External composition for skin
A cosmetic composition with nicotinamide, preservatives, and organic acids prevents precipitation, stabilizing the mixture and enhancing skin benefits like whitening and anti-aging.
Patent Information
- Application Number
- JP2025175326
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2019-07-26
- Filing Date
- 2025-10-17
- Publication Date
- 2026-01-21
AI Technical Summary
Cosmetic compositions containing preservatives and organic acids or amphiphilic components often experience precipitation issues.
A composition containing nicotinamide, preservatives, and compounds such as organic acids or amphiphilic compounds is formulated to inhibit precipitation, using specific ratios and combinations of ingredients like tranexamic acid, lactic acid, citric acid, and nicotinamide to stabilize the mixture.
The composition effectively prevents precipitation, ensuring stability and efficacy of the cosmetic formulation while maintaining desired skin benefits like whitening and anti-aging.
Smart Images

Figure 2026010127000001 
Figure 2026010127000002 
Figure 2026010127000003
Abstract
Description
[Technical Field]
[0001] The present invention relates to a composition for external use on the skin. More specifically, the present invention relates to a composition containing nicotinamide. The present invention relates to a composition for external use on the skin. [Background technology]
[0002] Nicotinamide is a vitamin that has been used in the skin care field for a long time. It is an ingredient used to promote circulation, anti-inflammatory, and promote ceramide synthesis, and is also effective in improving beauty. It is also known to have whitening, anti-wrinkle and anti-aging effects.
[0003] For example, Patent Document 1 discloses that riboflavin, pyridoxine hydrochloride, nicotinamide and papain are A whitening agent containing one or more active ingredients selected from the group consisting of calcium anthrate and calcium benzoate is proposed. It is being done.
[0004] In addition, Patent Document 2 discloses a method for producing a compound containing (a) nicotinic acid amide and (b) urea and a compound having 2 to 28 carbon atoms. It is characterized by containing one or more selected from the group consisting of α-hydroxycarboxylic acid compounds. Cosmetics that have the following characteristics have been proposed: anti-aging skin products. [Prior art documents] [Patent documents]
[0005] [Patent Document 1] Japanese Patent Application Laid-Open No. 2004-217629 [Patent Document 2] Japanese Patent Application Publication No. 10-130135 Summary of the Invention [Problem to be solved by the invention]
[0006] Cosmetics and the like generally contain preservatives together with active ingredients and the like. When organic acids or amphiphilic ingredients are added to preservatives, precipitation that does not occur with either ingredient alone occurs. However, a new problem was discovered:
[0007] The present invention is capable of suppressing precipitation even in a composition containing a preservative and an organic acid or an amphiphilic component. The object of the present invention is to provide a composition for external use on the skin. [Means for solving the problem]
[0008] As a result of extensive research to solve the above problems, the present inventors have found that a preservative and an organic acid or both are combined. The precipitation caused by the combination of solvent components is suppressed by adding nicotinamide. The present invention has been completed based on the findings that the above-mentioned invention can be controlled.
[0009] That is, the present invention provides the following external skin compositions. Section 1. (A) nicotinamide 3% by mass or more; (B) preservatives; and (C) a compound selected from the group consisting of organic acids, organic acid salts, derivatives of organic acids, and amphiphilic compounds; A composition for external use on the skin containing at least one of the following: Section 2. The component (C) is Tranexamic acid or its salt, lactic acid or its salt, citric acid or its salt, succinic acid or its salt salts, salicylic acid or its salts, gluconic acid or its salts, phytic acid or its salts, tartaric acid or Its salts, sodium ascorbyl phosphate, magnesium ascorbyl phosphate Nesium, 2-O-ethyl ascorbic acid, 3-O-ethyl ascorbic acid, and ascorbic acid Item 1, wherein the compound is at least one selected from the group consisting of benzoyl benzoate-2-glucoside. A composition for topical application to the skin. Section 3. The component (C) is a compound represented by the following general formula (I), a phosphorylcholine-containing polymer , dicarboxylic acid esters, and alkanediols having 5 to 10 carbon atoms. Item 3. The composition for external use on skin according to Item 1 or 2, wherein the composition is one or more of the following: [ka] (In the formula, Z is a hydrogen atom or a hydroxy compound having 1 to 30 carbon atoms, and n hydroxy groups are selected from the group consisting of means the residue obtained by removing; AO means an oxyalkylene group having 3 to 4 carbon atoms; EO means an oxyethylene group; BO means an oxyalkylene group having 4 carbon atoms; n means 1 to 9; a, b, and c represent the average number of moles of AO, EO, and BO added, respectively, and are independently 0 to 100. The value is 200. However, a, b, and c cannot all be 0. Also, when n is 2 or more, Multiple a's, b's, and c's may be the same or different. When Z is a hydrogen atom, n is 1. be. In addition, AO and EO may be added randomly or in the form of blocks. Section 4. The component (C) is a compound represented by the following general formula (II), 2-methacryloyloxy Ethylphosphorylcholine-Butyl Methacrylate Copolymer, (Eicosanedioic Acid / Tetradeca Decaglyceryl cyclohexanedicarboxylate, bisethoxydiglycol cyclohexanedicarboxylate, succinic acid Diethylhexyl succinate, diethoxyethyl succinate, and dialkanediol having 5 to 10 carbon atoms Item 3. The compound according to any one of items 1 to 3, wherein the compound is one or more selected from the group consisting of ols. Compositions for topical use on the skin: [ka] (In the formula, Z is a hydrogen atom or a hydroxy compound having 1 to 30 carbon atoms, and n hydroxy groups are selected from the group consisting of means the residue obtained by removing; AO means an oxyalkylene group having 3 to 4 carbon atoms; EO means an oxyethylene group; n means 1 to 9; a and b respectively represent the average number of moles of AO and EO added, and are independently 0 to 200. However, a and b cannot all be 0. Also, when n is 2 or more, multiple a and b They may be the same or different. When Z is a hydrogen atom, n is 1. In addition, AO and EO may be added randomly or in the form of blocks. Section 5. In the general formulas (I) and (II), Z is a hydrogen atom or a group having a carbon number of 4-24 alkyl monoalcohol, glycerin, trimethylolpropane, erythritol Pentaerythritol, alkyl glucoside with 1 to 24 carbon atoms, diglycerin, Citrate, dipentaerythritol, sorbitol, inositol, sucrose, threitol Obtained by removing n hydroxy groups from halo or maltitol Item 5. The composition for external application to skin according to Item 3 or 4, wherein the composition is a residue. Section 6. In the general formulas (I) and (II), Z is a hydrogen atom or a group having a carbon number of 4-24 alkyl monoalcohol, glycerin, alkyl glucoside with 1-24 carbon atoms or a residue obtained by removing n hydroxy groups from diglycerol. Item 5. The composition for external application to skin according to Item 3 or 4. Section 7. The component (B) is a parahydroxybenzoic acid ester, benzoic acid, a benzoate, or a dehydroacetic acid. Acid, dehydroacetate, thymol, isopropylmethylphenol, caprylhydroxam Acid, iodopropynyl butylcarbamate, salts of iodopropynyl butylcarbamate, Butylcarbamic acid iodide propynyl derivatives, sorbic acid, sorbates, chlorobutanoates Item 1 is at least one selected from the group consisting of methylisothiazoline and methylisothiazoline. 7. A composition for external use on skin according to any one of claims 1 to 6. Section 8. Item 8. The composition for external use on skin according to any one of items 1 to 7, further comprising an ultraviolet absorber. Section 9. Item 9. The composition for external use on skin according to Item 8, wherein the total content of the ultraviolet absorbers is 20% by mass or less. Section 10. Item 10. The composition for external use on skin according to any one of items 1 to 9, further comprising an ultraviolet protection agent. Section 11. The ultraviolet absorber is a salicylic acid-based ultraviolet absorber, a cinnamic acid-based ultraviolet absorber, a benzoyl Methane-based UV absorbers, benzoate derivative UV absorbers, triazine derivative UV absorbers Absorbents, benzalmalonate derivative UV absorbers, octocrylene UV absorbers, imipenem UV absorbers consisting of dazole sulfonic acid derivatives and benzophenone derivatives Item 11. The composition for external application to skin according to any one of items 1 to 10, wherein the composition is one or more selected from the group consisting of: Section 12. The ultraviolet absorber is 2-ethylhexyl, 4-tert-butyl paramethoxycinnamate. -4'-Methoxydibenzoylmethane, 2-[4-(diethylamino)-2-hydroxy Benzoyl]benzoic acid hexyl ester, 2,4-bis-[{4-(2-ethylhexyl Oxy)-2-hydroxy}-phenyl]-6-(4-methoxyphenyl)-1,3,5 -triazine, 2,4,6-tris[4-(2-ethylhexyloxycarbonyl)aniline 2-phenylbenzimidazole-5-sulfonic acid Item 12. The composition for external use on the skin according to any one of items 1 to 11, wherein the composition is one or more selected from the group consisting of: thing. Section 13. Item 13. The composition according to any one of items 1 to 12, further comprising 0.001 to 10% by mass of a whitening component. A composition for topical application to the skin. Section 14. Item 14. The composition according to any one of items 1 to 13, further comprising 0.001 to 5% by mass of an anti-inflammatory component. A composition for topical application to the skin. Section 15. Item 15. The composition for external use on skin according to any one of Items 1 to 14, further comprising an acidic mucopolysaccharide. . Section 16. Furthermore, one or more selected from the group consisting of oils, surfactants, and thickeners Item 16. The composition for external application to skin according to any one of items 1 to 15, comprising: [Effects of the Invention]
[0010] According to the present invention, it is possible to provide a composition for external use on skin in which deposition is inhibited. DETAILED DESCRIPTION OF THE INVENTION
[0011] In this specification, the unit of content "% by mass" is synonymous with "g / 100g".
[0012] The composition for external use on skin of the present invention comprises: (A) Nicotinamide; (B) preservatives; and (C) a compound selected from the group consisting of organic acids, organic acid salts, derivatives of organic acids, and amphiphilic compounds; and at least one of the above-mentioned compounds.
[0013] [(A) Nicotinamide] The nicotinamide contained in the topical skin composition of the present invention is a compound containing nicotinic acid (vitamin B3 / Nicotinamide is a water-soluble vitamin and is an amide compound of niacin. It may be an extract from a substance, or may be a substance synthesized by a known method. , and those listed in the 17th edition of the Japanese Pharmacopoeia can be used. In addition to improving rough skin, it is known to inhibit melanin production and have whitening effects.
[0014] In the composition for external use on skin of the present invention, the content of component (A) in the total amount of the composition is The content of component (A) is set appropriately based on the balance with the total amount of the composition. From the viewpoint of providing sufficient effectiveness in whitening, anti-aging, etc., it is preferable to use an amount of 3% by mass or more. More preferably, it is 4% by mass or more, and even more preferably, it is 5% by mass or more. The content of component (A) is preferably 20 mass % based on the total amount of the composition. % by mass or less, more preferably 15% by mass or less, even more preferably 10% by mass or less, particularly The content of the component (A) is preferably 8% by mass or less relative to the total amount of the composition. Preferably, 3% by mass to 20% by mass, more preferably, 3% by mass to 15% by mass, and even more preferably is 3% by mass to 10% by mass, and even more preferably 4% by mass to 8% by mass.
[0015] [(B) Preservatives] The preservative contained in the external skin composition of the present invention is used in the fields of pharmaceuticals, quasi-drugs, and cosmetics. It is a compound that is commonly used as an ingredient in external skin preparations and is solid at room temperature (20°C). It is a water-soluble preservative that can be dissolved in water. The "preservative" is any preservative that can be dissolved in water even slightly. For example, a percentage of 0.01% or more The composition for external application to the skin of the present invention is preferably soluble in water at a concentration of 0.05% or more. Examples of preservatives included in this product include methyl parahydroxybenzoate and ethyl parahydroxybenzoate. propyl parahydroxybenzoate, butyl parahydroxybenzoate, and other parahydroxybenzoates esters (parabens); benzoic acid or benzoates such as sodium benzoate; dehydroacetic acid or dehydroacetates such as sodium dehydroacetate; methylphenol, caprylhydroxamic acid, iodide propynyl butylcarbamate, or salts or derivatives of butylcarbamic acid iodopropynyl; sorbic acid or sorbic acid Examples include potassium sorbate, chlorobutanol, and methylisothiazoline. .
[0016] Here, the salt of component (B) of the present invention may be an alkali metal salt such as sodium or potassium. The component (B) of the present invention may be any one of these compounds alone or two or more of them. The above can be used in combination, but among them, parahydroxybenzoic acid ester, benzoic acid , Benzoate, Dehydroacetic Acid, Dehydroacetate, Isopropylmethylphenol, Caprylic / Capric Triglyceride Hydroxamic acid, butylcarbamic acid iodide propynyl, butylcarbamic acid iodide propynyl Salts or derivatives of ropinil, sorbic acid, sorbates, chlorobutanol, and methylisothiazolinone Preferably, one or more selected from the group consisting of methyl parahydroxybenzoate, Ethyl parahydroxybenzoate, Propyl parahydroxybenzoate, Benzoic acid, Sodium benzoate Isopropylmethylphenol, Caprylhydroxamic acid, Iodobutylcarbamate Propylene chloride, sorbic acid, sodium sorbate, potassium sorbate, and chloropropane. More preferably, the compound is at least one selected from the group consisting of methyl parahydroxybenzoate, Ethyl parahydroxybenzoate, Propyl parahydroxybenzoate, Benzoic acid, Sodium benzoate Isopropylmethylphenol, Caprylhydroxamic acid, Iodobutylcarbamate from the group consisting of propynyl nitrite, sorbic acid, potassium sorbate, and chlorobutanol More preferably, one or more selected from the above are selected from methyl parahydroxybenzoate, ethyl parahydroxybenzoate, propyl parahydroxybenzoate, benzoic acid, caprylhydroxamic acid, butylcarbamate One or more selected from the group consisting of propynyl phosphate, sorbic acid, and chlorobutanol are even more preferred, and methyl parahydroxybenzoate, ethyl parahydroxybenzoate, benzoic acid and sorbic acid are particularly preferred.
