Composition containing an ether of an aliphatic alcohol and glycerin

Abstract

A novel composition is provided, which comprises (A) an ether of an aliphatic alcohol and glycerin and (B) an acyl glutamic acid lysine salt.

Description

[Technical Field]

[0001] This invention relates to novel compositions, etc. [Background technology]

[0002] Ethers of aliphatic alcohols, such as alkylglyceryl ethers, and glycerin are used to obtain moisturizing, emulsifying, deodorizing, and antibacterial properties. For example, Japanese Patent Publication No. 2000-191488 (Patent Document 1) lists alkyl glyceryl ether as a surfactant constituting a specific deodorizing cosmetic composition. [Prior art documents] [Patent Documents]

[0003] [Patent Document 1] Japanese Patent Publication No. 2000-191488 [Overview of the project] [Problems that the invention aims to solve]

[0004] The object of the present invention is to provide novel compositions, etc., containing ethers of aliphatic alcohols and glycerin. [Means for solving the problem]

[0005] As described above, ethers of aliphatic alcohols and glycerin are used as surfactants, etc. (Patent Document 1).

[0006] However, the inventors' research has shown that such aliphatic alcohol and glycerin ethers do not function as surfactants; rather, they have poor dispersion or solubility in water and other liquids, often resulting in turbidity.

[0007] Under these circumstances, the inventors diligently conducted research to solve the above problems and discovered that a novel composition can be obtained by combining an aliphatic alcohol, a glycerin ether, and an acyl glutamate lysine salt. Furthermore, they found that in such a composition, the aliphatic alcohol and the glycerin ether can be efficiently dissolved or dispersed. After further research, the inventors completed the present invention.

[0008] In other words, the present invention relates to the following inventions, etc. [1] A composition containing (A) an ether of an aliphatic alcohol and glycerin and / or (B) an acyl glutamate lysine salt [usually, at least (A) an ether of an aliphatic alcohol and glycerin, particularly (A) an ether of an aliphatic alcohol and glycerin and (B) an acyl glutamate lysine salt]. [2] The composition according to [1], wherein component (A) is glycerin mono-2-ethylhexyl ether and component (B) is dilauroyl glutamate lysine salt. [3] (A) The composition according to [1] or [2], wherein the proportion of component is less than 0.5% by mass. [4] (B) The composition according to any one of [1] to [3], wherein the proportion of component (B) is 1% by mass or less. [5] The composition according to any one of [1] to [4], wherein the proportion of component (B) is greater than 0.05 parts by mass per 1 part by mass of component (A). [6] The composition according to any one of [1] to [5], wherein the proportion of component (A) is less than 0.5% by mass, and the proportion of component (B) is greater than 0.05 parts by mass and less than or equal to 100 parts by mass per 1 part by mass of component (A). [7] Furthermore, the composition according to any one of [1] to [6], further comprising (C) a water-soluble component. [8] The composition according to [7], wherein component (C) satisfies the requirements of having a logP value of 0 or less and a molecular weight of 1000 or less. [9] (C) The composition according to [7] or [8], comprising a water-soluble whitening ingredient.

[10] The composition according to any one of [7] to [9], wherein component (C) comprises at least one selected from ascorbic acids, tranexamic acids, epsilon-aminocaproic acids, hydroquinones, nicotinamides, glycyrrhizic acids, allantoins, and riboflavins.

[11] The composition according to any one of [7] to

[10] , wherein component (C) comprises at least one selected from ascorbic acid, ascorbic acid phosphate, alkyl ascorbate, ascorbic acid-2-glucoside, tranexamic acid, epsilonaminocaproic acid, hydroquinone, arbutin, nicotinamide, glycyrrhizic acid, allantoin, riboflavin, and salts thereof.

[12] The composition according to any one of [7] to

[11] , wherein the proportion of component (C) is 0.05% by mass or more.

[13] A composition according to any one of [1] to

[12] for use as a leave-on cosmetic.

[14] (A) An agent for improving the solubility or dispersibility of an ether of an aliphatic alcohol and glycerin, and (B) an agent containing an acyl glutamate lysine salt.

[15] (C) An agent for improving the transdermal absorption of water-soluble components, comprising (A) an ether of an aliphatic alcohol and glycerin or (B) an acyl glutamate lysine salt.

[16] (C) An agent for improving the transdermal absorption of water-soluble components, comprising (A) an ether of an aliphatic alcohol and glycerin and (B) an acyl glutamate lysine salt.

[17] (A) A method for improving the solubility or dispersibility of an ether of an aliphatic alcohol and glycerin, comprising the coexistence of (A) an ether of an aliphatic alcohol and glycerin and (B) an acyl glutamate lysine salt.

[18] A method for improving the transdermal absorbability of a water-soluble component (C), which comprises allowing the water-soluble component (C) to coexist with either an ether of an aliphatic alcohol and glycerol (A) or an acylglutamic acid lysine salt (B).

[19] A method for improving the transdermal absorbability of a water-soluble component (C), which comprises allowing the water-soluble component (C) to coexist with both an ether of an aliphatic alcohol and glycerol (A) and an acylglutamic acid lysine salt (B).

Effects of the Invention

[0009] The present invention can provide a novel composition. Such a composition comprises an ether of an aliphatic alcohol and glycerol, and an acylglutamic acid lysine salt.

[0010] In another aspect of the present invention, a composition capable of improving the solubility or dispersibility of an ether of an aliphatic alcohol and glycerol can be provided. As described above, the ether of an aliphatic alcohol and glycerol may cause clouding or the like, but such clouding or the like can be efficiently suppressed by combining it with the specific component, acylglutamic acid lysine salt.

Modes for Carrying Out the Invention

[0011] [1. Composition] The composition of the present invention contains at least one selected from (A) an ether of an aliphatic alcohol and glycerol and (B) an acylglutamic acid lysine salt. In particular, the composition of the present invention may contain (A) an ether of an aliphatic alcohol and glycerol and (B) an acylglutamic acid lysine salt.

[0012] (A) Ether of aliphatic alcohol and glycerin (component (A)) The aliphatic alcohol may be a linear or branched alcohol, and may be a saturated or unsaturated alcohol.

[0013] The number of carbon atoms in an aliphatic alcohol is not particularly limited, but may be, for example, 4 or more carbon atoms (e.g., 4 to 30 carbon atoms), 6 or more carbon atoms (e.g., 6 to 24 carbon atoms), 8 or more carbon atoms (e.g., 8 to 22 carbon atoms), or 23 or more carbon atoms. Furthermore, the number of carbon atoms in an aliphatic alcohol may be, for example, 40 or less, 30 or less, 24 or less, 22 or less, 18 or less, 16 or less, 14 or less, 12 or less, or 11 or less.

[0014] The aliphatic alcohol may be a polyol (a polyol other than glycerol), and is usually a monool.

[0015] Specific examples of aliphatic alcohols include saturated or unsaturated aliphatic alcohols (chain or branched aliphatic alcohols, e.g., C2-ethylhexanol, caprylic alcohol, pelargon alcohol, caprine alcohol, isodecanol, lauryl alcohol, myristyl alcohol, cetyl alcohol, stearyl alcohol, cetostearyl alcohol, hexyldodecanol, isostearyl alcohol, octyldodecanol, behenyl alcohol, 2-decyl-1-tetradecanol, palmitrail alcohol, oleyl alcohol, linoleyl alcohol, linolenyl alcohol, etc.) 4-30 Saturated or unsaturated aliphatic alcohols, C 6-24 Examples include saturated or unsaturated aliphatic alcohols.

[0016] The aliphatic alcohol and glycerin ether may be a monoether (glycerin monoether), diether, or triether, but is preferably a mono or diether, and may contain at least a monoether.

[0017] Furthermore, if the ether is a polyether (di or triether), the aliphatic alcohol may be the same or a different aliphatic alcohol.

[0018] Representative ethers of aliphatic alcohols and glycerin include, for example, glycerin mono-2-ethylhexyl ether (ethylhexylglycerin), glycerin monocaprylic ether, glycerin monoisodecyl ether, glycerin monocetyl ether (chymyl alcohol), glycerin monostearyl ether (batyl alcohol), glycerin monoisostearyl ether, glycerin monobehenyl ether, and glycerin monooleyl ether (cerakyl alcohol).

[0019] Aliphatic alcohols and glycerin ethers may be used individually or in combination of two or more.

[0020] In particular, glycerin mono-2-ethylhexyl ether can be suitably used from the viewpoint of its effect in inhibiting bacterial growth. Therefore, component (A) may contain at least glycerin mono-2-ethylhexyl ether.

[0021] Note that component (A) may be synthesized or commercially available.

[0022] If component (A) contains glycerin mono-2-ethylhexyl ether, the proportion of glycerin mono-2-ethylhexyl ether to the total amount of component (A) may be selected from a range of, for example, 10% by mass or more, and may be 30% by mass or more, preferably 50% by mass or more, and more preferably 70% by mass or more (for example, 80% by mass or more, 85% by mass or more, 90% by mass or more, 95% by mass or more, 99% by mass or more, 100% by mass, etc.).

