Cosmetic

Abstract

To provide a cosmetic that is free from stickiness and exhibits superior quick affinity with the skin.SOLUTION: A cosmetic in one aspect according to the present invention includes (A) polyoxyethylene hydrogenated castor oil, (B) a polyglyceryl fatty acid ester, (C) an oil component, and (D) a pyrimidylpyrazole compound or a pharmacologically acceptable salt thereof.SELECTED DRAWING: None

Description

Technical Field

[0001] The present invention relates to cosmetics.

Background Art

[0002] In cosmetics used for the purpose of suppressing moisture evaporation from the skin to maintain moisture and softening the skin, not only an emollient effect but also a good feeling in use are required. Usually, the higher the oil content, the higher the moisturizing and emollient effects are obtained. On the other hand, when the oil content is high, stickiness becomes strong and the feeling in use deteriorates. Conversely, when the oil content is reduced and the proportion of aqueous components is increased, although the stickiness is reduced, the emollient effect tends to be inferior. Therefore, it is particularly difficult to achieve an emollient effect in cosmetics with a large amount of aqueous components such as lotion.

[0003] On the other hand, for example, Patent Document 1 discloses that a composition containing polyoxyethylene hydrogenated castor oil and polyglycerin fatty acid ester, which are known to have an emollient effect, a polyhydric alcohol, and a specific anionic surfactant, can provide the effects of lotion even when diluted by being put into a bathtub.

Prior Art Documents

Patent Documents

[0004]

Patent Document 1

Summary of the Invention

Problems to be Solved by the Invention

[0005] In view of the above, an aspect of the present invention aims to provide a cosmetic that is non-greasy and excellent in quick adaptability.

Means for Solving the Problems

[0006] In order to solve the above problems, one aspect of the cosmetic according to the present invention contains (A) polyoxyethylene hydrogenated castor oil, (B) polyglycerol fatty acid ester, (C) oil, and (D) a pyrimidylpyrazole compound represented by the following general formula (1) or a pharmacologically acceptable salt thereof.

[0007]

Chemistry

Advantages of the Invention

[0008] According to one aspect of the present invention, it is possible to provide a cosmetic that is not sticky and has excellent familiarity.

Modes for Carrying Out the Invention

[0009] Hereinafter, embodiments of the present invention will be described in detail. Note that the embodiments are not limited by the following description and can be appropriately changed without departing from the gist of the present invention. In addition, in this specification, "~" indicating a numerical range means including the numerical values described before and after it as the lower limit value and the upper limit value, unless otherwise specified.

[0010] (Cosmetic) The cosmetic according to one embodiment contains (A) polyoxyethylene hydrogenated castor oil, (B) polyglycerol fatty acid ester, (C) oil, and (D) a pyrimidylpyrazole compound represented by the following general formula (1) or a pharmacologically acceptable salt thereof, and further contains other components as necessary.

[0011] The inventor has found that the composition of Patent Document 1 can stably incorporate an emollient oil without greasiness, but has a problem of being inferior in the quickness of skin adaptation. On the other hand, the cosmetic according to one embodiment is non-greasy and excellent in the quickness of adaptation.

[0012] <(A) Polyoxyethylene hydrogenated castor oil> Polyoxyethylene hydrogenated castor oil (hereinafter sometimes referred to as “component (A)”) is a compound known as a hydrophilic nonionic surfactant, and a compound usually used in external skin preparations such as pharmaceuticals is incorporated.

[0013] The average added mole number of ethylene oxide in the polyoxyethylene chain in component (A) is not particularly limited and can be appropriately selected according to the purpose, but is preferably 20 moles to 100 moles, more preferably 40 moles to 100 moles, and still more preferably 40 moles to 80 moles. When the average added mole number of ethylene oxide in the polyoxyethylene chain in component (A) is 20 moles to 100 moles, the stability of the cosmetic is good.

[0014] As a specific example of component (A), PEG-60 hydrogenated castor oil having an average added mole number of ethylene oxide in the polyoxyethylene chain of about 60 moles is particularly preferable.

[0015] Component (A) may be appropriately synthesized by a known method or a commercially available product may be used. Examples of commercially available products of component (A) include NIKKOL HCO-60 (manufactured by Nikko Chemicals Co., Ltd.).

[0016] The content of component (A) in the cosmetic according to one embodiment is not particularly limited and can be appropriately selected according to the purpose, but is preferably 0.01% by mass to 5% by mass, more preferably 0.05% by mass to 1% by mass, and still more preferably 0.1% by mass to 0.5% by mass based on the total mass of the cosmetic.

[0017] <(B) Polyglycerin fatty acid ester> The polyglycerol fatty acid ester (hereinafter sometimes referred to as the “component (B)”) is an ester obtained from polyglycerol and a fatty acid.

[0018] The fatty acid in the component (B) is a branched or straight-chain saturated or unsaturated fatty acid, with a branched-chain saturated fatty acid being preferred.

