CN113164799A - Composition comprising ethers synthesized from fatty alcohols and glycerol - Google Patents

Composition comprising ethers synthesized from fatty alcohols and glycerol Download PDF

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CN113164799A
CN113164799A CN201980078658.5A CN201980078658A CN113164799A CN 113164799 A CN113164799 A CN 113164799A CN 201980078658 A CN201980078658 A CN 201980078658A CN 113164799 A CN113164799 A CN 113164799A
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component
acid
mass
composition
water
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北冈侑
藤田雅
黑木未知瑠
桝本爱
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Rohto Pharmaceutical Co Ltd
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/44Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/02Preparations for care of the skin for chemically bleaching or whitening the skin

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Dermatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Emergency Medicine (AREA)
  • Cosmetics (AREA)

Abstract

The present invention provides a novel composition. The composition comprises (A) an ether synthesized from a fatty alcohol and glycerin and (B) an acyl glutamic acid lysine salt.

Description

Composition comprising ethers synthesized from fatty alcohols and glycerol
Technical Field
The present invention relates to a novel composition and the like.
Background
Ethers synthesized from fatty alcohols and glycerin, such as alkyl glyceryl ethers, are used to obtain moisturizing effect, emulsifying effect, deodorizing effect, antibacterial effect, and the like.
For example, Japanese patent application laid-open No. 2000-191488 (patent document 1) discloses an alkyl glyceryl ether as a surfactant constituting a specific deodorant cosmetic composition.
Patent document 1: japanese patent laid-open publication No. 2000-191488
Disclosure of Invention
The object of the present invention is to provide a novel composition and the like comprising an ether synthesized from a fatty alcohol and glycerin.
As described above, ethers synthesized from fatty alcohols and glycerin are used as surfactants and the like (patent document 1).
However, according to the studies of the present inventors, it has been found that such an ether synthesized from a fatty alcohol and glycerin cannot be used as a surfactant, but is rather poor in dispersion or solubility in water or the like, and often causes cloudiness or the like.
Under such circumstances, the present inventors have made intensive studies to solve the above problems, and as a result, have found that a novel composition is obtained by combining an ether synthesized from an aliphatic alcohol and glycerin with an acyl glutamic acid lysine salt; further, the present inventors have made further studies to effectively dissolve or disperse an ether synthesized from a fatty alcohol and glycerin in such a composition, and have completed the present invention.
That is, the present invention relates to the following aspects.
[1]
A composition comprising (A) an ether synthesized from a fatty alcohol and glycerin and/or (B) an acyl glutamic acid lysine salt [ usually, at least (A) an ether synthesized from a fatty alcohol and glycerin, particularly (A) an ether synthesized from a fatty alcohol and glycerin and (B) an acyl glutamic acid lysine salt ].
[2]
The composition according to [1], wherein the component (A) is mono-2-ethylhexyl glyceryl ether and the component (B) is dilaurylglutamic acid lysine salt.
[3]
The composition according to [1] or [2], wherein the proportion of the component (A) is less than 0.5% by mass.
[4]
The composition according to any one of [1] to [3], wherein the proportion of the component (B) is 1% by mass or less.
[5]
The composition according to any one of [1] to [4], wherein the proportion of the component (B) is more than 0.05 part by mass relative to 1 part by mass of the component A.
[6]
The composition according to any one of [1] to [5], wherein the proportion of the component (A) is less than 0.5 mass%, and the proportion of the component (B) is more than 0.05 parts by mass and 100 parts by mass or less with respect to 1 part by mass of the component (A).
[7]
The composition according to any one of [1] to [6], wherein the composition further comprises (C) a water-soluble ingredient.
[8]
The composition according to [7], wherein the component (C) has a logP value of 0 or less and a molecular weight of 1000 or less.
[9]
The composition according to [7] or [8], wherein the (C) component comprises a water-soluble whitening ingredient.
[10]
The composition according to any one of [7] to [9], wherein the component (C) contains at least one selected from the group consisting of ascorbic acids, thrombolic acids, epsilon-aminocaproic acids, hydroquinones, nicotinamides, glycyrrhizic acids, allantoines and riboflavin.
[11]
The composition according to any one of [7] to [10], wherein the component (C) comprises at least one selected from the group consisting of ascorbic acid, ascorbic acid phosphate, ascorbic acid alkyl ester, ascorbic acid-2-glucoside, tranexamic acid, epsilon-aminocaproic 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 the component (C) is 0.05% by mass or more.
[13]
The composition according to any one of [1] to [12], wherein the composition is used for a leave-on cosmetic.
[14] A preparation for improving the solubility or dispersibility of (A) an ether synthesized from a fatty alcohol and glycerin, which contains (B) an acyl glutamic acid lysine salt.
[15]
A preparation for improving the transdermal absorbability of (C) a water-soluble ingredient, which contains (A) an ether synthesized from a fatty alcohol and glycerin or (B) an acylglutamic acid lysine salt.
[16]
A preparation for improving the transdermal absorbability of (C) a water-soluble ingredient, which comprises (A) an ether synthesized from an aliphatic alcohol and glycerin and (B) an acylglutamic acid lysine salt.
[17]
A method for improving the solubility or dispersibility of (a) an ether synthesized from a fatty alcohol and glycerin, which coexists with (B) an acyl glutamic acid lysine salt.
[18]
A method for improving the transdermal absorbability of (C) a water-soluble ingredient by allowing (C) the water-soluble ingredient to coexist with (a) an ether synthesized from a fatty alcohol and glycerin or (B) an acylglutamic acid lysine salt.
[19]
A method for improving the percutaneous absorbability of (C) a water-soluble component, which comprises allowing (C) a water-soluble component, (A) an ether synthesized from a fatty alcohol and glycerin, and (B) an acylglutamic acid lysine salt to coexist.
In the present invention, a novel composition can be improved. Such compositions comprise an ether synthesized from a fatty alcohol and glycerol, and an acyl glutamic acid lysine salt.
In other embodiments of the present invention, a composition can be provided that can improve the solubility or dispersibility of ethers synthesized from fatty alcohols and glycerin. As described above, although ethers synthesized from fatty alcohols and glycerin cause cloudiness and the like, the combination with a specific component, i.e., an acylglutamic acid lysine salt, can effectively suppress the cloudiness and the like.
Detailed Description
[1. composition ]
The composition of the present invention contains at least one selected from (A) ethers synthesized from fatty alcohols and glycerin and (B) acyl glutamic acid lysine salts. In particular, the composition of the present invention may also contain (a) an ether synthesized from a fatty alcohol and glycerin and (B) an acyl glutamic acid lysine salt.
(A) Ether synthesized from fatty alcohol and glycerin ((A) component)
The aliphatic alcohol may be a chain alcohol or a branched alcohol, and may be a saturated alcohol or an unsaturated alcohol.
The number of carbon atoms of the aliphatic alcohol is not particularly limited, and may be, for example, 4 or more (for example, 4 to 30 carbon atoms), 6 or more (for example, 6 to 24 carbon atoms), 8 or more (for example, 8 to 22 carbon atoms), or the like, or 23 or more. The number of carbon atoms of the 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.
The fatty alcohol may be a polyhydric alcohol (a polyhydric alcohol other than glycerin), and may be a monohydric alcohol in general.
Specific examples of the fatty alcohol include: saturated or unsaturated fatty alcohols (linear or branched fatty alcohols, e.g., C.sub.C.) such as 2-ethylhexanol, octanol, nonanol, decanol, isodecanol, lauryl alcohol, myristyl alcohol, cetyl alcohol, stearyl alcohol, cetostearyl alcohol, hexyldodecanol, isostearyl alcohol, octyldodecanol, behenyl alcohol, 2-decyl-1-tetradecanol, palmitoyl alcohol, oleyl alcohol, linoleyl alcohol, linolenyl alcohol, etc4-30Saturated or unsaturated fatty alcohol, C6-24Saturated or saturatedUnsaturated fatty alcohols, etc.), etc.
The ether synthesized from the fatty alcohol and glycerin may be any of monoethers (monoethers of glycerin), diethers, and triethers, and preferably a monoether or diether, and particularly may contain at least a monoether.
In the case where the ether is a polyether (di-or tri-ether), the fatty alcohols may be the same or different fatty alcohols.
As representative ethers synthesized from fatty alcohols and glycerin, there may be mentioned, for example: mono 2-ethylhexyl glyceryl ether (ethylhexyl glycerol), monooctyl glyceryl ether, monoisodecyl glyceryl ether, monocetyl glyceryl ether (shark liver alcohol), monostearyl glyceryl ether (batyl alcohol), monoisostearyl glyceryl ether, monobehenate glyceryl ether, monooleyl glyceryl ether (batyl alcohol), and the like.
The ethers synthesized from fatty alcohols and glycerin may be used alone or in combination of two or more.
Among them, mono 2-ethylhexyl glyceryl ether can be suitably used from the viewpoint of an inhibitory effect on the growth of bacteria. Therefore, the component (a) may contain at least mono 2-ethylhexyl glyceryl ether.
The component (a) may be a composition or a commercially available product.
When the component (a) contains mono 2-ethylhexyl glyceryl ether, the proportion of mono 2-ethylhexyl glyceryl ether to the entire component (a) may be selected from, for example, a range of about 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 or the like).
