Cosmetic

Abstract

To provide a cosmetic excellent in storage stability.SOLUTION: The cosmetic comprises (A) tranexamic acid, a tranexamic acid derivative or a salt thereof, (B) a compound having a carbonyl group, (C) a cyclic carboxamide derivative having a specific structure or a salt thereof, glycylglycine, a glycylglycine derivative or a salt thereof, and (E) water.SELECTED DRAWING: None

Description

[Technical Field]

[0001] The present invention relates to a cosmetic preparation comprising tranexamic acid, a tranexamic acid derivative, or a salt thereof. [Background technology]

[0002] Tranexamic acid (or its derivatives) is used in cosmetics because of its skin-whitening and roughness-reducing properties. Sugars are also commonly used in cosmetics for moisturizing and skin conditioning purposes. However, it is known that the combined use of tranexamic acid and sugars can cause discoloration due to heat or over time.

[0003] As a means for suppressing the above-mentioned discoloration, it is known to use sodium pyrosulfite or another inorganic salt in combination, but sodium pyrosulfite can produce an unpleasant odor, and there is a limit to the amount that can be added, particularly in the case of fragrance-free products. As another means for suppressing discoloration, the combined use of a compound having a specific amide structure has also been proposed (for example, Patent Document 1). [Prior art documents] [Patent documents]

[0004] [Patent Document 1] Japanese Patent Application Laid-Open No. 2016-27037 Summary of the Invention

[0005] The inventors have found that the combined use of tranexamic acid with not only sugars but also other compounds having or forming a carbonyl group often results in browning and unpleasant odors. Surprisingly, they have found that combining these with a specific cyclic carboxamide derivative can suppress discoloration due to heat or aging and the generation of unpleasant odors. The present invention is based on these findings.

[0006] According to the present invention, the following inventions are provided. [1] (A) tranexamic acid, a tranexamic acid derivative, or a salt thereof, (B) a compound having a carbonyl group, (C) A cyclic carboxamide derivative represented by formula (1) or a salt thereof [ka] (In the formula, R 1 represents a hydrocarbon group having 1 to 6 carbon atoms which may be substituted with a hydroxyl group, or a hydrogen atom, X is -CH2- or -N(R 2 )-, where R 2 represents a hydrocarbon group having 1 to 6 carbon atoms which may be substituted with a hydroxyl group, or a hydrogen atom, and n is an integer from 1 to 3; (D) glycylglycine, a glycylglycine derivative, or a salt thereof, and (E)Water A cosmetic comprising: The blending amount of component (A) is 0.5 to 3.5% by mass relative to the total amount of the cosmetic, The blending amount of component (B) is 0.01 to 3 mass% relative to the total amount of the cosmetic, The blending amount of component (C) is 0.8 to 2 mass% relative to the total amount of the cosmetic, The blending amount of component (D) is 0.1 to 2.5% by mass relative to the total amount of the cosmetic, The blending amount of component (E) is 40 to 99 mass% relative to the total amount of the cosmetic, A cosmetic preparation in which the mass ratio of component (C) to component (D) is 1:0.03 to 1:3. [2] In the formula (1) of component (C), R 1 is a hydroxyalkyl group having 1 to 3 carbon atoms, X is -CH2- or -NH-, and The cosmetic according to [1], wherein n is 1. [3] The cosmetic preparation according to [1] or [2], wherein the component (C) is 1-(2-hydroxyethyl)-2-imidazolidinone. [4] The cosmetic preparation according to any one of [1] to [3], wherein the component (B) is a sugar. [5] The cosmetic preparation according to any one of [1] to [4], wherein the component (B) is selected from the group consisting of monosaccharides, oligosaccharides, polysaccharides, glycosides, and sugar alcohols.

[0007] According to the present invention, it is possible to provide a cosmetic preparation having excellent storage stability. In particular, the present invention can suppress discoloration and the generation of unpleasant odors caused by the reaction between tranexamic acid or its derivatives and a compound having a carbonyl group or a compound capable of forming a carbonyl group over time or under heating conditions.