[0019] The number of carbon atoms of the fatty acid in the component (B) is not particularly limited and can be appropriately selected according to the purpose, but 16 to 22 is preferred, and 18 to 22 is more preferred.

[0020] The average degree of polymerization of polyglycerol in the component (B) is not particularly limited and can be appropriately selected according to the purpose, but 5 or less is preferred, and 2 or less is more preferred. Here, the “average degree of polymerization” is the average of the number of glycerin bonds.

[0021] The number of added fatty acids in the component (B) is not particularly limited and can be appropriately selected according to the purpose, and can be mono-, di-, tri-, or more, but di- or more is preferred, and 2 to 5 is more preferred.

[0022] Specific examples of the component (B) include polyglyceryl monostearate, polyglyceryl monooleate, polyglyceryl dioleate, polyglyceryl monoisostearate, polyglyceryl diisostearate, polyglyceryl triisostearate, etc. These may be used alone or in combination of two or more. Among these, polyglyceryl diisostearate is preferred, and polyglyceryl diisostearate-2 is more preferred.

[0023] The HLB value of the component (B) is not particularly limited and can be appropriately selected according to the purpose, but 8 or less is preferred, and 5 or less is more preferred.

[0024] (B) component may be synthesized appropriately by a known method or a commercially available product may be used. Examples of the synthesis method of (B) component include, for example, a method of subjecting a fatty acid and polyglycerin to an esterification reaction in the presence of an alkali catalyst such as sodium hydroxide. The esterification can be carried out until the esterification rate of the polyglycerin fatty acid ester reaches a desired value.

[0025] Examples of commercially available products of (B) component include, for example, WOGEL-18DV (manufactured by Matsumoto Fine Chemical Co., Ltd.), EMALEX DISG-2, EMALEX DISG-2EX (both manufactured by Nippon Emulsion Co., Ltd.), Cosmol 42V (manufactured by Nisshin Oillio Group, Ltd.), and the like.

[0026] The content of (B) component in the cosmetic according to one embodiment is not particularly limited and can be appropriately selected according to the purpose. However, with respect to the total mass of the cosmetic, 0.01% by mass to 5% by mass is preferable, 0.05% by mass to 1% by mass is more preferable, and 0.1% by mass to 0.5% by mass is even more preferable.

[0027] <(C) oil component> The oil component (hereinafter sometimes referred to as “(C) component”) is not particularly limited and can be appropriately selected according to the purpose, but an ester oil is preferable.

[0028] There are no particular restrictions on the ester oil, and it can be appropriately selected according to the purpose. For example, glyceryl tri(2-ethylhexanoate) (glyceryl triisooctanoate), pentaerythritol tetra(2-ethylhexanoate) (pentaerythritol tetraoctanoate), glyceryl triisopalmitate, octyl isopalmitate, isopropyl isostearate, isostearyl isostearate, isocetyl isostearate, hexyl isostearate, myristyl isostearate, isocetyl octanoate, cetyl isooctanoate, isostearyl octanoate, isodecyl isononanoate, octyldodecyl dimethyloctanoate, oleyl myristate, isostearyl erucate, isocetyl stearate, octyl stearate, isostearyl palmitate, isocetyl palmitate, octyl palmitate, isostearyl myristate, isocetyl myristate, octyldodecyl myristate, decyl myristate, isopropyl palmitate, isopropyl myristate, trimethylolpropane triisostearate, neopentyl glycol dicaprate, dioctyl sebacate, octyldodecyl 12-stearoyloxystearate, dioctyldodecyl stearoylglutamate, dioctyl adipate, diisostearyl malate, octyl methoxycinnamate, octyldodecyl lactate, isostearyl lactate, octyl dimethylaminobenzoate, etc. can be mentioned. These may be used alone or in combination of two or more. Among these, as the component (C), an oil having an emollient action is preferable, and it is more preferable to contain at least one selected from the group consisting of glyceryl tri(2-ethylhexanoate) and pentaerythritol tetra(2-ethylhexanoate) in terms of improving the quickness of familiarity.

[0029] (C) component may be synthesized appropriately by a known method or a commercially available product may be used. Examples of commercially available products of the (C) component include NIKKOL TRIFAT S-308 (glyceryl tri(2-ethylhexanoate), manufactured by Nikko Chemicals Co., Ltd.), RA-PE-408 (pentaerythritol tetra(2-ethylhexanoate), manufactured by Nippon Fine Chemical Co., Ltd.), etc.

[0030] In the content of the component (C) in the cosmetic according to one embodiment, there is no particular limitation, and it can be appropriately selected according to the purpose. However, with respect to the total mass of the cosmetic, 1% by mass or less is preferable, 0.01% by mass to 0.1% by mass is more preferable, 0.1% by mass to 0.8% by mass is still more preferable, and 0.1% by mass to 0.5% by mass is particularly preferable.