When the composition contains the component (a), the content of the component (a) in the composition may be selected depending on the use of the composition, and may be, for example, about 0.0001 to 5% by mass, preferably about 0.001 to 2% by mass, more preferably about 0.01 to 1% by mass, further preferably about 0.03 to 0.7% by mass, and further more preferably about 0.05 to 0.5% by mass (e.g., about 0.05% by mass or more and less than 0.5% by mass), and particularly about 0.5% by mass or less [ e.g., about 0.5% by mass or less (e.g., about 0.45% by mass or less), 0.4% by mass or less (e.g., about 0.35% by mass or less), 0.3% by mass or less (e.g., about 0.25% by mass or less), 0.2% by mass or less (e.g., about 0.15% by mass) ] based on the total amount of the composition.
By using the component (A) within such a range, the function of the component (A) can be effectively exhibited. In addition, if the amount is within such a range, the bacteriostatic effect and the like can be exhibited in a range where skin irritation is little (or no irritation).
When the composition contains the component (C), the permeability (permeability) of the component (C) can be effectively improved by including the component (a) in the composition (particularly in combination with the component (B)), as described below.
(B) Acyl glutamic acid lysine salt ((B) component)
In the acyl glutamic acid lysine salt, examples of the acyl group include an acyl group (fatty acid acyl group, aliphatic acyl group) corresponding to a fatty acid (aliphatic group).
Such fatty acids may be linear or branched fatty acids, or may be saturated or unsaturated fatty acids.
The number of carbon atoms of the fatty acid is not particularly limited, and may be, for example, 4 or more (for example, 4 to 30 carbon atoms), 8 or more (for example, 8 to 24 carbon atoms), 10 or more (for example, 12 to 22 carbon atoms), or the like.
The fatty acid may be a polybasic fatty acid, but may typically be a mono-fatty acid.
Specific examples of the fatty acid include: saturated or unsaturated aliphatic acids (chain or branched fatty acids, e.g., 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 acid4-30Saturated or unsaturated aliphatic acid, C8-24Saturated or unsaturated fatty acids, etc.), and the like.
The acyl glutamic acid lysine salt may be a monoacyl glutamic acid lysine salt, and particularly may be a diacyl glutamic acid lysine salt.
In the diacylglutamic acid lysine salt, the two acyl groups (fatty acids) may be the same or different acyl groups (fatty acids).
Among the acyl glutamine lysine salts, salts are not particularly limited, and examples thereof include: salts with inorganic bases [ e.g., ammonium salts; and salts with alkali metals (sodium, potassium, etc.), alkaline earth metals (calcium, magnesium, etc.), metals such as aluminum, etc.) ], salts with organic bases (for example, salts with organic amines such as methylamine, triethylamine, triethanolamine, etc.), salts with amino acids (for example, arginine salts, etc.), etc.
Representative salts are alkali metal salts such as sodium salts.
Specific examples of the acyl glutamic acid lysine salt include: diacyl glutamic acid lysines { e.g., dilauroyl glutamic acid lysine (e.g., sodium dilauroyl glutamic acid lysine), dimyristoyl glutamic acid lysine (e.g., sodium dimyristoyl glutamic acid lysine), distearoyl glutamic acid lysine (e.g., sodium distearoyl glutamic acid lysine), dioleoyl glutamic acid lysine (e.g., sodium dioleoyl glutamic acid lysine), and the like.
The acyl glutamic acid lysine salt may be used alone or in combination of two or more.
Among them, a dilauroyl glutamic acid lysine salt such as sodium dilauroyl glutamic acid lysine can be suitably used.
The component (B) can be synthesized by a conventional method [ for example, a method of reacting a lysine salt (for example, L-lysine hydrochloride) with N-acyl glutamic anhydride (for example, N-acyl-L-glutamic anhydride) ], or a commercially available product can be used. For example, sodium dilauroylglutamic acid lysine can be used as a substance obtained from "Pellicor LB-10" or "Pellicor L-30" manufactured by Asahi Kasei Chemicals Co., Ltd.
When the composition contains the component (B), the content of the component (B) in the composition can be selected according to the use of the composition, and may be, for example, about 0.00001 to 20 mass%, preferably about 0.0001 to 10 mass%, more preferably about 0.001 to 5 mass%, and still more preferably about 0.01 to 3 mass% with respect to the total amount of the composition. The content of the component (B) in the composition may be 2% by mass or less (e.g., 1% by mass or less, 0.00001 to 1% by mass, etc.), or may be 2% by mass or more (e.g., more than 2% by mass, 2.5% by mass or more, 3 to 5% by mass, etc.).
When the composition contains the component (a) and the component (B), the proportion of the component (B) may be, for example, 0.001 to 1000 parts by mass (for example, 0.003 to 800 parts by mass), preferably 0.005 to 500 parts by mass (for example, 0.007 to 300 parts by mass), and more preferably about 0.01 to 100 parts by mass (for example, 0.03 to 80 parts by mass) relative to 1 part by mass of the component (a).
The proportion of the component (B) may be, for example, 0.001 part by mass or more [ e.g., 0.005 part by mass or more (e.g., 0.01 to 500 parts by mass), 0.02 part by mass or more (e.g., 0.025 to 300 parts by mass), 0.03 part by mass or more (e.g., 0.05 to 100 parts by mass), 0.05 part by mass or more (e.g., more than 0.05 part 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) ] or less with respect to 1 part by mass of the component (a), and may be 0.01 part by mass or less [ e.g., 0.007 part by mass or less (e.g., 0.001 to 0.005 part by mass), 0.005 part by mass or less (e.g., 0.002 to 0.005 part by mass) ].
By using the component (B) in such a ratio, the solubility or dispersibility of the component (a) can be effectively improved. Therefore, the stability of the preparation containing component (a) can be improved, and the function of component (a) (for example, the function as an emulsification aid) can be effectively exhibited according to the purpose of use of component (a).
In addition, as described below, in the composition containing the component (C), by containing the component (B) (particularly, in the above-mentioned ratio) in the composition (particularly, in combination with the component (a)), the permeability (permeability) of the component (C) can be effectively improved.
(C) Water-soluble component ((C) component)
The compositions of the present invention may also contain water soluble ingredients. As described above, the composition of the present invention usually contains (a) an ether synthesized from a fatty alcohol and glycerin and/or (B) an acylglutamic acid lysine salt, but by combining these components [ (component (a) and/or component (B) (for example, at least component (a), particularly component (a) and component (B)) with a water-soluble component, the function of the water-soluble component can be effectively exerted.
For example, the composition can be used in combination with the component (a) and/or the component (B) to promote distribution to or diffusion in the skin, or to improve transdermal absorption (permeability) of a water-soluble component.
As described above, the solubility or dispersibility of the component (a) can be improved by combining the component (a) with the component (B), but the effect of improving the percutaneous absorption of the water-soluble component can be promoted together with the effect of improving the solubility or dispersibility of the component (a).
In particular, water-soluble components (for example, water-soluble whitening components such as ascorbic acids and thrombolic acids described later) are often difficult to reach a target site because of low skin permeability.
Therefore, in order to effectively exert the function of the water-soluble component (whitening effect, etc.) in the aqueous composition for outer skin, the composition containing the component (C) may contain both the component (a) and the component (B).
The water-soluble component is not particularly limited in the degree of water solubility, and the logP value can be used as an index.
For example, as the water-soluble component, a water-soluble component having 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.), more preferably-5 or more (e.g., -4.5 to 0, -4 to-0.08, etc.) can be used, and particularly a water-soluble component having a logP value of-3 or more (e.g., -2.5 to 0, -2 to-0.1) can also be used.
Note that the distribution coefficient logP (logP)OW) Value is as POW[ concentration of detection substance in octyl alcohol layer (mol/L)/concentration of detection substance in Water layer (mol/L) ]]Common logarithm of (log)10POW) But are well known values.
The logP value can be measured (determined, calculated) by, for example, Japanese Industrial Standard Z7260-107(2000) "measurement of partition coefficient (1-octanol/water) -flask shaking method".
The molecular weight (formula weight) of the water-soluble component is not particularly limited, and may be, for example, 2000 or less (e.g., 1800 or less), preferably 1500 or less (e.g., 1200 or less), and more preferably 1000 or less (e.g., 800 or less, 700 or less, 600 or less, 500 or less).
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, or the like.
The water-soluble component may be water-soluble, and may generally have a function depending on the kind of the component. The water-soluble component may be, for example, a whitening component (water-soluble whitening component), an anti-inflammatory component, an antioxidant component, an anti-wrinkle component, a component for promoting collagen synthesis, an active oxygen-removing component, a metabolism (turn over) promoting component, an anti-aging component, a blood circulation-promoting component, a keratolytic component, or the like.
In the present invention, as described above, the water-soluble component can be efficiently transdermally absorbed, and thus these functions can be effectively exerted.
Specific examples of the water-soluble component (e.g., water-soluble whitening component) include: ascorbic acids, amino acids, hydroquinones, nicotinamides (e.g., nicotinamide, etc.), glycyrrhetinic acids, allantoins (e.g., allantoin, etc.), riboflavin (e.g., riboflavin, etc.), peptides (e.g., glutathione, etc.), extracts [ e.g., placenta (placenta extract), chamomile extract, etc. ], and the like.
Examples of the ascorbic acids include: ascorbic acid, ascorbic acid derivatives, and salts thereof.
The ascorbic acid may be any of D-form, L-form, and a mixture thereof, and L-form [ L-ascorbic acid (vitamin C) ] may be suitably used.
Examples of ascorbic acid derivatives include: phosphoric acid esters (e.g., ascorbic acid monophosphate, ascorbic acid diphosphate, ascorbic acid triphosphate, etc.), sulfuric acid esters (e.g., ascorbic acid-2-sulfuric acid ester), ascorbic acid alkyl esters (e.g., ascorbic acid alkyl esters such as ascorbic acid methyl ester and ascorbic acid ethyl ester), glycosides of ascorbic acid (e.g., ascorbic acid-2-glucoside, etc.), and the like.