[0008] The present invention relates to a cosmetic comprising (A) tranexamic acid, a tranexamic acid derivative, or a salt thereof, (B) a compound having a carbonyl group or a compound capable of forming a carbonyl group, and (C) a cyclic carboxamide derivative having a specific structure or a salt thereof.

[0009] (A) tranexamic acid, a tranexamic acid derivative, or a salt thereof, The cosmetic according to the present invention comprises (A) tranexamic acid, a tranexamic acid derivative, or a salt thereof (hereinafter, sometimes referred to as component (A); the same applies to other components). Examples of component (A) include tranexamic acid (trans-4-aminomethylcyclohexane-1-carboxylic acid), tranexamic acid esters (e.g., vitamin esters such as vitamin A ester, vitamin E ester, vitamin C ester, and vitamin D ester, phenyl esters, hydroquinone esters, and gentisic acid esters), tranexamic acid amide (e.g., methylamide or a salt thereof), and tranexamic acid dimer, with tranexamic acid being preferred. Examples of their salts include metal salts such as magnesium salt, calcium salt, sodium salt, and potassium salt; and inorganic salts such as phosphate, hydrochloride, hydrobromide, and sulfate.

[0010] One or more types of component (A) can be blended in. The blend amount of component (A) is preferably 0.1 to 5 mass %, more preferably 0.5 to 3.5 mass %, relative to the total amount of the cosmetic.

[0011] (B) A compound having a carbonyl group or a compound having the ability to form a carbonyl group The cosmetic according to the present invention comprises (B) a compound having a carbonyl group or a compound capable of forming a carbonyl group. It is generally known that browning occurs when the amino groups of amino acids, proteins, and amines react with the carbonyl groups of reducing sugars, etc. This reaction, also known as the Maillard reaction, is said to produce brown pigments and odorous substances. Component (B) is a component that can react with component (A) having an amino group to cause a Maillard reaction. Examples of component (B) include sugars and polyalkylene glycol derivatives, and sugars are particularly preferred because they can more effectively exhibit the effects of the present invention.

[0012] The sugars are not particularly limited, but examples thereof include monosaccharides, oligosaccharides, polysaccharides, glycosides, and sugar alcohols. In the present invention, oligosaccharides refer to those obtained by dehydration condensation of 2 to 10 monosaccharide molecules, and polysaccharides refer to those obtained by dehydration condensation of 11 or more monosaccharide molecules.

[0013] Examples of monosaccharides include tetroses such as D-erythrulose, D-erythrose, and D-threose; aldopentoses such as D-arabinose, L-arabinose, D-xylose, D-lyxose, L-lyxose, and D-ribose; ketopentoses such as D-xylulose, L-xylulose, D-ribulose, and L-ribulose; aldohexoses such as D-galactose, L-galactose, D-glucose, D-talose, and D-mannose; ketohexoses such as L-sorbose, D-tagatose, D-psicose, and D-fructose; branched sugars such as D-apiose and D-hamamelose; pentoses such as ribose, arabinose, and xylose; hexoses such as glucose, galactose, and fructose; amino sugars such as glucosamine and galactosamine, and derivatives of these monosaccharides.

[0014] Oligosaccharides include homooligosaccharides containing only one of the above-mentioned monosaccharides, and heterooligosaccharides containing two or more of them. Examples of homooligosaccharides include xylooligosaccharides such as xylobiose, xylotriose, xylotetraose, and xylopentaose; galactooligosaccharides such as agarobiose and carabiose; glucooligosaccharides such as maltose, maltotriose, maltotetraose, maltopentaose, isomaltose, sophorose, cellobiose, cellotriose, cellotetraose, cellopentaose, trehalose, neotrehalose, and isotrehalose; mannooligosaccharides; and fructooligosaccharides such as inulobiose, inulotriose, inulotetraose, and inulopentaose. Examples of heterooligosaccharides include vicianose, isoprimeverose, sambubiose, primeverose, lycotetraose, solabioose, melibiose, manninotriose, lactose, licobiose, lycotriose, epicellobiose, sucrose, turanose, maltulose, isokestose, erlose, kestose, gentianose, lactulose, epigentibiose, isolichnose, umbelliferose, sesamos, raffinose, lychnose, lobinobiose, silanobiose, rutinose, chacotriose, solatriose, and α-glucan oligosaccharides (glucose oligomers with a degree of polymerization of 2 to 10). Among oligosaccharides, disaccharides are preferred.