[0023] If the composition contains component (A), the amount of component (A) in the composition can be selected according to the intended use of the composition, but may be, for example, 0.0001 to 5% by mass, preferably 0.001 to 2% by mass, more preferably 0.01 to 1% by mass, even more preferably 0.03 to 0.7% by mass, and even more preferably 0.05 to 0.5% by mass (for example, 0.05% or more and less than 0.5% by mass) relative to the total amount of the composition, and may be particularly 0.5% by mass or less [for example, less than 0.5% by mass (for example, 0.45% by mass or less), 0.4% by mass or less (for example, 0.35% by mass or less), 0.3% by mass or less (for example, 0.25% by mass or less), 0.2% by mass or less (for example, 0.15% by mass or less), etc.].

[0024] By using component (A) within this range, its function can be efficiently exerted. Furthermore, within this range, it can exert its effect, such as inhibiting bacteria, with little (or no) skin irritation.

[0025] Furthermore, as described later, if the composition contains component (C), the permeability (permeability) of component (C) can be efficiently improved by including component (A) in the composition (especially in combination with component (B)).

[0026] (B) Acyl glutamate lysine salt (Component (B))

[0027] In acyl glutamate lysine salts, the acyl can be, for example, an acyl corresponding to a fatty acid (aliphatic) (fatty acid acyl, aliphatic acyl).

[0028] Such fatty acids may be chain-like or branched fatty acids, and may be saturated or unsaturated fatty acids.

[0029] The number of carbon atoms in a fatty acid is not particularly limited, but may be, for example, 4 or more carbon atoms (e.g., 4 to 30 carbon atoms), 8 or more carbon atoms (e.g., 8 to 24 carbon atoms), or 10 or more carbon atoms (e.g., 12 to 22 carbon atoms).

[0030] The fatty acids may be polyunsaturated fatty acids, but they are usually monofatty acids.

[0031] Specific fatty acids include, for example, saturated or unsaturated aliphatic acids (chain or branched fatty acids, for example, C) such as caprylic acid, pelargonic acid, capric acid, lauric acid, myristic acid, palmitic acid, stearic acid, isostearic acid, behenic acid, palmitoleic acid, oleic acid, linoleic acid, and linolenic acid. 4-30 Saturated or unsaturated aliphatic acids, C 8-24 Examples include saturated or unsaturated fatty acids.

[0032] The acyl glutamate lysine salt may also be a monoacyl glutamate lysine salt, and in particular, a diacyl glutamate lysine salt.

[0033] In addition, in diacyl glutamate lysine salt, the two acyls (fatty acids) may be the same or different.

[0034] In acyl glutamate lysine salts, the salt is not particularly limited and examples include salts with inorganic bases [e.g., ammonium salts; salts with metals such as alkali metals (sodium, potassium, etc.), alkaline earth metals (calcium, magnesium, etc.), and aluminum], salts with organic bases (e.g., salts with organic amines such as methylamine, triethylamine, and triethanolamine), and salts with amino acids (e.g., arginine salts).

[0035] Typical salts are alkali metal salts such as sodium salts.

[0036] Specific examples of acyl glutamate lysine salts include diacyl glutamate lysine salts (for example, dilauroyl glutamate lysine salt (e.g., dilauroyl glutamate lysine sodium), dimyristoyl glutamate lysine salt (e.g., dimyristoyl glutamate lysine sodium), distearoyl glutamate lysine salt (e.g., distearoyl glutamate lysine sodium), and dilinoleoyl glutamate lysine salt (e.g., dilinoleoyl glutamate lysine sodium).

[0037] Acyl glutamate lysine salts may be used alone or in combination of two or more types.

[0038] In particular, di-fatty acid acyl glutamate lysine salts such as dilauroyl glutamate lysine sodium can be suitably used.

[0039] Furthermore, component (B) may be synthesized by conventional methods [for example, by reacting a lysine salt (e.g., L-lysine hydrochloride) with an N-acyl glutamic acid anhydride (e.g., N-acyl-L-glutamic acid anhydride)], or a commercially available product may be used. For example, dilauroyl glutamic acid lysine sodium may be obtained as "Pellicea LB-10" or "Pellicea L-30" manufactured by Asahi Kasei Chemicals Corporation.

[0040] If the composition contains component (B), the amount of component (B) in the composition can be selected according to the intended use of the composition, but may be, for example, 0.00001 to 20% by mass, preferably 0.0001 to 10% by mass, more preferably 0.001 to 5% by mass, and even more preferably 0.01 to 3% by mass, relative to the total amount of the composition. Furthermore, the amount of component (B) in the composition may be 2% by mass or less (for example, 1% by mass or less, 0.00001 to 1% by mass, etc.), or 2% by mass or more (for example, more than 2% by mass, 2.5% by mass or more, 3% by mass or more, 3 to 5% by mass, etc.).

[0041] Furthermore, if the composition contains component (A) and component (B), the proportion of component (B) may be, for example, 0.001 to 1000 parts by mass (e.g., 0.003 to 800 parts by mass), preferably 0.005 to 500 parts by mass (e.g., 0.007 to 300 parts by mass), and more preferably 0.01 to 100 parts by mass (e.g., 0.03 to 80 parts by mass), per 1 part by mass of component (A).

[0042] Furthermore, the proportion of component (B) may be, for example, 0.001 parts by mass or more [for example, 0.005 parts by mass or more (e.g., 0.01 to 500 parts by mass), 0.02 parts by mass or more (e.g., 0.025 to 300 parts by mass), 0.03 parts by mass or more (e.g., 0.05 to 100 parts by mass), 0.05 parts by mass or more (e.g., more than 0.05 parts by mass, more than 0.05 parts by mass and 100 parts by mass or less, 0.07 to 100 parts by mass), 1 part by mass or more (e.g., 1 to 300 parts by mass), etc.] per 1 part by mass of component (A), or 0.01 parts by mass or less [for example, 0.007 parts by mass or less (e.g., 0.001 to 0.005 parts by mass), 0.005 parts by mass or less (e.g., 0.002 to 0.005 parts by mass), etc.].

[0043] By using component (B) in this proportion, the solubility or dispersibility of component (A) can be efficiently improved. Therefore, the stability of formulations containing component (A) can be improved, and the function of component (A) (for example, its function as an emulsifying agent) can be efficiently exercised according to its intended use.

[0044] Furthermore, as described later, in compositions containing component (C), the permeability (permeability) of component (C) can be efficiently improved by including component (B) (especially in combination with component (A)) in the composition (especially in the proportions mentioned above).

[0045] (C) Water-soluble component ((C) component) The compositions of the present invention may contain water-soluble components. As described above, the compositions of the present invention typically contain (A) an ether of an aliphatic alcohol and glycerin and / or (B) an acyl glutamate lysine salt. By combining such components [component (A) and / or component (B) (for example, at least component (A), particularly component (A) and component (B)]] with water-soluble components, the functions of the water-soluble components can be efficiently exhibited.

[0046] For example, by combining it with component (A) and / or component (B), the distribution to or diffusion into the skin may be promoted, thereby improving the transdermal absorption (permeability) of water-soluble components.

[0047] As mentioned above, combining component (A) and component (B) can improve the solubility or dispersibility of component (A), and the effect of improving the transdermal absorption of water-soluble components may be enhanced in conjunction with this effect of improving the solubility or dispersibility of component (A). In particular, water-soluble ingredients (for example, water-soluble whitening ingredients such as ascorbic acid and tranexamic acid, which will be discussed later) have low skin permeability and often fail to reach the target area. Therefore, in order to efficiently exert the functions of the water-soluble components (such as whitening effects) in an aqueous skin composition, the composition containing component (C) may contain both component (A) and component (B).

[0048] In water-soluble components, the degree of water solubility is not particularly limited, but the logP value may be used as an indicator.

[0049] For example, as a water-soluble component, a water-soluble component with a logP value of 0 or less (e.g., -10 to 0), preferably -8 or more (e.g., -7.5 to 0, -7 to -0.05, etc.), and more preferably -5 or more (e.g., -4.5 to 0, -4 to -0.08, etc.) may be used, and water-soluble components with a logP value of -3 or more (e.g., -2.5 to 0, -2 to -0.1) can also be used.

[0050] Note that the distribution coefficient is logP(logP OWThe value is P OW [1- Concentration of test substance in octanol layer (mol / L) / Concentration of test substance in aqueous layer (mol / L)] - Common logarithm (log 10 P OW This is a value known as ). The logP value may be measured (determined, calculated) according to, for example, Japanese Industrial Standard Z7260-107 (2000) "Measurement of partition coefficient (1-octanol / water) - Flask shaking method".

