Oral composition

Abstract

To provide an oral composition containing a high concentration of fluorine together with hinokitiol, while ensuring stability of hinokitiol.SOLUTION: An oral composition comprises (A) hinokitiol and (B) a fluorine compound in an amount of 0.1 wt.% or more in terms of fluorine. Further, a thickening anhydrous silicic acid (C) is added to the composition in an amount of 160 to 218 pts.wt. per 1 pt.wt. of component (A). This constitution can improve the stability of component (A).SELECTED DRAWING: None

Description

Technical Field

[0001] The present invention relates to an oral composition containing high-concentration fluorine.

Background Art

[0002] As a component to be blended into a dentifrice for preventing dental caries, fluorine compounds such as sodium fluoride, sodium monofluorophosphate, and stannous fluoride are used. The fluorine compound supplies fluoride ions to the tooth surface, imparts to the tooth resistance to acids produced by cariogenic bacteria, repairs initial dental caries by remineralization, and can restore it to the original healthy dentin. Furthermore, fluoride ions also have an action of suppressing the growth of cariogenic bacteria.

[0003] In addition, a bactericide is used as a component to be blended into a dentifrice for reducing the number of pathogenic bacteria of dental caries or periodontal disease. Although many bactericides are known to be blended into oral compositions, hinokitiol is widely used in oral compositions because of its low toxicity and broad antibacterial spectrum. However, hinokitiol is not necessarily a stable compound.

[0004] For this reason, when hinokitiol is formulated into an oral composition or the like, various stabilization methods are employed. For example, Patent Document 1 describes blending disodium edetate, butylhydroxyanisole, and dibutylhydroxytoluene into a hinokitiol formulation, Patent Document 2 describes blending a water-soluble inorganic salt such as sodium chloride into an oral composition containing hinokitiol, Patent Document 3 describes blending ethyl alcohol in an amount of 1% by weight or more into a hinokitiol-containing hydrophilic paste-like composition and using, as a container, an aluminum tube coated with a specific resin and baked, and Patent Document 4 describes blending a predetermined edetate, ethanol, and water in a specific ratio into an oral composition containing hinokitiol.

Prior Art Documents

Patent Documents

[0005] [Patent Document 1] Japanese Patent Application Laid-Open No. 59-210040 [Patent Document 2] Japanese Patent Application Laid-Open No. 4-198121 [Patent Document 3] Japanese Patent Application Laid-Open No. 2002-3354 [Patent Document 4] Japanese Patent Application Laid-Open No. 2010-150155 [Summary of the Invention] [Problems to be Solved by the Invention]

[0006] In order to further improve the effect of the fluorine compound incorporated in the oral composition, it is desirable to incorporate it at a higher concentration. However, the present inventors faced the problem that when hinokitiol coexists in an oral composition containing a high concentration of fluorine, the stability of hinokitiol is significantly reduced. This problem was so significant that it could not be solved even when a component known to stabilize hinokitiol was incorporated.

[0007] Therefore, an object of the present invention is to provide an oral composition containing a high concentration of fluorine together with hinokitiol, in which hinokitiol is stabilized. [Means for Solving the Problems]

[0008] As a result of intensive studies, the present inventors unexpectedly found that hinokitiol is stabilized by incorporating thickening anhydrous silicic acid into an oral composition containing a high concentration of fluorine and hinokitiol. The present invention has been completed by further studies based on this finding.

[0009] That is, the present invention provides an invention in the following aspects. Item 1. Containing (A) hinokitiol, (B) a fluorine compound, and (C) thickening anhydrous silicic acid, The content of the component (B) is 0.1% by weight or more in terms of the amount of fluorine, An oral composition wherein the content of the component (C) is 160 to 218 parts by weight per 1 part by weight of the component (A). Item 2. The oral composition according to Item 1, wherein the content of the component (B) is in terms of fluorine amount and is 2 parts by weight or more per 1 part by weight of the component (A). Item 3. The oral composition according to Item 1 or 2, wherein the content of the component (A) is 0.005 to 0.2% by weight. Item 4. The oral composition according to any one of Items 1 to 3, which is a dentifrice abrasive. Item 5. A method for improving the stability of the component (A) in an oral composition containing (A) hinokitiol and (B) a fluorine compound having a fluorine amount of 0.1% by weight or more, The method, wherein the oral composition is further blended with (C) thickening anhydrous silicic acid in an amount of 160 to 218 parts by weight per 1 part by weight of the component (A) to improve the stability of the component (A).