[0015] Examples of polysaccharides include xanthan gum, cellulose, guar gum, starch, pullulan, dextran, fructan, mannan, agar, carrageenan, chitin, chitosan, pectin, alginic acid, starch, glycogen, hyaluronic acid, etc. Polysaccharides also include derivatives of these sugars substituted with methyl groups, ethyl groups, hydroxyethyl groups, hydroxypropyl groups, acetyl groups, stearoxy groups, glycerol, propylene glycol, etc. These substituents can be used alone or in combination. Specific examples of polysaccharides having a substituent include hydroxyethyl cellulose, hydroxyethyl ethyl cellulose, hydroxyethyl guar gum, hydroxyethyl starch, methyl cellulose, methyl guar gum, methyl starch, ethyl cellulose, ethyl guar gum, ethyl starch, hydroxypropyl cellulose, hydroxypropyl guar gum, hydroxypropyl starch, hydroxyethyl methyl cellulose, hydroxyethyl methyl guar gum, hydroxyethyl methyl starch, hydroxypropyl methyl cellulose, hydroxypropyl methyl guar gum, hydroxypropyl methyl starch, stearoxyhydroxypropyl methyl cellulose, acetylated hyaluronic acid, propylene glycol alginate, and propylene glycol hyaluronate.

[0016] Examples of glycosides include arbutin, ascorbic acid glucoside, glucosylceramide, anthocyanin, rutin, hesperidin, and daidzin. Examples of sugar alcohols include xylitol, trehalose, maltitol, mannitol, sorbitol, erythritol, arabitol, ribitol, galactitol, glucitol, and erythritol.

[0017] Although polyalkylene glycol derivatives and the like can also be used as component (B), it is preferable to use sugars. In order to further exert the effects of the present invention, the sugars are preferably selected from the group consisting of monosaccharides, oligosaccharides, and glycosides, more preferably monosaccharides or disaccharides, and even more preferably fructose, glucose, mannose, or maltose.

[0018] One or more types of component (B) can be blended in. The blend amount of component (B) is preferably 0.001 to 5 mass %, more preferably 0.01 to 3 mass %, relative to the total amount of the cosmetic.

[0019] (C) Cyclic carboxamide derivative or salt thereof The cosmetic according to the present invention comprises a cyclic carboxamide derivative represented by formula (1) or a salt thereof. [ka] During the ceremony, R 1 represents a hydrocarbon group having 1 to 6 carbon atoms which may be substituted with a hydroxyl group, or a hydrogen atom, X is -CH2- or -N(R 2 )-, where R 2 represents a hydrocarbon group having 1 to 6 carbon atoms which may be substituted with a hydroxyl group, or a hydrogen atom, and n is an integer of 1 to 3. The hydrocarbon group is not particularly limited and may be, for example, an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, a cycloalkylalkyl group, a haloalkyl group, an alkoxyalkyl group, or an alkoxycarbonylalkyl group, and is preferably an alkyl group.

[0020] In a preferred embodiment, in the formula (1) of the component (C), R 1 is a hydroxyalkyl group having 1 to 3 carbon atoms, X is -CH2- or -NH-, and n is 1. Specific examples of the cyclic carboxamide derivative represented by formula (1) include the following. [ka] Component (C) is most preferably 1-(2-hydroxyethyl)-2-imidazolidinone.

[0021] Component (C) may be a salt of the cyclic carboxamide derivative represented by formula (1). The type of salt is not particularly limited as long as it is pharmacologically acceptable, and may be an inorganic salt or an organic salt. Examples of inorganic salts include hydrochloride, sulfate, phosphate, hydrobromide, sodium salt, potassium salt, magnesium salt, calcium salt, magnesium salt, and ammonium salt. Examples of organic salts include acetate, lactate, maleate, fumarate, tartrate, methanesulfonate, p-toluenesulfonate, triethanolamine salt, and amino acid salt.