Examples of the salt 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 ], etc. ], 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. ], and the like.
As representative ascorbic acids, there may be mentioned: ascorbic acid (particularly, vitamin C), ascorbic acid phosphate (ascorbic acid phosphate, ascorbic acid monophosphate, and the like), ascorbic acid alkyl ester [ particularly, ethyl ascorbate (3-O-ethyl ascorbic acid, ethyl VC, and the like), and the like ], ascorbic acid-2-glucoside, salts thereof (for example, sodium ascorbate phosphate, magnesium ascorbate phosphate, and the like), and the like.
Examples of the amino acids include: blood coagulation acids, epsilon-aminocaproic acids (epsilon-aminocaproic acid and salts thereof), and the like.
Examples of the blood coagulation acids include: tranexamic acid, tranexamic acid derivatives { e.g., a polymer of tranexamic acid [ e.g., tranexamic acid dimer such as trans-4- (trans-aminomethylcyclohexanecarbonyl) aminomethylcyclohexanecarboxylic acid hydrochloride ], an ester of tranexamic acid with hydroquinone (e.g., 4' -hydroxyphenyl trans-4-aminomethylcyclohexanecarboxylate), an ester of tranexamic acid with gentisic acid [ e.g., 2- (trans-4-aminomethylcyclohexylcarbonyloxy) -5-hydroxybenzoic acid ], an amide of tranexamic acid [ e.g., trans-4-aminomethylcyclohexanecarboxylic acid methyl ester amide and salts thereof, trans-4- (p-methoxybenzoyl) aminomethylcyclohexanecarboxylic acid, trans-4-guanidinomethylcyclohexanecarboxylic acid ], and salts thereof.
As the salt, in addition to the exemplified salts [ e.g., alkali metal salts (e.g., sodium salts, potassium salts), amine salts (e.g., triethanolamine salts), etc. ], salts with amino acids (e.g., basic amino acids such as arginine, lysine, histidine, ornithine), etc. may be cited.
Typical examples of the amino acids include: tranexamic acid, thromboplastin salts (e.g., sodium salt, potassium salt, triethanolamine salt, arginine salt, etc.), epsilon-aminocaproic acid, and the like.
Examples of the hydroquinones include: hydroquinone, hydroquinone glycosides, salts of these, and the like.
Examples of hydroquinone glycosides include: hexosides of glucosides (e.g., hydroquinone α -D-glucose, hydroquinone β -D-glucose (arbutin), hydroquinone α -L-glucose, hydroquinone β -L-glucose), galactosides (e.g., hydroquinone α -D-galactose, hydroquinone β -D-galactose, hydroquinone α -L-galactose, hydroquinone β -L-galactose, etc.); pentose glycosides (e.g., hydroquinone α -D-ribose, hydroquinone β -D-ribose, hydroquinone α -L-ribose, hydroquinone β -L-ribose), arabinosides (e.g., hydroquinone α -D-arabinose, hydroquinone β -D-arabinose, hydroquinone α -L-arabinose, hydroquinone β -L-arabinose), and the like; aminoglycosides such as glucosamine 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); uronic acid glycosides such as glucuronic acid glycosides (e.g., hydroquinone α -D-glucuronic acid, hydroquinone β -D-glucuronic acid, hydroquinone α -L-glucuronic acid, hydroquinone β -L-glucuronic acid), galacturonic acid glycosides (e.g., hydroquinone α -D-galacturonic acid, hydroquinone β -D-galacturonic acid, hydroquinone α -L-galacturonic acid, hydroquinone β -L-galacturonic acid), and the like.
As representative hydroquinones, there may be mentioned: hydroquinone, arbutin (hydroquinone beta-D-glucose), salts of these, and the like.
Examples of the glycyrrhizic acid include: glycyrrhizic acid, glycyrrhetate, and the like. Examples of the salt include: the exemplified salts [ e.g., 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.), etc. ], and the like. Representative glycyrrhetate includes dipotassium glycyrrhizinate, monoammonium glycyrrhizinate, etc.
Among these water-soluble components, ascorbic acids, blood coagulation acids, epsilon-amino caproic acids, hydroquinones, nicotinamides, glycyrrhizic acids, allantoins, riboflavin compounds and the like are preferable.
In particular, from the viewpoint of water solubility and molecular properties, ascorbic acid derivatives (e.g., ascorbic acid phosphate, ascorbic acid alkyl ester, ascorbic acid-2-glucoside), tranexamic acid, epsilon-aminocaproic acid, hydroquinone glycoside (e.g., arbutin), niacinamide, glycyrrhizic acid, allantoin, riboflavin, salts thereof (e.g., sodium ascorbate, magnesium ascorbate phosphate, dipotassium glycyrrhizinate, etc.), and the like can be suitably used.
The water-soluble ingredients may be used alone or in combination of two or more.
When the composition contains the component (C), the content of the component (C) in the composition may be selected depending on the use of the composition, the function of the water-soluble component (C), and the like, and may be, for example, about 0.001 to 10% by mass, preferably about 0.01 to 8% by mass, and more preferably about 0.05 to 5% by mass, based on the total amount of the composition. The content of the component (C) in the composition may be 3% by mass or less (e.g., 1% by mass or less, 0.1% by mass or less, 0.001 to 0.1% by mass, etc.), or may be 0.01% by mass or more (e.g., 0.05% by mass or more, 1% by mass, etc.).
When the composition contains the component (a), the proportion of the component (C) may be, for example, 0.1 to 5000 parts by mass (for example, 0.3 to 3000 parts by mass), preferably 0.5 to 1000 parts by mass (for example, 0.7 to 800 parts by mass), and more preferably about 1 to 500 parts by mass (for example, 5 to 400 parts by mass, 1 to 100 parts by mass) relative to 1 part by mass of the component (a).
When the composition contains the component (B), the proportion of the component (C) may be, for example, 0.001 to 2000 parts by mass (for example, 0.005 to 1500 parts by mass), preferably 0.01 to 1000 parts by mass (for example, 0.02 to 500 parts by mass), and more preferably about 0.1 to 300 parts by mass (for example, 0.2 to 200 parts by mass) relative to 1 part by mass of the component (B).
When the composition contains the component (a) and the component (B), the proportion of the component (C) may be, for example, 0.001 to 1000 parts by mass (for example, 0.005 to 800 parts by mass), preferably 0.01 to 500 parts by mass (for example, 0.02 to 400 parts by mass), and more preferably about 0.05 to 300 parts by mass (for example, 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 the component (a) and the component (B).
Active ingredient
The composition of the present invention may contain an active ingredient as required. Specific examples of the active ingredient include: moisturizing component, antiinflammatory component, antibacterial component, vitamins, peptide or its derivative, amino acid or its derivative, cell activating component, antiaging component, blood circulation promoting component, cutin softening component, whitening component, astringing component, and ultraviolet-proof component.
In the present invention, even when these active ingredients are contained, the functions of the components (a) to (C) can be effectively exhibited.
The active ingredient may be a component corresponding to the component (C) or may be a component other than the component (C).
Examples of the moisture-retaining component include: polyols such as glycerol, propane diol, propylene glycol, 1, 3-butylene glycol, dipropylene glycol, polyethylene glycol, diglycerin, trehalose, inositol, sorbitol; high molecular compounds such as collagen, elastin, keratin, chitin, chitosan, fucoidan sulfate, hyaluronic acids (e.g., hydrolyzed hyaluronic acid, acetylated hyaluronic acid, sodium hyaluronate, etc.); amino acids such as glycine, aspartic acid, arginine; natural moisturizing factors such as sodium lactate, urea, sodium pyrrolidone carboxylate; lipids such as ceramides, cholesterol, phospholipids; plant extract extracts such as chamomile extract, witch hazel extract, tea extract, lemon extract, centella extract, artichoke extract, and the like.
As the anti-inflammatory component, there may be mentioned: plant-derived (e.g., comfrey) ingredients, zinc oxide, pyridoxine hydrochloride, tocopherol acetate, salicylic acid or its derivatives, epsilon-aminocaproic acid, and the like.
As the antibacterial component, there may be mentioned: chlorhexidine, salicylic acid, benzalkonium chloride, rivanol, ethanol, benzethonium chloride, cresol, gluconic acid and its derivatives, povidone iodine, potassium iodide, iodine, isopropylmethylphenol, triclocarban, triclosan, pravastatin, proquinuclidine, parabens, phenoxyethanol, 1, 2-pentanediol, alkyldiaminoglycine hydrochloride, iodopropynyl n-butyl carbamate, caprylyl hydroxamic acid, methylisothiazolinone, sorbic acid, β -glycyrrhetinic acid, components derived from plants (e.g., sophora flavescens, rosemary, mulberry, eucalyptus, etc.), and the like.