Advantages of the Invention

[0010] According to the present invention, there is provided an oral composition containing a high concentration of fluorine together with hinokitiol and having hinokitiol stabilized.

Modes for Carrying Out the Invention

[0011] 1. Oral composition The oral composition of the present disclosure is characterized by containing (A) hinokitiol (hereinafter, also referred to as the "component (A)"), a predetermined amount of (B) a fluorine compound (hereinafter, also referred to as the "component (B)"), and a predetermined ratio of (C) thickening anhydrous silicic acid (hereinafter, also referred to as the "component (C)"). The oral composition of the present disclosure contains the component (A) together with a predetermined amount of the component (B) and contains the component (C), thereby improving the stability of the component (A).

[0012] Hereinafter, the oral composition of the present disclosure will be described in detail. In this specification, a numerical range indicated by two numerical values and "~" shall include the two numerical values as the lower limit value and the upper limit value. For example, the notation of 2 to 15% by weight means 2% by weight or more and 15% by weight or less.

[0013] (A) Hinokitiol The oral composition of the present disclosure contains hinokitiol as component (A). Component (A) is significantly destabilized by containing component (B) in the high-concentration fluorine amount described below, but in the oral composition of the present disclosure, component (A) is stabilized.

[0014] As component (A) used in the oral composition of the present disclosure, either natural product-derived hinokitiol or chemically synthesized hinokitiol may be used. Further, as the material used for blending component (A) in the oral composition of the present disclosure, it does not matter whether it is a purified product or a roughly purified product. For this reason, as a material for blending component (A) in the oral composition of the present disclosure, for example, hinokitiol-containing essential oil obtained from trees may be used.

[0015] The content of component (A) in the oral composition of the present disclosure is appropriately set according to the dosage form and / or use of the oral composition, etc., but examples thereof include 0.005 to 0.2% by weight, preferably 0.01 to 0.1% by weight, more preferably 0.01 to 0.07% by weight, and still more preferably 0.03 to 0.05% by weight.

[0016] (B) Fluorine compound The oral composition of the present disclosure contains a fluorine compound as component (B). The fluorine compound is a known component generally blended in oral compositions.

[0017] As the component (B), specifically, at least one selected from the group consisting of alkali metal fluorides, fluorophosphoric acid, and salts of fluorophosphoric acid can be mentioned. In the oral composition of the present disclosure, as the component (B), one kind of the three fluorine compounds of alkali metal fluoride, fluorophosphoric acid, and salts of fluorophosphoric acid may be used alone, or two or more kinds may be used in combination.

[0018] The alkali metal fluoride is not particularly limited as long as it is pharmaceutically acceptable, and specifically, sodium fluoride, potassium fluoride, etc. can be mentioned. These alkali metal fluorides may be used alone or in combination of two or more. Among these alkali metal fluorides, preferably sodium fluoride can be mentioned.

[0019] The fluorophosphoric acid is not particularly limited as long as it is pharmaceutically acceptable, and specifically, monofluorophosphoric acid, difluorophosphoric acid, etc. can be mentioned. These fluorophosphoric acids may be used alone or in combination of two or more. Among these fluorophosphoric acids, preferably monofluorophosphoric acid can be mentioned.

[0020] The salt of fluorophosphoric acid is not particularly limited as long as it is pharmaceutically acceptable. For example, the alkali metal salt of the above fluorophosphoric acid, more specifically, the sodium salt, potassium salt, etc. of the above fluorophosphoric acid can be mentioned. These salts of fluorophosphoric acid may be used alone or in combination of two or more. Among these salts of fluorophosphoric acid, preferably the sodium salt can be mentioned.

[0021] Among the above components (B), preferably, alkali metal fluoride, salts of fluorophosphoric acid; more preferably, alkali metal fluoride, salts of monofluorophosphoric acid; still more preferably, sodium fluoride, sodium monofluorophosphate, and particularly preferably sodium monofluorophosphate can be mentioned.