[0022] One or more types of component (C) can be blended in. The blend amount of component (C) is preferably 0.05 to 2.5 mass%, more preferably 0.8 to 2 mass%, and even more preferably 1.2 to 1.8 mass%, relative to the total amount of the cosmetic.

[0023] As described above, the combination of components (A) and (B) can cause discoloration and unpleasant odors. The present inventors have surprisingly found that the discoloration and unpleasant odors can be suppressed by further combining component (C) with the combination of components (A) and (B).

[0024] (D) Glycylglycine, a glycylglycine derivative, or a salt thereof The cosmetic composition according to the present invention may further comprise (D) glycylglycine, a glycylglycine derivative, or a salt thereof. The effects of the present invention can be more pronounced by further combining component (D) in addition to component (C) to suppress discoloration and unpleasant odor generation with components (A) and (B).

[0025] Glycylglycine and glycylglycine derivatives are preferably represented by formula (2). [ka] During the ceremony, R 2 are each independently hydrogen or methyl, and m is 1 or 2. Examples of compounds represented by formula (2) include the following: [ka] Component (D) is most preferably glycylglycine.

[0026] Component (D) may be a salt of glycylglycine or a glycylglycine derivative. The type of salt is not particularly limited as long as it is pharmacologically acceptable, and examples include hydrochloride, sulfate, phosphate, hydrobromide, sodium salt, potassium salt, magnesium salt, calcium salt, magnesium salt, and ammonium salt. Examples of organic salts include acetate, lactate, maleate, fumarate, tartrate, methanesulfonate, p-toluenesulfonate, triethanolamine salt, and amino acid salt.

[0027] The component (D) can be blended in one or more types. The component (D) may produce an unpleasant odor when combined with the component (B) at a high blend rate, so consideration is needed, particularly when using it in fragrance-free cosmetics. The blending amount of the component (D) is preferably 0.05 to 5 mass%, more preferably 0.1 to 2.5 mass%, and even more preferably 0.5 to 1.5 mass%, based on the total amount of the cosmetic. By keeping the blending amount within this range, discoloration can be suppressed while the odor originating from the component (D) can be suppressed. The mass ratio of the component (C) to the component (D) is preferably 1:0.03 to 1:3, more preferably 1:0.1 to 1:2.5, and even more preferably 1:0.3 to 1:0.8.

[0028] The cosmetic preparation according to the present invention may contain a pH adjuster, such as a buffer such as lactic acid-sodium lactate, citric acid-sodium citrate, or succinic acid-sodium succinate.

[0029] The cosmetic preparation according to the present invention may contain water. As the water, water used in cosmetics, quasi-drugs, etc., such as purified water, ion-exchanged water, tap water, etc., can be used. The amount of water to be blended is preferably 40 to 99% by mass relative to the total amount of the cosmetic according to the present invention. In another embodiment of the present invention, the cosmetic does not contain water.

[0030] In addition to the above-mentioned components, the cosmetic composition according to the present invention may contain, as needed, ingredients commonly used in cosmetics, such as oily components, ultraviolet absorbers, surfactants, moisturizers, thickeners, polyhydric alcohols, powder components, antioxidants, preservatives, etc.

[0031] Other ingredients that can be added include caffeine, tannin, verapamil and its derivatives, licorice extract, glabridin, hot water extract of fire thorn fruit, various herbal medicines, tocopherol acetate, glycyrrhizic acid and its derivatives or salts thereof; other whitening agents such as alkoxysalicylic acid or its salts, such as 4-methoxysalicylic acid potassium salt, vitamin C, magnesium ascorbyl phosphate, and ascorbic acid glucoside; and chelating agents.

[0032] The formulation of the cosmetic according to the present invention is not particularly limited, and examples thereof include a solution system, a solubilized system, an emulsion system, a powder dispersion system, a two-layer water-oil system, and a three-layer water-oil-powder system. Examples of the cosmetic according to the present invention include skin care cosmetics (e.g., lotion, emulsion, cream, serum, pack, etc.), makeup cosmetics (e.g., foundation, makeup base, etc.), skin cleansers (e.g., face wash, makeup remover, etc.), sunscreen cosmetics, ointments, etc.