As vitamins, the following can be suitably used: vitamin E compounds such as dl-alpha-tocopherol, dl-alpha-tocopherol acetate, dl-alpha-tocopherol succinate, and dl-alpha-tocopherol calcium succinate; vitamins B2 such as riboflavin, flavin mononucleotide, flavin adenine dinucleotide, riboflavin butyrate, riboflavin tetrabutyrate, riboflavin 5' -phosphate sodium, riboflavin tetranicotinate, etc.; nicotinic acids such as dl- α -tocopherol nicotinate, benzyl nicotinate, methyl nicotinate, β -butoxyethyl nicotinate, and 1- (4-methylphenyl) ethyl nicotinate; vitamin C compounds such as ascorbyl pro-A, ascorbyl stearate, ascorbyl palmitate, and L-ascorbyl dipalmitate; vitamin D compounds such as hesperidin methyl, ergocalciferol, cholecalciferol, etc.; vitamin K such as phylloquinone and farnesoquinone, gamma-oryzanol, dibenzoyl thiamine, and dibenzoyl thiamine hydrochloride; vitamins B1 such as thiamine hydrochloride, thiamine hexadecyl hydrochloride, thiamine thiocyanate, thiamine lauryl hydrochloride, thiamine nitrate, thiamine monophosphate, thiamine lysine hydrochloride, thiamine triphosphate, thiamine monophosphate phosphate, thiamine monophosphate, thiamine diphosphate hydrochloride, thiamine triphosphate monophosphate, and the like; vitamin B6 such as pyridoxine hydrochloride, pyridoxine acetate, pyridoxal hydrochloride, pyridoxal 5' -phosphate, and pyridoxamine hydrochloride; vitamins B12 such as cyanocobalamin, hydroxycobalamin, and deoxyadenosylcobalamin; folic acid such as folic acid and pteroylglutamic acid; nicotinic acids such as nicotinic acid and nicotinamide; pantothenic acids such as pantothenic acid, calcium pantothenate, Panthenol (pantonol), D-pantetheine, D-pantethine, coenzyme A, and panthenyl ethyl ether; biotin such as biotin and biocytin; ascorbic acid derivatives such as ascorbic acid, sodium ascorbate, dehydroascorbic acid, sodium ascorbyl phosphate, magnesium ascorbyl phosphate, and the like, i.e., vitamin C; and retinoid factors such as carnitine, pyrroloquinoline quinone, ferulic acid, α -lipoic acid, orotic acid, and the like, and known ingredients that can be used in cosmetics, pharmaceuticals, and cosmeceuticals.
As the peptide or derivative thereof, there may be mentioned: keratin degrading peptides, hydrolyzed keratin, collagen, fish-derived collagen, telogen, gelatin, elastin degrading peptide, collagen degrading peptide, hydrolyzed collagen, hydroxypropylammonium chloride hydrolyzed collagen, elastin degrading peptide, conchiolin degrading peptide, hydrolyzed conchiolin degrading peptide, silk protein degrading peptide, hydrolyzed silk, lauroyl hydrolyzed silk sodium, soybean protein degrading peptide, hydrolyzed soybean protein, wheat protein degrading peptide, hydrolyzed wheat protein, casein degrading peptide, acylated peptide (palmitoyl oligopeptide, palmitoyl pentapeptide, palmitoyl tetrapeptide, etc.), and the like.
Examples of the amino acid or its derivative 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, creatine, and the like.
As the cell activating components, there can be mentioned: amino acids such as γ -aminobutyric acid and ∈ -aminopropionic acid; vitamins such as retinol, thiamine, riboflavin, pyridoxine hydrochloride, and pantothenic acids; α -hydroxy acids such as glycolic acid and lactic acid; tannin, flavonoids, saponin, allantoin, photosensitizer No. 301 (Takanal), and ingredients derived from plants (e.g., soybean, blueberry, lemon grass, aloe, chlorella, blackberry, coix seed, chamomile, houttuynia cordata, hops, carrot, etc.); royal jelly, royal jelly extract; whey, yogurt extract, hydrolyzed milk protein, whey-derived extract, yeast extract, and the like.
Examples of the anti-aging component include: hydrolyzed soy protein, retinoids (retinol, retinoic acid, retinal, etc.), ursolic acid, peptides (caproyltetrapeptide-3, oligopeptide-24, etc.), ingredients derived from plants (e.g., artichoke, Rosa roxburghii, seaweed, Vaccinium myrtillus, birch, Plantago major, Angelica sinensis, Scutellaria baicalensis, Hypericum erectum, comfrey, Rosa multiflora, Lilium blackberry, houttuynia cordata, Tilia miqueliana, moutan bark, etc.), pangamic acid, kinetin, ursolic acid, Curcuma longa extract, sphingosine derivatives, silicon, silicic acid, N-methyl-L-serine, mevalonic lactone, etc.
Examples of the blood circulation-promoting component include: ingredients derived from plants (e.g., asian ginseng, angelica keiskei, arnica, ginkgo biloba, fennel, plectranthus, oaken, chamomile, carrot, gentian violet, burdock, rice, hawthorn, shiitake, hawthorn, juniper, ligusticum wallichii, swertia japonica, thyme, clove, dried orange peel, angelica, peach kernel, spruce, carrot, garlic, broom cypress, grape, peony, horse chestnut, lemon balm, grapefruit, coix seed, rosemary, rose hip, peach, apricot, walnut, corn); glucosyl hesperidin, and the like.
Examples of the keratolytic ingredient include: salicylic acid, glycolic acid, tartaric acid, phytic acid, sulfur, and the like.
Examples of the whitening component include tocopherol.
Examples of the astringent components include: zinc p-phenolsulfonate, zinc oxide, menthol, ethanol, and the like.
Examples of the ultraviolet screening component include: 2-ethylhexyl p-methoxycinnamate, hexyl 2- [4- (diethylamino) -2-hydroxybenzoyl ] benzoate, 2,4, 6-tris [4- (2-ethylhexyloxycarbonyl) anilino ] -1,3, 5-triazine, t-butylmethoxydibenzoylmethane, ethylhexyl dibenzylidene dioxoimidazolidine hexanoate, ethylhexyltriazoline, p-aminobenzoic acid and its derivatives, octyl p-dimethylaminobenzoate, ethylene glycol salicylate, dihydroxybenzophenone, titanium dioxide, zinc oxide, and the like.
The active ingredients may be used alone or in combination of two or more.
Additive agent
The composition of the present invention may further contain additives such as surfactants, antioxidants, preservatives, thickeners, pH adjusters, buffers, isotonic agents, thickeners or thickening agents, oils, stabilizers, irritation reducing agents, colorants, perfumes, chelating agents, and the like, as necessary.
In the present invention, even when these additives are contained, the functions of the components (a) to (C) can be effectively exhibited.
The additive may be a component corresponding to the component (C) or may be a component other than the component (C).
Examples of the surfactant include nonionic surfactants. Specific examples of the surfactant (nonionic surfactant) include: polyglycerol-2 oleate, polyglycerol-10 pentaoleate, polyglycerol-10 laurate, polyglycerol-10 myristate, polyglycerol-10 stearate, polyglycerol-10 isostearate, polyglycerol-10 oleate, polyglycerol-10 distearate, polyglycerol-10 diisostearate, polyglycerol-10 tristearate, polyglycerol-10 trioleate, polyglycerol-10 pentastearate, polyglycerol-10 pentahydroxystearate, polyglycerol-10 pentaisostearate, polyglycerol-10 pentaoleate, polyglycerol-10 decaoleate, polyglycerol-2 stearate, polyglycerol-2 isostearate, polyglycerol-6 myristate, polyglycerol-6 laurate, polyglycerol-6 stearate, Polyglyceryl fatty acid esters such as polyglyceryl-6 tristearate, polyglyceryl-6 pentastearate, glycerin-4 oleic acid polyester, and polyglyceryl-6 stearate; 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, PEG-100 hydrogenated castor oil, and other PEG [ polyethylene glycol or Polyoxyethylene (POE) ] hydrogenated castor oil (POE hydrogenated castor oil); POE castor oil such as POE castor oil 3, POE castor oil 4, POE castor oil 6, POE castor oil 7, POE castor oil 10, POE castor oil 13.5, POE castor oil 17, POE castor oil 20, POE castor oil 25, POE castor oil 30, POE castor oil 35, and 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, and sorbitan trioleate; polysorbates (POE sorbitan fatty acid esters) such as POE (20) sorbitan monolaurate (polysorbate 20), POE (20) sorbitan monopalmitate (polysorbate 40), POE (20) sorbitan monostearate (polysorbate 60), POE (20) sorbitan tristearate (polysorbate 65), POE (20) sorbitan monooleate (polysorbate 80), and POE (20) sorbitan trioleate (polysorbate 85); POEPOP glycol (196E.O.) (67P.O.) (or polyoxyethylene (196) polyoxypropylene (67) glycol, which are the same in the same expression manner below, poloxamer 407), POEPOP glycol (20E.O.) (20P.O.), POEPOP glycol (42E.O.) (67P.O.) (poloxamer 403), POEPOP glycol (54E.O.) (39P.O.) (poloxamer 235), POEPOP glycol (124E.O.) (39P.O.), POEPOP glycol (160E.O.) (30 epop 30P.O.), POP glycol (200E.O.) (70P.O.), POEPOP glycol (30E.O.) (150 POP 150P.O.) (poloxamer 188), and other POE/diols; 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 (40e.o., polyethylene glycol stearate 40), polyethylene glycol monostearate (45 E.O), polyethylene glycol monostearate (55 E.O), polyethylene glycol monostearate (75 E.O), polyethylene glycol monostearate (140 E.O) and the like; POE alkyl ethers such as POE (9) lauryl ether; POE-POP alkyl ethers such as POE (20) POP (4) hexadecyl ether; POE alkyl phenyl ethers such as POE (10) nonyl phenyl ether. In the above-exemplified compounds, POE represents polyoxyethylene, POP represents polyoxypropylene, and the number in parentheses represents the number of moles added.
Examples of the antioxidant include: dibutylhydroxytoluene, butylhydroxyanisole, sorbic acid, sodium sulfite, ascorbic acid, isoascorbic acid, L-cysteine hydrochloride and the like.
Examples of the preservative (preservative) include: for example, 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, alkanediols, glycerol fatty acid esters, and the like.