[0022] In the oral composition of the present disclosure, the content of component (B) is 0.1% by weight or more in terms of the amount of fluorine (F). An oral composition containing component (B) at a high concentration of 0.1% by weight or more in terms of the amount of fluorine significantly reduces the stability of component (A). However, the oral composition of the present disclosure contains component (A) at a high concentration together with component (B), and the stability of component (A) is improved.

[0023] In the oral composition of the present disclosure, from the viewpoint of obtaining better stability of component (A), the content of component (B) is preferably 0.1 to 0.3% by weight, more preferably 0.1 to 0.25% by weight, still more preferably 0.1 to 0.2% by weight, and even more preferably 0.1 to 0.15% by weight in terms of the amount of fluorine. Since the oral composition of the present disclosure is excellent in the stability of component (A), even if the amount of component (B) that destabilizes component (A) is large, the effect of improving stability can be effectively obtained. From such a viewpoint, preferred contents of component (B) include preferably 0.12 to 0.2% by weight, more preferably 0.13 to 0.2% by weight, and still more preferably 0.14 to 0.2% by weight.

[0024] In the oral composition of the present disclosure, the ratio of the content of component (B) to the content of component (A) is determined according to the contents of the above components. For example, in terms of the amount of fluorine of component (B) per 1 part by weight of component (A), for example, 2 parts by weight or more can be mentioned.

[0025] In the oral composition of the present disclosure, from the viewpoint of obtaining better stability of component (A), the amount of fluorine of component (B) per 1 part by weight of component (A) is preferably 2 to 10 parts by weight, more preferably 2 to 8 parts by weight, still more preferably 2 to 6 parts by weight, and even more preferably 2 to 4 parts by weight. Since the oral composition of the present disclosure is excellent in the stability of component (A), even if the ratio of component (B) that destabilizes component (A) is large, the effect of improving stability can be effectively obtained. From such a viewpoint, preferred values of the amount of fluorine of component (B) per 1 part by weight of component (A) include preferably 2.2 to 10 parts by weight, more preferably 2.5 to 10 parts by weight, still more preferably 3 to 10 parts by weight, and even more preferably 3.5 to 10 parts by weight.

[0026] (C) Viscosity-increasing anhydrous silicic acid The oral composition of the present disclosure contains thickening silicic anhydride as component (C). In an oral composition containing component (A) and a high-concentration component (B), the stability of component (A) is significantly reduced. However, in the oral composition of the present disclosure, the stability of component (A) is improved by the incorporation of component (C).

[0027] The thickening silicic anhydride used as component (C) refers to silicic anhydride having a liquid absorption amount of 2 to 3 ml / g. In this specification, the liquid absorption amount is the liquid absorption amount per gram (ml / g), and is taken as the measured value obtained by the following measurement method. (Measurement method for liquid absorption amount) Weigh 1.0 g of the sample onto a clean glass plate, and while dropping a small amount of a 42.5 wt% glycerin aqueous solution using a micro burette, mix the sample uniformly with a stainless-steel spatula. The liquid amount (ml) required until the sample becomes a single mass and can be cleanly peeled off from the glass plate with a spatula is taken as the liquid absorption amount.

[0028] In the oral composition of the present disclosure, the content of component (C) is 160 to 218 parts by weight per 1 part by weight of (A). From the viewpoint of improving the stability of component (A), the content of component (C) is preferably 160 to 215 parts by weight, more preferably 160 to 205 parts by weight or 162 to 203 parts by weight, still more preferably 170 to 201 parts by weight or 173 to 185 parts by weight per 1 part by weight of (A).

[0029] The content of component (C) in the oral composition of the present disclosure is determined according to the content of the above-mentioned component (A) and the ratio of component (C). For example, it is 5 to 12 wt%, 5 to 10 wt% or 6 to 9 wt%, preferably 6.3 to 8.7 wt% or 6.5 to 8.5 wt%, more preferably 6.8 to 8.2 wt% or 7 to 8 wt%.

[0030] (D) Other component - 1 In addition to the aforementioned components, the oral composition of the present disclosure can further contain one or more components selected from the group consisting of (D1) a predetermined water-soluble inorganic salt; (D2) aluminum lactate; (D3) alanine and / or lysine; (D4) edetic acid and / or its salt; and (D5) ethanol, from the viewpoint of further enhancing the stability of the component (A). Note that the oral composition of the present disclosure may not contain these components, and it is possible to improve the stability of the component (A) even without containing these components.

