Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
  • A61K8/362—Polycarboxylic acids
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
  • A61K8/365—Hydroxycarboxylic acids; Ketocarboxylic acids
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/37—Esters of carboxylic acids
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/39—Derivatives containing from 2 to 10 oxyalkylene groups
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
  • A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/67—Vitamins
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
  • A61Q17/04—Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q19/00—Preparations for care of the skin

Definitions

• the present invention relates to an external composition for skin. More particularly, the present invention relates to a topical skin composition containing nicotinamide.
• Patent Document 1 proposes a whitening agent containing at least one selected from the group consisting of riboflavin, pyridoxine hydrochloride, nicotinic acid amide, and calcium pantothenate as an active ingredient.
• Patent Document 2 is characterized by containing (a) nicotinic acid amide and (b) one or more kinds selected from the group consisting of urea and an ⁇ -hydroxycarboxylic acid compound having 2 to 28 carbon atoms. Skin anti-aging cosmetics have been proposed.
• the object of the present invention is to provide a composition for external use on the skin in which precipitation is suppressed even if the composition contains a preservative and an organic acid or an amphipathic component.
• the present invention provides the following external composition for skin.
• Item 1. (A) Nicotinic acid amide 3% by mass or more; An external skin composition containing (B) a preservative; and (C) at least one selected from the group consisting of an organic acid, an organic acid salt, a derivative of an organic acid, and an amphipathic compound.
• the component (C) is Tranexamic acid or its salt, lactic acid or its salt, citric acid or its salt, succinic acid or its salt, salicylic acid or its salt, gluconic acid or its salt, phytic acid or its salt, tartaric acid or its salt, ascorbic acid phosphate Item 2.
• the item according to Item 1 which is at least one selected from the group consisting of sodium, magnesium ascorbyl phosphate, 2-O-ethylascorbic acid, 3-O-ethylascorbic acid, and ascorbic acid-2-glucoside.
• the component (C) is one or two selected from the group consisting of a compound represented by the following general formula (I), a phosphorylcholine-containing polymer, a divalent carboxylic acid ester, and an alkanediol having 5 to 10 carbon atoms.
• the external composition for skin according to Item 1 or 2 above:
• Z represents a hydrogen atom or a residue obtained by removing n hydroxy groups from a hydroxy compound having 1 to 30 carbon atoms;
• AO means an oxyalkylene group having 3-4 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 mean the average number of moles of addition of AO, EO, and BO, and are independently 0 to 200.
• a, b, and c are not all 0.
• n is 2 or more, a, b and c may be the same or different.
• Z is a hydrogen atom, n is 1.
• the AO and EO may be added randomly or in the form of blocks.
• the component (C) is a compound represented by the following general formula (II), 2-methacryloyloxyethylphosphorylcholine/butyl methacrylate copolymer, (eicosanedioic acid/tetradecanedioic acid) decaglyceryl, cyclohexanedicarboxylic acid bisethoxy.
• Item 4 The item according to any one of items 1 to 3, which is one or more selected from the group consisting of diglycol, diethylhexyl succinate, diethoxyethyl succinate, and alkanediol having 5 to 10 carbon atoms.
• Topical composition for skin (In the formula, Z represents a hydrogen atom or a residue obtained by removing n hydroxy groups from a hydroxy compound having 1 to 30 carbon atoms; AO means an oxyalkylene group having 3-4 carbon atoms; EO means an oxyethylene group; n means 1 to 9; a and b mean the average number of moles of addition of AO and EO, respectively, and are independently 0 to 200. However, a and b do not all become 0. When n is 2 or more, a and b may be the same or different. When Z is a hydrogen atom, n is 1. The AO and EO may be added randomly or in the form of blocks. ) Item 5.
• Z is a hydrogen atom, or an alkyl monoalcohol having 4 to 24 carbon atoms, glycerin, an alkyl glucoside having 1 to 24 carbon atoms, or diglycerin to n.
• Item 5 The external composition for skin according to Item 3 or 4, which is a residue obtained by removing one hydroxy group.
• the component (B) comprises paraoxybenzoic acid ester, benzoic acid, benzoate, dehydroacetic acid, dehydroacetate, thymol, isopropylmethylphenol, capryl hydroxamic acid, butylcarbamic acid iodopropynyl, butylcarbamic acid iodopropynyl.
