JP2010100564A - External preparation for skin - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide an external preparation for skin comprising a soap-based emulsion with smooth use feeling while suppressing "stickiness" caused by formulating tranexamic acid. <P>SOLUTION: This external preparation for skin is a soap-based emulsion including (A) at least one kind selected from tranexamic acid and its derivatives, (B) 2-amino-2-methyl-1,3-propanediol and/or 2-amino-2-hydroxymethyl-1,3-propanediol, and (C) one or more kinds of higher fatty acids. <P>COPYRIGHT: (C)2010,JPO&INPIT

Description

  The present invention relates to an external preparation for skin containing tranexamic acid and having a smooth feeling of use without causing “stickiness”. More specifically, in a soap-based emulsion containing tranexamic acid, 2-amino-2-methyl-1,3-propanediol and / or 2-amino-2-hydroxymethyl-1,3- is used as a neutralizing agent. The present invention relates to an external preparation for skin containing propanediol.

  Tranexamic acid has an antiplasmin action and is blended in various skin cosmetics as an active ingredient for preventing rough skin and whitening. For example, Patent Document 1 discloses the antipigmenting action of tranexamic acid, and exemplifies various skin care cosmetics such as lotions, emulsions, and creams.

  In general, among skin care cosmetics, soap-based emulsions (emulsions and creams) using higher fatty acid salts as surfactants are particularly excellent in use feelings such as familiarity, moisturization, and softness of the skin after use. However, there is a problem that “stickiness” occurs when tranexamic acid is added to such a soap-based emulsion having excellent usability.

For example, Patent Document 2 describes that an alkyl-modified carboxyvinyl polymer is used in place of a commonly used surfactant in order to improve “stickiness” in an emulsion composition containing tranexamic acid. . However, in Patent Document 2, the cause of “stickiness” is defined as a conventional general-purpose surfactant (which seems to contain higher fatty acid soap), and “stickiness” is changed by replacing it with a specific polymer thickener. Suppressed. That is, in the soap-based emulsion having an excellent feeling as described above, it has not yet been achieved to suppress the “stickiness” that occurs when tranexamic acid is blended.
JP-A-1-93519 JP-A-9-263510

  Therefore, the subject in this invention is providing the skin external preparation with a smooth feeling of use which suppresses the "stickiness" which arises by mix | blending tranexamic acid with a soap-type emulsion.

  In order to solve the above-mentioned problems, the present inventors have conducted intensive research. As a result, by adding a specific neutralizing agent in the emulsion, the stickiness is not produced even when tranexamic acid is added. As a result, the present invention has been completed.

  That is, the present invention provides (A) at least one selected from tranexamic acid and derivatives thereof, (B) 2-amino-2-methyl-1,3-propanediol and / or 2-amino-2-hydroxymethyl. A topical skin preparation characterized by being a soap-based emulsion containing -1,3-propanediol and (C) one or more of higher fatty acids.

  Even if the skin external preparation of the present invention contains tranexamic acid and / or a derivative thereof, it does not cause “stickiness” due to them, and can maintain the excellent feeling of use possessed by the soap-based emulsion. The skin is smooth and fresh, and the skin feels good.

  The external preparation for skin of the present invention contains at least one (component A) selected from tranexamic acid and its derivatives. Tranexamic acid (trans-4-aminomethylcyclohexane-1-carboxylic acid) and derivatives thereof are generally used as antiplasmin agents, and are known as components having particularly high safety in skin external use applications such as cosmetics. Yes.

  Tranexamic acid and its derivatives blended in the external preparation for skin of the present invention may be those conventionally used in cosmetics and the like, and are not particularly limited. For example, tranexamic acid salts (magnesium salts, calcium salts, sodium salts, potassium salts and other metal salts, phosphate salts, hydrochloride salts, hydrobromide salts, sulfate salts, etc.), tranexamic acid esters (vitamin A acid esters, Vitamin esters such as vitamin A ester, vitamin E ester, vitamin C ester, vitamin D ester; phenyl ester; hydroquinone ester; gentisic acid ester, etc.), amides of tranexamic acid (such as methyl amide or a salt thereof); dimer of tranexamic acid Examples include the body.

  The blending amount of tranexamic acid and / or a derivative thereof in the external preparation for skin of the present invention is not particularly limited, but is usually 0.0001 to 30% by mass, preferably 0.01 to 10% by mass, particularly preferably 0.2 to 3% by weight. When the blending amount is less than 0.0001% by mass, it is difficult to sufficiently obtain the effect of whitening such as tranexamic acid or a derivative thereof, and even if the blending amount exceeds 30% by mass, further improvement of the effect cannot be obtained. .