[0031] (D1) Predetermined water-soluble inorganic salt The predetermined water-soluble inorganic salt is selected from the group consisting of sodium chloride, potassium chloride, sodium hydrogen carbonate, sodium carbonate, potassium hydrogen carbonate, potassium carbonate, sodium monohydrogen phosphate, sodium dihydrogen phosphate, potassium monohydrogen phosphate, potassium dihydrogen phosphate, sodium sulfate, and potassium sulfate. These predetermined water-soluble inorganic salts may be used alone or in combination of two or more. Among these predetermined water-soluble inorganic salts, preferably sodium chloride is mentioned.

[0032] When the oral composition of the present disclosure contains the component (D1), its content is not particularly limited, and examples thereof include 0.005 to 10% by weight, preferably 0.08 to 5% by weight, 0.08 to 3% by weight, or 0.08 to 1.5% by weight.

[0033] (D2) Aluminum lactate When the oral composition of the present disclosure contains the component (D2), its content is not particularly limited, and examples thereof include 0.1 to 5% by weight, preferably 0.2 to 3.5% by weight, more preferably 0.2 to 2.5% by weight.

[0034] (D3) Alanine and / or lysine As alanine and lysine, any of the D-form, L-form, and DL-form may be used. Among these components, preferably alanine is mentioned, and more preferably DL-alanine is mentioned.

[0035] When the oral composition of the present disclosure contains the component (D3), its content is not particularly limited, but in total, for example, 0.01 to 5% by weight, preferably 0.05 to 3% by weight, more preferably 0.05 to 1% by weight, or 0.05 to 0.5% by weight can be mentioned.

[0036] (D4) Edetic acid and / or its salt The salts of edetic acid are not particularly limited as long as they are pharmaceutically acceptable. For example, disodium edetate, trisodium edetate, tetrasodium edetate, tetrasodium edetate dihydrate, tetrasodium edetate tetrahydrate, dipotassium edetate dihydrate, etc. can be mentioned. These salts of edetic acid may be used alone or in combination of two or more. Among edetic acid and its salts, preferably salts of edetic acid, more preferably disodium edetate can be mentioned.

[0037] When the oral composition of the present disclosure contains the component (D4), its content is not particularly limited, but in total, for example, 0.05 to 0.6% by weight, preferably 0.1 to 0.3% by weight can be mentioned.

[0038] (D5) Ethanol When the oral composition of the present disclosure contains the component (D5), its content is not particularly limited, but for example, 0.2 to 3.5% by weight, preferably 0.6 to 1.5% by weight can be mentioned.

[0039] (E) Other component - 2 In addition to the aforementioned components, the oral composition of the present disclosure may or may not contain components commonly used in the art according to the dosage form of the oral composition, as long as the effects of the present invention are not impaired. Examples of such components regardless of whether they are contained or not include water, preservatives, bactericides other than hinokitiol, antibacterial agents, anti-inflammatory agents, glucosyltransferase (GTase) inhibitors, plaque inhibitors, hypersensitivity inhibitors, calculus preventives, abrasives, plant extracts (including crude drug extracts), adhesives, thickeners, excipients, lubricants, fragrances, sweeteners, cooling agents, pigments, deodorants, surfactants, pH adjusters, etc.

[0040] Examples of preservatives, bactericides, and antibacterial agents include benzoic acid or its salts, salicylic acid or its salts, sorbic acid or its salts, paraoxybenzoic acid esters, decalinium chloride, benzethonium chloride, benzalkonium chloride, chlorhexidine chloride, chlorhexidine gluconate, isopropylmethylphenol, triclosan, cetylpyridinium chloride, lysozyme chloride, chlorhexidine hydrochloride, potassium iodide, and the like.

[0041] Examples of anti-inflammatory agents include tranexamic acid, epsilon-aminocaproic acid, allantoin chloroaluminum hydroxide, allantoin dihydroxyaluminum, allantoin, azulene, glycyrrhizinate, glycyrrhetinic acid, sodium chloride, vitamins, and the like.