[0051] The molecular weight (chemical formula weight) of the water-soluble component is not particularly limited, but may be, for example, 2000 or less (e.g., 1800 or less), preferably 1500 or less (e.g., 1200 or less), and even more preferably 1000 or less (e.g., 800 or less, 700 or less, 600 or less, 500 or less, etc.). The lower limit of the molecular weight (formula weight) of the water-soluble component is not particularly limited and may be, for example, 50, 70, 80, 90, 100, 110, 120, 130, 140, 150, etc.

[0052] Furthermore, while water-soluble ingredients only need to be water-soluble, they may also have functions depending on the type of ingredient. Examples of water-soluble ingredients may include whitening ingredients (water-soluble whitening ingredients), anti-inflammatory ingredients, antioxidant ingredients, anti-wrinkle ingredients, collagen synthesis promoting ingredients, reactive oxygen species scavenging ingredients, cell turnover promoting ingredients, anti-aging ingredients, blood circulation promoting ingredients, and keratin softening ingredients. As described above, the present invention allows for efficient transdermal absorption of water-soluble components, thus enabling the efficient performance of such functions.

[0053] Specific water-soluble ingredients (e.g., water-soluble whitening ingredients) include, for example, ascorbic acid, amino acids, hydroquinones, nicotinamides (e.g., nicotinamide), glycyrrhizic acid, allantoins (e.g., allantoin), riboflavins (e.g., riboflavin), peptides (e.g., glutathione), and extracts [e.g., placenta (placenta extract), chamomile extract, etc.].

[0054] Examples of ascorbic acid compounds include ascorbic acid, ascorbic acid derivatives, and salts thereof.

[0055] Ascorbic acid may be the D-isomer, the L-isomer, or a mixture thereof, but the L-isomer [L-ascorbic acid (vitamin C)] may be preferably used.

[0056] Examples of ascorbic acid derivatives include phosphate esters (e.g., ascorbic acid monophosphate, ascorbic acid diphosphate, ascorbic acid triphosphate, etc.), sulfate esters (e.g., ascorbic acid 2-sulfate), alkyl ascorbic acid (e.g., alkyl ascorbic acid such as methyl ascorbic acid and ethyl ascorbic acid), and glycosides of ascorbic acid (e.g., ascorbic acid 2-glucoside, etc.).

[0057] Examples of salts include metal salts {e.g., alkali metal salts (e.g., sodium, potassium, etc.), polyvalent metal salts [e.g., alkali metal salts (e.g., magnesium, calcium, barium, etc.), aluminum salts, zinc salts, iron salts]}, ammonium salts (e.g., ammonium, tricyclohexylammonium, etc.), amine salts [e.g., alkylamines (e.g., methylamine, triethylamine, diethylamine, etc.), alkanolamines (e.g., monoethanolamine, diethanolamine, triethanolamine, monoisopropanolamine, diisopropanolamine, triisopropanolamine, etc.), cyclic amines (e.g., morpholine salts, piperazine salts, pyrrolidine salts, tripyridine salts, picoline salts), etc.].

[0058] Representative ascorbic acid derivatives include ascorbic acid (especially vitamin C), ascorbic acid phosphate esters (such as ascorbyl phosphate and ascorbic acid monophosphate), alkyl ascorbic acid [especially ethyl ascorbate (3-O-ethyl ascorbic acid or VC ethyl, etc.)], ascorbic acid-2-glucoside, and their salts (e.g., sodium ascorbate, sodium ascorbyl phosphate, magnesium ascorbyl phosphate, etc.).

[0059] Examples of amino acids include tranexamic acids and epsilon-aminocaproic acids (such as epsilon-aminocaproic acid and its salts).

[0060] Examples of tranexamic acids include tranexamic acid, tranexamic acid derivatives {e.g., polymers of tranexamic acid [e.g., tranexamic acid dimers such as trans-4-(trans-aminomethylcyclohexanecarbonyl)aminomethylcyclohexanecarboxylic acid hydrochloride], esters of tranexamic acid and hydroquinone (e.g., 4'-hydroxyphenyl ester of trans-4-aminomethylcyclohexanecarboxylic acid), esters of tranexamic acid and gentisic acid [e.g., 2-(trans-4-aminomethylcyclohexylcarbonyloxy)-5-hydroxybenzoic acid], amides of tranexamic acid [e.g., trans-4-aminomethylcyclohexanecarboxylic acid methylamide and its salts, trans-4-(p-methoxybenzoyl)aminomethylcyclohexanecarboxylic acid, trans-4-guanidinomethylcyclohexanecarboxylic acid], etc.}, and salts thereof.

[0061] Examples of salts include the salts mentioned above [for example, alkali metal salts (e.g., sodium salts, potassium salts), amine salts (e.g., triethanolamine salts)], as well as salts with amino acids (e.g., basic amino acids such as arginine, lysine, histidine, and ornithine).

[0062] Representative amino acids include, for example, tranexamic acid, tranexamic acid salts (e.g., sodium salt, potassium salt, triethanolamine salt, arginine salt, etc.), and epsilonaminocaproic acid.

[0063] Examples of hydroquinones include hydroquinone, hydroquinone glycosides, and salts thereof.

[0064] Examples of hydroquinone glycosides include glucose glycosides (e.g., hydroquinone α-D-glucose, hydroquinone β-D-glucose (arbutin), hydroquinone α-L-glucose, hydroquinone β-L-glucose) and galactose glycosides (e.g., hydroquinone α-D-galactose, hydroquinone β-D-galactose, hydroquinone α-L-galactose, hydroquinone β-L-galactose) Hexose glycosides (such as ctose); pentose glycosides such as ribose glycosides (e.g., hydroquinone α-D-ribose, hydroquinone β-D-ribose, hydroquinone α-L-ribose, hydroquinone β-L-ribose), arabinose glycosides (e.g., hydroquinone α-D-arabinose, hydroquinone β-D-arabinose, hydroquinone α-L-arabinose, hydroquinone β-L-arabinose); gluco Aminoglycosides such as samine glycosides (e.g., hydroquinone α-D-glucosamine, hydroquinone β-D-glucosamine, hydroquinone α-L-glucosamine, hydroquinone β-L-glucosamine), galactosamine glycosides (e.g., hydroquinone α-D-galactosamine, hydroquinone β-D-galactosamine, hydroquinone α-L-galactosamine, hydroquinone β-L-galactosamine); glucuro Examples include uronic acid glycosides such as hydroquinone α-D-glucuronic acid, hydroquinone β-D-glucuronic acid, hydroquinone α-L-glucuronic acid, and hydroquinone β-L-glucuronic acid, as well as galacturonic acid glycosides such as hydroquinone α-D-galacturonic acid, hydroquinone β-D-galacturonic acid, hydroquinone α-L-galacturonic acid, and hydroquinone β-L-galacturonic acid.

[0065] Representative hydroquinones include hydroquinone, arbutin (hydroquinone β-D-glucose), and their salts.

[0066] Examples of glycyrrhizic acid compounds include glycyrrhizic acid and glycyrrhizinate salts. Examples of salts include the salts exemplified above [for example, alkali metal salts (e.g., sodium salt, potassium salt, etc.), alkaline earth metal salts (e.g., calcium salt, magnesium salt, etc.), aluminum salts, ammonium salts, amine salts (e.g., methylamine salt, triethylamine salt, diethylamine salt, triethanolamine salt, morpholine salt, piperazine salt, pyrrolidine salt, tripyridine salt, picoline salt, etc.)]. Representative glycyrrhizinate salts include dipotassium glycyrrhizinate and monoammonium glycyrrhizinate.

[0067] Among these water-soluble components, ascorbic acid, tranexamic acid, epsilon-aminocaproic acid, hydroquinone, nicotinamide, glycyrrhizic acid, allantoin, and riboflavin are preferred.

[0068] In particular, among these, ascorbic acid, ascorbic acid derivatives (e.g., ascorbic acid phosphate ester, alkyl ascorbate, ascorbic acid-2-glucoside), tranexamic acid, epsilonaminocaproic acid, hydroquinone, hydroquinone glycosides (e.g., arbutin), nicotinamide, glycyrrhizic acid, allantoin, riboflavin, and their salts (e.g., sodium ascorbate, magnesium ascorbyl phosphate, dipotassium glycyrrhizate, etc.) may be preferably used from the viewpoint of water solubility and molecular size.

[0069] Water-soluble components may be used individually or in combination of two or more types.

[0070] If the composition contains component (C), the amount of component (C) in the composition can be selected according to the intended use of the composition and the function of the water-soluble component (C), but may be, for example, 0.001 to 10% by mass, preferably 0.01 to 8% by mass, and more preferably 0.05 to 5% by mass, relative to the total amount of the composition. Furthermore, the amount of component (C) in the composition may be 3% by mass or less (for example, 1% by mass or less, 0.1% by mass or less, 0.001 to 0.1% by mass, etc.) or 0.01% by mass or more (for example, 0.05% by mass or more, 1% by mass or more, etc.).