  The external preparation for skin of the present invention is a soap-based emulsion. In the present specification, the “soap emulsion” means an emulsion using a higher fatty acid soap or a mixture of a higher fatty acid soap and a nonionic surfactant as a surfactant (emulsifier).

  Higher fatty acid soap, in a narrow sense, refers to an alkali metal salt of a higher fatty acid, but in practice, it is not necessary to add it in the form of a metal salt, and at least part of it is ionized even if it is added in the form of a higher fatty acid. Act as a surfactant. Therefore, the external preparation for skin of the present invention is a soap-based emulsion containing one or more higher fatty acids as essential components.

  Although it will not specifically limit as a higher fatty acid mix | blended with the skin external preparation of this invention, if it acts as surfactant (emulsifier), Preferably, it selects from C8-C22 higher fatty acid. Specifically, fatty acid mixtures obtained by high-pressure decomposition of animal oils such as beef tallow and animal fats, coconut oil, palm kernel oil, soybean oil, olive oil, cottonseed oil and other vegetable oils by conventional methods, and separation and purification of these Examples of the resulting higher fatty acid include lauric acid, myristic acid, palmitic acid, stearic acid, isostearic acid, behen (behenine) acid, oleic acid, isomyristic acid, and isopalmitic acid.

Although the compounding quantity of the higher fatty acid in the skin external preparation of this invention is not specifically limited, Usually, 0.01-10 mass%, Preferably you may be 0.1-5 mass%. If the blending amount is less than 0.01% by mass, sufficient emulsifying action is difficult to obtain, and if it exceeds 10% by mass , stickiness or the like may occur and the intended usability may not be obtained.

Moreover, you may mix | blend a nonionic surfactant in addition to a higher fatty acid with the skin external preparation of this invention. By blending a nonionic surfactant, the emulsion can be further stabilized.
Examples of the nonionic surfactant used in the present invention include lipophilic nonionic surfactants such as sorbitan fatty acid esters (for example, sorbitan monooleate, sorbitan monoisostearate, sorbitan monolaurate, sorbitan). Monopalmitate, sorbitan monostearate, sorbitan sesquioleate, sorbitan trioleate, diglycerol sorbitan penta-2-ethylhexylate, diglycerol sorbitan tetra-2-ethylhexylate); glycerin polyglycerin fatty acids (eg mono cottonseed oil) Fatty acid glycerin, glyceryl monoerucate, glyceryl sesquioleate, glyceryl monostearate, α, α'-oleic acid pyroglutamate glycerin, monostearate glycerin malate, etc.); B propylene glycol fatty acid esters (e.g., propylene glycol monostearate, etc.); hydrogenated castor oil derivatives; glycerol alkyl ethers, and the like.

Examples of hydrophilic nonionic surfactants include POE sorbitan fatty acid esters (for example, POE sorbitan monooleate, POE sorbitan monostearate, POE sorbitan monooleate, POE sorbitan tetraoleate, etc.); POE sorbite fatty acid ester (E.g., POE sorbite monolaurate, POE sorbite monooleate, POE sorbite pentaoleate, POE sorbite monostearate, etc.); POE glycerin fatty acid esters (e.g., POE glycerin monostearate, POE glycerin monoisostearate) POE monooleate such as POE glycerin triisostearate); POE fatty acid esters (for example, POE distearate, POE monodiolate, distearies) POE alkyl ethers (for example, POE lauryl ether, POE oleyl ether, POE stearyl ether, POE-behenyl ether, POE-2-octyldodecyl ether, POE cholestanol ether, etc.); Pluronic type (for example, POE / POP alkyl ethers (for example, POE / POP cetyl ether, POE / POP-2-decyltetradecyl ether, POE / POP monobutyl ether, POE / POP hydrogenated lanolin, POE / POP glycerin ether, etc.) ); Tetra POE / Tetra POP ethylenediamine condensates (eg, Tetronic, etc.); POE castor oil hydrogenated castor oil derivatives (eg, POE castor oil, POE hydrogenated castor oil, POE hydrogenated castor) Pear oil monoisostearate, POE hydrogenated castor oil triisostearate, POE hydrogenated castor oil monopyroglutamic acid monoisostearic acid diester, POE hydrogenated castor oil maleic acid, etc.); POE beeswax lanolin derivatives (eg POE sorbite beeswax etc.) Alkanolamides (eg coconut oil fatty acid diethanolamide, lauric acid monoethanolamide, fatty acid isopropanolamide, etc.); POE propylene glycol fatty acid ester; POE alkylamine; POE fatty acid amide; sucrose fatty acid ester; Reyl phosphoric acid and the like can be mentioned.
When a nonionic surfactant is blended, the blending amount is about 0.01 to 10% by mass.