[0042] Examples of GTase inhibitors include extracts of plants in the genus Commelina of the Commelinaceae family, extracts of plants in the genus Vitis of the Vitaceae family, dextranase, mutanase, tastein, tannins, ellagic acid, polyphenols, oolong tea extract, green tea extract, assemblage, taiso, wikyo, peony, gentiana, senso, gentian, coptis, and the like.

[0043] Examples of plaque inhibitors include zinc citrate, gluconic acid, and the like.

[0044] Examples of hypersensitivity inhibitors include potassium nitrate, strontium chloride, and the like.

[0045] Examples of calculus preventives include polyphosphates, zeolite, ethanehydroxydiphosphonate, and the like.

[0046] Examples of the abrasive include, for example, dicalcium phosphate (dihydrate or anhydride), monocalcium phosphate, tricalcium phosphate, calcium pyrophosphate, calcium carbonate, aluminum hydroxide, alumina, magnesium carbonate, magnesium phosphate, insoluble sodium metaphosphate, insoluble potassium metaphosphate, titanium oxide, zeolite, hydrous silicic acid (provided that the liquid absorption amount per gram is less than 2 ml / g for the material dried at 105°C for 4 hours), titanium silicate, zirconium silicate, abrasive silica (referring to the material with a liquid absorption amount less than 2 ml / g), etc.

[0047] Examples of the plant extract include licorice extract, peony extract, mulberry extract, birch extract, kumanazasa extract, saffron extract, loquat leaf extract, waremokou extract, tea extract, licorice root extract, carrot extract, aconite extract, turmeric extract, white mustard extract, sage extract, etc.

[0048] As the adhesive, a thickening polysaccharide is sufficient. For example, pullulan esters such as pullulan and pullulan phosphate, polysaccharides such as starch; cellulose-based polymer substances such as hydroxypropyl cellulose, hydroxyethyl cellulose, hydroxypropyl methyl cellulose, hydroxyethyl methyl cellulose, carboxymethyl cellulose, carboxymethyl cellulose salts (sodium carboxymethyl cellulose, potassium carboxymethyl cellulose, etc.), methyl cellulose, ethyl cellulose, polyacrylic acid, polyacrylate salts (sodium polyacrylate, octyl acrylate-acrylic acid copolymer, etc.), copolymers of methacrylic acids (polymers of methacrylic acid and n-butyl acrylate, polymers of methacrylic acid and methyl methacrylate, polymers of methacrylic acid and ethyl acrylate, etc.); synthetic polymer substances such as carboxyvinyl polymer, polyethylene glycol, polyvinyl pyrrolidone, polyvinyl alcohol; natural polymer substances such as lectin, alginic acid, alginate salts (sodium alginate, potassium alginate, magnesium alginate, propylene glycol alginate, triethanolamine alginate, triisopropanolamine alginate, ammonium alginate, butylamine alginate, diamylamine alginate, etc.), sodium chondroitin sulfate, agar, chitosan, carrageenan; amino acid-based polymer substances such as collagen and gelatin; natural rubber-based polymer substances such as gum arabic, karaya gum, tragacanth gum, xanthan gum, locust bean gum, guar gum, tamarind gum, gellan gum, etc.

[0049] As the thickening agent, for example, polyhydric alcohols and / or sugar alcohols such as glycerin, sorbitol, ethylene glycol, propylene glycol, polyethylene glycol, polypropylene glycol, xylitol, maltitol, lactitol, etc. can be mentioned.

[0050] As the excipient, for example, lactose, sucrose, mannitol, starch, dextrin, crystalline cellulose, etc. can be mentioned.

[0051] Examples of the lubricant include magnesium stearate, talc, sodium stearyl fumarate, and the like.

[0052] Examples of the fragrance include natural fragrances (such as star anise oil and clove oil), synthetic fragrances, and blended fragrances thereof.

[0053] Examples of the sweetener include sodium saccharin, stevioside, stevia extract, aspartame, xylitol, starch syrup, honey, sorbitol, maltitol, mannitol, erythritol, saccharides (such as lactose, sucrose, fructose, and glucose), and the like.

[0054] Examples of the cooling agent include camphor, borneol, geraniol, and essential oils containing these.

[0055] Examples of the pigment include natural pigments, synthetic pigments, and mixtures thereof.