[0017] These can be synthesized, or commercially available products can be used as they are. The component (B) is a commercially available product, but is not particularly limited thereto. For example, in addition to commercially available reagents, Kins M, Ethyl parahydroxybenzoate, Mekkins P, Butyl parahydroxybenzoate (para hydroxybenzoic acid esters) (both manufactured by Ueno Pharmaceutical Co., Ltd.), methyl parahydroxybenzoate, para Ethyl hydroxybenzoate, propyl parahydroxybenzoate (both API Corporation) Isopropylmethylphenol, thymol (both manufactured by Osaka Kasei Co., Ltd.), I PMP-TN (manufactured by Technoble Co., Ltd.); Zeastat, Spectrastat E, G (caprylhydroxamic acid) (all manufactured by INOLEX); GLYCASIL, GLYCASIL2000, GLYCASIL L, GLYCASIL S (butyl cal Propynyl iodide bamate) (both manufactured by Lonza); Chloretone (chlorobutanolate) (manufactured by Sekisui Medical Co., Ltd.) or the like is used.
[0018] In the composition for external use on skin of the present invention, the total content of the component (B) relative to the total amount of the composition is preferably Preferably, it is 0.0001 to 6 mass%, more preferably 0.001 to 3 mass%, and even more preferably Preferably, the content is 0.01 to 1.5% by mass, more preferably 0.05 to 1% by mass, and particularly preferably The content is usually 0.1 to 0.5 mass %.
[0019] In the topical skin composition of the present invention, the ratio of the total content of component (B) to component (A) is Although not particularly limited, the ratio of the component (B) to 1 part by mass of the component (A) is preferably 0.00. 0.01 to 2 parts by mass, more preferably 0.001 to 1 part by mass, and even more preferably 0.01 to 0 0.5 parts by mass.
[0020] In the composition for external use on skin of the present invention, the ratio of the amount of the parahydroxybenzoic acid ester to the total amount of the composition is The total content is not particularly limited as long as the effects of the present invention are achieved. The total content of the above is preferably 0.001 mass % or more, more preferably 0.001 mass % or more, based on the total amount of the composition. is 0.005% by mass or more, more preferably 0.01% by mass or more, and even more preferably The content is preferably 0.05% by mass or more, and particularly preferably 0.1% by mass or more. The content of the benzoic acid ester is preferably 1% by mass or less, more preferably 1% by mass or less, based on the total amount of the composition. Preferably, it is 0.7% by mass or less, more preferably, it is 0.5% by mass or less, and even more preferably, it is Preferably, the content is 0.3% by mass or less, and particularly preferably 0.2% by mass or less. The total content of benzoic acid esters is preferably 0.005 to 1 mass % based on the total amount of the composition. % by mass, more preferably 0.01 to 0.5% by mass, even more preferably still more preferably The content is preferably 0.05 to 0.3 mass %, and particularly preferably 0.1 to 0.2 mass %.
[0021] In the composition for external use on skin of the present invention, the content of benzoic acid or sodium benzoate relative to the total amount of the composition is The content of benzoic acid or benzoin alone is not particularly limited as long as the effects of the present invention are achieved. The content of sodium carbonate is preferably 0.001% by mass or more, more preferably 0.001% by mass or more, based on the total amount of the composition. More preferably, it is 0.005% by mass or more, even more preferably, it is 0.01% by mass or more, and even more preferably, it is 0.005% by mass or more, and ...05% by mass or more, and even more preferably, it is 0.005% by mass or more More preferably, it is 0.05% by mass or more. The content is preferably 1 mass % or less, more preferably 0.7 mass %, based on the total amount of the composition. % by mass or less, more preferably 0.5% by mass or less, and even more preferably 0.3% by mass or less The total content of benzoic acid or sodium benzoate is less than 100% of the total amount of the composition. Preferably, the content is 0.005 to 1 mass %, more preferably, 0.01 to 0.5 mass %, and further preferably, The most preferable range is 0.05 to 0.3 mass %.
[0022] [(C) component] The component (C) contained in the topical skin composition of the present invention is an organic acid, an organic acid salt, or an organic acid derivative. and at least one selected from the group consisting of amphiphilic compounds.
[0023] ((C-1) Organic acid, organic acid salt, or organic acid derivative) The organic acids, organic acid salts, and organic acid derivatives used in the present invention include pharmaceuticals, quasi-drugs, and the like. The use of compounds that are commonly used as ingredients in topical skin preparations in the field of topical or cosmetic products. This can be done.
[0024] In the present invention, the organic acid is an acid having an organic group and a molecular weight of 1000 or less, preferably 700 or less. , more preferably 500 or less, even more preferably 350 or less, particularly preferably 30 The organic acid is an acid of an organic compound having a molecular weight of 0 or less. The organic acid is preferably a water-soluble organic acid. The organic acid is Carboxylic acid having a carboxyl group, sulfonic acid having a sulfo group, or phosphoric acid having a More specifically, the organic acid may be, but is not limited to, , for example, ascorbic acid, tranexamic acid, citric acid, salicylic acid, lactic acid, tartaric acid, Glycolic acid, succinic acid, oxalic acid, gluconic acid, fumaric acid, aspartic acid, pyrrolidone capric acid, ε-aminocaproic acid, glutamic acid, aminoethylsulfonic acid, ellagic acid, Ujic acid, glycyrrhizic acid, glycyrrhetinic acid, phytic acid, ferulic acid, glycolic acid , azelaic acid, etc. Among them, ascorbic acid, tranexamic acid, citric acid, Salicylic acid, lactic acid, tartaric acid, malic acid, succinic acid, gluconic acid, aspartic acid, pylori donorcarboxylic acid, ε-aminocaproic acid, glutamic acid, aminoethylsulfonic acid, ella Glycine, Kojic acid, Glycyrrhizic acid, Glycyrrhetinic acid, Phytic acid, Ferulic acid, Gly Preferably, one or more selected from the group consisting of cholic acid and azelaic acid are used, and ascorbic acid is preferably used. Acid, tranexamic acid, citric acid, salicylic acid, lactic acid, tartaric acid, malic acid, succinic acid, Gluconic acid, pyrrolidone carboxylic acid, ε-aminocaproic acid, glutamic acid, kojic acid, Licyrrhizic acid, glycyrrhetinic acid, phytic acid, ferulic acid, glycolic acid, azelaic acid More preferably, one or more selected from the group consisting of ascorbic acid, tranexamic acid, Sucralic acid, citric acid, salicylic acid, lactic acid, succinic acid, tartaric acid, gluconic acid, kojic acid, and one or more selected from the group consisting of lactic acid, glycolic acid, and glycyrrhizic acid. More preferred are ascorbic acid, tranexamic acid, citric acid, lactic acid, gluconic acid, salicylic acid. one or more selected from the group consisting of lactic acid, tartaric acid, phytic acid, and kojic acid More preferably, the acid is selected from the group consisting of ascorbic acid, tranexamic acid, citric acid, and lactic acid. One or more of the above are particularly preferred.
[0025] In the present invention, the organic acid salt refers to a salt of such an organic acid. Examples of salts include, but are not limited to, salts with organic bases (e.g., trime diethylamine salt, triethylamine salt, monoethanolamine salt, triethanolamine salt salts with tertiary amines such as pyridine salts; salts with basic ammonia such as arginine or lysine; salts with inorganic bases (e.g., inorganic acid salts such as hydrochlorides, sulfates, phosphates, etc.) : Ammonium salts; alkali metal salts such as sodium salts and potassium salts; calcium salts, ma alkaline earth metal salts such as magnesium salts; or zinc salts, aluminum salts, etc. Among these, preferred organic acid salts are triethanolamine salts, monoammonium salts, and naphthalene salts. The thorium salt, potassium salt, dipotassium salt, magnesium salt, or zinc salt is particularly preferred. Suitable organic acid salts are sodium, dipotassium, or magnesium salts.
[0026] In the present invention, preferred organic acid salts are sodium ascorbate and tranexamate. Salicylate, Calcium tranexamate, Sodium salicylate, Calcium salicylate, Salicylate Magnesium salicylate, potassium salicylate, sodium lactate, sodium tartrate, citric acid Sodium citrate, disodium citrate, trisodium citrate, potassium citrate, succinic acid Sodium succinate, disodium succinate, sodium oxalate, calcium gluconate, Zinc gluconate, sodium pyrrolidone carboxylate, zinc pyrrolidone carboxylate, gluta Sodium glycyrrhizinate, dipotassium glycyrrhizinate, monoammonium glycyrrhizinate, Examples include sodium phytate, sodium glycolate, and ammonium glycolate. Among these, sodium ascorbate, tranexamic acid hydrochloride, and calcotranexamic acid Sodium, Sodium Salicylate, Sodium Lactate, Sodium Tartrate, Sodium Citrate Disodium citrate, trisodium citrate, sodium succinate, disodium succinate Thorium, calcium gluconate, zinc gluconate, zinc pyrrolidone carboxylate, pyrolyl Sodium glutamate, sodium glycyrrhizinate, dipotassium glycyrrhizinate, Monoammonium ricyrrhizinate, sodium phytate, sodium glycolate, ammonium succinate, sodium succinate, and disodium succinate Preferably, one or more selected from the following are used, and sodium ascorbate, sodium salicylate, etc. Sodium, Sodium Lactate, Sodium Citrate, Disodium Citrate, Trisodium Citrate Calcium, zinc gluconate, sodium pyrrolidone carboxylate, sodium glutamate, One or more selected from the group consisting of sodium succinate and disodium succinate More preferred are sodium ascorbate, sodium lactate, sodium citrate, One or more selected from the group consisting of sodium succinate and disodium succinate is even more preferred.
[0027] In the present invention, the term "derivative of organic acid" refers to such a derivative of organic acid, and the molecular weight of the derivative is 100 0 or less, preferably 800 or less, more preferably 600 or less, and even more preferably 5 00 or less, particularly preferably 450 or less, and most preferably 350 or less. The organic acid derivative is preferably a water-soluble organic acid derivative.
[0028] In the present invention, the organic acid derivatives include sodium ascorbyl phosphate. ascorbic acid phosphate esters such as magnesium ascorbyl phosphate; Ascorbic acid sulfate esters such as disodium ascorbic acid sulfate; 2-O-ethyl Ascorbic acid, alkyl ascorbic acids such as 3-O-ethyl ascorbic acid; ascorbic acid Ascorbic acid glycosides such as 2-glycoside of ascorbic acid; isostearyl ascorbyl phosphate Disodium, Trisodium Ascorbyl Palmitate Phosphate; Glyceryl Ascorbate Acid, Bisglyceryl Ascorbate, Alkylglyceryl Ascorbate; (Ascorbic Acid Ascorbyl / Tocopheryl Phosphate, Potassium Ascorbyl / Tocopheryl Phosphate, Maleate Tocopheryl Ascorbate; Ascorbyl Tetrahexyldecanoate, L Dipalmitate -Oil-soluble ascorbic acid derivatives such as ascorbyl; dimers of tranexamic acid; tranexamic acid Amides of tranexamic acid such as tranexamic acid methylamide hydrochloride; tranexamic acid hydroquinone Vitamin esters; Vitamin A ester, Vitamin E ester, Vitamin C ester, etc. tranexamic acid vitamin esters such as esters and alkyl esters; tranexamic acid Antiseptic ester; Tranexamic acid cetyl hydrochloride; Ethylene glycol salicylate, Polyhydric alcohol esters such as dipropylene glycol licylate; methyl salicylate, salicylate Alkyl salicylates such as 2-ethylhexyl licylate; 4-methoxysalicylic acid, 4-methylsalicylic acid, Alcosyl salicylic acid or its salt such as potassium thixosalicylate; stearoyl glutamate Sodium lauroyl glutamate, sodium dilauroyl glutamate acylamino acid or its salt, such as sodium glycyrrhetinate, and stearyl glycyrrhetinate Among these, sodium ascorbyl phosphate is particularly preferred. Sodium, magnesium ascorbyl phosphate, disodium ascorbyl sulfate Thorium, 2-O-ethyl ascorbic acid, 3-O-ethyl ascorbic acid, ascorbic acid Phosphate-2-glucoside, disodium isostearyl ascorbyl phosphate, palmitic acid Trisodium Ascorbyl Phosphate, Glyceryl Ascorbate, Bisglyceryl Ascorbate Ascorbic Acid, Hexyl 3-Glyceryl Ascorbate, 3-Glyceryl Ascorbate, Milli Styryl 3-glyceryl ascorbate, 3-laurylglyceryl ascorbate, (Ascorbyl Ascorbyl / Tocopheryl Phosphate, Potassium Ascorbyl / Tocopheryl Phosphate, Ascorbyl tocopheryl leate, tranexamic acid methylamide hydrochloride, tranexamic acid Cetyl Salicylate Hydrochloride, Ethylene Glycol Salicylate, Methyl Salicylate, 2-Ethyl Salicylate Cylhexyl, 4-methoxysalicylic acid, potassium 4-methoxysalicylate, stearyl Sodium lauroyl glutamate, Sodium lauroyl glutamate, Dilauroyl glutamine one or more selected from the group consisting of sodium lysine phosphate, and stearyl glycyrrhetinate Preferably, two or more of the above are used, and sodium ascorbyl phosphate, ascorbyl phosphate, Ascorbic acid ester magnesium, ascorbic acid sulfate disodium, 2-O-ethyl ascorbic acid Ascorbic acid, 3-O-ethyl ascorbic acid, ascorbic acid-2-glucoside, iso Disodium stearyl ascorbyl phosphate, trisodium ascorbyl palmitate phosphate Um, Glyceryl Ascorbate, Bisglyceryl Ascorbate, Hexyl 3-Glyceryl 3-glyceryl ascorbate, myristyl 3-glyceryl ascorbate Acid, 3-Laurylglyceryl Ascorbic Acid, 4-Methoxysalicylic Acid, 4-Methoxysalicylic Acid Potassium licylate, sodium stearoyl glutamate, sodium lauroyl glutamate sodium dilauroyl glutamate lysine; More preferably, two or more of the above are used, and sodium ascorbyl phosphate, ascorbic acid Magnesium phosphate, disodium ascorbyl sulfate, 2-O-ethyl Ascorbic acid, 3-O-ethyl ascorbic acid, ascorbic acid-2-glucoside, Glyceryl ascorbate, bisglyceryl ascorbate, hexyl 3-glyceryl ascorbate Ascorbic acid, 3-glyceryl ascorbate, potassium 4-methoxysalicylate, stearyl alcohol sodium dilauroyl glutamate and sodium dilauroyl glutamate lysine More preferably, one or more selected from the group consisting of sodium ascorbic acid phosphate Thorium, magnesium ascorbyl phosphate, ascorbyl sulfate 2 Sodium, 2-O-ethyl ascorbate, 3-O-ethyl ascorbate, and ascorbate One or more selected from the group consisting of corbic acid-2-glucoside are even more preferred. It's nice.