[0031] <(D) Pyrimidylpyrazole compound represented by the general formula (1) or a pharmacologically acceptable salt thereof> The pyrimidylpyrazole compound represented by the general formula (1) or a pharmacologically acceptable salt thereof (hereinafter sometimes referred to as "component (D)") has very low cytotoxicity. Further, it can also act as a whitening agent.

[0032] In the general formula (1), R 1 , R 3 , R 4 , and R 6 each independently represents an alkyl group having 1 to 3 carbon atoms. In one embodiment, R 1 , R 3 , R 4 , and R 6 The "alkyl group having 1 to 3 carbon atoms" represented by is a linear, branched, or cyclic saturated hydrocarbon group having 1 to 3 carbon atoms. Further, in one embodiment, "each independently" means that R 1 , R 3 , R 4 , and R 6 may be different alkyl groups having 1 to 3 carbon atoms respectively, or may be the same alkyl group having 1 to 3 carbon atoms.

[0033] R 1 , R 3 , R 4 , and R 6 Examples of the alkyl group having 1 to 3 carbon atoms represented by include a methyl group, an ethyl group, an n-propyl group, an isopropyl group, a cyclopropyl group, and the like. Among these, R 1 , R 3 , R 4 , and R 6Examples of the alkyl group having 1 to 3 carbon atoms shown by include a methyl group and an ethyl group, with a methyl group being more preferred.

[0034] In general formula (1), R 2 and R 5 each independently represent a hydrogen atom or an alkyl group having 1 to 3 carbon atoms. In one embodiment, R 2 and R 5 The "alkyl group having 1 to 3 carbon atoms" shown by is a linear, branched, or cyclic saturated hydrocarbon group having 1 to 3 carbon atoms. Also, in one embodiment, "each independently" means that R 2 and R 5 may be different hydrogen atoms or alkyl groups having 1 to 3 carbon atoms, or may be the same hydrogen atom or alkyl group having 1 to 3 carbon atoms.

[0035] R 2 and R 5 Examples of the alkyl group having 1 to 3 carbon atoms shown by include a methyl group, an ethyl group, an n-propyl group, an isopropyl group, a cyclopropyl group, and the like. R 2 and R 5 are preferably hydrogen atoms.

[0036] Examples of the pharmacologically acceptable salts of the pyrimidylpyrazole compound represented by general formula (1) include inorganic acid salts such as hydrochloride, hydrobromide, sulfate, and phosphate; organic acid salts such as acetate, propionate, citrate, lactate, oxalate, maleate, fumarate, succinate, tartrate, and methanesulfonate.

[0037] The pyrimidylpyrazole compound represented by general formula (1) may be appropriately synthesized by a known method or a commercially available product may be used.

[0038] Typical synthesis examples of the pyrimidylpyrazole compounds represented by the general formula (1) will be described below, but are not limited thereto. As a synthesis example of the pyrimidylpyrazole compound represented by the general formula (1), a method of synthesizing by the reaction shown in the following Scheme 1 can be mentioned. The reaction shown in the following Scheme 1 can be carried out, for example, according to the methods described in JP-A-62-000404, Dharmpal S Dodd et al., Tetrahedron Letters, Volume 45, Issue 22, 2004, p.4265-4267, Gazzetta Chemica Italiana, Vol. 93, Parte I, 1963, p. 100, etc.

[0039] [Chemical formula]

[0040] In Scheme 1, the reaction between the hydrazine compound represented by the general formula (2) and the 1,3-dicarbonyl compound represented by the general formula (3a) or the 1-sulfonyl-3-carbonyl compound represented by the general formula (3b) can be carried out, for example, in a suitable solvent such as methanol, under an acid catalyst such as hydrochloric acid or acetic acid, and heating if necessary.

[0041] For the pharmacologically acceptable salts of the pyrimidylpyrazole compounds represented by the general formula (1), those appropriately synthesized by known methods may be used, or commercially available products may be used. As a synthesis example of the pharmacologically acceptable salts of the pyrimidylpyrazole compounds represented by the general formula (1), a method of converting the pyrimidylpyrazole compound represented by the general formula (1) into an acid addition salt appropriately selected from known methods can be mentioned. Examples of the acids used in the method of converting into an acid addition salt include inorganic acids such as hydrochloric acid, hydrobromic acid, sulfuric acid, and phosphoric acid; and organic acids such as acetic acid, propionic acid, citric acid, lactic acid, oxalic acid, maleic acid, fumaric acid, succinic acid, tartaric acid, and methanesulfonic acid.

[0042] As the starting material for Scheme 1, the hydrazine compound represented by the general formula (2) may be synthesized as appropriate by a known method or a commercially available product may be used. As an example of the synthesis of the hydrazine compound represented by the general formula (2), a method of synthesizing by the reaction shown in Scheme 2 below can be mentioned. The reaction shown in Scheme 2 below can be carried out, for example, according to the method described in JP-A-8-208620.