[0056] Examples of the deodorant include copper gluconate, zinc chloride, sodium copper chlorophyllin, raw coffee bean extract, burdock powder, green tea, roasted rice bran extract, kaki tannin, and the like.

[0057] Examples of surfactants include anionic surfactants such as sodium polyoxyethylene lauryl ether sulfate, sodium lauryl sulfate, sodium myristyl sulfate, sodium N-lauroyl glutamate, sodium N-lauroyl sarcosinate, sodium lauroyl methyl taurate, sodium N-myristyl sarcosinate, sodium N-palmitoyl glutamine, sodium N-methyl-N-acyl taurate, sodium dodecylbenzenesulfonate, sodium hydrogenated coconut fatty acid monoglyceride monosulfate, sodium lauryl sulfacetate, sodium α-olefin sulfonate; nonionic surfactants such as polyoxyethylene hydrogenated castor oil, sucrose fatty acid ester, maltose fatty acid ester, maltitol fatty acid ester, lactitol fatty acid ester, sorbitan fatty acid ester, polyoxyethylene sorbitan monostearate, polyoxyethylene higher alcohol ether, polyoxyethylene polyoxypropylene copolymer, polyoxyethylene polyoxypropylene fatty acid ester, polyglycerin fatty acid ester; amphoteric surfactants such as coconut oil fatty acid amidopropyl betaine, lauryldimethylaminoacetic acid betaine, lauryldimethylamine oxide, 2-alkyl-N-carboxymethyl-N-hydroxyethylimidazolium betaine, N-lauryl diaminoglycine, N-myristyl diaminoglycine, sodium N-alkyl-1-hydroxyethylimidazoline betaine; cationic surfactants such as lauryltrimethylammonium chloride, stearyltrimethylammonium chloride, benzethonium chloride, benzalkonium chloride, stearyldimethylbenzylammonium chloride.

[0058] Examples of pH adjusters include acetic acid, hydrochloric acid, sulfuric acid, nitric acid, citric acid, phosphoric acid, sodium hydroxide, potassium hydroxide, sodium acetate, sodium carbonate, sodium citrate, sodium hydrogen citrate, sodium phosphate, disodium hydrogen phosphate, etc.

[0059] When the oral composition of the present disclosure contains the above components, the above components may be used alone or in combination of two or more. Among the above components, the oral composition of the present disclosure particularly preferably contains (E1) water, (E2) benzoic acid or its salt, salicylic acid or its salt, sorbic acid or its salt, and / or paraoxybenzoic acid ester; preferably paraoxybenzoic acid ester, (E3) cetylpyridinium chloride, lysozyme chloride, and / or chlorhexidine hydrochloride; preferably cetylpyridinium chloride, (E4) titanium oxide, hydrous silicic acid (however, the liquid absorption amount per gram is less than 2 ml / g for the one dried at 105 °C for 4 hours with a sample size of 1 g), and / or abrasive silica (referring to the one with a liquid absorption amount less than 2 ml / g), (E5) peony root extract, Japanese angelica root extract, mulberry bark extract, birch bark extract, kudzu leaf extract, saffron extract, loquat leaf extract, Chinese gromwell root extract, tea extract, licorice extract, carrot extract, aconite root extract, turmeric extract, Japanese butterbur extract, and / or sage extract; preferably peony root extract, Japanese angelica root extract, and / or mulberry bark extract, (E6) thickening polysaccharides; preferably carrageenan and / or xanthan gum; more preferably carrageenan, (E7) polyhydric alcohol and / or sugar alcohol; preferably glycerin and / or sorbitol, (E8) copper gluconate, (E9) surfactant; preferably anionic surfactant and / or nonionic surfactant; more preferably sodium lauryl sulfate, sodium myristyl sulfate, sodium N-lauroylglutamate, sodium N-lauroylsarcosinate, sodium lauroylmethyl taurine, sodium N-myristylsarcosinate, sodium N-palmitoylglutamate, sodium N-methyl-N-acyl taurine, and polyoxyethylene hydrogenated castor oil can be included.