[0029] These can be synthesized, or commercially available products can be used as they are.
[0030] These organic acids, organic acid salts, and organic acid derivatives may be used alone or in combination of two or more. It can also be used.
[0031] In particular, when the component (B) is a parahydroxybenzoate, the component (C-1) Ascorbic acid, ascorbate, alkyl ascorbate, phosphate ascorbate If it contains ascorbic acid, sodium ascorbate, or ascorbic acid esters, Sodium ascorbyl phosphate, sodium ascorbyl phosphate, Magnesium, disodium ascorbyl sulfate, 2-O-ethyl ascorbic acid , 3-O-ethyl ascorbic acid, ascorbic acid-2-glucoside, isostearyl Disodium Ascorbyl Phosphate, Trisodium Ascorbyl Palmitate Phosphate, Glycerol Ascorbic Acid, Bisglyceryl Ascorbic Acid, Hexyl 3-Glyceryl Ascorbate Ascorbic Acid, 3-Glyceryl Ascorbate, Myristyl 3-Glyceryl Ascorbate, 3-La Uryl glyceryl ascorbate, (ascorbyl / tocopheryl) phosphate, (ascorbyl Ascorbyl Tocopheryl Phosphate, and Ascorbyl Tocopheryl Maleate Combining two or more different ingredients selected from the group In view of the above, sodium ascorbyl phosphate and sodium ascorbyl phosphate are preferred. Ester magnesium, disodium ascorbyl sulfate, 2-O-ethyl ascorbyl Consists of ascorbic acid, 3-O-ethyl ascorbic acid, and ascorbic acid-2-glucoside It is more preferred to combine two or more different components selected from the group.
[0032] The component (C-1) of the present invention may include ascorbic acid, tranexamic acid, citric acid, salicylic acid, and the like. acid, lactic acid, acetic acid, tartaric acid, malic acid, succinic acid, oxalic acid, gluconic acid, fumaric acid, Propionic acid, aspartic acid, pyrrolidone carboxylic acid, ε-aminocaproic acid, glutamine Acid, Aminoethylsulfonic Acid, Ellagic Acid, Kojic Acid, Glycyrrhizic Acid, Glycyrrhizic Acid Acid, Phytic Acid, Ferulic Acid, Glycolic Acid, Azelaic Acid, Ascorbic Acid, Phosphate Ascorbic acid ester, ascorbic acid sulfate, alkyl ascorbic acid, ascorbic acid glycoside , Disodium Isostearyl Ascorbyl Phosphate, Trisodium Ascorbyl Palmitate Phosphate Sodium, glyceryl ascorbate derivative, tranexamic acid dimer, tranexamic Acid amides, tranexamic acid esters, alkyl tranexamates, polyhydric alkyl salicylates Cholic esters, alkyl salicylates, alkoxysalicylic acids, acyl amino acids, glyceryl One or more selected from the group consisting of luretin esters and salts thereof are preferred. Ascorbic acid, tranexamic acid, citric acid, salicylic acid, lactic acid, tartaric acid, malic acid , succinic acid, gluconic acid, pyrrolidone carboxylic acid, ε-aminocaproic acid, glutamic acid , Kojic acid, Glycyrrhetinic acid, Phytic acid, Ferulic acid, Glycolic acid, Azelaic acid , sodium ascorbate, tranexamic acid hydrochloride, calcium tranexamate, salicylic acid Sodium tartrate, sodium lactate, sodium tartrate, sodium citrate, citric acid Disodium, trisodium citrate, sodium succinate, disodium succinate, Calcium Gluconate, Zinc Gluconate, Sodium Pyrrolidonecarboxylate, Pyrrolidone Carboxylate Zinc carbonate, monosodium glutamate, sodium phytate, sodium glycolate ammonium glycolate, dipotassium glycyrrhizinate, monoaluminum glycyrrhizinate ammonium, sodium ascorbyl phosphate, ascorbyl phosphate Magnesium, disodium ascorbyl sulfate, 2-O-ethyl ascorbic acid Acid, 3-O-ethyl ascorbic acid, ascorbic acid-2-glucoside, isostearyl Disodium ascorbyl phosphate, trisodium ascorbyl palmitate phosphate, glycolic acid Ceryl ascorbate, bisglyceryl ascorbate, hexyl 3-glyceryl ascorbate Ascorbic Acid, 3-Glyceryl Ascorbate, Myristyl 3-Glyceryl Ascorbate, 3- Laurylglyceryl Ascorbate, Potassium Ascorbyl Tocopheryl Phosphate, and ascorbyl tocopheryl maleate, tranexamic acid methylamide hydrochloride, tranexamic acid Cetyl xamate hydrochloride, ethylene glycol salicylate, methyl salicylate, salicylic acid 2-Ethylhexyl, 4-Methoxysalicylic Acid, Potassium 4-Methoxysalicylate, Stearyl Sodium aroyl glutamate, sodium lauroyl glutamate, dilauramidoglutamide sodium glutamate lysine, and stearyl glycyrrhetinate One or more of these is more preferred, and ascorbic acid, tranexamic acid, citric acid, salicylic acid, etc. Acid, lactic acid, gluconic acid, kojic acid, tartaric acid, phytic acid, glycolic acid, ascorbic acid Sodium citrate, sodium salicylate, sodium lactate, sodium citrate, citric acid Disodium, trisodium citrate, sodium succinate, disodium succinate, Sodium lolidonecarboxylate, sodium glutamate, dipotassium glycyrrhizinate , Monoammonium glycyrrhizinate, Sodium ascorbyl phosphate, Ascorbyl Magnesium ascorbate phosphate, 2-O-ethyl ascorbic acid, 3-O-ethyl Ascorbic acid, ascorbic acid-2-glucoside, sodium stearoyl glutamate um, sodium lauroyl glutamate, sodium dilauramidoglutamide lysine More preferably, one or more selected from the group consisting of citric acid, lactic acid, tranexamic acid, Acid, salicylic acid, gluconic acid, phytic acid, tartaric acid, sodium lactate, sodium citrate Ascorbic acid phosphate sodium, ascorbic acid phosphate magnesium Sodium, 2-O-ethyl ascorbic acid, 3-O-ethyl ascorbic acid, ascorbic acid Acid-2-glucoside, sodium succinate, disodium succinate are even more preferred. tranexamic acid, citric acid, lactic acid, salicylic acid, gluconic acid, phytic acid, tartaric acid, Disodium succinate, sodium ascorbyl phosphate, ascorbyl phosphate Acid ester magnesium, 2-O-ethyl ascorbic acid, 3-O-ethyl ascorbic acid and ascorbic acid-2-glucoside. Preferred.
[0033] In the composition for external use on skin of the present invention, the organic acid, organic acid salt, or organic acid The total content of the derivatives is preferably 0.001 to 10% by mass, more preferably 0.00 5 to 7 mass%, more preferably 0.01 to 5 mass%, and even more preferably 0.05 to The content is 5% by mass, and particularly preferably 0.1 to 3% by mass.
[0034] In the topical skin composition of the present invention, the organic acid, organic acid salt, or organic acid The ratio of the total content of the organic derivatives is not particularly limited, but is preferably 1 part by mass of the component (A) to 1 part by mass of the organic derivatives. The amount of the acid, organic acid salt, or organic acid derivative is preferably 0.001 to 3.5 parts by mass, more preferably Preferably, it is 0.01 to 2 parts by mass, and more preferably 0.05 to 1 part by mass.
[0035] In the composition for external use on skin of the present invention, the total amount of ascorbic acid, its salts, or its derivatives is The content is not particularly limited, but is preferably 0.001 to 10% by mass, more preferably 0.001 to 10% by mass. 0.01 to 7 mass%, more preferably 0.05 to 5 mass%, and even more preferably 0. The content is 1 to 5 mass %, and particularly preferably 0.5 to 3 mass %. In the topical skin composition of the present invention, the total amount of tranexamic acid, its salts, or its derivatives is The content is not particularly limited, but is preferably 0.1 to 5 mass%, more preferably 0.5 It is preferably from 1 to 5% by mass, and more preferably from 1 to 3% by mass.
[0036] ((C-2) Amphiphilic Compound) The amphiphilic component contained in the topical skin composition as component (C-2) of the present invention is a single molecule. Both hydrophilic and hydrophobic groups (lipophilic groups) are present in the water phase and the oil phase (organic phase). This refers to all compounds that have affinity for
[0037] Such amphiphilic compounds are not particularly limited, but examples thereof include alkyleneoxy derivatives, phosphorylcholine-containing polymers, dicarboxylic acid esters, or polycarboxylic acids having 5 to 1 carbon atoms The component (C-2) of the present invention includes any of these compounds. The component (C-2) may be used alone or in combination of two or more thereof. By blending it with component (A) and component (B), a high concentration of nicotinamide is obtained. It is possible to provide a composition for external use on skin in which deposition is suppressed even when the composition is blended with do.
[0038] The component (C-2) is preferably an alkylene oxide derivative represented by the following general formula (I): 2-Methacryloyloxyethyl phosphorylcholine-butyl methacrylate copolymer Decaglyceryl (Eicosanedioate / Tetradecanedioate), Cyclohexanedicarboxylic Acid Bisulfite ethoxydiglycol, diethylhexyl succinate, diethoxyethyl succinate, and and alkanediols having 5 to 10 carbon atoms.
[0039] [ka] (In the formula, Z is a hydrogen atom or a hydroxy compound having 1 to 30 carbon atoms, and n hydroxy groups are selected from the group consisting of means the residue obtained by removing; AO means an oxyalkylene group having 3 to 4 carbon atoms; EO means an oxyethylene group; BO means an oxyalkylene group having 4 carbon atoms; n means 1 to 9; a, b, and c represent the average number of moles of AO, EO, and BO added, respectively, and are independently 0 to 100. The value is 200. However, a, b, and c cannot all be 0. Also, when n is 2 or more, Multiple a's, b's, and c's may be the same or different. When Z is a hydrogen atom, n is 1. do. In addition, AO and EO may be added randomly or in the form of blocks.
[0040] From the viewpoint of providing a good topical skin composition, the alkylene oxide derivative is preferably The compound is preferably a compound represented by the following general formula (II).
[0041] [ka] (In the formula, Z is a hydrogen atom or a hydroxy compound having 1 to 30 carbon atoms, and n hydroxy groups are selected from the group consisting of means the residue obtained by removing; AO means an oxyalkylene group having 3 to 4 carbon atoms; EO means an oxyethylene group; n means 1 to 9; a and b respectively represent the average number of moles of AO and EO added, and are independently 0 to 200. However, a and b cannot all be 0. Also, when n is 2 or more, multiple a and b They may be the same or different. When Z is a hydrogen atom, n is 1. In addition, AO and EO may be added randomly or in the form of blocks.
[0042] The alkylene oxide derivative used in the present invention is a polymer of a specific alkylene glycol. (when Z is a hydrogen atom) or a specific hydroxy compound (corresponding to Z) with a specific alkylene oxide groups (corresponding to the moieties excluding Z in general formulas (I) and (II)) are added. A compound (Z is a compound obtained by removing n hydroxy groups from a hydroxy compound having 1 to 30 carbon atoms) (wherein the group is a group obtained by
[0043] In the alkylene oxide derivative used in the present invention, the precipitation of the topical skin preparation is suppressed. From the viewpoint of providing a composition, AO is an oxyalkylene group having 3 to 4 carbon atoms, for example: Oxypropylene group, oxybutylene group (oxy-n-butylene group, oxyisobutylene group oxyt-butylene group), oxytrimethylene group, oxytetramethylene group, etc. AO is preferably an oxypropylene group, an oxybutylene group, more preferably It is an oxypropylene group.
[0044] In the alkylene oxide derivatives used in the present invention, BO is an oxyalkyl having 4 carbon atoms. Examples of oxybutylene groups include oxyn-butylene groups (oxyn-butylene groups, oxyisobutylene groups). oxymethyl group, ... It is an oxybutylene group.
[0045] In the alkylene oxide derivative used in the present invention, a, b, and c are each independently a, b, and c are each independently preferably 1 to 200. More preferably, it is 2 to 150, even more preferably, it is 2 to 100, and particularly preferably Preferably, it is between 2 and 70.
[0046] In chemical formula (I), a+b+c is the total number of AO, EO, and BO monomer units. is preferably 3 or more, more preferably 5 or more, from the viewpoint of significantly exhibiting the effects of the present invention. More preferably, it is 10 or more. In addition, a+b+c is a value from the viewpoint of significantly exhibiting the effects of the present invention. preferably 450 or less, more preferably 350 or less, and even more preferably 300 or less, Particularly preferably, it is 250 or less.
[0047] In the chemical formula (II), the total number of AO and EO monomer units, a+b, is From the viewpoint of significantly achieving the brightness effect, the number is preferably 3 or more, more preferably 5 or more, and even more preferably In addition, a+b is preferably 10 or more from the viewpoint of significantly exhibiting the effects of the present invention. Preferably, the molecular weight is 400 or less, more preferably 300 or less, even more preferably 250 or less, and particularly preferably is less than 200.