[0043] [Chemical formula]

[0044] In addition, the hydrazine compound represented by the general formula (2) used as the starting material for Scheme 1 can also be synthesized from the pyrimidine compound represented by the general formula (5) having a leaving group Z by the reaction shown in Scheme 3 below. Examples of the leaving group Z in the pyrimidine compound represented by the general formula (5) include halogen. The reaction shown in Scheme 3 below can be carried out, for example, according to the methods described in Takeo Naito et al., Chemical and Pharmaceutical Bulletin, 1969, Vol. 17, No. 7, pp. 1467-1478, Kaname Takagi et al., Chemical and Pharmaceutical Bulletin, 1963, Vol. 11, No. 11, pp. 1382-1388, Kenzo Shirakawa, Yakugaku Zasshi, 1953, Vol. 73, No. 6, pp. 635-639, etc.

[0045] [Chemical formula]

[0046] Regarding the other compounds used in the reactions of Schemes 1 to 3, those synthesized as appropriate by a known method may be used, or commercially available products may be used.

[0047] In the reactions of Schemes 1 to 3, when a functional group is present in the molecule and this functional group may interfere with the reaction or there is a risk of such interference, it is preferable to efficiently proceed the reaction using an appropriate protecting group. The use of the protecting group can be carried out, for example, according to the methods described in "GREENE'S PROTECTIVE GROUPS IN ORGANIC SYNTHESIS" by Theodora W. Greene, Peter G. M. Wuts, etc.

[0048] In addition, in the reactions of Schemes 1 to 3, when isomers such as conformational isomers, geometric isomers, and optical isomers exist, by appropriately selecting and separating the raw materials and reaction conditions, they can be obtained as pure isomers or geometric isomers. The pyrimidylpyrazole compound represented by the general formula (1) or a pharmacologically acceptable salt thereof includes pure isomers or a mixture thereof.

[0049] As the pyrimidylpyrazole compound represented by the general formula (1) or a pharmacologically acceptable salt thereof, R 1 , R 3 , R 4 , and R 6 are methyl groups, and R 2 and R 5 are hydrogen atoms, and 2-(3,5-dimethylpyrazol-1-yl)-4,6-dimethylpyrimidine hydrochloride (also referred to as "dimethylpyrazolyl dimethylpyrimidine hydrochloride") is particularly preferred.

[0050] In the cosmetic according to one embodiment, the content of component (D) is not particularly limited and can be appropriately selected according to the purpose. However, based on the total mass of the cosmetic, 0.1% by mass to 1.5% by mass is preferable, 0.1% by mass to 1% by mass is more preferable, and from the perspective of a moist feeling, 0.5% by mass to 1% by mass is even more preferable. When the content of component (D) is 0.1% by mass or more, stickiness and the speed of skin adaptation can be preferably improved. Also, even if the content of component (D) is excessively blended, a remarkable effect commensurate with the increase in amount may not be obtained, and it may affect formulation design and usability, etc. Therefore, it is preferably 1.5% by mass or less.

[0051] <Other components> The cosmetic according to one embodiment may contain components other than component (A), component (B), component (C), and component (D). The other components are not particularly limited and can be appropriately selected from known components used in cosmetics. For example, glycols, glycerins, sugar alcohols, saccharides, powders, pigments, dyes, polymers, solvents, pH adjusters, surfactants other than component (A) and component (B), oils other than component (C), fragrances, drugs other than component (D), etc. can be mentioned. These may be used alone or in combination of two or more.

[0052] In the cosmetic according to one embodiment, the content of the other components is not particularly limited as long as the effects of the cosmetic are not impaired, and can be appropriately selected according to the purpose.

[0053] <<Glycols>> Examples of glycols include propylene glycol, dipropylene glycol, 1,3 - butylene glycol, 1,4 - butylene glycol, diethylene glycol, triethylene glycol, polyethylene glycol, etc.

[0054] <<Glycerins>> Examples of glycerins include glycerin, diglycerin, polyglycerin, etc.

[0055] <<Sugar alcohols>> Examples of sugar alcohols include sorbitol, mannitol, maltitol, xylitol, and erythritol.

[0056] <<Sugars>> Examples of sugars include fructose, glucose, galactose, maltose, lactose, and trehalose.

[0057] <<Powder>> The powder may be an inorganic powder or an organic powder.

[0058] Examples of inorganic powders include mica, talc, kaolin, sericite (sericite), muscovite, phlogopite, synthetic mica, red mica, biotite, lithia mica, synthetic mica, anhydrous silicic acid (silica), aluminum silicate, barium silicate, calcium silicate, magnesium silicate, strontium silicate, aluminum oxide, barium sulfate, zeolite, titanium oxide, zinc oxide, and boron nitride.