Examples of the thickener include: guar gum, locust bean gum, carrageenan, xanthan gum, carboxymethyl cellulose, hydroxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl methyl cellulose, polyvinyl alcohol, polyvinylpyrrolidone, carboxyvinyl polymer, alkyl acrylate copolymer, polyethylene glycol, bentonite, hydroxyethyl acrylate/Na acryloyldimethyl taurate copolymer, (ammonium acryloyldimethyl taurate/vinylpyrrolidone) copolymer, and the like.
Examples of the pH adjuster 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.), organic bases (triethanolamine, diisopropanolamine, triisopropanolamine, etc.), and the like.
Examples of the buffer include: boric acid-based buffers, phosphoric acid-based buffers, carbonic acid-based buffers, citric acid-based buffers, acetic acid-based buffers, and the like.
Examples of isotonic agents include: sodium chloride, potassium chloride, calcium chloride, magnesium chloride, potassium acetate, sodium acetate, magnesium sulfate, glycerol, propylene glycol, and the like.
As the thickener or thickening agent, there may be mentioned: guar gum, hydroxypropyl guar gum, cellulose-based high molecular compounds (e.g., methylcellulose, ethylcellulose, hydroxypropylmethylcellulose, hydroxyethylcellulose, sodium carboxymethylcellulose, etc.), gum arabic, karaya gum, xanthan gum, agar, alginic acid, α -cyclodextrin, dextrin, dextran, mucopolysaccharide (e.g., heparin-like substances, heparin sulfate, acetylclerotic sulfate, heparan, hyaluronic acid, hyaluronate (sodium salt, etc.), starch, chitin and its derivatives, chitosan and its derivatives, carrageenan, sorbitol, polyvinyl-based high molecular compounds (polyvinylpyrrolidone, polyvinyl alcohol, carboxyvinyl polymer, etc.), alkali metal salts (sodium salt, potassium salt, etc.) of polyacrylic acid, amine salts (monoethanolamine salt, diethanolamine salt, etc.) of polyacrylic acid, ammonium salts (monoethanolamine salt, diethanolamine salt, etc.), etc., of polyacrylic acid, etc., and the like, Triethanolamine salt, etc.), casein, gelatin, collagen, pectin, elastin, ceramide, liquid paraffin, glycerin, polyethylene glycol, polyethyleneimine alginate (sodium salt, etc.), alginic acid ester (propylene glycol ester, etc.), tragacanth powder (トラガント powder), triisopropanolamine, etc.
Examples of the oil component include: hydrocarbon oils (e.g., liquid paraffin, liquid isoparaffin, squalane, squalene, oligomers of α -olefin), fats and oils { e.g., vegetable oils [ e.g., soybean oil, rapeseed oil, corn oil, sesame oil, linseed oil, safflower oil, sunflower seed oil, cottonseed oil, nut oil (macadamia nut oil, hazelnut oil, peanut oil, almond oil, walnut oil, etc.), seed oils (grape seed oil, pumpkin seed oil, etc.), lemon oil, tea seed oil, perilla oil, borage oil, olive oil, rice bran oil, wheat germ oil, coconut oil, palm olein, palm kernel oil, etc. ], animal oils (e.g., fish oil, liver oil, whale oil, etc.), Medium Chain Triglycerides (MCT), etc. ], ester oils { e.g., adipates (e.g., diisobutyl adipate, di-2-ethylhexyl adipate, dibutyl adipate) }, Isooctanoate [ e.g., Triisooctanoic acid glyceride (trisooctanoic acid glyceride) ], isononanoate (e.g., isononyl isononanoate), myristate (e.g., isopropyl myristate), isostearate (e.g., batyl isostearate), sebacate (e.g., diethyl sebacate), etc. ], silicone oil, fatty acid (e.g., isostearic acid, etc.), higher alcohol, and the like.
The oil component may be in the form of a solid, a liquid, a semisolid, or a paste (for example, a substance having a viscosity of about 5000 to 100000 mPas at 30 ℃) at room temperature (25 ℃). In addition, the composition of the present invention may or may not contain such an oil [ e.g., a cream-like oil (cream oil) ]. When such an oil component is contained, 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), or the like.
Examples of the stabilizer include: sodium polyacrylate, dibutylhydroxytoluene, butylhydroxyanisole, etc.
Examples of the irritation-relieving agent include: glycyrrhrizae radix extract/sodium alginate, etc.
Examples of the coloring material include pigments described in a legal pigment handbook (published by japan cosmetic industry association (2004)) and the like.
Examples of the perfume include: essential oils such as lavender oil, rosemary oil, sage oil, thyme oil, bergamot oil, eucalyptus oil, peppermint oil, spearmint oil, peppermint oil, orange oil, lemon oil, grapefruit oil, and other citrus essential oils, blended flavors, and the like.
Examples of the chelating agent include: EDTA disodium salt, EDTA calcium disodium salt, etc.
The additives may be used alone or in combination of two or more.
Base or carrier
The compositions of the present invention may generally comprise a base or carrier.
Examples of the base or carrier include: water, water-soluble solvents [ lower alcohols (e.g., ethanol, isopropanol), polyols (e.g., glycerin, propylene glycol, propane diol, polyethylene glycol (polyethylene glycol), 1, 3-butylene glycol, isoprene glycol, dipropylene glycol, etc.), etc. ], oily bases, and the like. The water may be used as a physiological saline solution or the like.
The base or the carrier may be used singly or in combination of two or more.
In particular, the composition of the present invention may be an aqueous composition (for example, a composition comprising water, physiological saline, water or a mixed solvent of physiological saline and a water-soluble solvent).
When water and another base or carrier (e.g., a water-soluble solvent) are combined, the ratio of water to the other base or carrier (mass ratio) may be, for example, about 99.9/0.1 to 10/90 (e.g., 99.5/0.5 to 30/70), preferably about 99/1 to 40/60 (e.g., 98/2 to 50/50), and more preferably about 97/3 to 60/40 (e.g., 95/5 to 70/30).
When the composition of the present invention contains water (particularly, an aqueous composition), the proportion of water in the composition may be selected from the range of 10% by mass or more (for example, 20% by mass or more), and may be, 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).
The upper limit of the amount of water in the composition can be appropriately selected depending on the use of the composition, and may be, for example, 99 mass%, 98 mass%, 97 mass%, 96 mass%, 95 mass%, 94 mass%, 93 mass%, 92 mass%, 91 mass%, 90 mass%, or the like.
In the present invention, the component (a) can be contained in such an aqueous composition with excellent solubility or dispersibility. In the present invention, even in the case of an aqueous composition containing component (C), excellent transdermal absorbability of component (C) can be effectively achieved.
Thus, according to the present invention, a high-quality aqueous composition can be efficiently obtained.
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 about 3 to 8.
Properties, uses, methods of preparation and the like
The composition of the present invention can be prepared by mixing the above-mentioned components (for example, a composition containing at least the components (a) to (B) and a base or a carrier, a composition containing at least the component (a) and a base or a carrier, a composition containing at least the components (a) to (C) and a base or a carrier, and the like).
The form of the composition of the present invention is not particularly limited, and may be any form such as liquid, fluid, gel, and semi-solid. In addition, the composition can be prepared into a liquid, a fluid, a gel, a semisolid, or the like by the preparation at the time of use. The semisolid shape refers to a shape having plasticity, that is, being capable of being deformed by applying force, for example, like ointment.
The composition is preferably in the form of a liquid (liquid).
The viscosity of the liquid composition (liquid composition) at 25 ℃ may be, for example, 500Pa · s or less, preferably 400Pa · s or less, and more preferably 300Pa · s or less.
The viscosity can be measured at 25 ℃ using, for example, a rotational viscometer (RB80L type viscometer, manufactured by Toki Sangyo).
The compositions of the present invention may be opaque (cloudy) or transparent. In the present invention, even in the case of an aqueous composition containing the component (a), a transparent (or less turbid) composition can be effectively obtained.
When the composition of the present invention is in an emulsified state, it may be any of O/W type (oil-in-water type) and W/O type (water-in-oil type), and may be O/W type in general.
The use of the composition of the present invention is not particularly limited, and the composition can be used as a composition for external use (external preparation), particularly a composition for skin (composition for external application to skin).
In addition, the composition of the present invention can also be used as a leave-on composition (leave-on composition). As described above, the present invention is directed to a composition containing a water-soluble component (C), which can improve transdermal absorbability by the component (a) and/or the component (B), and is therefore also suitable for leave-on use in which removal by washing or the like is not required.
Such a composition (external composition) may be any of cosmetics (cosmetic materials), drugs (external drugs), and cosmeceuticals.
The form of the composition is not particularly limited, and examples thereof include: liquid, suspension, emulsion, cream, ointment, gel, liniment, lotion, aerosol, etc.
Specific forms of the composition include, for example, pharmaceutical compositions: examples of the external composition for cosmeceutics or cosmetics include liquids, lotions, creams, ointments, gels, and the like: makeup base (e.g., lotion, emulsion, gel, cream, beauty lotion, sunscreen, primary pack (pack), mask, body lotion, etc.), makeup cosmetic (e.g., foundation, makeup base, lip gloss, lipstick, blush, etc.), cleansing cosmetic (e.g., cleansing cosmetic such as face toilet, makeup remover, body wash, shampoo), cleanser (e.g., face toilet, makeup remover, face toilet, etc.), cleansing sheet (particularly no-wash cosmetic); bathing agents, etc.
Among them, the composition containing (C) a water-soluble component can be suitably used as a leave-on composition (for example, a leave-on cosmetic such as a base cosmetic (foundation), a makeup cosmetic, and a sunscreen cream, and particularly, a base cosmetic such as a cosmetic lotion and a cosmetic liquid).
