production and after storage at 50°C for 1 month The toothpaste composition immediately after production and the prepared toothpaste composition (about 90 g) filled in an aluminum laminate tube were placed in a 50°C constant temperature bath for 1 month for storage, and then returned to room temperature. The toothpaste composition after storage at 50°C for 1 month was evaluated. For 7 randomly selected panelists, an appropriate amount (1 g) of the toothpaste composition was applied to a toothbrush (manufactured by Lion, Clinica Hubrush 4-row head, medium), and the gums and gingiva were brushed in the normal way for 3 minutes for massage. After that, the mouth was rinsed with water, and the persistence of the penetration feeling was judged at the following 7 levels immediately after and after storage at 50°C for 1 month. The average score of the 7 people was calculated and shown according to the following evaluation criteria. [Scoring criteria for penetration feeling] 7: Feel a very strong penetration feeling 6: Feel a fairly strong penetration feeling 5: Feel a slightly strong penetration feeling 4: It's hard to say either way 3: Don't feel much penetration feeling 2: Hardly feel any penetration feeling 1: Don't feel any penetration feeling at all [Evaluation criteria for penetration feeling: "〇" and "◎" are considered qualified. ] ◎: The average score of 7 people is 6.0 or more 〇: The average score of 7 people is 5.0 or more and less than 6.0 ×: The average score of 7 people is less than 5.0

[0036] (2) Feeling during use (irritation to the tongue during use) For seven randomly selected panelists, an appropriate amount (1 g) of the dentifrice composition was applied to a toothbrush (manufactured by Lion, Clinica Hubrush 4-row head, medium), and the gums and gingiva were brushed in the normal manner for 3 minutes. The irritation sensation on the tongue during brushing was judged on the following four levels. The average score of the seven panelists was calculated, and the results are shown according to the following evaluation criteria. <Scoring Criteria for Irritation to the Tongue> 4 points: No irritation to the tongue was felt. 3 points: Slight irritation to the tongue was felt. 2 points: Some irritation to the tongue was felt. 1 point: Irritation to the tongue was felt. 〈Evaluation Criteria for Irritation to the Tongue: “〇” and “◎” are considered passing.〉 ◎: The average score of the seven panelists is 3.5 points or more. ○: The average score of the seven panelists is 3.0 points or more and less than 3.5 points. ×: The average score of the seven panelists is less than 3.0 points.

[0037]

Table 1

[0038]

Table 2

[0039]

Table 3

[0040]

Table 4

[0041]

Table 5

[0042] A dentifrice composition with the following formulation was prepared by a conventional method. When the same evaluation as above was conducted, the same effects were obtained.

[0043]

Table 6

[0044] The raw materials used in the above examples are shown below. Chlorobutanol (trade name: Chlorobutanol, manufactured by Merck) Sodium chloride (trade name: Selected Special Grade Salt, manufactured by Nippon Suisan Kaisha, Ltd.) Potassium chloride (trade name: Potassium Chloride, manufactured by Tomita Pharmaceutical Co., Ltd.) Potassium nitrate (trade name: Potassium Nitrate, manufactured by Otsuka Chemical Co., Ltd.) Sodium sulfate anhydrous (trade name: Sodium Sulfate Anhydrous, manufactured by Tomita Pharmaceutical Co., Ltd.) Sodium pyrrolidonecarboxylate (trade name: AJIDEW N-50, manufactured by Ajinomoto Health Supply Co., Ltd.) Sodium metaphosphate anhydrous (trade name: Sodium Metaphosphate Anhydrous, manufactured by Taiheiyo Chemical Industry Co., Ltd.) Sodium fluoride (trade name: Sodium Fluoride, manufactured by Stella Chemifa Co., Ltd.) Sodium hydrogen carbonate (trade name: Sodium Bicarbonate, manufactured by Asahi Glass Co., Ltd.) Trisodium phosphate dodecahydrate (trade name: Trisodium Phosphate (Crystal), manufactured by Taiheiyo Chemical Industry Co., Ltd.) Sodium hydroxide (trade name: Sodium Hydroxide, manufactured by Fujifilm Wako Pure Chemical Corporation) Xanthan gum (trade name: Monatugum DA, manufactured by CP Kelco) Sodium carboxymethyl cellulose (trade name: CMC1260, manufactured by Daicel Finechem Co., Ltd.)

Claims

1. (A) Chlorobutanol (B) A compound containing Na or K: 0.25 to 8% by mass in terms of Na and K, and (C) Water: 20 to 80% by mass An oral composition having a pH of 6.0 to 8.5 and containing the same.

2. The oral composition according to Claim 1, wherein the content of component (A) is 0.001 to 0.2% by mass.

3. The oral composition according to Claim 1, wherein component (B) is at least one selected from sodium chloride, sodium sulfate, potassium chloride, potassium nitrate, xanthan gum, and sodium carboxymethyl cellulose.

4. The oral composition according to Claim 1 or 2, wherein the content of component (B) is 0.3 to 8.0% by mass in terms of Na and K.

5. The oral composition according to Claim 1 or 2, wherein the mass ratio of (B) in terms of Na and K / (A) is 3 to 500.

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