[0059] Examples of organic powders include polyamide resin powder (nylon powder), polyethylene powder, polymethyl methacrylate powder, polystyrene powder, calcium carbonate powder, magnesium carbonate powder, styrene-acrylic acid copolymer resin powder, and cellulose powder.

[0060] <<Pigments>> Examples of pigments include inorganic pigments, organic pigments, pearl pigments, and metal powder pigments.

[0061] Examples of inorganic pigments include inorganic white pigments such as titanium dioxide and zinc oxide; inorganic red pigments such as iron oxide (red iron oxide); inorganic yellow pigments such as yellow iron oxide and yellow ocher; black pigments such as black iron oxide and carbon black; inorganic green pigments such as chromium oxide, chromium hydroxide, and cobalt titanate; and inorganic blue pigments such as ultramarine and Prussian blue.

[0062] Examples of organic pigments include Pigment Red 3, Pigment Red 104, Pigment Red 106, Pigment Red 201, Pigment Red 202, Pigment Red 204, Pigment Red 205, Pigment Red 220, Pigment Red 226, Pigment Red 227, Pigment Red 228, Pigment Red 230, Pigment Red 401, Pigment Red 405, Pigment Red 505, Pigment Orange 203, Pigment Orange 204, Pigment Orange 205, Pigment Yellow 4, Pigment Yellow 5, Pigment Yellow 202, Pigment Yellow 203, Pigment Yellow 205, Pigment Yellow 401, Pigment Blue 1, Pigment Blue 404, Pigment Green 3, and their zirconium lakes, barium lakes, or aluminum lakes, etc.

[0063] Examples of pearl pigments include titanium oxide-coated mica, colored titanium oxide-coated mica, bismuth oxychloride, fish scale foil, etc.

[0064] Examples of metal powder pigments include aluminum powder, copper powder, etc.

[0065] <<Dye>> Examples of dyes include natural dyes such as chlorophyll, β-carotene, etc.

[0066] <<Polymers>> Examples of polymers include plant-based polymers, animal-based polymers, microbial-based polymers, starch-based polymers, cellulose-based polymers, alginic acid-based polymers, vinyl-based polymers, acrylic-based polymers, inorganic water-soluble polymers, etc. These polymers may act as thickeners.

[0067] Examples of plant-based polymers include gum arabic, tragacanth gum, galactan, guar gum, carob gum, karaya gum, gellan gum, carrageenan, pectin, agar, etc.

[0068] Examples of animal-based polymers include collagen, casein, albumin, gelatin, etc.

[0069] Examples of microbial polymers include xanthan gum, dextran, succinoglucan, pullulan, etc.

[0070] Examples of starch polymers include vegetable starches such as corn, wheat, potato, and rice; carboxymethyl starch; methylhydroxypropyl starch, etc.

[0071] Examples of cellulose polymers include methyl cellulose, nitrocellulose, ethyl cellulose, methylhydroxypropyl cellulose, hydroxyethyl cellulose, sodium cellulose sulfate, hydroxypropyl cellulose, sodium carboxymethyl cellulose, crystalline cellulose, etc.

[0072] Examples of alginate polymers include sodium alginate, propylene glycol alginate, etc.

[0073] Examples of vinyl polymers include polyvinyl alcohol, polyvinyl acetate, polyvinyl methyl ether, polyvinyl pyrrolidone, copolymers of vinyl pyrrolidone and vinyl acetate, carboxyvinyl polymer, etc.

[0074] Examples of acrylic polymers include sodium polyacrylate, polyethyl acrylate, alkanolamine polyacrylate, copolymers of alkyl methacrylate and dimethylaminoethyl methacrylate, poly2 - acrylamido - 2 - methylpropanesulfonic acid, polymethacryloyloxytrimethylammonium, etc.

[0075] Examples of inorganic water - soluble polymers include polyethyleneimine, cationic polymer, bentonite, magnesium aluminum silicate, laponite, hectorite, silicic anhydride, etc.

[0076] <<Solvent>> Examples of the solvent include water, lower alcohols, etc. Examples of the lower alcohol include alcohols having 5 or less carbon atoms. Specific examples of the lower alcohol include methanol, ethanol, propyl alcohol, isopropyl alcohol, 2-amino-2-methyl-1-propanol, 2-amino-2-methyl-1,3-propanediol, etc.

[0077] <<pH adjuster>> Examples of the pH adjuster include potassium hydroxide, sodium hydroxide, triethanolamine, sodium carbonate, lactic acid, citric acid, sodium citrate, glycolic acid, succinic acid, tartaric acid, malic acid, sodium hydrogen carbonate, ammonium hydrogen carbonate, etc.

[0078] <<Surfactant other than component (A) and component (B)>> Examples of the surfactant other than component (A) and component (B) include anionic surfactants, cationic surfactants, nonionic surfactants, amphoteric surfactants, etc.