• Item 7 The external skin application according to any one of Items 1 to 6, which is at least one selected from the group consisting of a salt, a propynyl iodide butylcarbamate derivative, sorbic acid, a sorbate salt, chlorobutanol, and methylisothiazoline. Composition.
• Items 1 to 6 which is at least one selected from the group consisting of a salt, a propynyl iodide butylcarbamate derivative, sorbic acid, a sorbate salt, chlorobutanol, and methylisothiazoline.
• the external composition for skin according to any one of Items 1 to 10, which is one or more selected from the group consisting of a system ultraviolet absorber, an imidazolesulfonic acid derivative ultraviolet absorber, and a benzophenone derivative ultraviolet absorber.
• the ultraviolet absorber is para-methoxycinnamic acid 2-ethylhexyl, 4-tert-butyl-4′-methoxydibenzoylmethane, 2-[4-(diethylamino)-2-hydroxybenzoyl]benzoic acid hexyl ester, 2,4 -Bis-[ ⁇ 4-(2-ethylhexyloxy)-2-hydroxy ⁇ -phenyl]-6-(4-methoxyphenyl)-1,3,5-triazine, 2,4,6-tris[4-( Any one of items 1 to 11, which is at least one selected from the group consisting of 2-ethylhexyloxycarbonyl)anilino]-1,3,5-triazine and
• the nicotinic acid amide contained in the external composition for skin of the present invention is an amide compound of nicotinic acid (vitamin B 3 /niacin) and is a water-soluble vitamin.
• the nicotinic acid amide may be an extract from a natural product or a product synthesized by a known method. Specifically, those listed in the 17th revised Japanese Pharmacopoeia can be used. In addition to the blood circulation promoting action and the rough skin improving action, a melanin production inhibiting action and a whitening effect are known.
• the antiseptic agent contained in the external composition for skin of the present invention is a compound usually used as a component of the external preparation for skin in the fields of medicines, quasi drugs or cosmetics, which is solid at room temperature (20°C) and It is a water-soluble preservative that can be dissolved in.
• the “water-soluble preservative” may be any preservative that is slightly soluble in water. For example, it may be dissolved in water at a rate of 0.01% or more, preferably at a rate of 0.05% or more.
• alkali metal salts such as sodium and potassium are preferable.
• any one of these compounds may be used alone, or two or more thereof may be used in combination, and among them, paraoxybenzoic acid ester, benzoic acid, benzoic acid salt, dehydroacetic acid, dehydroacetic acid salt.
• Such component (B) is not particularly limited as a commercially available product, but for example, in addition to available reagents, platinum M, ethyl paraoxybenzoate, platinum P, butyl paraoxybenzoate (paraoxybenzoic acid ester) (any Ueno Pharmaceutical Co., Ltd.), methyl paraoxybenzoate, ethyl paraoxybenzoate, propyl paraoxybenzoate (all manufactured by API Corporation); isopropylmethylphenol, thymol (both manufactured by Osaka Kasei Co., Ltd.), IPMP-TN (Tech Noble),; Zeastat, Spectrastat E, G, etc.
• platinum M ethyl paraoxybenzoate
• platinum P butyl paraoxybenzoate
• paraoxybenzoic acid ester any Ueno Pharmaceutical Co., Ltd.
• methyl paraoxybenzoate ethyl paraoxybenzoate
• propyl paraoxybenzoate all manufactured by API Corporation
• capryl hydroxamic acid (capryl hydroxamic acid) (all are manufactured by INOLEX); GLYCASIL, GLYCASIL2000, GLYCASIL L, GLYCASIL S (butyl propionyl iodide butylcarbamate) (All are Lonza). ); Chlorethone (chlorobutanol) (manufactured by Sekisui Medical Co., Ltd.) and the like are used.
• the total content of paraoxybenzoic acid ester based on the total amount of the composition is not particularly limited as long as the effects of the present invention are exhibited.
• the total content of paraoxybenzoic acid ester is preferably 0.001% by mass or more, more preferably 0.005% by mass or more, further preferably 0.01% by mass or more, based on the total amount of the composition.
• the content is more preferably 0.05% by mass or more, and particularly preferably 0.1% by mass or more.
• the content of the paraoxybenzoic acid ester is preferably 1% by mass or less, more preferably 0.7% by mass or less, still more preferably 0.5% by mass or less, and still more preferably, based on the total amount of the composition.