[0071] If the composition contains component (A), the proportion of component (C) may be, for example, 0.1 to 5000 parts by mass (e.g., 0.3 to 3000 parts by mass), preferably 0.5 to 1000 parts by mass (e.g., 0.7 to 800 parts by mass), and more preferably 1 to 500 parts by mass (e.g., 5 to 400 parts by mass, 1 to 100 parts by mass), per 1 part by mass of component (A).

[0072] If the composition contains component (B), the proportion of component (C) may be, for example, 0.001 to 2000 parts by mass (e.g., 0.005 to 1500 parts by mass), preferably 0.01 to 1000 parts by mass (e.g., 0.02 to 500 parts by mass), and more preferably 0.1 to 300 parts by mass (e.g., 0.2 to 200 parts by mass), per 1 part by mass of component (B).

[0073] If the composition contains components (A) and (B), the proportion of component (C) may be, for example, 0.001 to 1000 parts by mass (e.g., 0.005 to 800 parts by mass), preferably 0.01 to 500 parts by mass (e.g., 0.02 to 400 parts by mass), and more preferably 0.05 to 300 parts by mass (e.g., 0.1 to 200 parts by mass, 0.5 to 50 parts by mass), relative to 1 part by mass of the total amount of components (A) and (B).

[0074] Active ingredients The composition of the present invention may optionally contain active ingredients. Specific examples of active ingredients include, for example, moisturizing ingredients, anti-inflammatory ingredients, antibacterial ingredients, vitamins, peptides or their derivatives, amino acids or their derivatives, cell-activating ingredients, anti-aging ingredients, blood circulation-promoting ingredients, keratin-softening ingredients, whitening ingredients, astringent ingredients, and UV-protective ingredients. In this invention, even if such active ingredients are included, the functions of components (A) to (C) can be effectively exerted. Furthermore, the active ingredient may be an ingredient that falls under ingredient (C), or it may be an ingredient that does not fall under that category.

[0075] Examples of moisturizing ingredients include polyhydric alcohols such as glycerin, propanediol, propylene glycol, 1,3-butylene glycol, dipropylene glycol, polyethylene glycol, diglycerin, trehalose, inositol, and sorbitol; high molecular weight compounds such as collagen, elastin, keratin, chitin, chitosan, fucoidan, and hyaluronic acids (e.g., hydrolyzed hyaluronic acid, acetylated hyaluronic acid, sodium hyaluronate, etc.); amino acids such as glycine, aspartic acid, and arginine; natural moisturizing factors such as sodium lactate, urea, and sodium pyrrolidone carboxylate; lipids such as ceramide, cholesterol, and phospholipids; and plant extracts such as chamomile extract, witch hazel extract, tea extract, lemon extract, centella asiatica extract, and artichoke extract.

[0076] Examples of anti-inflammatory components include those derived from plants (e.g., comfrey), zinc oxide, pyridoxine hydrochloride, tocopherol acetate, salicylic acid or its derivatives, and ε-aminocaproic acid.

[0077] Examples of antibacterial components include chlorhexidine, salicylic acid, benzalkonium chloride, acrinol, ethanol, benzethonium chloride, cresol, gluconic acid and its derivatives, povidone-iodine, potassium iodide, iodine, isopropylmethylphenol, triclocarban, triclosan, photosensitizer 101, photosensitizer 201, parabens, phenoxyethanol, 1,2-pentanediol, alkyldiaminoglycine hydrochloride, iodidepropynyl butylcarbamate, caprylhydroxamic acid, methylisothiazolinone, sorbic acid, β-glycyrrhetinic acid, and components derived from plants (e.g., Sophora flavescens, rosemary, mulberry, eucalyptus, etc.).

[0078] Vitamins include vitamin E derivatives such as dl-α-tocopherol, dl-α-tocopherol acetate, dl-α-tocopherol succinate, and dl-α-tocopherol calcium succinate; vitamin B2 derivatives such as riboflavin, flavin mononucleotide, flavin adenine dinucleotide, riboflavin butyrate, riboflavin tetrabutyrate, riboflavin 5'-phosphate sodium, and riboflavin tetranicotinate; and dl-α-tocopherol nicotinate, benzyl nicotinate, methyl nicotinate, and β-butyrate nicotinate. Nicotinic acids such as oxyethyl nicotinate and 1-(4-methylphenyl)ethyl nicotinate; vitamin C compounds such as ascorbigen-A, ascorbic acid stearate, ascorbic acid palmitate, and L-ascorbyl dipalmitate; vitamin D compounds such as methyl hesperidin, ergocalciferol, and cholecalciferol; vitamin K compounds such as phylloquinone and farnoquinone; γ-oryzanol, dibenzoylthiamine, dibenzoylthiamine hydrochloride; thiamine hydrochloride, thiamine cetyl hydrochloride, thiamine thiocyanate, and thiamine lauryl salt Vitamin B1s such as salts, thiamine nitrate, thiamine monophosphate, thiamine lysine salt, thiamine triphosphate, thiamine monophosphate phosphate, thiamine monophosphate, thiamine diphosphate, thiamine diphosphate hydrochloride, thiamine triphosphate, thiamine triphosphate monophosphate; Vitamin B6s such as pyridoxine hydrochloride, pyridoxine acetate, pyridoxal hydrochloride, pyridoxal 5'-phosphate, pyridoxamine hydrochloride; Vitamin B1s such as cyanocobalamin, hydroxocobalamin, deoxyadenosylcobalamin Vitamin B12s; folic acid derivatives such as folic acid and pteroylglutamic acid; nicotinic acid derivatives such as nicotinic acid and nicotinamide; pantothenic acid derivatives such as pantothenic acid, calcium pantothenate, pantothenyl alcohol (panthenol), D-panthesine, D-pantethine, coenzyme A, and pantothenyl ethyl ether; biotin derivatives such as biotin and biotisine; vitamin C derivatives such as ascorbic acid, sodium ascorbate, dehydroascorbic acid, sodium ascorbate phosphate, and magnesium ascorbate phosphate;Vitamin-like factors such as carnitine, pyrroloquinoline quinone, ferulic acid, alpha-lipoic acid, and orotic acid, as well as other known ingredients that can be used in cosmetics, pharmaceuticals, and quasi-drugs, may be used as appropriate.

[0079] Examples of peptides or their derivatives include keratin-degrading peptides, hydrolyzed keratin, collagen, fish-derived collagen, atelocollagen, gelatin, elastin, elastin-degrading peptides, collagen-degrading peptides, hydrolyzed collagen, hydroxypropylammonium chloride hydrolyzed collagen, elastin-degrading peptides, conchiolin-degrading peptides, hydrolyzed conchiolin, silk protein-degrading peptides, hydrolyzed silk, sodium lauroyl hydrolyzed silk, soy protein-degrading peptides, hydrolyzed soy protein, wheat protein, wheat protein-degrading peptides, hydrolyzed wheat protein, casein-degrading peptides, and acylated peptides (such as palmitoyl oligopeptides, palmitoyl pentapeptides, and palmitoyl tetrapeptides).

[0080] Examples of amino acids or their derivatives include betaine (trimethylglycine), proline, hydroxyproline, arginine, lysine, serine, glycine, alanine, phenylalanine, β-alanine, threonine, glutamic acid, glutamine, asparagine, aspartic acid, cysteine, cystine, methionine, leucine, isoleucine, valine, histidine, taurine, γ-aminobutyric acid, γ-amino-β-hydroxybutyric acid, carnitine, carnosine, and creatine.

[0081] Cell-activating components include amino acids such as γ-aminobutyric acid and ε-aminopronic acid; vitamins such as retinol, thiamine, riboflavin, pyridoxine hydrochloride, and pantothenic acids; α-hydroxy acids such as glycolic acid and lactic acid; tannins, flavonoids, saponins, allantoin, photosensitizer 301, plant-derived components (for example, soybean bilberry, lemongrass, aloe vera, chlorella, iris, coix seed, chamomile, houttuynia cordata, hops, carrots, etc.); royal jelly and royal jelly extract; whey-derived extracts such as whey, yogurt extract, hydrolyzed milk protein, and yeast extract.

[0082] Examples of anti-aging ingredients include hydrolyzed soy protein, retinoids (retinol, retinoic acid, retinal, etc.), ursolic acid, peptides (caprooyl tetrapeptide-3, oligopeptide-24, etc.), ingredients derived from plants (e.g., artichoke, Rosa rugosa, seaweed, bilberry, birch, plantain, angelica tree, scutellaria baicalensis, St. John's wort, comfrey, neem, rosehip, iris, geranium, linden, peony root, etc.), pangamic acid, kinetin, ursolic acid, turmeric extract, sphingosine derivatives, silicon, silicic acid, N-methyl-L-serine, mevalonolactone, etc.).