[0079] <<Oil component other than component (C)>> Examples of the oil component other than component (C) include fats and oils, waxes, hydrocarbon oils, higher fatty acids, higher alcohols, silicone oils, oil-soluble drugs, etc. These may be used alone or in combination of two or more.

[0080] <<Drug other than component (D)>> Examples of the drug other than component (D) include salt-type drugs, vitamins, ultraviolet absorbers, chelating agents, preservatives, plant extracts, moisturizing agents, anti-inflammatory agents, whitening agents, cooling agents, amino acids, antioxidants, bactericides, etc.

[0081] - Salt-type drug - The salt-type drug means a water-soluble drug capable of forming a salt. The salt-type drug is not particularly limited as long as it is a water-soluble drug that can be usually formulated in cosmetics, and can be appropriately selected according to the purpose. For example, salts of L-ascorbic acid or its derivatives, salts of tranexamic acid or its derivatives, salts of alkoxysalicylic acid or its derivatives, salts of glutathione or its derivatives, etc. can be mentioned.

[0082] L-ascorbic acid is generally called vitamin C, has cell respiration, enzyme activation, and collagen formation effects due to its strong reducing action, and also has a melanin reduction effect. Examples of L-ascorbic acid derivatives include L-ascorbic acid monoesters such as L-ascorbic acid monophosphate ester and L-ascorbic acid-2-sulfate ester; L-ascorbic acid triesters such as L-ascorbic acid triphosphate ester; L-ascorbic acid glucosides such as L-ascorbic acid 2-glucoside, etc.

[0083] Examples of tranexamic acid derivatives include dimers of tranexamic acid such as trans-4-(trans-aminomethylcyclohexanecarbonyl)aminomethylcyclohexanecarboxylic acid hydrochloride; ester forms of tranexamic acid and hydroquinone such as 4-(trans-aminomethylcyclohexanecarboxylic acid 4'-hydroxyphenyl ester; ester forms of tranexamic acid and gentisic acid such as 2-(trans-4-aminomethylcyclohexylcarbonyloxy)-5-hydroxybenzoic acid; amide forms of tranexamic acid such as trans-4-aminomethylcyclohexanecarboxylic acid methylamide, trans-4-(p-methoxybenzoyl)aminomethylcyclohexanecarboxylic acid, trans-4-guanidinomethylcyclohexanecarboxylic acid, etc.

[0084] As the alkoxysalicylic acid, for example, those in which the hydrogen atom at the 3-position, 4-position, or 5-position of salicylic acid is substituted with an alkoxy group. The alkoxy group as the substituent is preferably any one of a methoxy group, an ethoxy group, a propoxy group, an isopropoxy group, a butoxy group, and an isobutoxy group, and more preferably a methoxy group or an ethoxy group. Specific examples of the alkoxysalicylic acid include 3-methoxysalicylic acid, 3-ethoxysalicylic acid, 4-methoxysalicylic acid, 4-ethoxysalicylic acid, 4-propoxysalicylic acid, 4-isopropoxysalicylic acid, 4-butoxysalicylic acid, 5-methoxysalicylic acid, 5-ethoxysalicylic acid, 5-propoxysalicylic acid, and the like.

[0085] There is no particular limitation on the salt of the drug, and examples thereof include alkali metal salts or alkaline earth metal salts such as sodium salt, potassium salt, and calcium salt; ammonium salts; amino acid salts, and the like.

[0086] -Vitamins- Examples of the vitamins include water-soluble vitamins such as vitamin B6 hydrochloride, pantothenyl ethyl ether, pyridoxine hydrochloride, nicotinamide, pantothenic acid, and biotin.

[0087] -UV Absorbents- Examples of the UV absorbents include benzoic acid-based UV absorbents such as para-aminobenzoic acid; anthranilic acid-based UV absorbents such as methyl anthranilate; salicylic acid-based UV absorbents such as octyl salicylate; cinnamic acid-based UV absorbents such as isopropyl paramethoxycinnamate and octyl paramethoxycinnamate; UV absorbents such as urocanic acid and ethyl urocanate; benzophenone-based UV absorbents such as 2-hydroxy-4-methoxybenzophenone and dihydroxybenzophenone; benzotriazole-based UV absorbents; 2-phenylbenzimidazole-5-sulfonic acid, and the like.

[0088] -Chelating Agents- Examples of chelating agents include citramalic acid, agaric acid, glyceric acid, shikimic acid, hinokitiol, gallic acid, tannic acid, caffeic acid, trisodium ethylenediamine-N,N,N',N'-tetraacetate dihydrate (EDTA-2Na), ethylenediamine tetraacetic acid, diethylenetriamine pentaacetic acid, phytic acid, polyphosphoric acid, metaphosphoric acid, their analogs, their alkali metal salts, their carboxylic acid esters, and the like.

