Cosmetic

Abstract

A cosmetic comprising: (A) a compound having an amino group; (B) a sugar; (C) is selected from the group consisting of an alkyl group having 1 to 3 carbon atoms (in general formula (1), R1, R3, R4 and R6 are each independently an alkyl group having 1 to 3 carbon atoms, and R2 and R5 are each independently a hydrogen atom or an alkyl group having 1 to 3 carbon atoms). ) one or more of the compounds represented by the formula (1) and pharmacologically acceptable salts thereof; and (D) water. # imgabs0 #

Description

Technical Field

[0001] The present invention relates to cosmetics. Background Art

[0002] Since tranexamic acid and its derivatives have the effects of improving rough skin, whitening effects, etc., they are ingredients mixed in cosmetics, perfumes, etc. In addition, since saccharides not only have moisturizing effects, skin conditioning effects, etc., but also show an appeal to customers, they are ingredients mixed in cosmetics, perfumes, etc.

[0003] However, when a compound having an amino group typified by tranexamic acid is used in combination with a sugar, discoloration sometimes occurs due to heat or over time.

[0004] Therefore, in the prior art, various means for suppressing the above discoloration have been proposed.

[0005] For example, in Patent Document 1, an external preparation containing tranexamic acid, a saccharide, and an acylamino compound is proposed, and in Patent Document 2, a cosmetic containing tranexamic acid, a saccharide, and an acetophenone derivative is proposed, and it is explained that coloring caused by heat or over time is suppressed by a specified mixing.

[0006] In addition, as a skin external preparation having excellent whitening effects, pyrimidinylpyrazole compounds are known. For example, in Patent Document 3, it is described that pyrimidinylpyrazole compounds have excellent effects of suppressing melanogenesis in skin pigment cells and are useful as whitening agents.

[0007] Prior Art Documents

[0008] Patent Documents

[0009] Patent Document 1: International Publication No. 2016 / 002787

[0010] Patent Document 2: Japanese Unexamined Patent Application Publication No. 2022-158539

[0011] Patent Document 3: Japanese Patent No. 4586108 Summary of the Invention

[0012] Problems to be Solved by the Invention

[0013] The techniques proposed in Patent Documents 1 and 2 have a certain effect on suppressing discoloration caused by heat or over time when tranexamic acid and a sugar are used in combination.

[0014] Based on the above situation, an object of the present invention is to provide a cosmetic that contains a compound having an amino group and a sugar, but discoloration caused by heat or over time is suppressed, and further value as a cosmetic is imparted by an ingredient mixed for the purpose of suppressing discoloration.

[0015] Means for Solving the Problem

[0016] The present invention is as follows.

[0017] <<Solution 1>> A cosmetic, comprising:

[0018] (A) A compound having an amino group;

[0019] (B) A sugar;

[0020] (C) One or more selected from the compounds represented by the following general formula (1) and their pharmacologically acceptable salts,

[0021]

[0022] (In general formula (1), R1, R3, R4 and R6 are each independently an alkyl group having 1 to 3 carbon atoms, and R2 and R5 are each independently a hydrogen atom or an alkyl group having 1 to 3 carbon atoms.); and

[0023] (D) Water.

[0024] <<Solution 2>> The cosmetic according to Solution 1, wherein the component (A) is one or more selected from amino acids, amino acid derivatives, aromatic amines, dipeptides and proteins.

[0025] <<Solution 3>>

[0026] The cosmetic according to Solution 2, wherein the component (A) is one or more selected from tranexamic acid, glycylglycine and L-theanine.

[0027] <<Solution 4>> The cosmetic according to Solution 1, wherein the component (B) comprises one or more selected from maltitol, sorbitol, fructose, erythritol, trehalose, xylitol, tremella polysaccharide, hyaluronic acid and hyaluronate.

[0028] <<Solution 5>> The cosmetic according to Solution 1, wherein the component (C) is selected from

[0029] a compound in which R1, R3, R4 and R6 in the above general formula (1) are methyl groups and R2 and R5 are hydrogen atoms, a compound in which R1, R2, R3, R4 and R6 in the above general formula (1) are methyl groups and R5 is a hydrogen atom, and

[0030] a compound in which R1, R3, R4 and R6 in the above general formula (1) are methyl groups and R2 and R5 are ethyl groups

[0031] one or more.

[0032] <<Solution 6>> The cosmetic according to Solution 2, wherein the component (C) is selected from

[0033] Compounds in which R1, R3, R4 and R6 in the above general formula (1) are methyl and R2 and R5 are hydrogen atoms, compounds in which R1, R2, R3, R4 and R6 in the above general formula (1) are methyl and R5 is a hydrogen atom, and

[0034] Compounds in which R1, R3, R4 and R6 in the above general formula (1) are methyl and R2 and R5 are ethyl

[0035] One or more of them.