[0083] Examples of blood circulation-promoting ingredients include those derived from plants (for example, ginseng, angelica tree, arnica, ginkgo, fennel, laurel, watercress, chamomile, Roman chamomile, carrot, gentian, burdock, rice, hawthorn, shiitake mushroom, European hawthorn, European juniper, cinnamon, gentian, thyme, clove, dried tangerine peel, angelica, peach kernel, spruce, carrot, garlic, butcher's broom, grape, peony, horse chestnut, lemon balm, yuzu, coix seed, rosemary, rosehip, peach, apricot, walnut, corn); glucosyl hesperidin, etc.

[0084] Examples of keratin-softening ingredients include salicylic acid, glycolic acid, fruit acids, phytic acid, and sulfur.

[0085] Examples of skin-whitening ingredients include tocopherol.

[0086] Examples of astringent components include zinc paraphenolsulfonate, zinc oxide, menthol, and ethanol.

[0087] Examples of UV protection ingredients include 2-ethylhexyl paramethoxycinnamate, hexyl 2-[4-(diethylamino)-2-hydroxybenzoyl]benzoate, 2,4,6-tris[4-(2-ethylhexyloxycarbonyl)anilino]-1,3,5-triazine, t-butyl methoxydibenzoylmethane, ethylhexyl dibenzylidene dioxoimidazolidine propyronate, etorhexyl triazoline, para-aminobenzoic acid and its derivatives, octyl paradimethylaminobenzoate, ethylene glycol salicylate, dihydroxybenzophenone, titanium dioxide, and zinc oxide.

[0088] The active ingredients may be used alone or in combination of two or more.

[0089] additives The composition of the present invention may optionally contain additives such as surfactants, antioxidants, preservatives, thickeners, pH adjusters, buffers, isotonic agents, thickeners or viscosity modifiers, oils, stabilizers, irritation reducers, colorants, fragrances, chelating agents, etc. In this invention, even if such additives are included, the functions of components (A) to (C) can be effectively exerted. The additive may be an ingredient that falls under component (C), or it may be an ingredient that does not fall under that category.

[0090] Examples of surfactants include nonionic surfactants. Specific examples of surfactants (nonionic surfactants) include polyglyceryl-2 oleate, polyglyceryl-10 pentaoleate, polyglyceryl-10 laurate, polyglyceryl-10 myristate, polyglyceryl-10 stearate, polyglyceryl-10 isostearate, polyglyceryl-10 oleate, polyglyceryl-10 distearate, polyglyceryl-10 diisostearate, polyglyceryl-10 tristearate, polyglyceryl-10 trioleate, polyglyceryl-10 pentastearate, polyglyceryl-10 pentahydroxystearate, polyglyceryl-10 pentaisostearate, polyglyceryl-10 pentaoleate, polyglyceryl-10 decaoleate, polyglyceryl-2 stearate, iso Polyglycerin fatty acid esters such as polyglyceryl-2 stearate, polyglyceryl-6 myristate, polyglyceryl-6 laurate, polyglyceryl-6 stearate, polyglyceryl-6 tristearate, polyglyceryl-6 pentastearate, polyglyceryl-4 oleate, and polyglyceryl-6 stearate; PEG [polyethylene glycol or polyoxyethylene (POE)] hydrogenated castor oil (POE hydrogenated castor oil) such as PEG-5 hydrogenated castor oil, PEG-10 hydrogenated castor oil, PEG-20 hydrogenated castor oil, PEG-40 hydrogenated castor oil, PEG-50 hydrogenated castor oil, PEG-60 hydrogenated castor oil, and PEG-100 hydrogenated castor oil; POE castor oil 3, POE castor oil 4, POE castor oil 6, POE castor oil 7, POE castor oil 10, and POE castor oil 13.5. POE castor oil such as POE castor oil 17, POE castor oil 20, POE castor oil 25, POE castor oil 30, POE castor oil 35, POE castor oil 50; sorbitan fatty acid esters such as sorbitan sesquioleate, sorbitan laurate, sorbitan palmitate, sorbitan stearate, sorbitan sesquistearate, sorbitan tristearate, sorbitan isostearate, sorbitan sesquiisostearate, sorbitan oleate, sorbitan trioleate; POE(20) sorbitan monolaurate (polysorbate 20 Polysorbates (POE sorbitan fatty acid esters) such as POE(20) sorbitan monopalmitate (polysorbate 40), POE(20) sorbitan monostearate (polysorbate 60), POE(20) sorbitan tristearate (polysorbate 65), POE(20) sorbitan monooleate (polysorbate 80), POE(20) sorbitan trioleate (polysorbate 85); POEPOP glycol (196E.O.) (67P.O.) (or polyoxyethylene(196) polyoxypropylene(67) glycol Cole (the same applies in the following expressions, poloxamer 407), POEPOP glycol (20 E.O.) (20 P.O.), POEPOP glycol (42 E.O.) (67 P.O.) (poloxamer 403), POEPOP glycol (54 E.O.) (39 P.O.) (poloxamer 235), POEPOP glycol (124 E.O.) (39 P.O.), POEPOP glycol (160 E.O.) (30 P.O.), POEPOP glycol (200 E.O.) (70 P.O.), POEPOP glycol (30 E.O.) (150 P.O.) POE-POP glycols such as (Poloxamer 188); polyethylene glycol monostearate (2 E.O.), polyethylene glycol monostearate (4 E.O.), polyethylene glycol monostearate (9 E.O.), polyethylene glycol monostearate (10 E.O.), polyethylene glycol monostearate (23 E.O.), polyethylene glycol monostearate (25 E.O.), polyethylene glycol monostearate (32 E.O.), polyethylene glycol monostearate (40 E.O.)Examples include polyethylene glycol monostearate such as polyoxyl stearate (40), polyethylene glycol monostearate (45 E.O.), polyethylene glycol monostearate (55 E.O.), polyethylene glycol monostearate (75 E.O.), and polyethylene glycol monostearate (140 E.O.); POE alkyl ethers such as POE(9) lauryl ether; POE-POP alkyl ethers such as POE(20)POP(4) cetyl ether; and POE alkylphenyl ethers such as POE(10) nonylphenyl ether. In the compounds exemplified above, POE represents polyoxyethylene, POP represents polyoxypropylene, and the number in parentheses indicates the number of moles added.

[0091] Examples of antioxidants include dibutylhydroxytoluene, butylhydroxyanisole, sorbic acid, sodium sulfite, ascorbic acid, erythorbic acid, and L-cysteine ​​hydrochloride.

[0092] Examples of preservatives include benzoic acid, sodium benzoate, dehydroacetic acid, sodium dehydroacetate, isobutyl parahydroxybenzoate, isopropyl parahydroxybenzoate, butyl parahydroxybenzoate, ethyl parahydroxybenzoate, propyl parahydroxybenzoate, benzyl parahydroxybenzoate, methyl parahydroxybenzoate, phenoxyethanol, benzyl alcohol, chlorobutanol, sorbic acid and its salts, chlorhexidine gluconate, alkanediol, and glycerin fatty acid esters.

[0093] Examples of thickening agents include guar gum, locust bean gum, carrageenan, xanthan gum, carboxymethylcellulose, hydroxymethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, polyvinyl alcohol, polyvinylpyrrolidone, carboxyvinyl polymer, alkyl acrylate methacrylate copolymer, polyethylene glycol, bentonite, (hydroxyethyl acrylate / sodium acryloyldimethyltaurate) copolymer, (ammonium acryloyldimethyltaurate / vinylpyrrolidone) copolymer, and others.

[0094] Examples of pH adjusters include inorganic acids (hydrochloric acid, sulfuric acid, etc.), organic acids (lactic acid, sodium lactate, citric acid, sodium citrate, succinic acid, sodium succinate, etc.), inorganic bases (potassium hydroxide, sodium hydroxide, etc.), and organic bases (triethanolamine, diisopropanolamine, triisopropanolamine, etc.).

[0095] Examples of buffering agents include boric acid-based buffering agents, phosphate-based buffering agents, carbonate-based buffering agents, citrate-based buffering agents, and acetate-based buffering agents.

[0096] Examples of isotonic agents include sodium chloride, potassium chloride, calcium chloride, magnesium chloride, potassium acetate, sodium acetate, magnesium sulfate, glycerin, and propylene glycol.