[0060] When the oral composition of the present disclosure contains the component (E1), its content is not particularly limited, but in total, for example, 17 to 30% by weight, preferably 20 to 27% by weight can be mentioned. When the oral composition of the present disclosure contains the component (E2), its content is not particularly limited, but in total, for example, 0.01 to 0.2% by weight, preferably 0.05 to 0.15% by weight can be mentioned. When the oral composition of the present disclosure contains the component (E3), its content is not particularly limited, but in total, for example, 0.01 to 0.1% by weight, preferably 0.03 to 0.07% by weight can be mentioned. When the oral composition of the present disclosure contains the component (E4), its content is not particularly limited, but for titanium oxide, for example, 0.01 to 2% by weight, preferably 0.5 to 1.5% by weight, and for the above-mentioned hydrous silicic acid and / or the above-mentioned anhydrous silicic acid, in total, for example, 5 to 25% by weight, preferably 10 to 20% by weight can be mentioned. When the oral composition of the present disclosure contains the component (E5), its content is not particularly limited, but in total, for example, 0.1 to 0.45% by weight, preferably 0.2 to 0.35% by weight can be mentioned. When the oral composition of the present disclosure contains the component (E6), its content is not particularly limited, but in total, for example, 0.25 to 1.5% by weight, preferably 0.5 to 1% by weight can be mentioned. When the oral composition of the present disclosure contains the component (E7), its content is not particularly limited, but in total, for example, 30 to 60% by weight, preferably 35 to 55% by weight, for polyhydric alcohol, for example, 20 to 50% by weight, preferably 25 to 45% by weight, and for sugar alcohol, for example, 1 to 20% by weight, preferably 5 to 15% by weight can be mentioned. When the oral composition of the present disclosure contains the component (E8), its content is not particularly limited, but in total, for example, 0.01 to 0.3% by weight, preferably 0.05 to 0.15% by weight can be mentioned. When the oral composition of the present disclosure contains the component (E9), its content is not particularly limited, but in total, for example, 1 to 10% by weight, preferably 3 to 5% by weight can be mentioned.

[0061] Shape and dosage form The shape of the oral composition of the present disclosure is not particularly limited and may be any of liquid, solid, semi-solid (gel-like, ointment-like, paste-like), etc.

[0062] The dosage forms of the oral composition of the present disclosure are not limited as long as they can be applied in the oral cavity and stay in the oral cavity for a certain period of time. Examples include liquid dentifrices, paste dentifrices, gargles, oral coolants (such as mouth sprays), oral pastes, and oral hygiene agents such as gingival massage creams. Among these, liquid dentifrices, paste dentifrices, and oral pastes are preferred, liquid dentifrices and paste dentifrices are more preferred, and paste dentifrices are even more preferred.

[0063] Regarding the container for accommodating the oral composition of the present disclosure, preferably, a container is provided in which the contact surface with the oral composition of the present disclosure is made of a synthetic resin (examples include polyolefins such as polypropylene, high-density polyethylene, and low-density polyethylene).

[0064] 2. Method for improving the stability of hinokitiol As described above, in an oral composition containing (A) hinokitiol and (B) a fluorine compound having a fluorine content of 0.1% by weight or more, when (C) thickening anhydrous silicic acid is blended under the condition of 160 to 218 parts by weight per 1 part by weight of the (A) component, the stability of hinokitiol is improved as compared with the case where the condition is not satisfied. Therefore, the present invention further provides a method for improving the stability of the (A) component in an oral composition containing (A) hinokitiol and (B) a fluorine compound having a fluorine content of 0.1% by weight or more, the method comprising further blending (C) thickening anhydrous silicic acid into the oral composition so as to be 160 to 218 parts by weight per 1 part by weight of the (A) component, thereby improving the stability of the (A) component.

[0065] The types and amounts of components used in the enhancer and the enhancing method of the present invention, the composition to which it is applied, etc. are as described in the above "1. Oral composition".

Examples

[0066] Hereinafter, the present invention will be described in more detail with reference to examples, but the present invention is not limited to these examples.

[0067] Test example The dentifrice shown in Tables 1 to 3 was prepared and filled into an aluminum tube (cap material: polypropylene, innermost layer material of the tube: low-density polyethylene) in an amount of 40 g. Note that the "silicic anhydride (thickening property)" shown in the table is silicic anhydride with a liquid absorption of 2 to 3 ml / g, the "silicic anhydride (abrasiveness)" is silicic anhydride with a liquid absorption of less than 2 ml / g, and the "hydrous silicic acid" is silicic acid with a liquid absorption of less than 2 ml / g per 1 g of loss on drying (that is, the weight after drying 1 g under the conditions of 105 °C for 4 hours) (the same applies in the formulation examples described later).