[0048] In the above formulas (I) and (II), the objective is to provide a composition for external use on skin in which deposition is inhibited. wherein Z is a hydrogen atom or an alkyl monoalcohol having 4 to 24 carbon atoms; Glycerin, trimethylolpropane, erythritol, pentaerythritol, carbon number 1-24 alkyl glucoside, diglycerin, xylitol, dipentaerythritol , sorbitol, inositol, sucrose, trehalose, or maltitol The residue obtained by removing one hydroxy group from these alkoxy groups is It is preferably a residue derived from a methyl group compound, and is a hydrogen atom or a residue having a carbon number of 4-24 alkyl monoalcohol, glycerin (to which alkylene oxide groups may be added) hydroxy groups), pentaerythritol (a hydroxy group to which an alkylene oxide group can be added), alkylglucosides (with 4 hydroxy groups) and alkylglucosides (with 1 to 24 carbon atoms) diglycerin (four hydroxy groups to which alkylene oxide groups can be added) hydroxy groups) or sorbitol (hydroxy groups to which alkylene oxide groups can be added) The hydroxyl group is a residue obtained by removing n hydroxyl groups from 6 More preferably, it is a hydrogen atom or an alkyl monoalcohol having 4 to 24 carbon atoms. , glycerin, alkyl glucoside having 1 to 24 carbon atoms, diglycerin, or sorbitol It is more preferable that the residue is obtained by removing n hydroxy groups from , a hydrogen atom, or an alkyl monoalcohol having 4 to 24 carbon atoms, glycerin , alkyl glucosides with 1 to 5 carbon atoms, and removal of n hydroxyl groups from diglycerol It is more preferable that the residue is an alkylmono group having 4 to 24 carbon atoms. By removing n hydroxy groups from alcohol, glycerin, and diglycerin More preferably, it is a residue obtained from
[0049] In the chemical formula (I) or (II), Z is an alkyl monoalcohol having 4 to 24 carbon atoms. In this case, from the viewpoint of significantly exhibiting the effects of the present invention, butyl alcohol, tetradecyl tetradecyl ether, Alcohol, cetanol, and stearyl alcohol are preferred, and butyl alcohol, tetraethanol, Decyl tetraalcohol is particularly preferred.
[0050] In the chemical formula (I) or (II), when Z is an alkyl glucoside, the effect of the present invention is Among them, alkylglucosides having 1 to 24 carbon atoms are preferred from the viewpoint of significantly achieving the above-mentioned effects. Alkyl glucosides having 1 to 16 carbon atoms are more preferred, and alkyl glucosides having 1 to 10 carbon atoms are preferred. is even more preferred, and alkylglucosides having 1 to 5 carbon atoms are particularly preferred.
[0051] Such alkylene oxide derivatives can be synthesized by known methods. For example, hydroxy compounds having 1 to 30 carbon atoms, ethylene oxide, and alkane compounds having 3 to 4 carbon atoms. After addition polymerization of alkylene oxide, it is reacted with alkylene oxide having 4 carbon atoms. It is to be noted that the hydroxy compound having 1 to 30 carbon atoms is reacted with ethylene oxide and In the step of addition polymerization of alkylene oxide having 3 to 4 carbon atoms, ethylene oxide and The alkylene oxide may be randomly polymerized or block polymerized. The reaction can be carried out in the presence of an alkali catalyst, a phase transfer catalyst, a Lewis acid catalyst, or the like. For this purpose, it is preferable to use an alkali catalyst such as potassium hydroxide.
[0052] The molecular weight of such alkylene oxide derivatives is not limited as long as the effects of the present invention are achieved. However, from the viewpoint of significantly achieving the effects of the present invention, it is preferably 200 or more, and more preferably Preferably, it is 300 or more, and more preferably, it is 400 or more.
[0053] The properties of the alkylene oxide derivative are not limited as long as the effects of the present invention are exhibited. In the formulas (I) and (II), from the viewpoint of significantly exhibiting the effects of the present invention, preferably, Preferably, the ingredient is in a semi-solid (including a paste-like state) to liquid state at 25°C.
[0054] Such alkylene oxide derivatives include, for example, polyoxyalkylene glycerides. alkyl ether, polyoxyalkylene alkyl glucoside, polyoxypropylene alkyl ether, polyoxyethylene polyoxypropylene alkyl ether, polyoxyethylene Polyoxypropylene oxybutylene alkyl ether, polyoxyalkylene Lubit, polyoxyalkylene erythritol ether, polyoxyalkylene penta Erythritol ether, polyoxyalkylene diglyceryl ether, polyoxyal Chilen trimethylolpropane, polyoxypropylene glycol, polyoxyethylene Polyoxypropylene glycol, polyoxyalkylene xylitol, polyoxyal Dipentaerythritol, Polyoxyalkylene Inositol, Polyoxyalkylene trehalose ether, polyoxyalkylene trehalose ether, polyoxyal Examples include chiral maltitol ether.
[0055] Among them, alkylene oxide derivatives include polyoxyethylene glyceryl ether, poly Oxypropylene glyceryl ether, polyoxyethylene polyoxypropylene glycerin Ether, Polyoxybutylene Polyoxyethylene Polyoxypropylene Glyceryl Ether, Polyoxybutylene Polyoxyethylene Polyoxypropylene Alkyl Gluco Sid, Polyoxyethylene Polyoxypropylene Alkyl Glucoside, Polyoxyethylene Polyoxypropylene alkyl glucoside, polyoxypropylene alkyl glucoside alkyl ether, polyoxyethylene polyoxypropylene alkyl ether, poly Oxypropylene sorbitol, polyoxyethylene sorbitol, polyoxyethylene polyethylene Oxypropylene sorbitan, polyoxypropylene erythritol ether, polyoxypropylene sorbitan Diethylene erythritol ether, Polyoxyethylene pentaerythritol ether , polyoxyethylene polyoxypropylene erythritol ether, polyoxypropylene Pentaerythritol Ether, Polyoxyethylene Polyoxypropylene Pentaerythritol Ethritol ether, polyoxybutylene polyoxyethylene pentaerythritol ether ether, polyoxyethylene diglyceryl ether, polyoxypropylene diglyceryl Ether, Polyoxyethylene Polyoxypropylene Diglyceryl Ether, Polyoxy Butylene polyoxyethylene polyoxypropylene diglyceryl ether, polyoxyethylene Trimethylolpropane, Polyoxypropylene trimethylolpropane, Polyoxypropylene Oxyethylene polyoxypropylene trimethylolpropane, polyoxypropylene glycol Coal, Polyoxyethylene Polyoxypropylene Glycol, Polyoxybutylene Poly Oxyethylene polyoxypropylene glycol, polyoxyethylene xylitol, polyethylene Polyoxypropylene alkylene xylitol, polyoxyethylene polyoxypropylene Xylitol, Polyoxyethylene Polyoxypropylene Dipentaerythritol, Poly Oxyethylenedipentaerythritol, polyoxypropyldipentaerythritol, Polyoxyethylene inositol, polyoxypropylene inositol, polyoxyethylene Polyoxypropylene inositol, polyoxyethylene sucrose ether, poly Oxypropylene sucrose ether, polyoxyethylene polyoxypropylene sucrose trehalose ether, polyoxyethylene trehalose ether, polyoxypropylene trehalose treahol ether, polyoxyethylene polyoxypropylene trehalose ether, poly Oxyethylene maltitol ether, polyoxypropylene maltitol ether, and and polyoxyethylene polyoxypropylene maltitol ether. Preferably, one or more of the following are used: Polyoxyethylene glyceryl ether, polyoxypropylene glyceryl ether, Polyoxyethylene polyoxypropylene glyceryl ether, polyoxybutylene poly Oxyethylene polyoxypropylene glyceryl ether, polyoxybutylene polyoxy Ethylene polyoxypropylene alkyl glucoside, polyoxyethylene alkyl glucoside Coside, polyoxypropylene alkyl glucoside, polyoxypropylene alkyl ether ether, polyoxyethylene polyoxypropylene alkyl ether, polyoxypropylene sorbitol, polyoxyethylene sorbitol, polyoxyethylene polyoxypropylene Polyoxypropylene pentaerythritol ether, Polyoxypropylene pentaerythritol ether , polyoxyethylene pentaerythritol ether, polyoxybutylene polyoxyethylene Ethylene pentaerythritol ether, polyoxyethylene diglyceryl ether, poly Oxypropylene diglyceryl ether, polyoxyethylene polyoxypropylene diglyceride Glyceryl ether, polyoxybutylene polyoxyethylene polyoxypropylene diglyceride Ceryl ether, polyoxyethylene polyoxypropylene trimethylolpropane, poly Polyoxypropylene glycol, polyoxyethylene polyoxypropylene glycol, and polyoxybutylene polyoxyethylene polyoxypropylene glycol More preferably, one or more selected from the group Polyoxyethylene glyceryl ether, polyoxypropylene glyceryl ether, Polyoxyethylene polyoxypropylene glyceryl ether, polyoxybutylene poly Oxyethylene polyoxypropylene glyceryl ether, polyoxybutylene polyoxy Ethylene polyoxypropylene alkyl glucoside, polyoxypropylene alkyl glucoside Glucoside, Polyoxyethylene alkyl glucoside, Polyoxypropylene alkyl ether ether, polyoxyethylene polyoxypropylene alkyl ether, polyoxypropylene Polyoxyethylene polyoxypropylene sorbitan, polyoxyethylene Diglyceryl Ether, Polyoxypropylene Diglyceryl Ether, Polyoxyethylene Polyoxypropylene diglyceryl ether, polyoxybutylene polyoxyethylene Polyoxypropylene diglyceryl ether, polyoxypropylene glycol, poly Oxyethylene polyoxypropylene glycol and polyoxybutylene polyoxy One or more selected from the group consisting of ethylene polyoxypropylene glycol More preferably, Polyoxyethylene glyceryl ether, polyoxypropylene glyceryl ether, Polyoxyethylene polyoxypropylene glyceryl ether, polyoxybutylene poly Oxyethylene polyoxypropylene alkyl glucoside, polyoxypropylene alkyl alkyl glucoside, polyoxyethylene alkyl glucoside, polyoxypropylene alkyl ether, polyoxyethylene polyoxypropylene alkyl ether, polyoxypropylene Pyrensorbit, Polyoxyethylene Polyoxypropylene Sorbit, Polyoxyethylene Polyoxyethylene diglyceryl ether, polyoxypropylene diglyceryl ether, polyoxy One or two selected from the group consisting of ethylene polyoxypropylene diglyceryl ether More preferably, polyoxyethylene glyceryl ether, polyoxypropylene Polyoxyethylene glyceryl ether, polyoxyethylene polyoxypropylene glyceryl ether Polyoxybutylene polyoxyethylene polyoxypropylene methyl glucoside, poly Polyoxypropylene methyl glucoside, Polyoxyethylene methyl glucoside, Polyoxy Propylene alkyl ether, polyoxyethylene polyoxypropylene butyl ether Polyoxyethylene polyoxypropylene decyl tetradecyl ether, polyoxy Propylene sorbitol, polyoxypropylene diglyceryl ether, polyoxyethylene One or more selected from the group consisting of polyoxypropylene diglyceryl ether is even more preferred.
[0056] These alkylene oxide derivatives are UNILUBE 50MB-26 (polyoxyethylene Polyoxypropylene butyl ether (17E.O.) (17P.O.)), Unilever 50MB-168 (Polyoxyethylene Polyoxypropylene Butyl Ether (37E .O.)( 38P.O.)), Unilube 50MB-11 (Polyoxyethylene Polyoxy Propylene butyl ether (9E.O.) (10P.O.)), Unisafe 10P-8 ( Polyoxyethylene polyoxypropylene cetyl ether (10E.O.) (8P.O. )), Unilube MT-630B (Polyoxyethylene Polyoxypropylene Decyl Tetramethyl Ladecyl ether (30E.O.) (6P.O.)), Unilube MS-70K (Polio Polypropylene stearyl ether (15P.O.)), Uniol HS-1600D ( Polyoxyalkylene sorbitan), Pronon #208 (polyoxyethylene polyoxy Propylene glycol (150E.O.) (35P.O.)), Pronon #124P (Polyester Polyoxyethylene (20) Polyoxypropylene (20) Glycol), Uniol D- 2000 (polypropylene glycol), Macbiobride MG-10E (polyoxyethylene Methylethylene methyl glucoside (10E.O.)), Macbiobride MG-20E (Polyoxyethylene Diethylene methyl glucoside (20E.O.)), Macbiobride MG-10P (Poly Oxypropylene methyl glucoside (10P.O.), Macbiobride MG-20P ( Polyoxypropylene methyl glucoside (20P.O.), Wilbride MG207 0 (Polyoxybutylene polyoxyethylene polyoxypropylene methyl glucoside), Unilube 5TP-300KB (Polyoxyethylene Polyoxypropylene Pentaerythritol Trititol ether (5E.O.) (65P.O.); Unilube 50TG-32 (Poly Oxyethylene Polyoxypropylene Glyceryl Ether (24E.O.) (24P.O.) ), Wilbride S-753 (Polyoxybutylene Polyoxyethylene Polyoxypropylene Pyrene glyceryl ether (3B.O.) (8E.O.) (5P.O.)), Uniox G- 1200 (Polyoxyethylene glycerin (26E.O.)), Unilube DGP-70 0 (Polyoxypropylene diglyceryl ether (9P.O.)), Unilube DGP-9 50 (Polyoxypropylene diglyceryl ether (14P.O.)) (NOF Corporation) SY-DP14 (Polyoxypropylene diglyceryl ether (14P.O.)) , SY-DP9 (Polyoxypropylene diglyceryl ether (9P.O.)) (all from Osaka Niupol GP-1000 (PPG-16 glyceryl ether, manufactured by Nippon Pharmaceutical Co., Ltd.) Newpol SP-750 (polyoxyalkylene sorbitol ether), Newpol SP-750 (polyoxyalkylene sorbitol ether), -Pol PE-68 (Polyoxyethylene Polyoxypropylene Glycol (160E. O.) (30P.O.)), Newpol PE-78 (Polyoxyethylene Polyoxypropylene Propylene glycol (150E.O.) (35P.O.)), Nieupol GEP-28 00 (Polyoxyethylene polyoxypropylene glyceryl ether (24E.O.) ( 24P.O.) (all manufactured by Sanyo Chemical Co., Ltd.); Emulgen PP-290 (Polyoxy Ethylene polyoxypropylene glycol (160E.O.) (30P.O.), Kao NIKKOL SG-G2424 (Polyoxyethylene Polyoxypropylene) Glyceryl Ether (24E.O.) (24P.O.), NIKKOL SG-DTD 630 (Polyoxyethylene polyoxypropylene decyl tetradecyl ether (30E .O.) (6P.O.) (all manufactured by Nikko Chemicals); GLUCAM P-10 (polio Propylene methyl glucoside (10P.O.), GLUCAM P-20 (polio Polyoxypropylene methyl glucoside (20P.O.) GLUCAM E-10 (Polyoxy Diethylene methyl glucoside (10E.O.)), GLUCAM E-20 (Polyoxyethylene methyl glucoside) Ethylene methyl glucoside (20E.O.) (both manufactured by Lubrizol), Browno GL-26 (Polyoxyethylene glycerin (26E.O.)) (Aoki Oil & Fat Co., Ltd. It is commercially available under the name of "Made by" and others. As commercially available alkylene oxide derivatives, from the viewpoint of remarkably exhibiting the effects of the present invention, Unilube 50MB-26, Unilube 50MB-168, Uniol HS-1600D , Pronon #208, Pronon #124P, Uniol D-2000, McBio Bride MG-10E, McBio Bride MG-20E, McBio Bride MG-10P, McBio Obride MG-20P, Wilbride MG2070, Wilbride S-753, Yu Nilube 5TP-300KB, Unilube 50TG-32, Uniox G-1200, Unilube DGP-700, Unilube DGP-950, SY-DP14, SY-DP9 , Nieuport GP-1000, Nieuport SP-750, Nieuport PE-68, Nieupol PE-78, Nieupol GEP-2800, NIKKOL SG-G24 24, GLUCAM P-10, GLUCAM P-20, GLUCAM E-10, G One or more selected from the group consisting of LUCAM E-20 and Emulgen PP-290 It is preferable that the lubricant is UNILUBE 50MB-26, UNILUBE 50MB-168, or UNILUBE. HS-1600D, Pronon #208, Pronon #124P, Macbio Bride MG -10E, McBio Bride MG-20E, McBio Bride MG-10P, McBio Ride MG-20P, Wilbride MG2070, Unilube 50TG-32, SY- DP14, SY-DP9, GLUCAM P-10, GLUCAM P-20, GLUC AM E-10, GLUCAM E-20 Nieuport PE-68, Nieuport PE- 78, and Emulgen PP-290. Preferred are Unilube 50MB-26, Unilube 50MB-168, and Macbio Bride. MG-10E, McBio Bride MG-20E, McBio Bride MG-10P, McBio Obride MG-20P, Pronon #208, Pronon #124P, Wilbride MG 2070, Unilube 50TG-32, SY-DP14, SY-DP9, Newport P E-68, Nieuport PE-78, GLUCAM P-10, GLUCAM P-20 , GLUCAM E-10, GLUCAM E-20 and Emulgen PP-290 It is even more preferable that the compound is one or more selected from the group consisting of:
[0057] In the present invention, the alkylene oxide derivatives may be used alone or in combination of two or more. Any combination of the above may be used.