• the total content of paraoxybenzoic acid ester is preferably 0.005 to 1% by mass, more preferably 0.01 to 0.5% by mass, and even more preferably still more preferably to the total amount of the composition. It is preferably 0.05 to 0.3% by mass, and particularly preferably 0.1 to 0.2% by mass.
• the content of benzoic acid or sodium benzoate alone with respect to the total amount of the composition is not particularly limited as long as the effects of the present invention are exhibited.
• the content of benzoic acid or sodium benzoate is preferably 0.001 mass% or more, more preferably 0.005 mass% or more, still more preferably 0.01 mass% or more, relative to the total amount of the composition. Even more preferably, it is 0.05 mass% or more.
• the content of benzoic acid or sodium benzoate is preferably 1% by mass or less, more preferably 0.7% by mass or less, still more preferably 0.5% by mass or less, based on the total amount of the composition. Even more preferably, it is 0.3 mass% or less.
• the total content of benzoic acid or sodium benzoate is preferably 0.005 to 1% by mass, more preferably 0.01 to 0.5% by mass, and further preferably, based on the total amount of the composition. It is 0.05 to 0.3 mass %.
• the component (C) contained in the external composition for skin of the present invention is at least one selected from the group consisting of organic acids, organic acid salts, organic acid derivatives, and amphipathic compounds.
• organic acid ((C-1) Organic Acid, Organic Acid Salt, or Derivative of Organic Acid)
• organic acid salt or the derivative of the organic acid used in the present invention a compound usually used as a component of a skin external preparation in the fields of pharmaceuticals, quasi drugs or cosmetics can be used.
• organic acid for example, ascorbic acid, tranexamic acid, citric acid, salicylic acid, lactic acid, tartaric acid, malic acid, succinic acid, oxalic acid, gluconic acid, fumaric acid, aspartic acid.
• one or more selected from the group consisting of ascorbic acid, tranexamic acid, citric acid, lactic acid, gluconic acid, salicylic acid, tartaric acid, phytic acid, and kojic acid are even more preferable, and ascorbic acid, tranexamic acid, citric acid
• Particularly preferred is one or more selected from the group consisting of lactic acid and lactic acid.
• the organic acid salt refers to a salt of such an organic acid.
• Salts that form organic acid salts are pharmaceutically acceptable salts.
• salts with organic bases for example, salts with tertiary amines such as trimethylamine salt, triethylamine salt, monoethanolamine salt, triethanolamine salt, pyridine salt; bases such as arginine or lysine).
• Ammonium salt or a salt with an inorganic base (for example, inorganic acid salt such as hydrochloride, sulfate, and phosphate: ammonium salt; alkali metal salt such as sodium salt, potassium salt; calcium salt, magnesium salt, etc.
• organic acid salts are triethanolamine salt, monoammonium salt, sodium salt, potassium salt, dipotassium salt, magnesium salt, or zinc salt, and particularly preferable organic acid salt is sodium salt, dipotassium salt, or magnesium salt. Is.
• preferred organic acid salts are sodium ascorbate, tranexamate hydrochloride, calcium tranexamate, sodium salicylate, calcium salicylate, magnesium salicylate, potassium salicylate, sodium lactate, sodium tartrate, sodium citrate, disodium citrate, Trisodium citrate, potassium citrate, sodium succinate, disodium succinate, sodium oxalate, calcium gluconate, zinc gluconate, sodium pyrrolidonecarboxylate, zinc pyrrolidonecarboxylate, sodium glutamate, dipotassium glycyrrhizinate, monoglycyrrhizinate Examples thereof include ammonium, sodium phytate, sodium glycolate, ammonium glycolate and the like.
• One or more selected from the group consisting of sodium and disodium succinate are more preferable, and one selected from the group consisting of sodium ascorbate, sodium lactate, sodium citrate, sodium succinate, and disodium succinate 1 Even more preferably one species or two or more species.
• ascorbic acid phosphoric acid esters such as sodium ascorbic acid phosphoric acid ester and magnesium ascorbic acid phosphoric acid ester
• ascorbic acid sulfuric acid esters such as disodium ascorbic acid sulfuric acid ester
• 2-O-ethyl Alkyl ascorbic acids such as ascorbic acid and 3-O-ethylascorbic acid
• Ascorbic acid glycosides such as ascorbic acid-2-glucoside; Isostearyl ascorbyl phosphate disodium, palmitate ascorbyl phosphate 3 sodium
• Glyceryl ascorbic acid Bisglyceryl ascorbic acid, alkylglyceryl ascorbic acid; (ascorbyl/tocopheryl) phosphate, potassium (ascorbyl/tocopheryl) phosphate, ascorbyl tocopheryl maleate; ascorbyl tetrahexyldecanoate, oil-soluble ascorbic acid such as L-
• organic acids organic acid salts, or organic acid derivatives may be used alone or in combination of two or more.