[0089] -Preservative- Examples of preservatives include benzoic acid, salicylic acid, paraoxybenzoic acid esters (such as methylparaben, ethylparaben, butylparaben, etc.), sorbic acid, parachlorometacresol, hexachlorophene, benzalkonium chloride, chlorhexidine chloride, trichlorocarbanilide, photosensitizer, phenoxyethanol, and the like.

[0090] -Plant extract- Examples of plant extracts include Saururus chinensis extract, Phellodendron amurense extract, Glycyrrhiza glabra extract, Paeonia lactiflora extract, Portulaca oleracea extract, Luffa cylindrica extract, Saxifraga stolonifera extract, Eucalyptus globulus extract, Cinnamomum camphora extract, Malus pumila extract, Hieracium umbellatum extract, seaweed extract, Thymus vulgaris extract, and the like.

[0091] -Humectant- Examples of humectants include polyethylene glycol (hereinafter referred to as PEG), sodium chondroitin sulfate, sodium hyaluronate, sodium lactate, glucosamine, cyclodextrin, polyoxyethylene methyl glucoside (methyl gluceth-10), and the like. Further, the glycols, the glycerins, the sugar alcohols, and the saccharides can also be used as humectants.

[0092] -Anti-inflammatory agent- Examples of anti-inflammatory agents include azulene, glycyrrhizin, lysozyme chloride, pyridoxine hydrochloride, sulfur, and the like.

[0093] -Whitening agent- Examples of the whitening agent include arbutin, 4-methoxysalicylic acid, potassium 4-methoxysalicylate, tranexamic acid, ethyl vitamin C, magnesium ascorbyl phosphate, and the like. Further, the salt-type drug can also be used as a whitening agent.

[0094] -Cooling agent- Examples of the cooling agent include L-menthol, camphor, and the like.

[0095] -Antioxidant- Examples of the antioxidant include ascorbic acid, α-tocopherol, carotenoid, and the like.

[0096] <Dosage form> The dosage form of the cosmetic according to one embodiment is not particularly limited and can be appropriately selected according to the purpose. However, it is preferably a liquid cosmetic, more preferably a liquid emulsion cosmetic, and still more preferably an oil-in-water emulsion cosmetic.

[0097] The product form of the cosmetic according to one embodiment is not particularly limited and can be appropriately selected according to the purpose. For example, cosmetics for skin care such as lotion, cream, emulsion, essence, etc.; makeup cosmetics such as foundation, makeup base, etc.; sunscreen cosmetics; self-tanning cosmetics; skin cleansing cosmetics such as facial wash, makeup remover, etc.; ointment, etc. can be mentioned. Further, the product form of the cosmetic according to one embodiment may be a form impregnated in a base material such as a pack. Among these, as the product form of the cosmetic according to one embodiment, since it is not sticky, has excellent familiarity with the skin, and further has a moist feeling due to the component (C), it is preferably used as a lotion.

[0098] <Manufacturing method> The manufacturing method of the cosmetic according to one embodiment is not particularly limited, and preferably, it can be manufactured according to a method commonly used for liquid cosmetics, more preferably for oil-in-water emulsion cosmetics. For example, a method of mixing an aqueous component and an oily component and emulsifying them can be mentioned.

[0099] There are no particular restrictions on the emulsification method, and known methods can be used. For example, mechanical emulsification methods using high-pressure emulsifiers such as high-pressure homogenizers, high-shear dispersers, colloid mills, etc.; phase inversion emulsification methods; aggregation methods; liquid crystal emulsification methods; D-phase emulsification methods, etc. These methods can be used alone or in combination.

[0100] There are no particular restrictions on the emulsified particle size of the fine emulsion obtained by emulsification, and it can be appropriately selected according to the purpose. However, 0.01 μm to 1.0 μm is preferable, 0.01 μm to 0.5 μm is more preferable, and 0.01 μm to 0.1 μm is even more preferable.

Examples

[0101] Examples and comparative examples are given below to more specifically explain the embodiments, but the embodiments are not limited by these examples and comparative examples. In the examples and comparative examples, unless otherwise specified, the content of each component shown in Table 1 below indicates "mass%" based on the total mass of the cosmetic, and all values are in terms of pure components.

[0102] (Examples 1 to 4, and Comparative Examples 1 and 2) An oil-in-water emulsified cosmetic (lotion) having the composition and content (mass%) shown in Table 1 below was prepared by a conventional method. Since component (D) can also be used as a whitening agent, in Comparative Example 2, "potassium 4-methoxysalicylate" was used as the comparative component of component (D).

[0103] <Evaluation> For each of the prepared oil-in-water emulsified cosmetics of Examples 1 to 4 and Comparative Examples 1 and 2, "stickiness" and "quick adaptability" were evaluated by the following methods. The evaluation results are shown in Table 1 below.