[0058] Phosphorylcholine-containing polymers are made by using organic compounds containing phosphorylcholine as monomers. Although not particularly limited, it refers to polymers in general that exhibit the effects of the present invention remarkably. Among them, a monomer containing 2-methacryloyloxyethyl phosphorylcholine is polymerized. The polymer obtained by the reaction is a 2-methacryloyloxyphosphorylcholine-containing polymer. Among them, 2-methacryloyloxyethyl phosphorylcholine / methacrylic acid bromide is preferred. Copolymer (Polyquaternium-51), and polymethacryloyloxyethyl phosphonic acid Preferably, one or more selected from the group consisting of 2-methacryloylcholine, Diethylphosphorylcholine-butyl methacrylate copolymer is more preferred. Commercially available choline-containing polymers include Lipidure-PMB (2-methacryloyl Oxyethylphosphorylcholine-butyl methacrylate copolymer liquid, Polyquaternium-5 1), and Lipidure-HM (polymethacryloyloxyethyl phosphorylcholine ) (all manufactured by NOF Corporation) are preferably one or more selected from the group consisting of Li Pidure-PMB (2-methacryloyloxyethyl phosphorylcholine methacrylate) butyl acetate copolymer liquid) is more preferred.
[0059] Dicarboxylic acid esters are compounds that combine dicarboxylic acids with glycols, glycol ethers, etc. It is an ester condensed with a hydroxy group, and is not particularly limited, for example, (eicosane diamine). Polyglyceryl-10 tetradecanedioate, bisethoxycyclohexanedicarboxylic acid Diglycol, 1,4-cyclohexanedicarboxylic acid bis(triethylene glycol mono) Diethylene glycol monoethyl ether), adipate bis(diethylene glycol monoethyl ether), adipate Bis(triethylene glycol monoethyl ether) succinate, and diethoxyethyl succinate diethylhexyl succinate, especially eicosanedioic acid / tetradecanedioic acid Polyglyceryl-10, bisethoxydiglycol cyclohexanedicarboxylate, amber Diethoxyethyl succinate, diethylhexyl succinate are preferred, eicosanedioic acid / tetradecanoic acid are preferred. Polyglyceryl-10 Candioate, Bisethoxydiglyceryl Cyclohexanedicarboxylate Cyclohexanedicarboxylic acid bisethoxydiglycol is more preferred, In addition, commercially available products include, but are not limited to, diethoxyethyl succinate (C RODAMOL DES), diethylhexyl succinate (CRODAMOL OSU) ( Both are manufactured by Croda Japan Co., Ltd.), Neosolue-Aqua, Neosolue -AquaS (Polyglyceryl-10 (eicosanedioate / tetradecanedioate)), Neo Solue-Aqulio (cyclohexanedicarboxylic acid bisethoxydiglycol) ( Both are manufactured by Nippon Fine Chemical Co., Ltd.
[0060] In order to achieve the effects of the present invention more remarkably, the alkanediol preferably has 5 carbon atoms. The ratio is preferably from 1 to 10, more preferably from 5 to 8, and even more preferably from 5 to 6. For example, 1,2-penta 1,2-hexanediol, 1,2-octanediol are preferred, and 1,2 -Pentanediol, 1,2-hexanediol is more preferred, 1,2-pentanediol Furthermore, commercially available products include, but are not limited to, HYDROLITE -5, HYDROLITE-5 Green (manufactured by Symrise Co., Ltd.), KMO-6 (Osaka Organic Chemical Industry), Microcare Emollient PTGJ, Microcare Emo Ilient HXD (manufactured by THOR) can be used.
[0061] In the present invention, the component (C-2) may include, in addition to the alkylene oxide derivatives described above, 2-Methacryloyloxyethyl phosphorylcholine-butyl methacrylate copolymer, poly Methacryloyloxyethyl phosphorylcholine, (eicosanedioic acid / tetradecanedioic acid) Degaglyceryl, bisethoxydiglycol cyclohexanedicarboxylate, diethoxy succinate ethylhexyl, diethoxyethyl succinate, and alkanediols having 5 to 10 carbon atoms are preferred. In addition to the alkylene oxide derivatives mentioned above, 2-methacryloyloxyethyl phosphoryl Copolymer of methylcellulose and butyl methacrylate, (eicosanedioic acid / tetradecanedioic acid) Lyceryl, cyclohexanedicarboxylic acid bisethoxydiglycol, 1,2-pentanediol diol, 1,2-hexanediol, or 1,2-octanediol is more preferred, In addition to the alkylene oxide derivatives mentioned above, 2-methacryloyloxyethyl phosphorylco Phosphorus-butyl methacrylate copolymer, cyclohexanedicarboxylic acid bisethoxydiglycopolymer Even more preferred are 1,2-pentanediol and 1,2-hexanediol. The component (C-2) may be used alone or in any combination of two or more. It may also be used.
[0062] In the topical skin composition of the present invention, the total content of the component (C-2) is not particularly limited, and may be B) The amount is appropriately determined depending on the type of component and the type of other compounded components, but it is possible to significantly increase the effect of the present invention. From the viewpoint of achieving the above, the content is preferably 0.001 mass % or more, more preferably 0.001 mass % or more, based on the total amount of the composition. Preferably, it is 0.005% by mass or more, more preferably 0.01% by mass or more, and even more preferably It is preferably 0.05% by mass or more, and most preferably 0.1% by mass or more. The total content of the (C-2) component is preferably 20% by mass or less, more preferably 10% by mass or less, based on the total amount of the composition. More preferably, it is 15% by mass or less, even more preferably, it is 12% by mass or less, and even more preferably, it is Preferably, it is 10% by mass or less, and most preferably, 8% by mass or less. The total content of the component (C-2) is preferably 0.001 to 20 parts by mass based on the total amount of the composition. % by mass, more preferably 0.005 to 15% by mass, and even more preferably 0.01 to 12% by mass , even more preferably 0.05 to 10% by mass, and most preferably 0.1 to 8% by mass. be.
[0063] In the topical skin composition of the present invention, the ratio of the total content of component (C-2) to component (B) The ratio is not particularly limited, but it is preferable that the (C-2) component is used in an amount of 1 part by mass of the (B) component. 0.01 to 50,000 parts by mass, more preferably 0.05 to 10,000 parts by mass, and even more preferably The content is preferably 0.1 to 5000 parts by mass.
[0064] In the composition for external use on skin of the present invention, the ratio of the alkylene oxide derivative to the total amount of the composition is The content of the component is not particularly limited as long as the effects of the present invention are achieved. The content of the alkylene oxide derivative alone is preferably 0. 0.1% by mass or more, more preferably 0.1% by mass or more, and even more preferably 0.5% by mass or more That's all. The content of the alkylene oxide derivative alone is preferably 15 to 15% by weight based on the total amount of the composition. % by mass or less, more preferably 10% by mass or less, and even more preferably 8% by mass or less. . The content of the alkylene oxide derivative alone is preferably 0. It is preferably 0.1 to 15% by mass, more preferably 0.1 to 10% by mass, and even more preferably is 0.5 to 8 mass %, and even more preferably 0.5 to 5 mass %.
[0065] In the composition for external use on skin of the present invention, the amount of (eicosanedioic acid / tetradecanoic acid) relative to the total amount of the composition is The content of decaglyceryl benzoate alone is not particularly limited as long as the effects of the present invention are achieved. . The content of Decaglyceryl (Eicosanedioate / Tetradecanedioate) alone is the total amount of the composition. Preferably, it is 0.001 mass % or more, more preferably, it is 0.005 mass % or more. , more preferably 0.01% by mass or more, and even more preferably 0.05% by mass or more. is. The content of Decaglyceryl (Eicosanedioate / Tetradecanedioate) alone is the total amount of the composition. Preferably, it is 15% by mass or less, more preferably 10% by mass or less, and even more preferably Preferably, it is 8% by mass or less, and even more preferably, it is 5% by mass or less. The content of Decaglyceryl (Eicosanedioate / Tetradecanedioate) alone is the total amount of the composition. Preferably, the content is 0.001 to 15 mass%, more preferably 0.005 to 10 mass%. % by mass, more preferably 0.01 to 8% by mass, and even more preferably 0.05% by mass It is about 5% by mass.
[0066] In the composition for external use on skin of the present invention, the amount of cyclohexanedicarboxylic acid bicarbonate relative to the total amount of the composition is The content of ethoxydiglycol alone is not particularly limited as long as the effects of the present invention are achieved. . The content of bisethoxydiglycol cyclohexanedicarboxylate alone is the total amount of the composition. Preferably, it is 0.001 mass % or more, more preferably, it is 0.005 mass % or more. , more preferably 0.01% by mass or more, and even more preferably 0.05% by mass or more. is.
[0067] The content of bisethoxydiglycol cyclohexanedicarboxylate alone is the total amount of the composition. Preferably, it is 15% by mass or less, more preferably 10% by mass or less, and even more preferably Preferably, it is 8% by mass or less, and even more preferably, it is 5% by mass or less. The content of bisethoxydiglycol cyclohexanedicarboxylate alone is the total amount of the composition. Preferably, the content is 0.001 to 15 mass%, more preferably 0.005 to 10 mass%. % by mass, more preferably 0.01 to 8% by mass, and even more preferably 0.05% by mass The content of bisethoxydiglycol cyclohexanedicarboxylate alone is up to 5% by mass. The amount is preferably 10% by mass or less, more preferably 8% by mass or less, based on the total amount of the composition. The content is preferably 5% by mass or less, and more preferably 5% by mass or less.
[0068] The content of bisethoxydiglycol cyclohexanedicarboxylate alone is the total amount of the composition. Preferably, the content is 0.001 to 10 mass %, more preferably 0.005 to 8 mass %. %, more preferably 0.01 to 5 mass%, and even more preferably 0.05 to 3 mass%. %.
[0069] In the composition for external use on skin of the present invention, the amount of 2-methacryloyloxyethyl ether relative to the total amount of the composition is The content of the methylphosphorylcholine-butyl methacrylate copolymer alone is sufficient to achieve the effects of the present invention. There is no particular limitation as long as Monomers of 2-methacryloyloxyethyl phosphorylcholine-butyl methacrylate copolymers The content of the inorganic fine particles is preferably 0.0001 mass% or more, more preferably 0.0001 mass% or more, based on the total amount of the composition. Preferably, 0.001% by mass or more, more preferably 0.005% by mass or more, and even more preferably Preferably, it is 0.01 mass % or more. Monomers of 2-methacryloyloxyethyl phosphorylcholine-butyl methacrylate copolymers The content of the inorganic component is preferably 2 mass % or less, more preferably 1 mass % or less, based on the total amount of the composition. % by mass or less, more preferably 0.5% by mass or less, and even more preferably 0.2% by mass or less The following is the result. Monomers of 2-methacryloyloxyethyl phosphorylcholine-butyl methacrylate copolymers The content of the inorganic fine particles is preferably 0.0001 to 2 mass % based on the total amount of the composition, more preferably Preferably, the content is 0.001 to 1 mass%, more preferably 0.005 to 0.5 mass%, and even more preferably 0.005 to 0.5 mass%. More preferably, it is 0.01% by mass to 0.2% by mass.
[0070] In the composition for external use on skin of the present invention, the amount of alkanedioic acid having 5 to 10 carbon atoms relative to the total amount of the composition is The content of the alcohol alone is not particularly limited as long as the effects of the present invention are achieved. The content of the alkanediol having 5 to 10 carbon atoms alone is preferably is 0.0001 mass% or more, more preferably 0.001 mass% or more, and even more preferably is 0.01% by mass or more, and even more preferably 0.1% by mass or more. The content of the alkanediol having 5 to 10 carbon atoms alone is preferably is 10% by mass or less, more preferably 7% by mass or less, and even more preferably 5% by mass or less , and even more preferably 3% by mass or less. The content of the alkanediol having 5 to 10 carbon atoms alone is preferably is 0.0001 to 10 mass%, more preferably 0.001 to 7 mass%, and even more preferably The content is preferably 0.01 to 5 mass %, and even more preferably 0.1 to 3 mass %.