  Furthermore, the skin external preparation of the present invention contains 2-amino-2-methyl-1,3-propanediol and / or 2-amino-2-hydroxymethyl-1,3-propanediol as a neutralizing agent. It is characterized by.

  2-Amino-2-methyl-1,3-propanediol is conventionally used as a neutralizing agent (alkali agent) for emulsions. For example, Japanese Patent Application Laid-Open No. 2002-60313 discloses a skin external preparation containing a whitening component such as a hydroquinone glycoside, a betaine derivative, a higher fatty acid, and a specific neutralizing agent. It is described that the effect is excellent, and 2-amino-2-methyl-1,3-propanediol is used as a specific neutralizing agent (Examples 4 and 9). However, there is no example in which tranexamic acid is blended as a whitening component, and therefore there is no suggestion regarding “stickiness” due to tranexamic acid. Furthermore, 2-amino-2-methyl-1,3-propanediol is only described as a kind of L-serine, D-serine, DL-serine, alanine and the like used as a neutralizing agent.

  Japanese Patent Application Laid-Open No. 2006-256971 discloses a method for producing an emulsified composition in which fine particles of an oil phase containing a solid oil component are stably dispersed in an aqueous phase using a carboxyvinyl polymer without using a surfactant. And 2-amino-2-methyl-1,3-propanediol was used as a neutralizing agent (Examples 10, 12 and 13). However, what is described in this document is an emulsion using a carboxyvinyl polymer, which does not contain a surfactant, as in Patent Document 2.

  On the other hand, 2-amino-2-hydroxymethyl-1,3-propanediol is a compound in which one hydroxyl group is added to the 2-amino-2-methyl-1,3-propanediol. It is used as a stabilizer for extender pigments in Japanese Patent Application Laid-Open No. 2001-81012. However, there is no example which uses this as a neutralizer of an emulsion.

  In the external preparation for skin of the present invention, the soap emulsion containing tranexamic acid is 2-amino-2-methyl-1,3-propanediol or 2-amino-2-hydroxymethyl-1,3 as a neutralizing agent. -By first selecting propanediol or a combination thereof, the “stickiness” produced by the incorporation of tranexamic acid has been achieved for the first time.

  The amount of 2-amino-2-methyl-1,3-propanediol and / or 2-amino-2-hydroxymethyl-1,3-propanediol in the skin external preparation of the present invention is not particularly limited, Although it may vary depending on the type and blending amount of the fatty acid, it is usually 0.01 to 10% by mass, preferably 0.01 to 5% by mass. Most preferably, it is 0.01-2 mass%. When the blending amount is less than 0.01% by mass, it is difficult to obtain a sufficient neutralizing action.

  The external preparation for skin of the present invention is a soap-based emulsion, preferably an oil-in-water (O / W) emulsion, and specifically provided in the form of an emulsion, cream or the like. Moreover, since tranexamic acid and / or its derivatives are contained as essential components, it is particularly suitable for cosmetics for rough skin and whitening.

The skin external preparation composition of the present invention may contain, in addition to the above-described essential components, other components generally used in skin care cosmetics such as emulsions and creams.
Examples of other ingredients include, but are not limited to, moisturizers, alcohols, softeners (emollients), buffers, fragrances, preservatives, colorants, sequestering agents, UV absorbers, stabilizers, and antioxidants. Agents, thickeners, various medicinal ingredients, and the like.

  Hereinafter, the present invention will be described in more detail with specific examples, but these examples do not limit the technical scope of the present invention. In addition, all the compounding quantities in a following example, a comparative example, and a prescription example are the mass%.

(Examples and Comparative Examples)
An emulsion having the composition listed in Table 1 below was prepared. Using these emulsions, an actual use test was conducted by five specialist panels. The sensory evaluation of usability was ranked based on the following evaluation criteria. The results are shown in Table 1. Moreover, the viscosity and pH of each emulsion at 30 ° C. and the average emulsified particle diameter of dispersed oil droplets were measured, and these values are also shown in Table 1.