[0097] Examples of thickeners or viscosity-enhancing agents include guar gum, hydroxypropyl guar gum, cellulosic polymers (e.g., methylcellulose, ethylcellulose, hydroxypropyl methylcellulose, hydroxyethylcellulose, sodium carboxymethylcellulose, etc.), acacia gum, karaya gum, xanthan gum, agar, alginic acid, α-cyclodextrin, dextrin, dextran, mucopolysaccharides (e.g., heparinoids, heparin, heparin sulfate, heparan sulfate, heparinoids, hyaluronic acid, hyaluronic acid salts (sodium salts, etc.), etc.), starch, chitin and its derivatives, chitosan and its derivatives, carrageenan, sorbitan Examples include tol, polyvinyl polymer compounds (polyvinylpyrrolidone, polyvinyl alcohol, carboxyvinyl polymer, etc.), alkali metal salts of polyacrylic acid (sodium salt and potassium salt, etc.), amine salts of polyacrylic acid (monoethanolamine salt, diethanolamine salt, triethanolamine salt, etc.), casein, gelatin, collagen, pectin, elastin, ceramide, liquid paraffin, glycerin, polyethylene glycol, macrogol, polyethyleneimine alginate (sodium salt, etc.), alginate esters (propylene glycol ester, etc.), tragacanth powder, and triisopropanolamine.

[0098] Oils include hydrocarbon oils (e.g., liquid paraffin, liquid isoparaffin, squalane, squalene, α-olefin oligomers), fats and oils {e.g., vegetable oils [e.g., soybean oil, rapeseed oil, corn oil, sesame oil, flaxseed oil, safflower oil, sunflower oil, cottonseed oil, nut oils (macadamia nut oil, hazelnut oil, peanut oil, almond oil, walnut oil, etc.), seed oils (grape seed oil, pumpkin seed oil, etc.), lemon oil, camellia oil, tea seed oil, perilla oil, borage oil, olive oil, rice oil, rice bran oil, wheat germ oil, coconut oil, palm oil, palm olein, palm kernel oil, etc.], animal oils (e.g., fish oil, liver oil, whale oil, etc.), medium-chain triglycerides Examples include ester oils (e.g., MCT), ester oils (e.g., adipate esters (e.g., diisobutyl adipate, di-2-ethylhexyl adipate, dibutyl adipate), isooctanoate esters (e.g., glyceryl triisooctanoate (glyceride triisooctanoate)), isononanoate esters (e.g., isononyl isononanoate), myristicate esters (e.g., isopropyl myristate), isostearate esters (e.g., batyl isostearate), sebacate esters (e.g., diethyl sebacate), etc.), silicone oils, fatty acids (e.g., isostearic acid), and higher alcohols. The properties of the oil at room temperature (25°C) may be solid, liquid, semi-solid, or paste-like (for example, with a viscosity of approximately 5,000 to 100,000 mPa·s at 30°C). Furthermore, the composition of the present invention may or may not contain such oil [for example, paste-like oil (paste oil)]. If such oil is included, the proportion in the composition is not particularly limited and may be less than 15% by mass, 10% by mass or less (for example, less than 10% by mass), etc.

[0099] Examples of stabilizers include sodium polyacrylate, dibutylhydroxytoluene, and butylhydroxyanisole.

[0100] Examples of irritation-reducing agents include licorice extract and sodium alginate.

[0101] Examples of colorants include those listed in the Legal Colorants Handbook (compiled by the Japan Cosmetic Industry Association (2004), etc.).

[0102] Examples of fragrances include herbal essential oils such as lavender oil, rosemary oil, clary sage oil, thyme oil, bergamot oil, and eucalyptus oil; mint essential oils such as peppermint oil, spearmint oil, and peppermint oil; and various citrus essential oils such as orange oil, lemon oil, and grapefruit oil, as well as blended fragrances.

[0103] Examples of chelating agents include EDTA-disodium salt and EDTA-calcium-disodium salt.

[0104] Additives may be used individually or in combination of two or more types.

[0105] Base or carrier The compositions of the present invention may typically contain a base or a carrier.

[0106] Examples of bases or carriers include water, water-soluble solvents [lower alcohols (e.g., ethanol, isopropanol), polyhydric alcohols (e.g., glycerin, propylene glycol, propanediol, polyethylene glycol (macrogol), 1,3-butylene glycol, isoprene glycol, dipropylene glycol, etc.)], and oily bases. Water may be replaced with physiological saline solution. The base or carrier can be used individually or in combination of two or more types.

[0107] In particular, the composition of the present invention may be an aqueous composition (for example, a composition containing water, physiological saline, or a mixed solvent of water or physiological saline and a water-soluble solvent).

[0108] When water is combined with other base materials or carriers (e.g., water-soluble solvents), the ratio of these materials may be, for example, water / other base material or carrier (mass ratio) = 99.9 / 0.1~10 / 90 (e.g., 99.5 / 0.5~30 / 70), preferably 99 / 1~40 / 60 (e.g., 98 / 2~50 / 50), and even more preferably 97 / 3~60 / 40 (e.g., 95 / 5~70 / 30).

[0109] If the composition of the present invention contains water (especially if it is an aqueous composition), the proportion of water in the composition can be selected from a range of 10% by mass or more (for example, 20% by mass or more), for example, 30% by mass or more (for example, 40% by mass or more), preferably 50% by mass or more (for example, 60% by mass or more), and more preferably 60% by mass or more (for example, 70% by mass or more, 75% by mass or more, 80% by mass or more, etc.).

[0110] The upper limit of water content in the composition can be appropriately selected depending on the intended use of the composition, but may be, for example, 99% by mass, 98% by mass, 97% by mass, 96% by mass, 95% by mass, 94% by mass, 93% by mass, 92% by mass, 91% by mass, 90% by mass, etc.

[0111] In this invention, component (A) can be included in such aqueous compositions with excellent solubility or dispersibility. Furthermore, in this invention, excellent transdermal absorption of component (C) can be efficiently achieved even in aqueous compositions containing component (C). Thus, according to the present invention, high-quality aqueous compositions can be obtained efficiently.

[0112] pH The pH of the composition of the present invention may be, for example, 2 to 10, preferably 2.5 to 9, and more preferably 3 to 8.

[0113] Properties, uses, preparation methods, etc. The compositions of the present invention can be prepared by mixing the above components (for example, a composition comprising at least components (A) to (B) and a base or carrier, a composition comprising at least component (A) and a base or carrier, a composition comprising at least components (A) to (C) and a base or carrier, etc.).

[0114] The properties of the composition of the present invention are not particularly limited, and may be any of the following: liquid, fluid, gel, or semi-solid. Furthermore, it may be prepared as a liquid, fluid, gel, or semi-solid at the time of use. A semi-solid state refers to a state that has plasticity, such as an ointment, which can be deformed by applying force.

[0115] The preferred state of the composition is liquid (liquid formulation).

[0116] The viscosity of the liquid composition at 25°C may be, for example, 500 Pa·s or less, preferably 400 Pa·s or less, and more preferably 300 Pa·s or less. Viscosity can be measured at 25°C using, for example, a rotational viscometer (RB80L viscometer, manufactured by Toki Sangyo Co., Ltd.).

[0117] The compositions of the present invention may be opaque (turbid) or transparent. In the present invention, even an aqueous composition containing component (A) can efficiently yield a transparent (or less turbid) composition.

[0118] When the composition of the present invention is in an emulsified state, it may be either an O / W type (oil-in-water) or a W / O type (water-in-oil), but it is usually an O / W type.

[0119] The uses of the composition of the present invention are not particularly limited, but it may be used as a topical composition (topical preparation), and in particular as a skin composition (topical skin composition).

[0120] Furthermore, the composition of the present invention may also be used as a leave-on composition (leave-on type composition). As described above, the present invention includes a composition containing a water-soluble component (C) as one embodiment. Such a composition can improve transdermal absorption with components (A) and / or (B), and is therefore suitable for leave-on applications where removal by washing or the like is not expected.

[0121] Such compositions (external compositions) may be cosmetics, pharmaceuticals (external pharmaceuticals), or quasi-drugs.

[0122] The composition is not particularly limited in form, but examples include liquids, suspensions, emulsions, creams, ointments, gels, liniments, lotions, aerosols, and the like.

[0123] Specific forms of compositions include, for pharmaceutical compositions, liquids, emulsions, creams, ointments, gels, etc., and for quasi-drugs or cosmetic external compositions, examples include basic cosmetics (e.g., lotions, emulsions, gels, creams, serums, sunscreens, packs, masks, body lotions, etc.), makeup cosmetics (e.g., foundations, makeup bases, lip balms, lipsticks, blushes, etc.), cleansing cosmetics (e.g., facial cleansers, makeup removers, body washes, shampoos, etc.), cleansing agents (e.g., cleansing lotions, cleansing oils, cleansing creams, cleansing sheets) and other cosmetics (especially leave-on cosmetics); and bath additives.

[0124] In particular, compositions containing (C) water-soluble components may be suitably used as leave-on compositions (for example, leave-on cosmetics such as basic cosmetics, makeup cosmetics, and sunscreens, and especially basic cosmetics such as lotions and serums).

[0125] container The composition of the present invention may be contained in a container (filled, injected, sealed). The container can be any packaging body having a portion (surface) that comes into contact with the composition (formulation), and may consist of, for example, a container body portion that contains the composition (e.g., a liquid composition), a portion including the dispenser of the container (nozzle, inner stopper), a suction tube, a cap, etc.