[0071] In the topical skin composition of the present invention, the component (C) is any one of the components (C-1). It is also preferable to use one or more of the above in combination with one or more of the components (C-2). stomach.
[0072] In the topical skin composition of the present invention, the component (C) is any one of the components (C-1). It is also preferable to use one or more of the above in combination with one or more of the components (C-2). stomach.
[0073] Such a combination includes ascorbic acid and tranexamic acid as the component (C-1), Citric acid, salicylic acid, lactic acid, gluconic acid, kojic acid, tartaric acid, succinic acid, phytic acid, Glycolic acid, sodium ascorbate, sodium salicylate, sodium lactate, Sodium citrate, disodium citrate, trisodium citrate, sodium succinate , disodium succinate, sodium pyrrolidone carboxylate, monosodium glutamate, Dipotassium glycyrrhizinate, monoammonium glycyrrhizinate, phosphorus ascorbate Sodium ascorbate, magnesium ascorbyl phosphate, 2-O-ethyl ascorbyl Ascorbic acid, 3-O-ethyl ascorbic acid, ascorbic acid-2-glucoside, stearyl Sodium aroyl glutamate, sodium lauroyl glutamate, and dilauroyl glutamate Sodium glutamate lysine (C-2) component, polyoxyethylene glyceryl Ether, Polyoxypropylene Glyceryl Ether, Polyoxyethylene Polyoxypropylene Propylene glyceryl ether, polyoxybutylene polyoxyethylene polyoxypropylene ethylene glyceryl ether, polyoxybutylene polyoxyethylene polyoxypropylene Alkyl glucoside, polyoxyethylene methyl glucoside, polyoxypropylene methyl Glycoside, Polyoxypropylene Diglyceryl Ether, Polyoxyethylene Diglyceride Ceryl ether, polyoxypropylene alkyl ether, polyoxyethylene polyoxy Propylene decyl tetradecyl ether, polyoxyethylene polyoxypropylene bromide 2-Methacryloyloxyethylphosphorylcholine·Butyl methacrylate Copolymer liquid, polymethacryloyloxyethyl phosphorylcholine, (eicosanedioic acid / tetrahydrofuran) Polyglyceryl-10 toradecanedioate, bisethoxycyclohexanedicarboxylic acid glycerol, diethoxyethyl succinate, and diethylhexyl succinate. It is preferable to combine one or more of the above-mentioned compounds, (C-1) Ingredients: ascorbic acid, tranexamic acid, citric acid, lactic acid, salicylic acid, Luconic acid, phytic acid, tartaric acid, succinic acid, disodium succinate, ascorbic acid phosphorus Sodium ascorbate, magnesium ascorbyl phosphate, 2-O-ethyl ascorbyl Ascorbic acid, 3-O-ethyl ascorbic acid, and ascorbic acid-2-glucoside (C-2) component: polyoxyethylene glyceryl ether, polyoxypropylene Glyceryl ether, polyoxyethylene polyoxypropylene glyceryl ether, poly Polyoxybutylene Polyoxyethylene Polyoxypropylene Glyceryl Ether, Polyoxyethylene Butylene polyoxyethylene polyoxypropylene alkyl glucoside, polyoxy Ethylene methyl glucoside, polyoxypropylene methyl glucoside, polyoxyethylene Polyoxypropylene decyl tetradecyl ether, polyoxyethylene polyoxypropylene Propylene butyl ether, 2-methacryloyloxyethyl phosphorylcholine methacryl Butyl acrylate copolymer liquid, (eicosanedioic acid / tetradecanedioic acid) polyglyceryl-10, Bisethoxydiglycol cyclohexanedicarboxylate, diethoxyethyl succinate, and and diethylhexyl succinate, It is more preferable that
[0074] In particular, when the component (C-2) is added to the topical skin composition of the present invention, the preservative effect is sufficiently It maintains a good feel when used (penetration, moisturizing, etc.), and furthermore, it contains nicotinamide. This makes it possible to create a formulation that combines various efficacies with good stability (precipitation).
[0075] [Other useful ingredients] The composition for external use on skin of the present invention may contain other ingredients in addition to the ingredients (A), (B), and (C). To add useful effects, ultraviolet absorbers, ultraviolet protection agents, whitening ingredients, anti-inflammatory ingredients, or Acidic mucopolysaccharides can be added. These ingredients are used in pharmaceuticals and quasi-drugs. There are no particular limitations as long as it can be used in the field of cosmetics, and any suitable one can be selected. It can be used as such.
[0076] (ultraviolet absorber) The ultraviolet absorber is not limited, but preferably includes salicylic acid-based ultraviolet absorbers and cinnamon. Acid-based UV absorbers, benzoylmethane-based UV absorbers, benzoate ester derivative UV absorbers UV absorbers, triazine derivative UV absorbers, benzalmalonate derivative UV absorbers, octo Crylene-based UV absorbers, imidazole sulfonic acid derivative UV absorbers, benzophenone It may be a derivative ultraviolet absorber or the like.
[0077] In the present invention, such ultraviolet absorbers include, but are not limited to, paramethoxyphenyl ether 2-Ethylhexyl cinnamate, 4-tert-butyl-4'-methoxydibenzoylmethacrylate 2-[4-(diethylamino)-2-hydroxybenzoyl]benzoic acid hexyl ester Dimethoxybenzylidene dioxoimidazolidinepropionic acid 2-ethylhexyl ester , 2,2'-methylenebis[6-(2H-benzotriazol-2yl)-4-(1,1 ,3,3-tetramethylbutyl)phenol], 2,4-bis-[{4-(2-ethylhexyl)phenol] xyloxy)-2-hydroxy}-phenyl]-6-(4-methoxyphenyl)-1, 3,5-Triazine, 2,4,6-tris[4-(2-ethylhexyloxycarbonyl )Anilino]-1,3,5-triazine, dimethicone diethyl benzalmalonate, 2- Ano-3,3-diphenylprop-2-enoic acid 2-ethylhexyl ester, 2-phenyl Benzimidazole-5-sulfonic acid is preferred, and 2-ethyl paramethoxycinnamate is preferred. xyl, 4-tert-butyl-4'-methoxydibenzoylmethane, 2-[4-(diphenyl 2,4-bis-(2-hydroxybenzoyl)benzoic acid hexyl ester [{4-(2-ethylhexyloxy)-2-hydroxy}-phenyl]-6-(4-methyl- 2,4,6-tris[4-(2-ethylphenyl)-1,3,5-triazine, [xyloxycarbonyl]anilino]-1,3,5-triazine, 2-phenylbenzoyl Midazole-5-sulfonic acid is more preferred, and 2-ethylhexyl paramethoxycinnamate is preferred. , 2-[4-(diethylamino)-2-hydroxybenzoyl]benzoic acid hexyl ester 2,4-bis-[{4-(2-ethylhexyloxy)-2-hydroxy}-phenyl yl]-6-(4-methoxyphenyl)-1,3,5-triazine, 2,4,6-tris[ 4-(2-ethylhexyloxycarbonyl)anilino-1,3,5-triazine It is more preferred by et al.
[0078] The ultraviolet absorber may be a commercially available product or may be synthesized.
[0079] Commercially available products include, but are not limited to, Uvinul MC80 (BASF (manufactured by DSM Nutrition Japan), Parsol 1789 (manufactured by DSM Nutrition Japan), etc. They can be used in combination.
[0080] The total content of the ultraviolet absorber relative to the total amount of the external skin composition is preferably 1 to 20% by mass. , more preferably 3 to 20 mass %, even more preferably 5 to 20 mass %, and particularly preferably Preferably, it is 6 to 20 mass %, and most preferably 7 to 15 mass %.
[0081] In the topical skin composition of the present invention, the content ratio of the ultraviolet absorber to component (A) is Although not particularly limited, it is preferable that the amount of the hydroxyl group is 0.6 to 2 parts by mass per 1 part by mass of the total amount of the component (A). The amount is preferably 1 to 2 parts by mass, and more preferably 1.4 to 2 parts by mass.
[0082] (UV protection agent) Examples of ultraviolet protection agents include zinc oxide, titanium oxide, iron oxide, cerium oxide, and Zirconium, titanium silicate, zinc silicate, anhydrous silicic acid, cerium silicate, hydrous silicic acid, etc. Inorganic compounds such as hydrated silica, aluminum hydroxide, mica, and talc It is coated with inorganic powder such as acrylic, or made of polyamide, polyethylene, polyester, polystyrene , composites with resin powder such as nylon, silicone oil, and fatty acid aluminum salts , alkyl titanate, etc. Among them, zinc oxide, titanium oxide, etc. Inorganic compounds such as iron oxide, and the like, and the combination of these inorganic compounds with aluminum hydroxide, hydrous silica, malic acid, etc. It is preferable to use inorganic powder such as talc or silicone oil as the coating. When the amount of the active ingredient is added, the amount of the active ingredient can be appropriately selected in consideration of the feeling on the skin and the effect of the active ingredient. For example, 0.001 to 35% by mass, preferably 0.1 to 1% by mass, based on the total amount of the topical skin composition. 0% by mass.
[0083] In the present invention, the ultraviolet absorber or ultraviolet protection agent may be, but is not limited to, another component. The combination of these is not particularly limited. .
[0084] (whitening ingredient) The topical skin composition of the present invention can contain a whitening ingredient other than nicotinamide. For example, placenta, arbutin, rucinol, chamomilla ET, hydroquinone, Tocopherol (α, β, δ, etc.), plant extracts (e.g., iris root extract, artichoke extract, etc.) Month oil, aloe vera extract, acerola extract, rhizome extract, Scutellaria root extract, Glycine extract, Nettle extract, Seaweed extract, Pueraria root extract, Chamomile extract, Peony extract, Morus alba extract, soybean extract, tea extract, white tea extract, Calendula, Hamamelis, Job's Tears, Job's Tears Extract, Hop Extract, Prune Extract Liquid, licorice extract, oil-soluble licorice extract, meadowsweet extract, purple bark extract Alpinia Katsumadai Seed Extract, Grape Fruit Extract, Rosa Izayoi Extract, Lemon extract, kiwi extract, pine extract, neem leaf extract, artichoke extract, Horsetail extract, bark extract, evening primrose extract, evening primrose oil, bilberry leaf extract , Geranium globulus extract, Salicornia herb extract, White willow extract, Centella asiatica extract , and Cornus fruit extract, etc.) are listed. Among them, α-tocopherol, δ-tocopherol Ferrol, β-tocopherol, Iris root extract, Aloe vera extract, Acerola extract, Angelica extract, Scutellaria root extract, St. John's wort extract, Dead nettle extract, Seaweed extract , Pueraria lobata extract, Chamomile extract, Peony extract, Soybean extract Kisu, tea extract, Shirocha extract, calendula extract, witch hazel extract, Yokui Nin, Job's Tears Extract, Prune Extract, Licorice Extract, Oil-Soluble Licorice Extract, Alcohol Pinia Katsumadai seed extract, Grape fruit extract, Rosa rosa extract, Lemon extract Kiss, kiwi extract, artichoke extract, horsetail extract, barley extract, Japanese pine Night primrose extract, evening primrose oil, bilberry leaf extract, Geranium extract, Salicornia extract extract, white willow extract, Centella asiatica extract, and Cornus cherry fruit extract One or more of the following are preferred.
[0085] The skin external application composition of the present invention contains the above-described whitening ingredient other than nicotinamide. When blended, the amount of the ingredient can be selected appropriately taking into consideration the feel and effect on the skin. For example, when using ingredients other than plant extracts, the content of the ingredients other than plant extracts relative to the total amount of the external composition is, for example, 0. When using plant extracts, the content is calculated as the extract equivalent. and, for example, 0.00001 to 20% by mass, preferably 0.00001 to 20% by mass, based on the total amount of the composition for external use on skin. , 0.001 to 10% by mass.
[0086] (Anti-inflammatory ingredient) Anti-inflammatory ingredients include, for example, those derived from plants (e.g., comfrey, coptis, and houttuynia cordata). Ingredients derived from the ingredients: calamine, allantoin, zinc oxide, pyridoxine hydrochloride, acetic acid Tocopherol, menthol, camphor, turpentine, ufenamate, bufexamac , ibuprofen piconol, azulene and its derivatives (e.g., guaiazulene, azulene) When an anti-inflammatory component is added, the anti-inflammatory component of the present invention may be used. For example, 0.0003 to 10% by mass, preferably 0. The content is 0.01 to 5 mass %.
[0087] (acid mucopolysaccharides) Acidic mucopolysaccharides include hyaluronic acid and heparinoids.
[0088] Hyaluronic acid extracted from animal tissues and microorganisms generally has an average molecular weight of about 10 The present invention is based on the idea that the molecular weight of the polymer is 100,000 or more, and that the polymer has an extremely high molecular weight. Hyaluronic acid of molecular weight may be used, or high molecular weight hyaluronic acid may be decomposed or fermented by microorganisms. Low molecular weight hyaluronic acid and hyaluronic acid oligosaccharides (tetrasaccharides, hexasaccharides, octasaccharides, etc.) obtained by the above method , using unsaturated hyaluronic acid (having double bonds at the 4th and 5th positions of D-glucuronic acid) Good too.
[0089] Salts of hyaluronic acid or its derivatives are also usable, as long as they are pharmacologically or physiologically acceptable. Examples include, but are not limited to, alkali metals such as sodium and potassium, calcium, magnesium, etc. Examples of the salt include salts with alkaline earth metals such as sodium, and metals such as aluminum. Preferably, the salt of hyaluronic acid or a derivative thereof is a sodium salt, a potassium salt, A zinc salt is used.
[0090] Heparinoids are a general term for polysulfated mucopolysaccharides such as chondroitin polysulfate. 0.5 to 5 molecules on average, preferably 0.6 to 3 molecules on average, per monosaccharide molecule constituting the copolysaccharide More specifically, the heparinoid preferably has a sulfate group of heparin, Contains chondroitin sulfate D and chondroitin sulfate E, also known as droitin polysulfates. do.