• the component (C-1) includes ascorbic acid, ascorbate, alkyl ascorbate, ascorbyl phosphate, and ascorbyl glycoside.
• ascorbic acid sodium ascorbate, sodium ascorbate phosphate, magnesium ascorbate phosphate, disodium ascorbate sulfate, 2-O-ethylascorbic acid, 3-O-ethylascorbic acid, ascorbic acid -2-Glucoside, disodium isostearyl ascorbyl phosphate, trisodium ascorbyl palmitate, glyceryl ascorbic acid, bisglyceryl ascorbic acid, hexyl 3-glyceryl ascorbic acid, 3-glyceryl ascorbic acid, myristyl 3-glyceryl ascorbic acid, 3-lauryl glyceryl ascorbic acid, (ascorbyl/tocopheryl) phosphoric acid, potassium (ascorbyl/tocopheryl) phosphate, and ascorbyl tocopheryl maleate
• ascorbic acid tranexamic acid, citric acid, salicylic acid, lactic acid, acetic acid, tartaric acid, malic acid, succinic acid, oxalic acid, gluconic acid, fumaric acid, propionic acid, aspartic acid, pyrrolidone Carboxylic acid, ⁇ -aminocaproic acid, glutamic acid, aminoethylsulfonic acid, ellagic acid, kojic acid, glycyrrhizinic acid, glycyrrhetinic acid, phytic acid, ferulic acid, glycolic acid, azelaic acid, ascorbic acid phosphoric acid ester, ascorbic acid sulfuric acid ester, Alkyl ascorbic acid, ascorbic acid glycoside, isostearyl ascorbyl phosphate disodium, palmitate ascorbyl phosphate trisodium, glyceryl ascorbic
• Citric acid lactic acid, tranexamic acid, salicylic acid, gluconic acid, phytic acid, tartaric acid, sodium lactate, sodium citrate, sodium ascorbate phosphate, magnesium ascorbate phosphate, 2-O-ethylascorbic acid, 3- O-ethylascorbic acid, ascorbic acid-2-glucoside, sodium succinate, disodium succinate are even more preferable, and tranexamic acid, citric acid, lactic acid, salicylic acid, gluconic acid, phytic acid, tartaric acid, disodium succinate, One or two selected from the group consisting of sodium ascorbyl phosphate, magnesium ascorbyl phosphate, 2-O-ethylascorbic acid, 3-O-ethylascorbic acid, and ascorbic acid-2-glucoside The above is particularly preferable.
• the total content of the organic acid, the organic acid salt, or the derivative of the organic acid is preferably 0.001 to 10% by mass, and more preferably 0.005 to 7% with respect to the total amount of the composition. %, more preferably 0.01 to 5% by mass, even more preferably 0.05 to 5% by mass, and particularly preferably 0.1 to 3% by mass.
• the ratio of the total content of the organic acid, the organic acid salt, or the derivative of the organic acid to the component (A) is not particularly limited, but to 1 part by mass of the component (A),
• the amount of the organic acid, the organic acid salt, or the derivative of the organic acid is preferably 0.001 to 3.5 parts by mass, more preferably 0.01 to 2 parts by mass, still more preferably 0.05 to 1 part by mass.
• the total content of ascorbic acid, salts thereof, or derivatives thereof is not particularly limited, but is preferably 0.001 to 10% by mass, more preferably 0.01 to 7% by mass. %, more preferably 0.05 to 5% by mass, even more preferably 0.1 to 5% by mass, and particularly preferably 0.5 to 3% by mass.
• the total content of tranexamic acid, a salt thereof, or a derivative thereof is not particularly limited, but is preferably 0.1 to 5% by mass, more preferably 0.5 to 5% by mass. %, and more preferably 1 to 3% by mass.
• amphipathic component contained in the external composition for skin as the component (C-2) of the present invention has both a hydrophilic group and a hydrophobic group (lipophilic group) in one molecule, and as a result, the aqueous phase and the oil A general compound having an affinity for any of the phases (organic phase).