[0126] The materials that make up the container can be selected from a wide range, for example, at least part or all of the part that comes into contact with the composition may be plastic (e.g., olefin resins, styrene resins, acrylic resins, polyester resins, polycarbonate resins, fluororesins, chlorine resins (such as polyvinyl chloride), polyamide resins, polyacetal resins, polyphenylene ether resins (such as modified polyphenylene ether), polyarylate, polysulfone, polyimide resins, epoxy resins, cellulose resins (such as cellulose acetate), hydrocarbon resins which may be substituted with halogen atoms, etc.), glass, metal (such as aluminum), etc.

[0127] The container may be made of a single material or two or more materials.

[0128] Examples of olefin resins include ethylene resins [for example, polyethylene (including high-density polyethylene, low-density polyethylene, ultra-low-density polyethylene, linear low-density polyethylene, ultra-high molecular weight polyethylene, etc.), ethylene-propylene copolymers, etc.], propylene resins [for example, polypropylene (PP) (including isotactic polypropylene, syndiotactic polypropylene, atactic polypropylene, etc.), propylene-ethylene copolymers, etc.], and methylpentene resins (for example, polymethylpentene, etc.).

[0129] Examples of styrene-based resins include polystyrene and acrylonitrile-containing styrene-based resins (e.g., acrylonitrile-styrene copolymer (AS resin), acrylonitrile-butadiene-styrene copolymer (ABS resin), etc.).

[0130] Examples of acrylic resins include resins that use acrylic acid esters such as methyl acrylate, methacrylate esters such as methyl methacrylate, cyclohexyl methacrylate, and t-butylcyclohexyl methacrylate as polymerization components.

[0131] Examples of polyester resins include aromatic polyester resins [for example, resins having alkylene terephthalate units (alkylene terephthalate resins: for example, polyethylene terephthalate (PET), polytrimethylene terephthalate, polybutylene terephthalate (PBT), etc.), and resins having alkylene naphthalate units (for example, polyethylene naphthalate (PEN), polybutylene naphthalate, etc.)].

[0132] Examples of fluororesins include fluorine-substituted polyethylene (polytetrafluoroethylene, polychlorotrifluoroethylene, etc.), polyvinylidene fluoride, polyvinyl fluoride, perfluoroalkoxy fluororesins, tetrafluoroethylene-hexafluoropropylene copolymer, ethylene-tetrafluoroethylene copolymer, and ethylene-chlorotrifluoroethylene copolymer.

[0133] Polyacetal resins include those consisting solely of oxymethylene units, as well as those containing some oxyethylene units.

[0134] Examples of modified polyphenylene ethers include polystyrene-modified polyphenylene ether.

[0135] Examples of polyarylates include amorphous polyarylates.

[0136] Examples of polyimide resins include aromatic polyimides, such as those obtained by polymerizing pyromellitic dianhydride and 4,4'-diaminodiphenyl ether.

[0137] Examples of cellulose acetates include cellulose diacetate and cellulose triacetate.

[0138] Glass, plastic, and the like are preferred materials for the container. Therefore, at least a part of the container (or the material of the container) may be made of glass, plastic, or the like.

[0139] In particular, plastics such as olefin resins, styrene resins, and polyester resins (i.e., plastic containers) are preferred, ethylene resins, propylene resins, alkylene terephthalate resins, and polystyrene are more preferred, polypropylene, polyethylene terephthalate, and polystyrene are even more preferred, and polyethylene terephthalate is even more preferred.

[0140] The composition of the present invention can efficiently exhibit its function as a composition in a relatively wide variety of containers (or their materials, such as glass, plastic, and especially plastics such as PET).

[0141] The container material may also be a polymer blend with polymers other than the aforementioned polymer. When the container material of the container for containing the composition of the present invention is a blend polymer with the aforementioned polymer, the mixing ratio of the aforementioned polymer and polymers other than the aforementioned polymer is not particularly limited as long as the effects of the present invention are achieved, but it is preferable that the total weight of the aforementioned polymer is 30 w / w% or more, more preferably 50 w / w% or more, even more preferably 65 w / w% or more, and particularly preferably 80 w / w% or more, relative to the total amount of the constituent material.

[0142] The container may have at least a portion of its contact surface with the composition of the present invention made of the above material. For example, a layer or film made of the above material may be formed on the inner surface of the container, or the container itself may be molded from the above material.

[0143] Furthermore, the parts that make up the container (the container body, the part of the container including the dispensing port (nozzle, inner stopper), suction tube, cap, etc.) may be made of the above material, or the entire container may be made of the above material.

[0144] How to use The composition of the present invention may vary depending on the skin condition, age, and gender of the person using it, but it can be used, for example, in the following ways. For example, the composition (such as a composition containing (C) a water-soluble component) may be applied to the skin in an appropriate amount (for example, about 0.05 to 10 g) once or multiple times a day (for example, about 1 to 5 times, preferably 1 to 3 times). Alternatively, the composition may be applied so that the daily amount of (C) a water-soluble component (such as VC ethyl or tranexamic acid) is preferably about 0.01 to 500 mg, more preferably about 0.2 to 200 mg. The application period may be, for example, about 1 to 14 days, preferably about 3 to 14 days.

[0145] The composition of the present invention can be appropriately selected depending on the type of water-soluble component and the type of any active ingredient, but it can be suitably used for the prevention, treatment and / or improvement of diseases (or symptoms) such as melasma, age spots, acne, acne scars, wrinkles, and rough skin. Therefore, in addition to healthy individuals, people with these skin conditions can be suitable targets for use.

[0146] [2. Improvement of solubility or dispersibility] In one aspect of the present invention, the solubility or dispersibility of component (A) in the composition can be improved (or enhanced).

[0147] Accordingly, the following method is provided as an embodiment of the present invention. (A) A method for improving (or enhancing or assisting) the solubility or dispersibility of an ether of an aliphatic alcohol and glycerin, comprising the coexistence of (A) an ether of an aliphatic alcohol and glycerin and (B) an acyl glutamate lysine salt [or a method for containing (B) an acyl glutamate lysine salt in a composition containing (A) an ether of an aliphatic alcohol and glycerin (for example, a composition containing water)].

[0148] Furthermore, the following agent is provided as an embodiment of the present invention. (A) An agent for improving (or enhancing or assisting) the solubility or dispersibility (particularly solubility or dispersibility in solvents containing water) of an ether of an aliphatic alcohol and glycerin, and (B) an agent containing an acyl glutamate lysine salt (solubility enhancer, dispersibility enhancer, solubilizer, dispersion aid).

[0149] [3. Improved transdermal absorption] In one aspect of the present invention, (C) the transdermal absorption (skin penetration) of the water-soluble component can be improved (or enhanced).

[0150] Accordingly, the following method is provided as an embodiment of the present invention. (C) A method for improving (or enhancing or assisting) the transdermal absorption of a water-soluble component, comprising (C) a water-soluble component and (A) an ether of an aliphatic alcohol and glycerin and / or (B) an acyl glutamate lysine salt in the same location [or a method for containing (C) a water-soluble component in a composition containing (A) an ether of an aliphatic alcohol and glycerin and / or (B) an acyl glutamate lysine salt in the same location].

[0151] In this method, at least component (A) may be present (or included), and it is particularly preferable that component (A) and component (B) be present (or included).

[0152] Furthermore, the following agent is provided as an embodiment of the present invention. (C) An agent for improving (or enhancing or assisting) the transdermal absorption of water-soluble components, comprising (A) an ether of an aliphatic alcohol and glycerin and / or (B) an acyl glutamate lysine salt (transdermal absorption enhancer or improver, transdermal absorber, transdermal absorption promoter, transdermal absorption aid, transdermal absorption modifier).

[0153] This agent may contain at least component (A), and is particularly preferably containing component (A) and component (B).

[0154] The types and amounts of each component, the types and amounts of other components, the formulation form and use of the composition in each of the above embodiments are as described in [1. Composition]. [Examples]

[0155] The present invention will be described in more detail below with reference to examples, but the present invention is not limited in any way by these examples, and many modifications are possible within the technical concept of the present invention by those with ordinary skill in the art.

[0156] Test Example 1 (Solubility of Component (A)) The components shown in the table below were heated and mixed at 70°C for 5 minutes to prepare the composition. The prepared composition was then filled into a clear glass bottle at room temperature, and its state was observed visually.

[0157] In the table, the units for each component are in mass %) (the same applies below). Also, in the table, "Pellicea" refers to "Pellicea L-30" manufactured by Asahi Kasei Chemicals Corporation, which contains dilauroyl glutamate lysine sodium as a component (aqueous solution of dilauroyl glutamate lysine sodium / water = 29 / 71), and the values ​​in parentheses are the mass %) of "dilauroyl glutamate lysine sodium" (the same applies below).