[0091] In the present invention, such acidic mucopolysaccharides include, but are not limited to, hyaluronic acid, Acid, low molecular weight hyaluronic acid, hyaluronic acid oligosaccharide (tetrasaccharide), acetylated hyaluronic acid, Thionated hyaluronic acid, hydrolyzed alkyl hyaluronate (C12-13) glyceryl, crosslinked Bridge-type hyaluronic acid, carboxymethyl hyaluronic acid, alkylene glycol hyaluronate , hyaluronic acid dimethylsilanol, heparinoids and / or salts thereof are preferred. Hyaluronic acid, low molecular weight hyaluronic acid, acetylated hyaluronic acid, hyaluronic acid hydrochloride Hyaluronic Acid Propylene Glycol, Carboxymethyl Hyaluronic Acid, Propylene Glycol Recall, sodium hyaluronate, zinc hyaluronate, low molecular weight zinc hyaluronate, acetonitrile Calcium carbonated sodium hyaluronate, sodium hyaluronic acid crosspolymer, and heparin Similar substances are more preferred, such as sodium hyaluronate, zinc hyaluronate, and low molecular weight hyaluronate. Zinc phosphate, acetylated hyaluronic acid, hydroxypropyltrimonium hyaluronate, Propylene glycol hyaluronate, sodium hyaluronate crosspolymer, and heparin Even more preferred are benzophenone analogs.
[0092] The acidic mucopolysaccharides may be commercially available products or may be synthesized. .
[0093] Such acidic mucopolysaccharides include In the composition for external use on skin of the present invention, the amount of the compound is preferably 0.0001 to 1 % by mass, and more preferably 0.001 to 0.5% by mass.
[0094] [Other ingredients] The composition for external use on skin of the present invention may contain component (A), component (B), and the like, to the extent that the effect of the present invention is not impaired. In addition to the component (C), other components may be included. Specific examples of other components include: Examples of such ingredients include cooling ingredients, moisturizing ingredients, antibacterial or antiseptic ingredients, vitamins, amino acids, or the like. Derivatives, cell activating ingredients, anti-aging ingredients, blood circulation promoting ingredients, keratin softening ingredients, astringent ingredients, anti Examples include glycated components, peptides or derivatives thereof.
[0095] Examples of cooling ingredients include camphor and menthol (e.g., l-menthol, dl- Menthol, Menthyl Glyceryl Ether, Menthyl Lactate, Menthyl 3-Hydroxybutyrate acrylate, menthoxypropanediol, menthyl succinate, etc.), borneol, eugenol Monoterpenes such as ethanol, cineole, thymol, bisabolol, α-pinene, or limonene Sesquiterpenes such as cinnamon, diterpenes, eucalyptus oil, peppermint oil, clove oil, cinnamon oil, Parmint oil, mint oil, tea tree oil, chamomile oil, rosemary oil, lemon oil, Examples of essential oils include orange oil, thyme oil, sage oil, and clove oil.
[0096] Moisturizing ingredients include, for example, sodium hyaluronate, heparinoids, and chondroitin. such as sodium cellulose sulfate, collagen, elastin, keratin, chitin, and chitosan High molecular weight compounds or their hydrolysates; amino acids such as glycine and arginine; urea, and Natural moisturizing factors such as cellulose; lipids such as ceramides and phospholipids; trimethylglycine ( Betaine; Hydroxyethylurea; Acrylic acid, acrylamide, dimethyl chloride aryl ammonium copolymer; and Job's Tears seed extract, Artemisia princeps leaf extract, Chamomile Kiss, Hamamelis extract, Birch sap, Salicornia extract, Lilac extract, Tea extract, lavender oil, and plant extracts such as perilla extract; placenta extract, etc. Animal extracts, etc.
[0097] Examples of antibacterial or disinfectant ingredients include chlorhexidine, benzalkonium chloride, and Linoleic acid, sulfur, resorcinol, ethanol, benzethonium chloride, adapalene, peroxide Benzoyl, clindamycin, cresol, gluconic acid and its derivatives, povidone-iodine , potassium iodide, iodine, triclocarban, triclosan, photosensitizer No. 101, photosensitizer No. 201 No., phenoxyethanol, alkyldiaminoglycine hydrochloride, chlorhexidine gluconate Examples include zinc paraphenolsulfonate, picroton olamine, and miconazole. It can be obtained.
[0098] Vitamins include, for example, retinol derivatives (retinol, retinol acetate, palm oil, etc.) Vitamin A compounds such as retinol mitate, tocopheryl retinoate, tocopherol, Vitamin E compounds such as tocopherol acetate; Vitamin B2 compounds such as riboflavin; nicotinic acid Nicotinic acids other than nicotinic acid, vitamin D, vitamin K, gamma-oryzanol, vitamin B Vitamin B6 (pyridoxine hydrochloride, etc.); Vitamin B12; Folic acid; Panthenol pantothenic acids such as niacin, biotins, and vitamins such as carnitine and pyrroloquinoline quinone. Examples include agonist-like factors.
[0099] Examples of amino acids or derivatives thereof include betaine (trimethylglycine), proline hydroxyproline, arginine, lysine, serine, glycine, alanine, phenyl Alanine, β-alanine, threonine, glutamine, asparagine, aspartic acid, Stain, cystine, methionine, leucine, isoleucine, valine, histidine, tau Phosphorus, gamma-aminobutyric acid, gamma-amino-beta-hydroxybutyric acid, carnitine, carnosine, and chlorine Examples include reatine.
[0100] Examples of cell activation components include vitamins (retinol, thiamine, riboflavin, etc.) , pyridoxine hydrochloride, pantothenic acid pyrroloquinoline quinones, etc.); tannins, flavonoids Iodide, saponin, allantoin, placenta, proteoglycan, photosensitizer No. 301, plant extract Kiss (e.g., soybean, bilberry, lemongrass, aloe vera, chlorella, bead tree, Extracts of coix seed, chamomile, Houttuynia cordata, hops, carrots, etc.); royal jelly, Royal jelly extract; whey, yogurt extract, hydrolyzed milk protein, and other whey-derived extracts Examples of anti-aging ingredients include hydrolyzed soybean protein, yeast extract, etc. Pak, retinoids (retinol, retinoic acid, retinal, etc.), astaxanthin, Enzyme Q10, pangamic acid, ursolic acid, turmeric extract, sphingosine derivative , silicon, silicic acid, N-methyl-L-serine, mevalonolactone, peptides (caproic acid yltetrapeptide-3, oligopeptide-24, etc.), plant extracts (e.g., artichoke, Chalk, Rosa rugosa, seaweed, bilberry, birch, plantain, angelica, Ugon, St. John's wort, comfrey, neem, wild rose, blackberry, lady's wort, linden tree Among them, cell activating components and / or anti-aging components are Preventive ingredients include hydrolyzed soy protein, retinol, retinol acetate, and retinyl palmitate. Tinol, Caprooyl Tetrapeptide-3, Oligopeptide-24, Artichoke Leaf extract, seaweed extract, bilberry leaf extract, comfrey leaf extract, neem leaf extract, Geranium globulus extract is preferred.
[0101] Examples of blood circulation promoting ingredients include plants (e.g., ginseng, angelica tree, aloe vera, etc.). Nikka, ginkgo, fennel, emmeiso, Dutch oak, chamomile, Rhoma , carrot, gentian, burdock, rice, hawthorn, shiitake mushroom, hawthorn, sei Common juniper, Cnidium officinalis, Swertia japonica, Thyme, Clove, Citrus fruit, Angelica acutiloba, Peony, and Tou Carrots, garlic, butcherbloom, grapes, peonies, horse chestnuts, melissa, yuzu Zucchini, coix seed, rosemary, rose hip, tangerine, angelica tree, spruce, peach, apricot, Ingredients derived from walnuts and corn; dl-α-tocopherol acetate, nicotine Tocopherol acid, glucosyl hesperidin, hesperidin and glucosyl hesperidin Examples include:
[0102] Examples of keratin softening ingredients include lanolin, urea, and sulfur.
[0103] Examples of astringent ingredients include zinc paraphenolsulfonate, zinc oxide, menthol, and ethanol.
[0104] Examples of anti-glycation ingredients include Budreja axillaris leaf extract, plum fruit extract, and -Delweiss extract, ginkgo extract, cherry leaf extract, pomegranate extract, osmanthus leaf extract Co-extract, Hawthorn extract, Peony extract, Houttuynia cordata extract, Bilberry leaf Extract, green tea extract, black tea extract, horse chestnut extract, Roman chamomile extract, mugwort extract Plant extracts such as ginger, evening primrose oil, amla fruit, fruit juice or their extracts, L-arginine Examples include lactic acid bacteria, L-lysine, hydrolyzed casein, hydrolyzed tannins, and carnosine. .
[0105] Examples of peptides or derivatives thereof include keratin decomposition peptides and hydrolyzed keratin. , collagen, fish-derived collagen, atelocollagen, succinylated atelocollagen, Gelatin, elastin, elastin decomposition peptides, collagen decomposition peptides, hydrolyzed collagen collagen, hydroxypropyl ammonium chloride hydrolyzed collagen, elastin hydrolyzed peptide Peptide, conchiolin decomposition peptide, hydrolyzed conchiolin, silk protein decomposition peptide, Hydrolyzed silk, sodium lauroyl hydrolyzed silk, soy protein hydrolyzed peptide, dehydrated Soy protein, wheat protein, wheat proteolysis peptides, hydrolyzed wheat protein, casein hydrolysis peptides Peptides, acylated peptides (palmitoyl oligopeptides, palmitoyl pentapeptides, palmitoyl lumitoyl tetrapeptide, etc.).
[0106] The other components can be used alone or in combination of two or more. The present invention is not limited to the above, and known ingredients that are blended in external skin preparations such as cosmetics and pharmaceuticals can be used as appropriate. Cut.
[0107] [Base or carrier] The composition for external use on skin of the present invention is preferably a composition that does not interfere with the effects of the present invention from the viewpoints of improving the feeling of use, stability, etc. Unless otherwise specified, the composition does not contain a base or carrier in addition to the above components (A), (B), and (C). The base or carrier may be, for example, polyethylene glycol; glycol ether; esters; lower alcohols such as ethanol and isopropanol; oils; surfactants; thickeners These include, but are not limited to, cosmetics, pharmaceuticals, and other skin care products. Known components that are useful for the preparation of cellulose acetate may be used.
[0108] In the topical skin composition of the present invention, an oil may be used as a base or carrier. Such oils include, for example, hydrocarbon oils, ester oils, fats and oils, silicone oils, and the like. Specifically, liquid paraffin, liquid isoparaffin, Hydrocarbons such as warane, vaseline, gelled hydrocarbons, α-olefin oligomers; Crosslinked methylpolysiloxane, highly polymerized methylpolysiloxane, phenyl-modified silicone silicones such as cyclosilicone, polyether-modified silicone; higher alcohols ;Higher fatty acids;Isopropyl myristate, octyldodecyl myristate, palmitic Isopropyl Palmitate, Cetyl Palmitate, Isononyl Isononanoate, Diisopropyl Adipate Pill, Decyl Oleate, Isodecyl Oleate, Hexyldecyl Dimethyloctanoate, Diisopropyl sebacate, di-2-ethylhexyl sebacate, 2-hexyl myristate Sildecyl, 2-hexyldecyl palmitate, diisopropyl adipate, isononane Isotridecyl Lactate, Cetyl Lactate, Isostearyl Isostearate, 12-Hydroxystearate Cholesteryl tearic acid, cholesteryl stearate, cholesteryl oleate, macadamia Mia nut fatty acid phytosteryl, oleic acid phytosteryl, palmitic acid dextrin Inulin stearate, hydrogenated jojoba oil, ethylene glycol di-2-ethylhexyl Cole, dipentaerythritol fatty acid ester, neopentyl glycol dicaprate , Tri-2-ethylhexyl trimellitate, Tritridecyl trimellitate, Tri-2-ethyl Trimethylolpropane dihexylester, Trimethylolpropane triisostearate, Pentaerythritol tetra-2-ethylhexanoate, Glycerin tri-2-ethylhexanoate Serine, Trimethylolpropane Triisostearate, Caprylic / Capric Triglyceride ) Glyceryl, Tri(Caprylic / Capric / Myristic / Stearic)glycerin oleyl oleate, phytosteryl / octyldodecyl lauroyl glutamate Lauroyl glutamate (octyldodecyl / phytosteryl / behenyl), Triethyl enoate, Dimer dilinoleate (phytosteryl / isostearyl / cetyl / Stearyl / Behenyl), Dimer Dilinoleyl Dimer Dilinoleate, Tripolyhydrochloride Dipentaerythrityl Dihydroxystearate, Tri(behenic acid / isostearate / eicosane) Diacid) glyceryl esters, etc.; jojoba oil, beaucopa wax, etc.; avocado oil, macadamia Mia nut oil, kukui nut oil, hazelnut oil, corn oil, olive oil, safflower Rose oil, apricot kernel oil, cinnamon oil, jojoba oil, grape seed oil, sunflower oil, almond oil Oil, shea butter, camellia oil, rapeseed oil, sesame oil, cocoa butter, coconut oil, hardened coconut oil, palm Oil, palm kernel oil, Japanese laurel kernel oil, Japanese laurel, wheat germ oil, rice germ oil, rice bran oil, cottonseed oil, Examples of oils and fats include soybean oil, peanut oil, tea seed oil, evening primrose oil, and shea butter.