• Such an amphipathic compound is not particularly limited, and examples thereof include an alkylene oxide derivative, a phosphorylcholine-containing polymer, a divalent carboxylic acid ester, and an alkanediol having 5 to 10 carbon atoms.
• the component (C-2) of the present invention any of these compounds may be used alone or in combination of two or more. By blending the component (C-2) with the components (A) and (B), an external composition for skin in which precipitation is suppressed is provided even when a high concentration of nicotinic acid amide is blended. It becomes possible.
• the component (C-2) is preferably an alkylene oxide derivative represented by the following general formula (I), 2-methacryloyloxyethylphosphorylcholine/butyl methacrylate copolymer, (eicosanedioic acid/tetradecanedioic acid)decaglyceryl. , Bisethoxydiglycol cyclohexanedicarboxylate, diethylhexyl succinate, diethoxyethyl succinate, and one or more selected from the group consisting of alkanediols having 5 to 10 carbon atoms.
• general formula (I) 2-methacryloyloxyethylphosphorylcholine/butyl methacrylate copolymer, (eicosanedioic acid/tetradecanedioic acid)decaglyceryl.
• Z represents a hydrogen atom or a residue obtained by removing n hydroxy groups from a hydroxy compound having 1 to 30 carbon atoms;
• AO means an oxyalkylene group having 3-4 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 mean the average number of moles of addition of AO, EO, and BO, and are independently 0 to 200. However, a, b, and c are not all 0. When n is 2 or more, a, b and c may be the same or different.
• Z is a hydrogen atom, n is 1.
• the AO and EO may be added randomly or in the form of blocks.
• the alkylene oxide derivative is preferably a compound represented by the following general formula (II).
• Z represents a hydrogen atom or a residue obtained by removing n hydroxy groups from a hydroxy compound having 1 to 30 carbon atoms; AO means an oxyalkylene group having 3-4 carbon atoms; EO means an oxyethylene group; n means 1 to 9; a and b mean the average number of moles of addition of AO and EO, respectively, and are independently 0 to 200. However, a and b do not all become 0. When n is 2 or more, a and b may be the same or different. When Z is a hydrogen atom, n is 1.
• the AO and EO may be added randomly or in the form of blocks.
• AO is an oxyalkylene group having 3 to 4 carbon atoms, from the viewpoint of providing a composition for external use for skin in which precipitation is suppressed, and examples thereof include an oxypropylene group and an oxybutylene group.
• AO is preferably an oxypropylene group or an oxybutylene group, more preferably an oxypropylene group.
• BO is an oxyalkylene group having 4 carbon atoms, examples of which include oxybutylene group (oxy n-butylene group, oxyisobutylene group, oxy t-butylene group), oxytetramethylene. Groups and the like. It is preferably an oxybutylene group.
• a+b+c which is the total number of AO, EO, and BO monomer units, is preferably 3 or more, more preferably 5 or more, and further preferably 10 or more, from the viewpoint of markedly exhibiting the effect of the present invention.
• a+b+c is preferably 450 or less, more preferably 350 or less, further preferably 300 or less, and particularly preferably 250 or less, from the viewpoint of remarkably exerting the effect of the present invention.
• a+b which is the total number of AO and EO monomer units, is preferably 3 or more, more preferably 5 or more, and still more preferably 10 or more, from the viewpoint of significantly exhibiting the effect of the present invention. .. Further, a+b is preferably 400 or less, more preferably 300 or less, still more preferably 250 or less, and particularly preferably 200 or less, from the viewpoint of remarkably exerting the effect of the present invention.
• Z is a hydrogen atom, or an alkyl monoalcohol having 4 to 24 carbon atoms, glycerin, or tri, from the viewpoint of providing a composition for external use for skin in which precipitation is suppressed. Obtained by removing n hydroxy groups from methylolpropane, erythritol, pentaerythritol, alkyl glucosides having 1 to 24 carbon atoms, diglycerin, xylitol, dipentaerythritol, sorbitol, inositol, sucrose, trehalose, or maltitol.
• Such an alkylene oxide derivative can be synthesized by a known method. For example, it can be obtained by addition-polymerizing ethylene oxide and alkylene oxide having 3 to 4 carbon atoms to a hydroxy compound having 1 to 30 carbon atoms and then reacting with alkylene oxide having 4 carbon atoms.