Container with a lid
The composition of the present invention can be contained (filled, injected, sealed) in a container.
The container may be a package having a portion (surface) in contact with the composition (preparation), and may be composed of, for example, a container main body portion for containing the composition (e.g., liquid composition), a portion (nozzle, inner plug) including an extraction port of the container, a straw, a cap, and the like.
The material constituting the container may be selected from a wide range, and for example, at least a part or all of the part contacting the composition may be: plastics (for example, olefin resins, styrene resins, acrylic resins, polyester resins, polycarbonate resins, fluororesins, chlorine resins (polyvinyl chloride, etc.), polyamide resins, polyacetal resins, polyphenylene ether resins (modified polyphenylene ether, etc.), polyarylates, polysulfones, polyimide resins, epoxy resins, cellulose resins (cellulose acetate, etc.), hydrocarbon resins optionally substituted with halogen atoms, etc.), glass, metals (aluminum, etc.), and the like.
The container may be made of a single material or two or more materials.
Examples of the olefin-based resin include: ethylene resin [ e.g., polyethylene (including high-density polyethylene, low-density polyethylene, ultra-low-density polyethylene, linear low-density polyethylene, ultra-high-molecular-weight polyethylene, etc.), ethylene-propylene copolymer, etc. ], propylene resin [ e.g., polypropylene (PP) (isotactic polypropylene, syndiotactic polypropylene, atactic polypropylene, etc.), propylene-ethylene copolymer, etc. ], methylpentene resin (e.g., polymethylpentene, etc.), etc.
Examples of the styrene-based resin include: polystyrene, acrylonitrile-containing styrene resins (e.g., acrylonitrile-styrene copolymer (AS resin), acrylonitrile-butadiene-styrene copolymer (ABS resin), etc.), and the like.
Examples of the acrylic resin include: and resins containing, as a polymerization component, an acrylic acid ester such as methyl acrylate, a methacrylic acid ester such as methyl methacrylate, cyclohexyl methacrylate, t-butylcyclohexyl methacrylate, and the like.
Examples of the polyester-based resin include: an aromatic polyester-series resin [ for example, a resin having an alkylene terephthalate unit (an alkylene terephthalate-series resin: for example, polyethylene terephthalate (PET), polypropylene terephthalate, polybutylene terephthalate (PBT), etc.), a resin having an alkylene naphthalate unit (for example, polyethylene naphthalate (PEN), polybutylene naphthalate, etc.) ], and the like.
As the fluororesin, there may be mentioned: fluorine-substituted polyethylene (polytetrafluoroethylene, polychlorotrifluoroethylene, etc.), polyvinylidene fluoride, polyvinyl fluoride, perfluoroalkoxy fluororesin, tetrafluoroethylene/hexafluoropropylene copolymer, ethylene/tetrafluoroethylene copolymer, ethylene/chlorotrifluoroethylene copolymer, etc.
As the polyacetal-based resin, in addition to a resin composed of only oxymethylene units, a resin containing oxymethylene units in a part thereof can be cited.
The modified polyphenylene ether includes polystyrene modified polyphenylene ether and the like.
The polyarylate may be an amorphous polyarylate.
Examples of the polyimide-based resin include aromatic polyimides obtained by polymerizing pyromellitic dianhydride and 4, 4' -diaminodiphenyl ether.
As the cellulose acetate, there may be mentioned: cellulose diacetate, cellulose triacetate, and the like.
The material of the container is preferably glass, plastic, or the like. Therefore, at least a part of the container (or the material of the container) may be made of glass, plastic, or the like.
Particularly preferred are plastics (i.e., plastic containers) such as olefin resins, styrene resins, and polyester resins, more preferred are ethylene resins, propylene resins, alkylene terephthalate resins, and polystyrene, further preferred are polypropylene, polyethylene terephthalate, and polystyrene, and further more preferred is polyethylene terephthalate.
The composition of the present invention can effectively function as a composition in various containers (or materials thereof, glass, plastic, etc., particularly plastic such as PET).
The container may be made of a polymer blend with a polymer other than the above-mentioned polymers. When the container material of the container for containing the composition of the present invention is a polymer blend with the polymer, the mixing ratio of the polymer and the polymer other than the polymer is not particularly limited as long as the effect of the present invention can be obtained, and the total weight of the polymer is preferably 30 w/w% or more, more preferably 50 w/w% or more, further more preferably 65 w/w% or more, and particularly preferably 80 w/w% or more, based on the total weight of the entire constituent materials.
As the container, at least a part of a portion (contact surface) thereof to be in contact with the composition of the present invention may be composed of the above-mentioned material. For example, a layer or a film made of the above-described material may be formed on the inner surface of the container, or the container itself may be molded from the above-described material.
Further, the container may be constituted by the above-mentioned material in a part (a container body part, a part including an extraction port of the container (a nozzle, an inner stopper), a straw, a cap, or the like) constituting the container, or the container may be constituted by the above-mentioned material as a whole.
Application method
The method of using the composition of the present invention can be used, for example, in the following manner depending on the skin condition, age, sex, and the like of the subject to be used.
For example, the composition (composition containing (C) a water-soluble ingredient, etc.) may be applied to the skin in an appropriate amount (e.g., about 0.05 to 10g) once or more (e.g., about 1 to 5 times, preferably 1 to 3 times) per day. The composition may be applied so that the amount of the water-soluble component (C) (ethyl VC, tranexamic acid, etc.) used per day is preferably about 0.01 to 500mg, more preferably about 0.2 to 200 mg. The coating time may be, for example, about 1 to 14 days, preferably about 3 to 14 days.
The composition of the present invention can be suitably used for preventing, treating and/or improving diseases (or symptoms) such as chloasma, mottle, acne scar, wrinkle, rough skin, and the like, and the use thereof can be suitably selected depending on the kind of the water-soluble component (C) and the kind of the optional active ingredient. Therefore, in addition to healthy persons, persons having these skin symptoms can be used as applicable subjects.
[2. improving solubility or dispersibility ]
In one embodiment of the present invention, the solubility or dispersibility of the component (a) can be improved (or improved) in the composition.
Accordingly, as one embodiment of the present invention, the following method is provided.
A method for improving (or improving or assisting) the solubility or dispersibility of (A) an ether synthesized from a fatty alcohol and glycerin, which comprises allowing (A) the ether synthesized from a fatty alcohol and glycerin to coexist with (B) an acyl glutamic acid lysine salt [ or allowing (A) a composition comprising the ether synthesized from a fatty alcohol and glycerin (for example, a composition comprising water) to contain (coexist with) (B) an acyl glutamic acid lysine salt ].
In addition, the following formulations are provided as an embodiment of the present invention.
A preparation for improving (or improving or assisting) (A) solubility or dispersibility (particularly solubility or dispersibility in a solvent containing water) of an ether synthesized from a fatty alcohol and glycerin, which contains (B) an acylglutamic acid lysine salt (solubility-improving agent, dispersibility-improving agent, dissolution-assisting agent, dispersion-assisting agent).
[3. improving percutaneous absorbability ]
In one embodiment of the present invention, the percutaneous absorbability (skin permeability) of the (C) water-soluble ingredient can be improved.
Accordingly, as one embodiment of the present invention, the following method is provided.
A method for improving (or improving or assisting) the percutaneous absorbability of a water-soluble component (C) by allowing the water-soluble component (C) to coexist with (A) an ether synthesized from a fatty alcohol and glycerin and/or (B) an acyl glutamic acid lysine salt [ or by allowing a composition containing the water-soluble component (C) to contain (coexist with) (A) an ether synthesized from a fatty alcohol and glycerin and/or (B) an acyl glutamic acid lysine salt ].
In this method, at least the component (A) may be coexistent (or contained), and it is particularly preferable to coexist (or contain) the components (A) and (B).
In addition, the following formulations are provided as an embodiment of the present invention.
A preparation for improving (or improving or assisting) the percutaneous absorbability of (C) a water-soluble component, which comprises (A) an ether synthesized from an aliphatic alcohol and glycerin and/or (B) an acylglutamic acid lysine salt (percutaneous absorption improving or ameliorating agent, percutaneous absorption enhancer, percutaneous absorption auxiliary agent, percutaneous absorption regulator).
The preparation may contain at least the component (A), and particularly preferably contains the components (A) and (B).
In the above embodiments, the types and contents of the respective components, the types and contents of the other components, the formulation forms and uses of the composition, and the like are as described in [1. composition ].
Examples
The present invention will be described more specifically with reference to examples, but the present invention is not limited to these examples, and those skilled in the art can make various modifications without departing from the technical spirit of the present invention.
Experimental example 1 (solubility of component (A))
The ingredients shown in the following table were heated and mixed at 70 ℃ for 5 minutes to prepare a composition. Next, the obtained composition was charged into a transparent glass bottle at room temperature, and the state of the composition was observed visually.
In the table, the unit of each component is (mass%) (the same applies hereinafter). In the table, "Pellicer" represents "Pellicer L-30" (an aqueous solution of dilauryl glutamic acid lysine sodium/water of 29/71) manufactured by asti Kasei Chemicals co, ltd, which contains dilauryl glutamic acid lysine sodium as a constituent component, and the parenthesis represents the mass% of "dilauryl glutamic acid lysine sodium" (the same applies hereinafter).