[0158] [Table 1]

[0159] As is clear from the results in the table above, component (A), glycerin mono-2-ethylhexyl ether, was not soluble or dispersible in water, and the test solution separated (Test Examples 1A-1B). However, by adding component (B), dilauroyl glutamate lysine sodium, good solubility or dispersibility in water was observed, and the test solution became clear (Test Examples 1C-1F).

[0160] On the other hand, although the test solution no longer separated when various surfactants were used, its solubility or dispersibility was poor, and it became cloudy (Test example 1G~1L).

[0161] From these findings, it was surprisingly discovered that component (B) is a component that can effectively (and specifically) dissolve or disperse component (A).

[0162] Test Example 2 ((C) Permeability of water-soluble components) A composition with the composition shown in the table below was prepared.

[0163] Then, the permeability of (C) water-soluble component VC ethyl (3-O-ethyl ascorbic acid) was evaluated for each composition as follows.

[0164] Human 3D cultured epidermis was pre-cultured at 37°C (5-10% CO2) for 18-22 hours by adding 0.5 mL / well of the included dedicated assay medium to the bottom of the Transwell of the LabCyte EPI-MODEL24 (Japan Tissue Engineering Co., Ltd.). Subsequently, the dedicated assay medium was replaced with 0.5 mL of PBS, and the cells were pre-incubated for 30 minutes on a 37°C incubator. Then, the PBS was replaced with the same amount of fresh PBS, and 0.3 mL of the drug solution was added directly to the top of the cells, with the time of drug addition being considered zero. Subsequently, 0.1 mL of the drug solution was sampled from the bottom at predetermined intervals up to 360 minutes, and the same amount of PBS was immediately added. The sampled drug solution was quantified using HPLC, and the permeability coefficient (P) was calculated based on the following formula.

[0165] Note that all administered culture media, PBS, and drug solutions were warmed to 37°C before administration.

[0166] P = (ΔQ / Δt) × (1 / C0) × (1 / Area)

[0167] In the above formula, ΔQ / Δt represents the drug constant permeation rate, which is determined as the slope of the linear portion of the cumulative drug permeation amount-time curve. Further, C0 is the initial concentration of the administered drug, and Area is the permeation area (0.3215 cm 2 )

[0168] Further, the ratio of the permeation coefficient (Ps) containing various components (Test Examples 2B to 2J) to the permeation coefficient (Pc) not containing the components (Control, Test Example 2A) was calculated based on the following formula, and this was defined as the Enhancement Ratio (ER).

[0169] ER = Ps / Pc

[0170] The results are shown in the table below.

[0171]

Table 2

[0172] As is clear from the results in the above table, it was found that the permeability (percutaneous absorbability) of ethyl VC, which is the water-soluble component (C), is specifically improved in glycerin mono-2-ethylhexyl ether as the component (A) and sodium dilauroyl glutamate lysine as the component (B).

[0173] In particular, it was found that glycerin mono-2-ethylhexyl ether as the component (A) can improve the permeability of ethyl VC even when used in a very small amount (0.2% by mass), compared with components known as other surfactants and the like (5% by mass).

[0174] Test Example 3 ((C) Permeability of water-soluble components) Compositions having the compositions shown in the table below were prepared, and the permeability of ethyl VC (3-O-ethylascorbic acid) was evaluated in the same manner as in Test Example 2.

[0175] The results are shown in the table below.

[0176]

Table 3

[0177] As is clear from the results in the table above, the permeability (transdermal absorption) of (C) water-soluble component, VC ethyl, was found to be improved at various ratios with (A) component, glycerin mono-2-ethylhexyl ether, and (B) component, dilauroyl glutamate lysine sodium.

[0178] Furthermore, by combining component (A), glycerin mono-2-ethylhexyl ether, and component (B), dilauroyl glutamate lysine sodium, the permeability of VC ethyl was significantly (synergistically) improved.

[0179] On the other hand, combining glycerin mono-2-ethylhexyl ether with cyclohexanedicarboxylic acid bisethoxydiglycol did not improve the permeability of VC ethyl; in fact, it slightly decreased.

[0180] Test Example 4 ((C) Permeability of water-soluble components) Compositions with the compositions shown in the table below were prepared, and the permeability of various (C) water-soluble components was evaluated in the same manner as in Test Example 2.

[0181] The results are shown in the table below.

[0182] [Table 4]

[0183] As is clear from the results in the table above, it was found that component (A), glycerin mono-2-ethylhexyl ether, and component (B), dilauroyl glutamate lysine sodium, improve the permeability (transdermal absorption) of various water-soluble components (C).

[0184] Furthermore, by combining component (A), glycerin mono-2-ethylhexyl ether, and component (B), dilauroyl glutamate lysine sodium, the permeability was significantly (synergistically) improved, similar to VC ethyl.

[0185] Test Example 5 ((C) Permeability of water-soluble components) Compositions with the compositions shown in the table below were prepared, and the permeability of nicotinamide was evaluated in the same manner as in Test Example 2.

[0186] The results are shown in the table below. For example, the transmission coefficient (Pc) used for ER was the same as that of test example 5A for test examples 5C to 5D, and the transmission coefficient (Pc) used for test example 5B for test examples 5E to 5G.

[0187] [Table 5]

[0188] As is clear from the results in the table above, the permeability (transdermal absorption) of nicotinamide was found to be specifically improved in (A) component glycerol mono-2-ethylhexyl ether and (B) component dilauroyl glutamate lysine sodium, similar to the other (C) water-soluble components.

[0189] Furthermore, the combination of component (A), glycerin mono-2-ethylhexyl ether, and component (B), dilauroyl glutamate lysine sodium, showed a tendency to significantly (synergistically) improve permeability, similar to the other (C) water-soluble components.

[0190] [Examples of formulations] The composition was prepared according to the formulations listed in the table below. Note that in the table below, the units for each component are in mass %).

[0191] [Table 6]

[0192] [Table 7]

[0193] [Table 8]

[0194] [Table 9] [Industrial applicability]

[0195] The present invention can provide compositions that are useful as external compositions (for example, leave-on cosmetics).

Claims

1. (A) an ether of an aliphatic alcohol and glycerin, (B) diacyl glutamate lysine salt and (C) a water-soluble component, (C) Component comprises at least one selected from tranexamic acids, epsilon-aminocaproic acids, hydroquinones, nicotinamides, allantoins, and riboflavins. (B) The content of component is 2% by mass or less, A composition in which the proportion of component (A) is less than 0.5% by mass, or the proportion of component (B) is greater than 0.05 parts by mass per 1 part by mass of component (A).

2. (A) an ether of an aliphatic alcohol and glycerin, (B) diacyl glutamate lysine salt and (C) a water-soluble component, (C) Component comprises at least one selected from tranexamic acids, epsilon-aminocaproic acids, hydroquinones, nicotinamides, allantoins, and riboflavins. (B) The content of component is 2% by mass or less, (A) A composition in which the proportion of component is less than 0.5% by mass.

3. (A) an ether of an aliphatic alcohol and glycerin, (B) diacyl glutamate lysine salt and (C) a water-soluble component, (A) The component is glycerin mono-2-ethylhexyl ether, (B) Component is dilauroyl glutamate lysine salt, (C) Component comprises at least one selected from tranexamic acids, epsilon-aminocaproic acids, hydroquinones, nicotinamides, allantoins, and riboflavins. (B) The content of component is 2% by mass or less, A composition in which the proportion of component (A) is less than 0.5% by mass, or the proportion of component (B) is greater than 0.05 parts by mass per 1 part by mass of component (A).

4. The composition according to claim 1 or 3, wherein the proportion of component (A) is less than 0.5% by mass.

5. The composition according to any one of claims 1 to 4, wherein the proportion of component (B) is 1% by mass or less.

6. The composition according to any one of claims 1 to 5, wherein the proportion of component (B) is greater than 0.05 parts by mass per 1 part by mass of component (A).

7. The composition according to any one of claims 1 to 6, wherein the proportion of component (A) is less than 0.5% by mass, and the proportion of component (B) is greater than 0.05 parts by mass and less than or equal to 100 parts by mass per 1 part by mass of component (A).

8. The composition according to any one of claims 1 to 7, wherein component (C) comprises at least one selected from tranexamic acid, epsilonaminocaproic acid, hydroquinone, arbutin, nicotinamide, allantoin, riboflavin, and salts thereof.

9. The composition according to any one of claims 1 to 8, wherein the proportion of component (C) is 0.05% by mass or more.

10. The composition according to any one of claims 1 to 9, which is for use in leave-on cosmetics.

11. (C) An agent for improving the transdermal absorption of water-soluble components, comprising (A) an ether of an aliphatic alcohol and glycerin and (B) a diacyl glutamate lysine salt, wherein component (A) is glycerin mono-2-ethylhexyl ether, component (B) is dilauroyl glutamate lysine salt, and the proportion of component (B) is greater than 0.05 parts by mass per 1 part by mass of component (A).

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