Evaluation criteria:
<Evaluation of stickiness>
○: 4 or more panelists who responded that there was no stickiness △: 2 to 3 panelists who responded that there was no stickiness ×: 1 panel or less who responded that there was no stickiness <Evaluation of moistness>
○: 4 or more panelists who responded moistly △: 2 to 3 panelists who responded moistly ×: 1 or less panelists who responded moist

(Prescription Example 1)
cream:
Compounding ingredients Compounding amount (% by mass)
Purified water Residual glycerin 10
Butylene glycol 4
Dipropylene glycol 4
Stearic acid 0.4
Behenic acid 0.4
Isostearic acid 0.4
Self-emulsifying glyceryl monostearate 1
Polyoxyethylene glyceryl monostearate 1
Behenyl alcohol 3
Aminomethylpropanediol 0.15
Hardened oil 2
Squalane 6
Vaseline 3
Glyceryl tri-2-ethylhexanoate 4
Methyl polysiloxane 1
Tranexamic acid 2
Paraben appropriate amount perfume appropriate amount

Production method:
After dissolving the oil-soluble component in the oil, it was heated to 70 ° C. to obtain an oil phase. On the other hand, the water-soluble component was dissolved in purified water and heated to 70 ° C. to obtain an aqueous phase. The oil phase was added to the aqueous phase, stirred and mixed, and then cooled to room temperature to obtain a complaint.

(Prescription example 2)
Latex:
Compounding ingredients Compounding amount (% by mass)
Purified water Residual ethyl alcohol 3
Glycerin 5
Butylene glycol 5
Dipropylene glycol 5
Stearic acid 0.3
Behenic acid 0.3
Isostearic acid 0.3
Self-emulsifying glyceryl monostearate 1
Polyoxyethylene siglycerin monostearate 1
Behenyl alcohol 1
Carboxyvinyl polymer 0.15
Aminomethylpropanediol 0.15
Hardened oil 1
Squalane 4
Glyceryl tri-2-ethylhexanoate 3
Methyl polysiloxane 2
Tranexamic acid 2
Dipotassium glycyrrhizinate 0.05
Phenoxyethanol appropriate amount perfume appropriate amount

Production method:
After dissolving the oil-soluble component in the oil, it was heated to 70 ° C. to obtain an oil phase. On the other hand, the water-soluble component was dissolved in purified water and heated to 70 ° C. to obtain an aqueous phase. The oil phase was added to the aqueous phase, stirred and mixed, and then cooled to room temperature to obtain an emulsion.

(Prescription Example 3)
Latex:
Compounding ingredients Compounding amount (% by mass)
Purified water Residual ethyl alcohol 5
Glycerin 5
Butylene glycol 5
Stearic acid 0.5
Palmitic acid 0.5
Self-emulsifying glyceryl monostearate 1
Oleic acid (triethylene glycol / propylene glycol) 1
Cetanol 1
Carboxyvinyl polymer 0.1
Aminomethylpropanediol 0.2
Squalane 4
Methyl polysiloxane 2
Hardened oil 3
Tranexamic acid 2
Paraben appropriate amount perfume appropriate amount

Production method:
After dissolving the oil-soluble component in the oil, it was heated to 70 ° C. to obtain an oil phase. On the other hand, the water-soluble component was dissolved in purified water and heated to 70 ° C. to obtain an aqueous phase. The oil phase was added to the aqueous phase, stirred and mixed, and then cooled to room temperature to obtain an emulsion.

Claims (5)

(A) at least one selected from tranexamic acid and its derivatives,
(B) 2-amino-2-methyl-1,3-propanediol and / or 2-amino-2-hydroxymethyl-1,3-propanediol, and (C) one or more of higher fatty acids. A skin external preparation characterized by being a soap-based emulsion. (A) The amount of tranexamic acid or its derivative is 0.0001 to 30% by mass,
(B) The blending amount of 2-amino-2-methyl-1,3-propanediol and / or 2-amino-2-hydroxymethyl-1,3-propanediol is 0.01 to 10% by mass,
(C) The external preparation for skin according to claim 1, wherein the amount of the higher fatty acid is 0.01 to 10% by mass. The external preparation for skin according to claim 1 or 2, wherein the higher fatty acid (C) is selected from higher fatty acids having 8 to 22 carbon atoms. Fatty acid mixture obtained by high-pressure decomposition of vegetable oils such as animal fats and oils including beef tallow, sheep fat, coconut oil, palm kernel oil, soybean oil, olive oil, cottonseed oil, etc. by a conventional method, wherein the higher fatty acid having 8 to 22 carbon atoms is, The skin external application according to claim 3, characterized in that it is selected from lauric acid, myristic acid, palmitic acid, stearic acid, isostearic acid, behen (behenine) acid, oleic acid, isomyristic acid, isopalmitic acid and the like. Agent. The skin external preparation according to any one of claims 1 to 4, further comprising a nonionic surfactant.