• ethylene oxide and alkylene oxide may be randomly polymerized or block polymerized.
• an alkali catalyst, a phase transfer catalyst, a Lewis acid catalyst or the like can be used.
• an alkali catalyst such as potassium hydroxide.
• the property of the alkylene oxide derivative is not limited as long as the effects of the present invention are exhibited, but in the above formulas (I) and (II), from the viewpoint of remarkably exhibiting the effects of the present invention, it is preferably semi-solid at 25°C. It is preferable that the component is a liquid form (including paste form).
• alkylene oxide derivative for example, polyoxyalkylene glyceryl ether, polyoxyalkylene alkyl glucoside, polyoxypropylene alkyl ether, polyoxyethylene polyoxypropylene alkyl ether, polyoxyethylene polyoxypropyleneoxy butylene alkyl ether, Polyoxyalkylene sorbit, polyoxyalkylene erythritol ether, polyoxyalkylene pentaerythritol ether, polyoxyalkylene diglyceryl ether, polyoxyalkylene trimethylolpropane, polyoxypropylene glycol, polyoxyethylene polyoxypropylene glycol, polyoxyalkylene xylitol, Examples thereof include polyoxyalkylene dipentaerythritol, polyoxyalkylene inositol, polyoxyalkylene sucrose ether, polyoxyalkylene trehalose ether, and polyoxyalkylene maltitol ether.
• alkylene oxide derivatives are polyoxyethylene glyceryl ether, polyoxypropylene glyceryl ether, polyoxyethylene polyoxypropylene glyceryl ether, polyoxybutylene polyoxyethylene polyoxypropylene glyceryl ether, polyoxybutylene polyoxyethylene polyoxypropylene alkyl.
• Glucoside polyoxyethylene polyoxypropylene alkyl glucoside, polyoxyethylene alkyl glucoside, polyoxypropylene alkyl glucoside, polyoxypropylene alkyl glucoside, polyoxypropylene alkyl ether, polyoxyethylene polyoxypropylene alkyl ether, polyoxypropylene sorbit, polyoxyethylene sorbit, polyoxy Ethylene polyoxypropylene sorbitol, polyoxypropylene erythritol ether, polyoxyethylene erythritol ether, polyoxyethylene pentaerythritol ether, polyoxyethylene polyoxypropylene erythritol ether, polyoxypropylene pentaerythritol ether, polyoxyethylene polyoxypropylene pentaerythritol ether , Polyoxyethylene polyoxypropylene pentaerythritol ether , Polyoxybutylene polyoxyethylene pentaerythritol ether
• Glucoside polyoxyethylene methyl glucoside, polyoxypropylene alkyl ether, polyoxyethylene polyoxypropylene butyl ether, polyoxyethylene polyoxypropylene decyl tetradecyl ether, polyoxypropylene sorbit, polyoxypropylene diglyceryl ether, polyoxyethylene polyoxy Even more preferred is one or more selected from the group consisting of propylene diglyceryl ether.
• alkylene oxide derivatives include Unilube 50MB-26 (polyoxyethylene polyoxypropylene butyl ether (17EO) (17PO)) and Unilube 50MB-168 (polyoxyethylene polyoxypropylene butyl ether (37EO).
• antibacterial or bactericidal component examples include chlorhexidine, benzalkonium chloride, acrinol, sulfur, resorcin, ethanol, benzethonium chloride, adapalene, benzoyl peroxide, clindamycin, cresol, gluconic acid and its derivatives, and povidone iodine.
• Potassium iodide, iodine, triclocarban, triclosan photosensitizer No. 101, photosensitizer No. 201, phenoxyethanol, alkyldiaminoglycine hydrochloride, chlorhexidine gluconate, zinc paraphenolsulfonate, picrotone olamine, and miconazol, etc.
• chlorhexidine benzalkonium chloride
• acrinol sulfur
• resorcin ethanol
• benzethonium chloride adapalene
• benzoyl peroxide clin
• vitamins include retinol derivatives (retinol, retinol acetate, retinol palmitate, etc.), vitamin A compounds such as tocopheryl retinoate; vitamin E compounds such as tocopherol, tocopherol acetate; riboflavin, etc.
• amino acid or its derivative examples include betaine (trimethylglycine), proline, hydroxyproline, arginine, lysine, serine, glycine, alanine, phenylalanine, ⁇ -alanine, threonine, glutamine, asparagine, aspartic acid, cysteine, cystine, methionine.