[0033] The cosmetic of the present invention can be produced by a conventional method. When the cosmetic of the present invention is an emulsion cosmetic, the emulsification method is not particularly limited. [Example]

[0034] The present invention will be described in detail based on the following examples, but the present invention is not limited to these examples. Unless otherwise specified, the contents are expressed in mass % relative to the total amount.

[0035] [Examples 101 to 109 and Comparative Examples 101 to 103] Cosmetics according to Examples 101 to 109 and Comparative Examples 101 to 103 were prepared according to the formulations shown in Table 1. [Table 1]

[0036] [Examples 201 to 203 and Comparative Examples 201 to 203] Cosmetics according to Examples 201 to 203 and Comparative Examples 201 to 203 were prepared according to the formulations shown in Table 2. [Table 2]

[0037] [Color difference evaluation] The cosmetics of the Examples and Comparative Examples were placed in 50 ml sample tubes and kept warm in a thermostatic bath at 70°C for 3 days. After keeping the samples warm, the L, a, and b values ​​of the samples were measured using a color difference meter (Spectrophotometer CM-2002, Konica Minolta, Inc.), and the color difference ΔE from the measured value when ion-exchanged water was used was calculated from the colorimetric values. The results obtained are shown in Tables 1 and 2.

[0038] [Smell evaluation] The samples after the above-mentioned incubation were subjected to sensory evaluation by a panel of experts and judged according to the following criteria. The results are shown in Tables 1 and 2. A: There was almost no unpleasant odor. B: An unpleasant odor was detected. C: A strong unpleasant odor was felt. D: An unpleasant odor was felt very strongly.

[0039] [Example 301 and Comparative Example 301] Cosmetics of Example 301 and Comparative Example 301 were prepared with the formulations shown in Table 3, and the color difference and odor were evaluated in the same manner as above. The results obtained are shown in Table 3. [Table 3]

Claims

1. (A) tranexamic acid, a tranexamic acid derivative, or a salt thereof, (B) a compound having a carbonyl group, (C) A cyclic carboxamide derivative represented by formula (1) or a salt thereof 【Chemistry 1】 (In the formula, R １ represents a hydrocarbon group having 1 to 6 carbon atoms which may be substituted with a hydroxyl group, or a hydrogen atom, X is -CH ２ - or -N(R ２ )—, where R ２ represents a hydrocarbon group having 1 to 6 carbon atoms which may be substituted with a hydroxyl group, or a hydrogen atom, and n is an integer from 1 to 3), (D) glycylglycine, a glycylglycine derivative, or a salt thereof, and (E) Water A cosmetic comprising: The blending amount of component (A) is 0.5 to 3.5% by mass relative to the total amount of the cosmetic, The blending amount of component (B) is 0.01 to 3 mass% relative to the total amount of the cosmetic, The blending amount of component (C) is 0.8 to 2 mass% relative to the total amount of the cosmetic, The blending amount of component (D) is 0.1 to 2.5% by mass relative to the total amount of the cosmetic, The blending amount of component (E) is 40 to 99% by mass relative to the total amount of the cosmetic, A cosmetic preparation in which the mass ratio of component (C) to component (D) is 1:0.03 to 1:

3.

2. In the formula (1) of the component (C), R １ is a hydroxyalkyl group having 1 to 3 carbon atoms, X is -CH ２ - or -NH-, and The cosmetic according to claim 1, wherein n is 1.

3. 3. The cosmetic according to claim 1, wherein component (C) is 1-(2-hydroxyethyl)-2-imidazolidinone.

4. 3. The cosmetic preparation according to claim 1, wherein the component (B) is a sugar.

5. 3. The cosmetic preparation according to claim 1, wherein the component (B) is selected from the group consisting of monosaccharides, oligosaccharides, polysaccharides, glycosides, and sugar alcohols.

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