[0109] In the topical skin composition of the present invention, a surfactant that functions as a base or carrier is used. Such bases or carriers include, for example, sorbitan stearate, ceteth- Sorbitan sucrose, sorbitan oleate, sorbitan isostearate, laurate Sorbitan fatty acid esters such as sorbitan phosphate and sorbitan olive oil fatty acid; monola Polyoxyethylene (20) sorbitan laurate, polyoxyethylene monolaurate ( 80) Sorbitan, Polyoxyethylene Monostearate (20) Sorbitan, Monooleate Polyoxyethylene (20) sorbitan isostearate, Polyoxyethylene ( 20) Polyoxyethylene sorbitan fatty acid esters such as sorbitan; glycerin monoesters Glycerin fats such as glycerin monostearate, glycerin monomyristate, etc. Fatty acid esters: monoisostearyl glyceryl ether, monomyristyl glyceryl ether Glycerin alkyl ethers such as diglyceryl monostearate, decaglyceryl Decastearate, Decaglyceryl Decisostearate, Diglyceryl Diisostearate polyglycerol fatty acid esters such as propylene glycol monostearate; propylene glycol fatty acid esters; polyethylene glycol monostearate and other poly Polyethylene glycol fatty acid esters; Polyoxyethylene hydrogenated castor oil 40, Polyoxyethylene Polyoxyethylene hydrogenated castor oil 50, Polyoxyethylene hydrogenated castor oil 60, Polyoxyethylene Hydrogenated castor oil derivatives such as ethylene hydrogenated castor oil 80; polyoxyethylene mono-coconut oil fatty acid glycerol Polyoxyethylene glycerin fatty acid esters such as lyceryl; polyoxyethylene phyto Sterol, Polyoxyethylene phytostanol, Polyoxyethylene cholestanol Polyoxyethylene sterols, hydrogenated sterols, sucrose fatty acid esters, etc. N-acetyl esters such as tertiary carboxylic acid salts, alkyl phosphate ester salts, and sodium cocoyl glycinate Amino acid salts, acylated taurates; amines such as stearylamine and oleylamine Polyoxyethylene-methylpolysiloxane copolymer, lauryl PEG-9 polysiloxane Tylsiloxyethyl Dimethicone, PEG-9 Polydimethylsiloxyethyl Dimethicone, etc. Silicone surfactants or lecithin, hydrogenated lecithin, saponin, surfac Examples include naturally derived surfactants such as sodium tin, cholesterol, and bile acids. However, it is not limited to these.
[0110] Examples of thickeners include guar gum, locust bean gum, carrageenan, and xanthan gum. Tan gum, sclerotium gum, xanthan gum, gellan gum, dextran, pectin pullulan, agar, polyvinyl alcohol, polyvinylpyrrolidone, carboxyvinyl Polymer, acrylic acid alkyl methacrylate copolymer, (hydroxyethyl acrylate / Acryloyldimethyltaurate Na) Copolymer, (Sodium Acrylate / Acryloyldimethyltaurate Na) Copolymer Chiltaurate (Na) copolymer, polyacrylic acid amide, polyethylene glycol, aluminum Alginic acid, sodium alginate, propylene glycol alginate, macrogol cellulose, such as hydroxyethyl cellulose, sodium chondroitin sulfate, cellulose-based thickeners (hydroxyethyl cellulose, hydroxypropyl methylcellulose, Hydroxypropyl cellulose, hydrophobized hydroxypropyl methylcellulose, carboxy methyl cellulose, etc.)
[0111] The base or carrier may be used alone or in combination of two or more.
[0112] [Additives] The topical skin composition of the present invention may contain pharmaceuticals and quasi-drugs within the scope of the present invention without impairing the effects of the present invention. or known additives added to cosmetics, such as antioxidants, pH adjusters, stabilizers, Coloring agents, fragrances, powder and / or pearlescent luster imparting agents, irritation reducing agents, etc. may be added. .
[0113] Examples of antioxidants include dibutylhydroxytoluene and butylhydroxyanisole. Sodium sulfite, tocopherol, tocopherol derivatives, and L-cysteine salts Acid salts and the like.
[0114] Examples of pH adjusters include inorganic acids and organic bases.
[0115] Examples of stabilizers include sodium polyacrylate and dibutylhydroxytoluene. Examples of the irritation reducer include sweeteners, Herbal extracts and sodium alginate.
[0116] Colorants include pigment-grade titanium oxide, zinc oxide, iron oxide, organic pigments, talc, and sericite. Examples of suitable materials include chromium oxide, mica, synthetic mica, chromium oxide, and ultramarine.
[0117] Powder may also be added to improve texture or to impart a makeup effect. Boron nitride, silica, alumina, aluminum hydroxide, metal soap, silicone powder, poly Examples thereof include methyl methacrylate.
[0118] The additives can be used alone or in combination of two or more. There are no restrictions on the ingredients, and known ingredients that are blended in external skin preparations such as cosmetics and pharmaceuticals can be used as appropriate. .
[0119] [pH] The composition for external application to the skin of the present invention may generally have a pH of 2.0 to 9.0. From the viewpoint of low irritation to the skin and mucous membranes and good skin feel, a pH of 3 is preferable. pH 4.0 to 8.5, more preferably pH 4.0 to 8.0, and even more preferably pH 4.5 to 7.5, and even more preferably, pH 5.0 to 7.5.
[0120] [Method of manufacturing a composition for external use on skin] The method for producing the topical skin composition of the present invention is not particularly limited, and in addition to the above components (A) to (C), The above-mentioned other useful ingredients, other ingredients, bases, carriers, additives, etc., may be added as needed. The composition can be produced by selecting, blending, and emulsifying, if necessary, in a conventional manner.
[0121] [Properties and formulation] The form of the external skin composition of the present invention is not particularly limited, and may be liquid, fluid, or semi-solid. The formulation may be, for example, a liquid, a suspension, an emulsion, a cream, Emulsion, ointment, gel, liniment, lotion, aerosol, nonwoven fabric containing medicinal liquid It can be formulated as a sheet or stick containing the substance. Suitable formulations include creams, emulsions, ointments, gels, lotions, sheets, and sticks. Creams, emulsions, gels, lotions, and sheets are particularly suitable. When a formulation contains both an oily base and an aqueous base, such as a cream or ointment, it can be either a W / O type or an O / W type. However, the feeling of use of the topical skin composition of the present invention (stickiness, spreadability, moist feeling, fresh feeling) From the viewpoint of softness, penetration, etc., O / W types are more preferable.
[0122] [Usage] Specific uses of the composition for external use as a quasi-drug or cosmetic include, for example: Lotion, emulsion, gel, cream, serum, sunscreen, pack, mask, oil Ruin One Gel, Hand Cream, Body Lotion, Wipes and Body Cleanser as well as face washes, hand soaps, makeup removers, and body shampoos. Cleansing cosmetics such as shampoo, rinse, and treatment, BB cream, Foundation, makeup base, and other face makeup cosmetics, lip balm, lip Lip cosmetics such as liners and lip gels; hair rinses and hair treatments; Hair conditioner, hair gel, hair mousse, hair mist, hair lotion, style Among these, external use compositions for skin are That is, the composition for external use of the present invention is particularly preferred for use in pharmaceuticals, quasi-drugs, or cosmetics. The external composition for skin can be prepared as a composition for external use. In addition, the bases or carriers, additives, and active ingredients that can be used, as well as These preferences are the same as those for the topical composition of the present invention.
[0123] [container] The topical skin composition of the present invention can be packaged in a container of a shape and material appropriately selected depending on the purpose and application of the composition. Specific containers include spray types, bottles, etc. Tor type, tube type, jar type, dropper type, dispenser type, Examples of the external skin composition of the present invention include a stick type, a pouch bag, and a cheer pack. The product can be used in a desirable state from the viewpoint of ease of removal from the container, and therefore This allows for greater freedom in designing formulations containing nicotinamide at a concentration of: Even with high-concentration nicotinamide-containing formulations, it is not only suitable for jars and sticks, but also for sprays. It can be easily used in a wide variety of containers, including bottles, tubes and dispensers. It becomes Noh.
[0124] The container material is polyethylene terephthalate, polypropylene, polyethylene Polyethylene (HDPE, LDPE, LLDPE, etc.), ABS resin, ethylene vinyl alcohol resin Examples of suitable materials include plastic, polystyrene, glass, and metal (aluminum, etc.). The material is given various coating treatments taking into consideration strength, flexibility, weather resistance, and stability of the ingredients. These materials can be combined, for example, by mixing or laminating them to form container materials. Among them, polypropylene, polyethylene (HDPE, LDPE) PE, LLDPE, etc.), ethylene vinyl alcohol resin, metal (aluminum, etc.) is preferred.
[0125] [How to use, etc.] The topical skin composition of the present invention is expected to have the following effects: promoting blood circulation, anti-inflammatory properties, etc., due to the physiological activity of nicotinamide. It can be suitably used for the purpose of whitening, anti-wrinkle, anti-aging, and promoting ceramide synthesis. It is expected to have a brightening effect and is useful as a multi-functional formulation, including as a whitening agent and sunscreen. The topical skin composition of the present invention can be administered once or several times a day depending on the intended use. It can be used in known or customary dosages and administration.
[0126] [Precipitation suppression method] In another embodiment, the present invention relates to a method for preparing a topical skin composition containing (A) nicotinamide. It is also possible to provide a method for inhibiting bleeding, comprising: (A) nicotinamide; (B) a preservative; and (C) By preparing a composition for external use on the skin containing an organic acid, an organic acid salt, or an amphiphilic compound, This makes it possible to achieve inhibition of deposition of the topical skin composition.
[0127] As used herein, the term "precipitation" refers to, for example, the form in which the topical skin composition of the present invention is deposited. However, the components may appear as solids (e.g., solid precipitates, needle-like crystals, or fuzzy particles). It may be a visible deposit or a deposit that is difficult to detect by visual inspection. The degree of precipitation and the transparency of the solution were checked using a turbidity meter and an ultraviolet, visible, and infrared spectrophotometer (Model V-7 For example, the composition for external use on the skin of the present invention can be detected by a water-based method. When prepared as a composition, it is preferable that the composition is colorless and transparent. Precipitation may occur over time. Precipitation inhibition means preventing or delaying such precipitation. This also includes increasing and decreasing. [Example]
[0128] Next, the present invention will be described in detail with reference to examples, but the present invention is not limited to the following examples. It's not something like that.
[0129] The components used in the examples are as follows. The numerical values in each table correspond to the component names. This is the content of the ingredient itself.
[0130] Polyoxypropylene methyl glucoside (10P.O.): Macbiobride MG-1 0P (NOF Corporation) Polyoxyethylene polyoxypropylene butyl ether (17E.O.) (17P. O.): Unilube 50MB-26 (manufactured by NOF Corporation) Polyoxyethylene Polyoxypropylene Glyceryl Ether (24E.O.) (24 PO): Unilube 50TG-32 (NOF Corporation) Polyoxyethylene polyoxypropylene butyl ether (37E.O.) (38P.O .): Unilube 50MB-168 (manufactured by NOF Corporation) Polyoxybutylene polyoxyethylene polyoxypropylene methyl glucoside: Lubride MG2070 (manufactured by NOF Corporation) Polyoxypropylene diglyceryl ether (14P.O.): SY-DP14 (Sakamoto (Manufactured by Yakuhin Kogyo Co., Ltd.) Polyoxypropylene diglyceryl ether (9P.O.): SY-DP9 (Sakamoto Pharmaceuticals) (Manufactured by Kogyo Co., Ltd.) 2-Methacryloyloxyethylphosphorylcholine-Butyl Methacrylate Copolymer:L ipidure-PMB(BG) (NOF Corporation) Polyoxypropylene sorbitan (25P.O.): Uniol HS-1600D (Japan (manufactured by Yuru Co., Ltd.).
[0131] [Low temperature storage test] The compositions shown in Tables 1 to 7 were prepared by a conventional method, and 20 mL of each sample was placed in a 20 mL glass bottle. These compositions were stored in a constant temperature bath at 4°C for one week to allow the precipitation of crystals. The presence or absence of leakage was confirmed visually.
[0132] The results are also shown in Tables 1 to 7. All values in the tables are in mass %.
[0133] [Table 1]
[0134] [Table 2]
[0135] [Table 3]
[0136] [Table 4]
[0137] [Table 5]
[0138] [Table 6]
[0139] [Table 7]
[0140] As shown in Tables 1 to 7, in the comparative examples, the components (B) preservatives and (C) organic acids and organic acid salts When the compound is mixed with an organic acid derivative or an amphiphilic component, precipitation occurs. On the other hand, in the examples, (A) nicotinamide was further contained. In particular, as shown in Table 7, when (C (C-1) tranexamic acid as the component and (C-2) 2-methacryloyloxyethyl methyl methacrylate as the component The addition of methylphosphorylcholine-butyl methacrylate copolymer also showed a similar effect in inhibiting precipitation. The results were observed.
[0141] Furthermore, the compositions of the examples shown in Tables 1 to 7 also had an excellent feel when used.
[0142] [Formulation example] Compositions for external use on the skin of the present invention were prepared based on the formulations shown in Tables 8 to 28 below. The numerical values represent mass %.
[0143] [Table 8]
[0144] [Table 9]
[0145] [Table 10]
[0146] [Table 11]
[0147] [Table 12]
[0148] [Table 13]
[0149] [Table 14]
[0150] [Table 15]
[0151] [Table 16]
[0152] [Table 17]
[0153] Table 18
[0154] Table 19
[0155] Table 20
[0156] Table 21
[0157] Table 22
[0158] Table 23
[0159] Table 24
[0160] Table 25
[0161] Table 26
[0162] Table 27
[0163] [Table 28]
[0164] [Table 29] TIFF2026010127000034.tif170170
[0165] [Table 30]
[0166] [Table 31]
[0167] [Table 32]
[0168] In all formulation examples, a topical skin composition that does not precipitate over time and has a good feel when used was obtained. can be done.
Claims
[Claim 1] (A) nicotinamide (niacinamide) 3 to 10% by mass; (B) a preservative; and (C) 1 to 2% by mass of one or more selected from the group consisting of tranexamic acid and salts thereof; Contains A composition for topical application to skin may optionally contain, as an amphiphilic compound, one or more compounds selected from the group consisting of 2-methacryloyloxyethyl phosphorylcholine / butyl methacrylate copolymer (polyquaternium-51), polymethacryloyloxyethyl phosphorylcholine, bisethoxydiglycol cyclohexanedicarboxylate, polyglyceryl-10 (eicosadioate / tetradecanedioate), polyoxyethylene polyoxypropylene butyl ether, polyoxyethylene polyoxypropylene decyltetradecyl ether, polyoxyethylene glycerin, polyoxyethylene polyoxypropylene glyceryl ether, polyoxybutylene polyoxyethylene polyoxypropylene glyceryl ether, polyoxyethylene methyl glucoside, polyoxypropylene methyl glucoside, polyoxybutylene polyoxyethylene polyoxypropylene methyl glucoside, and polyoxyethylene polyoxypropylene glycol.
Citation Information
Patent Citations
Cosmetic for preventing aging of skin
JP1998130135A
Bleaching agent and vitamin-mixed composition
JP2004217629A