• antiaging component examples include hydrolyzed soybean protein, retinoid (retinol, retinoic acid, retinal, etc.), astaxanthin, coenzyme Q10, pangamic acid, ursolic acid, turmeric extract, sphingosine derivative, silicon, silicic acid, N-methyl- L-serine, mevalonolactone, peptides (caprooil tetrapeptide-3, oligopeptide-24, etc.), plant extracts (eg, artichoke, izayoi rose, seaweed, bilberry, birch, plantain psyllium, touki, swordfish, hypericum, comfree , Neem, Novara, Hyogi, Himefuuro, Bodaiju, Botanpi etc.) and the like.
• retinoid retinol, retinoic acid, retinal, etc.
• astaxanthin coenzyme Q10
• pangamic acid ursolic acid
• Examples of the blood circulation promoting component include plants (for example, Panax ginseng, ashitaba, arnica, ginkgo, fennel, emmezo, netherlands oak, chamomile, roma-chamomile, carrot, gentian, burdock, rice, hawthorn, shiitake mushroom, hawthorn, hazelnut , Senkyu, senburi, thyme, clove, chimpanzee, touki, tounin, spruce, carrot, garlic, butcha-bloom, grape, button, horse chestnut, melissa, yuzu, yokuinin, rosemary, rosehip, chimp, Components derived from (Touki, spruce, peach, apricot, walnut, and corn); dl- ⁇ -tocopherol acetate, tocopherol nicotinate, glucosyl hesperidin, hesperidin, and glucosyl hesperidin.
• keratin softening components examples include lanolin, urea, and sulfur.
• astringent components include zinc paraphenol sulfonate, zinc oxide, menthol, and ethanol.
• an oil functioning as a base or carrier can be used.
• oil components include hydrocarbon oils, ester oils, oils and fats, silicones and waxes.
• hydrocarbon oils such as ⁇ -olefin oligomers; dimethicone, crosslinked methylpolysiloxane, highly polymerized methylpolysiloxane, phenyl-modified silicone, cyclic silicone, Silicones such as polyether-modified silicones; higher alcohols; higher fatty acids; isopropyl myristate, octyldodecyl myristate, isopropyl palmitate, cetyl palmitate, isononyl isononanoate, diisopropyl adipate, decyl oleate, isodecyl oleate, dimethyloctane.
• Hexyldecyl acid salt diisopropyl sebacate, di-2-ethylhexyl sebacate, 2-hexyldecyl myristate, 2-hexyldecyl palmitate, diisopropyl adipate, isotridecyl isononanoate, cetyl lactate, isostearyl isostearate, 12-hydroxystearyl Cholesteryl acid salt, Cholesteryl stearate, Cholesteryl oleate, Macadamia nut fatty acid phytosteryl, Phytosteryl oleate, Dextrin palmitate, Inulin stearate, Hydrogenated jojoba oil, Di-2-ethylhexyl ethylene glycol, Dipentaerythritol fatty acid ester, Dicapric acid neo Pentyl glycol, tri-2-ethylhexyl trimellitate, tritridecyl trimellitate, trimethylo
• N-acyl amino acid salts acylated taurates
• amines such as stearylamine and oleylamine
• polyoxyethylene/methylpolysiloxane copolymers lauryl PEG-9 polydimethylsiloxyethyl dimethicone, PEG-9 polydimethylsiloxyethyl dimethicone, etc.
• silicone-based surfactants or naturally-derived surfactants such as lecithin, hydrogenated lecithin, saponin, sodium surfactin, cholesterol, and bile acid. Not limited.
• Copolymer (hydroxyethyl acrylate/acryloyl dimethyl taurine Na) copolymer, (Na acrylate/acryloyl dimethyl taurine Na) copolymer, polyacrylic amide, polyethylene glycol, alginic acid, sodium alginate, propylene glycol alginate, macrogol, Examples thereof include sodium chondroitin sulfate, and cellulosic thickeners such as hydroxyethyl cellulose (hydroxyethyl cellulose, hydroxypropylmethyl cellulose, hydroxypropyl cellulose, hydrophobized hydroxypropylmethyl cellulose, carboxymethyl cellulose, etc.).
• the base or carrier may be used alone or in combination of two or more.
• pH adjusters examples include inorganic acids and organic bases.
• stabilizers examples include sodium polyacrylate, dibutylhydroxytoluene, and butylhydroxyanisole.