[0104] <<Evaluation of stickiness>> The stickiness of each water-in-oil type emulsified cosmetic of Examples 1 to 4 and Comparative Examples 1 and 2 was evaluated by the following method. Ten professional evaluators applied the water-in-oil type emulsified cosmetics of Examples 1 to 4 and Comparative Examples 1 and 2 to their skin respectively, and then checked the stickiness of the skin. They evaluated based on the following evaluation criteria. [Evaluation Criteria for Stickiness] A (Very Good): 8 or more out of 10 responders answered that there was no stickiness. B (Good): 5 to 7 out of 10 responders answered that there was no stickiness. C (Somewhat Good): 3 to 4 out of 10 responders answered that there was no stickiness. D (Poor): 2 or less out of 10 responders answered that there was no stickiness.

[0105] [[Evaluation of Quick Adaptability]] The quick adaptability of each water-in-oil type emulsified cosmetic of Examples 1 to 4 and Comparative Examples 1 and 2 was evaluated by the following method. Ten professional evaluators applied the water-in-oil type emulsified cosmetics of Examples 1 to 4 and Comparative Examples 1 and 2 to their skin respectively, and then checked the quick adaptability of the skin when applying. They evaluated based on the following evaluation criteria. [Evaluation Criteria for Quick Adaptability] A (Very Good): 8 or more out of 10 responders answered that the adaptability was quick. B (Good): 5 to 7 out of 10 responders answered that the adaptability was quick. C (Somewhat Good): 3 to 4 out of 10 responders answered that the adaptability was quick. D (Poor): 2 or less out of 10 responders answered that the adaptability was quick.

[0106] [Table 1]

[0107] In addition, each component used in the examples and comparative examples is as follows.

[0108] · PEG-60 Hydrogenated Castor Oil: Trade name "NIKKOL HCO-60" (manufactured by Nikko Chemicals Co., Ltd.) · Polyglyceryl-2 diisostearate: Trade name "WOGEL-18DV" (manufactured by Matsumoto Fine Chemical Co., Ltd.) · Glyceryl tri(2-ethylhexanoate): Trade name "NIKKOL TRIFAT S-308" (manufactured by Nikko Chemicals Co., Ltd.) · Pentaerythritol tetra(2-ethylhexanoate): Trade name "RA-PE-408" (manufactured by Nippon Fine Chemical Co., Ltd.) · 2-(3,5-Dimethylpyrazol-1-yl)-4,6-dimethylpyrimidine hydrochloride: A compound represented by the following structural formula (1) and produced by the method described in Patent No. 4586108.

[0109]

Chemical formula

[0110] Examples of the embodiments of the present invention include, for example, the following. <1> (A) Polyoxyethylene hydrogenated castor oil, and (B) Polyglycerin fatty acid ester, and (C) Oil component, and (D) A pyrimidylpyrazole compound represented by the following general formula (1) or a pharmacologically acceptable salt thereof, and

[0111]

Chemical formula

[0112] As described above, the present invention has been described based on specific embodiments and examples. However, these embodiments and examples are merely presented as examples, and the present invention is not limited by the above embodiments and examples. The above embodiments can be implemented in various other forms, and various combinations, omissions, replacements, additions, changes, etc. can be made without departing from the gist of the invention. These embodiments and their modifications are included in the scope and gist of the invention, and are also included in the invention described in the claims and the equivalent scope thereof.

Claims

1. (A) Polyoxyethylene hydrogenated castor oil, and (B) polyglyceryl fatty acid ester, and (C) an oil component, and (D) a pyrimidylpyrazole compound represented by the following general formula (1) or a pharmacologically acceptable salt thereof, 【Chemical 1】 (In the general formula (1), R １ , R ３ , R ４ , and R ６ each independently represent an alkyl group having 1 to 3 carbon atoms, and R ２ and R ５ each independently represent a hydrogen atom or an alkyl group having 1 to 3 carbon atoms.) A cosmetic characterized by containing the same.

2. R in the above-mentioned (D) pyrimidylpyrazole compound represented by the general formula (1) or a pharmacologically acceptable salt thereof ２ and R ５ The cosmetic according to claim 1, wherein is a hydrogen atom.

3. R in the above-mentioned (D) pyrimidylpyrazole compound represented by the general formula (1) or a pharmacologically acceptable salt thereof １ , R ３ , R ４ , and R ６ is a methyl group, the cosmetic according to claim 1 or 2.

4. The cosmetic according to claim 1, wherein the content of the pyrimidylpyrazole compound represented by the general formula (1) or a pharmacologically acceptable salt thereof in (D) is 0.1% by mass to 1% by mass.

5. The cosmetic according to claim 1, wherein the oil component in (C) is an ester oil.

6. The cosmetic according to claim 5, wherein the ester oil contains at least one selected from the group consisting of glyceryl tri(2-ethylhexanoate) and pentaerythrityl tetra(2-ethylhexanoate).

7. The cosmetic according to claim 1, wherein the content of the oil component in (C) is 1% by mass or less.

8. The cosmetic according to claim 1, which is used for lotion.

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