[ Table 1]
Figure BDA0003089223350000221
From the results of the above table, it was found that the mono 2-ethylhexyl glyceryl ether as the component (a) was poor in solubility or dispersibility in water, and the test solutions were separated (test examples 1A to 1B), but when it was allowed to coexist with sodium dilauryl glutamic acid lysine as the component (B), good solubility or dispersibility in water was exhibited, and the test solutions were clear and transparent (test examples 1C to 1F).
On the other hand, by using various surfactants, the test solutions were not separated, but were poor in solubility and dispersibility, and cloudiness was generated (test examples 1G to 1L).
It has been found that, surprisingly, component (B) is a component which can dissolve or disperse component (A) effectively (and specifically).
Test example 2((C) permeability of Water-soluble component)
Compositions having the compositions shown in the following table were prepared.
Next, the permeability of ethyl VC (3-O-ethyl ascorbic acid) as the water-soluble component (C) was evaluated for each composition as described below.
Adding a matched special measuring culture medium of 0.5mL/well to the lower part of a Transwell of a human three-dimensional culture epidermis LabCyte EPI-MODEL24(J-TEC company), and adding the special measuring culture medium at 37 ℃ (5-10% CO)2) The pre-culture is carried out for 18-22 hours.
The dedicated assay medium was then replaced with 0.5ml PBS and pre-incubated for 30 minutes at 37 degrees in a constant temperature bath. PBS was replaced with an equal amount of fresh PBS, 0.3mL of the drug solution was added directly to the upper part of the cells, and the time of addition of the drug solution was recorded as zero.
After a predetermined time within 360 minutes, 0.1mL of the drug solution was sampled from the bottom with the lapse of time, and then an equal amount of PBS was added quickly. The sampled drug solution was quantified by HPLC, and the transmittance (P) was calculated based on the following equation.
The culture medium, PBS and the drug solution were heated to 37 ℃ and then administered.
P=(ΔQ/Δt)×(1/C0)×(1/Area)
In the above formula,. DELTA.Q/. DELTA.t represents a drug or the likeThe acceleration is obtained as the slope of the linear portion of the cumulative permeation amount-time curve of the drug. In addition, C0The initial concentration of the drug to be administered is shown, and Area is the permeation Area (0.3215 cm)2)。
Further, the Ratio of the transmittance (Ps) including various components (test examples 2B to 2J) and the transmittance (Pc) not including various components (control, test example 2A) was calculated based on the following formula, and this Ratio was referred to as Enhancement Ratio (ER).
ER=Ps/Pc
The results are shown in the following table.
[ Table 2]
Figure BDA0003089223350000231
From the results of the above table, it is clear that the permeability (percutaneous absorbability) of ethyl VC as the water-soluble component (C) is improved specifically in mono 2-ethylhexyl glyceryl ether as the component (a) and sodium dilaurylglutamic acid lysine as the component (B).
In particular, it is known that: the permeability of ethyl VC can be improved by using a very small amount (0.2 mass%) of mono 2-ethylhexyl glyceryl ether as component (a) as compared with a known component (5 mass%) such as other surfactants.
Test example 3((C) permeability of Water-soluble component)
Compositions having the compositions shown in the following table were prepared, and the permeability of ethyl VC (3-O-ethyl ascorbic acid) was evaluated in the same manner as in test example 2.
The results are shown in the following table.
[ Table 3]
Figure BDA0003089223350000241
From the results of the above table, it is clear that the permeability (percutaneous absorbability) of ethyl VC as the water-soluble component (C) is improved in various proportions in mono 2-ethylhexyl glyceryl ether as the component (a) and sodium dilauryl glutamic acid lysine as the component (B).
Further, by combining mono 2-ethylhexyl glyceryl ether as the component (a) and sodium dilauroylglutamic lysine as the component (B), the permeability of ethyl VC is significantly (synergistically) improved.
On the other hand, even when mono-2-ethylhexyl glyceryl ether is combined with cyclohexane dicarboxylic acid bisethoxydiglycol, the permeability of ethyl VC is not improved, but rather is reduced to some extent.
Test example 4((C) permeability of Water-soluble component)
Compositions having the compositions shown in the following table were prepared, and the permeability of each water-soluble component (C) was evaluated in the same manner as in test example 2.
The results are shown in the following table.
[ Table 4]
Figure BDA0003089223350000251
From the results of the above table, it is clear that the permeability (percutaneous absorbability) of various water-soluble components (C) is also improved in mono 2-ethylhexyl glyceryl ether as the component (a) and sodium dilaurylglutamic acid lysine as the component (B).
In addition, by combining mono 2-ethylhexyl glyceryl ether as component (a) and sodium dilauroylglutamic lysine as component (B), the permeability was also significantly (synergistically) improved in the same manner as in ethylvc.
Test example 5((C) permeability of Water-soluble component)
Compositions having the compositions shown in the following table were prepared, and the permeability of nicotinamide was evaluated in the same manner as in test example 2.
The results are shown in the following table.
In addition, as the transmittance (Pc), the transmittance (Pc) of test example 5A was used as ER in test examples 5C to 5D, and the transmittance (Pc) of test example 5B was used as ER in test examples 5E to 5G.
[ Table 5]
Figure BDA0003089223350000252
From the results of the above table, it is clear that the permeability (transdermal absorbability) of nicotinamide is also improved in the specificity in mono 2-ethylhexyl glyceryl ether as the component (a) and sodium dilaurylglutamic lysine as the component (B) in the same manner as in the other water-soluble components (C).
The tendency of a significant (synergistic) improvement in permeability by combining mono 2-ethylhexyl glyceryl ether as component (a) and sodium dilauroylglutamic lysine as component (B) was the same as that of the other water-soluble component (C).
[ preparation examples ]
The compositions were prepared according to the formulations described in the following tables. In the following table, the unit of each component is (mass%).
[ Table 6]
Name of ingredient Formulation example 1 Formulation example 2 Formulation example 3 Formulation example 4 Formulation example 5
3-O-Ethyl ascorbic acid 1 1
Ascorbic acid-2-glucoside 2 2
Ascorbic acid 3
Arbutin
L-ascorbic acid magnesium phosphate
Tranexamic acid
Nicotinamide
Hydroquinone
Allantoin 0.1
Glycyrrhizic acid dipotassium salt 0.05
Mono-2-ethylhexyl glyceryl ether 0.2 0.1 0.3 0.005 0.05
Pellicer L-30 1 0.5 0.01 0.2 0.3
Carboxyvinyl polymer 0.1 0.1 0.1 0.1 0.01
EDTA-2Na 0.05 0.05 0.05 0.05 0.05
1, 3-propanediol 2 5
1, 3-butanediol 5 6
Dipropylene glycol 5 5
Concentrated glycerin 4 4 6 6 8
Diglycerol 1 2
Anhydrous ethanol 2 2 2 5
Silicone solution mixture 0.1
Citric acid sodium salt 0.2 0.2
Citric acid anhydride 0.05 0.05
Phenoxyethanol 0.2 0.3
P-hydroxybenzoic acid methyl ester 0.2 0.2 0.2
Perfume 0.1 0.1 0.1 0.1 0.1
l-menthol (Standard of cosmeceutical raw materials) 0.05 0.05 0.1 0.05
Polyoxyethylene sorbitan laurate (20E.O) 0.1 0.2
Polyoxyethylene hydrogenated castor oil 40
Jojoba oil 0.1 0.1
Polyoxyethylene (20) polyoxypropylene (4) cetyl ether 0.3 0.2 0.4
PPG-6-decyltetradecanol polyether-30 0.2 0.2
d-delta-tocopherol 0.1 0.1 0.1
Grapefruit extract 0.5 0.5 0.5 0.5 0.1
Lemon extract 0.5 0.5 0.5 0.1
Kiwi fruit extract 0.1 0.1 0.1 0.1
Extract of globe artichoke 0.1 0.1 0.1 0.1 0.1
Semen Alpiniae extract 0.1 0.1 0.1 0.1 0.1
Hyaluronic acid Na 0.01 0.01 0.01 0.01
Hydrolyzed hyaluronic acid 0.01
Acetyl sodium hyaluronate 0.05 0.05 0.001
Ceramide 2 0.001 0.1 0.001
Ceramide 3 0.001 0.001
Pure water Residual amount of Residual amount of Residual amount of Residual amount of Residual amount of
100 100 100 100 100
[ Table 7]
Name of ingredient Formulation example 6 Formulation example 7 Formulation example 8 Formulation example 9 Formulation example 10
3-O-Ethyl ascorbic acid
Ascorbic acid-2-glucoside 0.01
Ascorbic acid
Arbutin 3
L-ascorbic acid magnesium phosphate 2
Tranexamic acid 2 2
Nicotinamide 4.5