• examples of the irritation reducing agent include licorice extract and sodium alginate.
• colorant examples include pigment grade titanium oxide, zinc oxide, iron oxide, organic pigments, talc, sericite, mica, synthetic mica, chromium oxide, and Gunjou.
• powder may be blended for the purpose of improving the feel and imparting a make-up effect, and specifically, boron nitride, silica, alumina, aluminum hydroxide, metal soap, silicone powder, polymethyl methyl methacrylate. Etc.
• the additives can be used alone or in combination of two or more.
• the present invention is not limited to these, and known ingredients that are blended in external preparations for skin such as cosmetics and pharmaceuticals can be appropriately used.
• the external composition for skin of the present invention may generally have a liquidity of pH 2.0 to 9.0, but preferably has a pH of 3 from the viewpoint of low irritation to the skin and mucous membranes and good feeling on skin use.
• the pH is from 0.0 to 8.5, more preferably from pH 4.0 to 8.0, still more preferably from pH 4.5 to 7.5, even more preferably from pH 5.0 to 7.5.
• the aqueous base such as an emulsion, a cream or an ointment
• it may be a W/O type or an O/W type, but the feeling of use of the external composition for skin of the present invention (
• the O/W type is more preferable from the viewpoints of stickiness, spreadability, moist feeling, freshness, permeation feeling, etc.).
• an external composition for skin is particularly preferable. That is, the external composition of the present invention can be a skin external composition for pharmaceuticals, quasi drugs, or cosmetics.
• the formulation form of the external composition for skin is the same as that of the external composition of the present invention.
• usable bases or carriers, additives, active ingredients, and preferable ones thereof are the same as those in the case of the external composition of the present invention.
• the external composition for skin of the present invention can be used by being housed in a container having an appropriately selected shape and material according to the purpose of use and application.
• Specific examples of the container include spray type, bottle type, tube type, jar type, spoid type, dispenser type, stick type, pouch bags, and cheer packs. Since the external composition for skin of the present invention can be used in a preferable state from the viewpoint of ease of taking out from a container, the degree of freedom in designing a formulation containing a high concentration of nicotinic acid amide can be increased. That is, even a high-concentration nicotinic acid amide-containing preparation can be easily used in various containers such as sprays, bottles, tubes and dispensers, as well as jars and sticks.
• the external composition for skin of the present invention can be suitably used for the purpose of promoting blood circulation, anti-inflammation, and promoting ceramide synthesis in expectation of physiological activity of nicotinic acid amide.
• whitening, anti-wrinkle and anti-aging effects can be expected, and it is useful as a multi-functional preparation including a whitening agent and a sunscreen.
• the external composition for skin of the present invention can be used once or several times a day in accordance with the intended use and the like in a well-known or commonly used usage and dose.
• the term "precipitation” means, for example, that the composition for external use of the present invention takes any form as a solid (for example, a solid precipitate, needle-like crystals or a hazy cotton-like substance). Substance). It can be visible precipitation. Alternatively, it is also possible to detect the degree of precipitation or the transparency of the solution, which is difficult to detect by visual inspection, with a turbidimeter and an ultraviolet visible infrared spectrophotometer (model V-770, manufactured by JASCO Corporation). For example, when the external composition for skin of the present invention is prepared as an aqueous composition, it is preferably colorless and transparent, but it may be deposited over time by a low temperature storage test. Deposition inhibition also includes preventing, delaying, and reducing such deposition.
• compositions of Examples shown in Tables 1 to 7 were excellent in usability.
• the external composition for skin of the present invention was prepared based on the formulations shown in Tables 8 to 28 below. Numerical values in the table mean mass%.
• an external composition for skin that does not precipitate with time and has a good feeling in use can be obtained.

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• 2020
  • 2020-01-31 WO PCT/JP2020/003593 patent/WO2020158908A1/ja not_active Ceased
  • 2020-01-31 TW TW109103070A patent/TW202045125A/zh unknown
  • 2020-01-31 JP JP2020520078A patent/JP6836017B2/ja not_active Ceased
  • 2020-01-31 CN CN202080011591.6A patent/CN113365601A/zh active Pending
• 2021
  • 2021-02-04 JP JP2021016218A patent/JP2021075549A/ja not_active Withdrawn
• 2023
  • 2023-09-08 JP JP2023146290A patent/JP2023171784A/ja not_active Withdrawn

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