[0068] The obtained dentifrice was stored at 50 °C for 1 month. The content of hinokitiol in the dentifrice before and after storage was quantified by the following method.

[0069] <Method for quantifying hinokitiol content> Approximately 2 g of the target sample was precisely weighed, 6 mL of an aqueous potassium hydroxide solution (147→1250) was added, shaken, and then irradiated with ultrasonic waves. 20 mL of methanol was added thereto, irradiated with ultrasonic waves, centrifuged, and the supernatant was separated. The residue was similarly operated twice using 10 mL of methanol, and the separated supernatants were combined. After adding 20 mL of an EDTA-potassium dihydrogen phosphate aqueous solution and 4 mL of dilute hydrochloric acid thereto, 5 mL of an internal standard solution (methanol solution of ethyl o-aminobenzoate (1→5000)) was accurately added, and methanol was added to make 100 mL, which was obtained as a sample solution.

[0070] Separately, quantitative hinokitiol was dried under reduced pressure (phosphorus (V) oxide, 4 hours), approximately 16 mg was precisely weighed, and methanol was added to make exactly 100 mL, which was used as a standard stock solution. 5 mL of the standard stock solution was accurately weighed, 10 mL of water, 50 mL of methanol, and 20 mL of an EDTA-potassium dihydrogen phosphate aqueous solution were added, and then 5 mL of the above internal standard solution was accurately added, and methanol was added to make 100 mL, which was obtained as a standard solution.

[0071] For 20 μL of the sample solution and the standard solution, a test was conducted by liquid chromatography under the following conditions, and the ratios QT and QS of the peak area of hinokitiol to the peak area of the internal standard substance were determined, respectively. Based on the following formula, the amount of hinokitiol in 100 g of the target sample was determined.

Equation

[0072] The relative amount (%) of hinokitiol after storage was derived as the "remaining amount of hinokitiol" with the amount of hinokitiol in the dentifrice before storage taken as 100%. The results are shown in Tables 1 to 3.

[0073]

Table 1

[0074]

Table 2

[0075]

Table 3

[0076] As shown in the comparison between Reference Example 1 and Comparative Examples 1, 2, and 4, when the content of component (B) was formulated at 0.1% by weight or more in terms of fluorine amount, the stability of hinokitiol as component (A) was significantly reduced. On the other hand, as shown in Examples 1 to 9, by formulating component (C) in an amount of 160 to 218 parts by weight per 1 part by weight of (A), the stability of hinokitiol was significantly improved. Also, as shown in Comparative Examples 3 and 5, when the blending amount of component (C) exceeded 218 parts by weight per 1 part by weight of (A), the stability of hinokitiol was significantly reduced.

[0077] Formulation example The oral compositions shown in Tables 4 to 6 were prepared. In any of the oral compositions, the stability of hinokitiol was improved as compared with the case where the blending amount of the component (C) deviated from the condition of 160 to 218 parts by weight per 1 part by weight of (A).

[0078]

Table 4

[0079]

Table 5

[0080]

Table 6

Claims

1. An oral composition comprising (A) hinokitiol, (B) a fluorine compound, and (C) thickening anhydrous silicic acid, wherein the content of the component (B) is 0.1% by weight or more in terms of fluorine content, and the content of the component (C) is 160 to 218 parts by weight per 1 part by weight of the component (A).

2. The oral composition according to claim 1, wherein the content of the component (B) is 2 parts by weight or more per 1 part by weight of the component (A) in terms of fluorine content.

3. The oral composition according to claim 1, wherein the content of the component (A) is 0.005 to 0.2% by weight.

4. The oral composition according to claim 1, which is a dentifrice.

5. A method for improving the stability of the component (A) in an oral composition comprising (A) hinokitiol and (B) a fluorine compound having a fluorine content of 0.1% by weight or more, wherein the stability of the component (A) is improved by further blending (C) thickening anhydrous silicic acid into the oral composition so that the amount thereof is 160 to 218 parts by weight per 1 part by weight of the component (A).

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