Hydroquinone 1
Allantoin
Glycyrrhizic acid dipotassium salt
Mono-2-ethylhexyl glyceryl ether 0.1 0.1 0.2 0.2
Pellicer L-30 3 0.5 0.4 0.5
Carboxyvinyl polymer 0.2 0.1
EDTA-2Na 0.05
1, 3-propanediol 5 4 7
1, 3-butanediol 4 3
Dipropylene glycol 5
Concentrated glycerin 8 8 10 4
Diglycerol 3
Anhydrous ethanol 0.5 1
Silicone solution mixture 0.5
Citric acid sodium salt 0.1 0.2
Citric acid anhydride 0.05 0.05
Phenoxyethanol 0.3
P-hydroxybenzoic acid methyl ester 0.2 0.2 0.2 0.2 0.25
Perfume 0.1 0.1 0.1
l-menthol (Standard of cosmeceutical raw materials)
Polyoxyethylene sorbitan laurate (20E.O) 0.1
Polyoxyethylene hydrogenated castor oil 40 0.2
Jojoba oil 0.25
Polyoxyethylene (20) polyoxypropylene (4) cetyl ether 0.2 0.2
PPG-6-decyltetradecanol polyether-30 0.2 0.2 0.2
d-delta-tocopherol 0.5 0.1 0.001 0.01
Grapefruit extract 0.5 0.5 0.1
Lemon extract 0.5 0.5 0.5 0.1 0.1
Kiwi fruit extract 0.1 0.1 0.1 0.1 0.1
Extract of globe artichoke 0.1 0.1 0.1 0.1 0.1
Semen Alpiniae extract 0.1 0.1 0.1
Hyaluronic acid Na 0.01 0.01 0.01
Hydrolyzed hyaluronic acid 0.1 0.05
Acetyl sodium hyaluronate 0.01 0.1
Ceramide 2 0.0001
Ceramide 3 0.0001
Pure water Residual amount of Residual amount of Residual amount of Residual amount of Residual amount of
100 100 100 100 100
[ Table 8]
Name of ingredient Formulation example 11 Formulation example 12 Formulation example 13 Formulation example 14 Formulation example 15 Formulation example 16
3-O-Ethyl ascorbic acid 1
Ascorbic acid-2-glucoside
Ascorbic acid
Arbutin
L-ascorbic acid magnesium phosphate
Tranexamic acid 1
Nicotinamide 3 3 5
Hydroquinone 1
Allantoin 0.1
Glycyrrhizic acid dipotassium salt 0.1 0.05
Mono-2-ethylhexyl glyceryl ether 0.25 0.25 0.01 0.1 0.15 0.1
Pellicer L-30 06 0.6 0.05 0.2 0.4 0.5
Carboxyvinyl polymer 0.4 0.4 0.1 0.1
EDTA-2Na 0.05 0.05 0.05 005 0.05 0.05
1, 3-propanediol 2
1, 3-butanediol 5 5 5 6 7 3
Dipropylene glycol
Concentrated glycerin 5 5 6 5 4
Diglycerol 4
Anhydrous ethanol 4 5 1
Silicone solution mixture 0.3
Citric acid sodium salt 0.5 0.5 0.2 0.2
Citric acid anhydride 0.05 0.05
Phenoxyethanol 0.2 0.2 0.3 0.25
P-hydroxybenzoic acid methyl ester 0.25
Perfume 0.2 0.3
l-menthol (Standard of cosmeceutical raw materials) 0.01 0.01
Polyoxyethylene sorbitan laurate (20E.O) 0.1
Polyoxyethylene hydrogenated castor oil 40 0.2 0.2 0.5
Jojoba oil 0.15 0.15
Polyoxyethylene (20) polyoxypropylene (4) cetyl ether 0.1 0.2
PPG-6-decyltetradecanol polyether-30 0.1
d-delta-tocopherol 0.01 0.01 0.01 0.01
Grapefruit extract 0.1 0.1 0.1 0.1 0.1
Lemon extract 0.1 0.1 0.1 0.1 0.1
Kiwi fruit extract 0.1 0.1 0.1 0.1 0.1 0.1
Extract of globe artichoke 0.1 0.1 0.1 0.1 0.1
Semen Alpiniae extract 0.1 0.1 0.1 0.1 0.1
Hyaluronic acid Na 0.01 0.01 0.01 0.01. 0.05
Hydrolyzed hyaluronic acid 0.05
Acetyl sodium hyaluronate 0.1 0.05
Ceramide 2 0.01 0.001
Ceramide 3 0.001 0.001
Pure water Residual amount of Residual amount of Residual amount of Residual amount of Residual amount of Residual amount of
100 100 100 100 100 100
[ Table 9]
Name of ingredient Formulation example 17 Formulation example 18 Formulation example 19 Formulation example 20 Formulation example 21 Formulation example 22
3-O-Ethyl ascorbic acid 1 1
Ascorbic acid-2-glucoside 2 2 0.1
Ascorbic acid
Arbutin 1
L-ascorbic acid magnesium phosphate
Tranexamic acid 1
Nicotinamide 5
Hydroquinone
Allantoin 0.1
Glycyrrhizic acid dipotassium salt 0.05 0.1
Mono-2-ethylhexyl glyceryl ether 0.2 0.1 0.3 0.005 0.15 0.25
Pellicer L-30 1 0.5 0.01 0.2 0.4 0.6
Carboxyvinyl polymer 0.1 0.1 0.1 0.1 0.1 0.4
EDTA-2Na 0.05 0.05 0.05 0.05 0.05 0.05
1, 3-propanediol 2
1, 3-butanediol 5 6 7 5
Dipropylene glycol 5 5
Concentrated glycerin 4 4 6 6 5 5
Diglycerol 1 2
Anhydrous ethanol 2 2 2 5 5
Silicone solution mixture 0.1
Citric acid sodium salt 0.2 0.2 0.5
Citric acid anhydride 0.05 0.05
Phenoxyethanol 0.2 0.2
P-hydroxybenzoic acid methyl ester 0.2 0.2 02
Perfume 0.1 0.1 0.1 0.1 0.3
l-menthol (Standard of cosmeceutical raw materials) 0.05 0.05 0.05 0.01
Polyoxyethylene sorbitan laurate (20E.O) 0.1 0.2 0.1
Polyoxyethylene hydrogenated castor oil 40 0.5
Jojoba oil 0.1 0.15
Polyoxyethylene (20) polyoxypropylene (4) cetyl ether 0.3 0.2 0.1
PPG-6-decyltetradecanol polyether-30 0.2 0.2
d-delta-tocopherol 0.1 0.1 001 0.01
Grapefruit extract 0.5 0.5 0.5 0.1 0.1
Lemon extract 0.5 0.5 0.5 0.1 0.1
Kiwi fruit extract 0.1 0.1 0.1 0.1 0.1 0.1
Extract of globe artichoke 0.1 0.1 0.1 0.1 0.1 0.1
Semen Alpiniae extract 0.1 0.1 0.1 0.1 0.1 0.1
Hyaluronic acid Na 0.01 001 0.01
Hydrolyzed hyaluronic acid 0.01
Heparin-like substances 0.1 0.1 0.3
Pure water Balance of Balance of Balance of Balance of Balance of Balance of
100 100 100 100 100 100
Industrial applicability of the invention
In the present invention, a composition which can be used as a composition for external use (for example, a leave-on cosmetic) or the like can be provided.

Claims (19)

1. A composition comprising a ether synthesized from a fatty alcohol and glycerol and B an acyl glutamic acid lysine salt.
2. The composition according to claim 1, wherein the component A is mono-2-ethylhexyl glyceryl ether and the component B is dilaurylglutamic acid lysine salt.
3. The composition according to claim 1 or 2, wherein the proportion of the component a is less than 0.5 mass%.
4. The composition according to any one of claims 1 to 3, wherein the proportion of the component B is 1% by mass or less.
5. The composition according to any one of claims 1 to 4, wherein the proportion of the component B is more than 0.05 parts by mass relative to 1 part by mass of the component A.
6. The composition according to any one of claims 1 to 5, wherein the proportion of the component A is less than 0.5 mass%, and the proportion of the component B is more than 0.05 mass parts and 100 mass parts or less with respect to 1 mass part of the component A.
7. The composition of any one of claims 1 to 6, wherein the composition further comprises a C water-soluble component.
8. The composition according to claim 7, wherein the component C has a logP value of 0 or less and a molecular weight of 1000 or less.
9. The composition of claim 7 or 8, wherein component C comprises a water-soluble whitening ingredient.
10. The composition according to any one of claims 7 to 9, wherein the component C comprises at least one selected from the group consisting of ascorbic acids, thrombolic acids, epsilon-amino caproic acids, hydroquinones, nicotinamides, glycyrrhetic acids, allantoins, and riboflavin.
11. The composition according to any one of claims 7 to 10, wherein the component C comprises at least one selected from the group consisting of ascorbic acid, ascorbic acid phosphate, ascorbic acid alkyl ester, ascorbic acid-2-glucoside, tranexamic acid, epsilon-aminocaproic acid, hydroquinone, arbutin, nicotinamide, glycyrrhizic acid, allantoin, riboflavin, and salts thereof.
12. The composition according to any one of claims 7 to 11, wherein the proportion of the component C is 0.05% by mass or more.
13. The composition according to any one of claims 1 to 12, wherein the composition is used in a leave-on cosmetic.
14. A formulation for improving the solubility or dispersibility of a ether synthesized from a fatty alcohol and glycerin, which contains B-acyl glutamic acid lysine salt.
15. A preparation for improving the transdermal absorbability of water-soluble components C, which contains A ether synthesized from fatty alcohol and glycerin or B-acyl glutamic acid lysine salt.
16. A preparation for improving the percutaneous absorbability of water-soluble components C, which comprises A an ether synthesized from a fatty alcohol and glycerin and B an acyl glutamic acid lysine salt.
17. A method for improving the solubility or dispersibility of an ether synthesized from a fatty alcohol and glycerin, which coexists an ether synthesized from a fatty alcohol and glycerin with B-acyl glutamic acid lysine salt.
18. A method for improving the transdermal absorbability of a water-soluble component C by allowing the water-soluble component C to coexist with an ether a synthesized from a fatty alcohol and glycerin or a lysine salt of B-acyl glutamic acid.
19. A method for improving the percutaneous absorbability of a water-soluble component C by allowing the water-soluble component C to coexist with an ether A synthesized from a fatty alcohol and glycerin and a lysine salt of acyl glutamic acid B.
CN201980078658.5A 2018-11-29 2019-11-26 Composition comprising ethers synthesized from fatty alcohols and glycerol Pending CN113164799A (en)

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