[0036] "Solution 7" The cosmetic according to Solution 3, wherein the above component (C) is selected from

[0037] Compounds in which R1, R3, R4 and R6 in the above general formula (1) are methyl and R2 and R5 are hydrogen atoms, compounds in which R1, R2, R3, R4 and R6 in the above general formula (1) are methyl and R5 is a hydrogen atom, and

[0038] Compounds in which R1, R3, R4 and R6 in the above general formula (1) are methyl and R2 and R5 are ethyl

[0039] One or more of them.

[0040] "Solution 8" The cosmetic according to any one of Solutions 1 to 7, wherein the blending amount of the above component (A) is 1.0 part by mass or more and 95 parts by mass or less with respect to the total 100 parts by mass of the above components (A) to (C).

[0041] "Solution 9" The cosmetic according to any one of Solutions 1 to 7, wherein the blending amount of the above component (B) is 1.0 part by mass or more and 90 parts by mass or less with respect to the total 100 parts by mass of the above components (A) to (C).

[0042] "Solution 10" The cosmetic according to any one of Solutions 1 to 7, wherein the blending amount of the above component (C) is 3.0 part by mass or more and 40 parts by mass or less with respect to the total 100 parts by mass of the above components (A) to (C).

[0043] "Solution 11" The cosmetic according to any one of Solutions 1 to 7, which is a skin cosmetic.

[0044] Effects of the Invention

[0045] According to the present invention, there is provided a cosmetic which, although containing a compound having an amino group and a sugar, is suppressed in discoloration caused by heat or over time, and has further value as a cosmetic by a component blended for the purpose of suppressing discoloration. Detailed Description of the Invention

[0046] "Cosmetics"

[0047] The cosmetics of the present invention contain:

[0048] (A) A compound having an amino group (amino compound);

[0049] (B) Sugar;

[0050] (C) One or more selected from the compounds represented by the above general formula (1) and their pharmacologically acceptable salts (hereinafter, sometimes collectively referred to as "pyrimidinylpyrazole compounds"); and

[0051] (D) Water.

[0052] The inventors have found that the discoloration caused by the combination of a compound having an amino group and sugar is suppressed by the mixing of pyrimidinylpyrazole compounds. It is speculated that this is because pyrimidinylpyrazole compounds have a structure containing a large number of nitrogen-carbon double bonds and thus act as antioxidants.

[0053] The present invention is proposed based on the above-mentioned understanding. It should be noted that the present invention is not bound by a specific theory.

[0054] Hereinafter, the elements constituting the cosmetics of the present invention will be described in turn.

[0055] "(A) Amino Compound"

[0056] The component (A) in the cosmetics of the present invention is an amino compound.

[0057] As the (A) amino compound, for example, in addition to amino acids, amino acid derivatives, aromatic amines, dipeptides, proteins, etc., other compounds not included in these concepts can also be cited.

[0058] Amino acids can be, for example, ectoine, glycine, cysteine, theanine, serine, hydroxyproline, aspartic acid, tranexamic acid, etc.;

[0059] Amino acid derivatives can be, for example, monosodium glutamate, cysteine hydrochloride, sodium stearoyl glutamate, potassium cocoyl glutamate, arginine cocoate, etc.;

[0060] Aromatic amines can be, for example, 4,4'-diaminodiphenylamine sulfate, etc.;

[0061] Dipeptides can be, for example, glycylglycine, aspartylarginine, etc.;

[0062] Proteins can be, for example, sericin, etc.;

[0063] Other compounds may be, for example, allantoin, sodium stearoyl methyl taurate, amino-terminated polydimethylsiloxane, betaine, etc.

[0064] As the (A) amino compound in the present invention, in particular, one or more selected from tranexamic acid, glycylglycine, and L-theanine can be cited.

[0065] 《(B) Sugar》

[0066] The component (B) in the cosmetic of the present invention is sugar. As the (B) sugar, monosaccharides, polysaccharides (including polysaccharide bodies), sugar alcohols, etc. can be cited, and it can also be a mixture containing two or more of them.

[0067] As monosaccharides, for example, erythrulose, erythrose, threose, arabinose, xylose, lyxose, ribose, xylulose, ribulose, galactose, glucose, talose, mannose, sorbose, tagatose, psicose, fructose, apiose, hamamelose, etc. can be cited.

[0068] As polysaccharides (including polysaccharide bodies), for example, xylobiose, agarobiose, carabios, maltose, isomaltose, sophorose, cellobiose, trehalose, neotrehalose, isotrehalose, inulobiose, vicianose, isoprimverose, sambubiose, primverose, solabiose, melibiose, lycovbiose, epicerobiose, sucrose, turanose, lactulose, epigenchibiose, robinobiose, silanobiose, rutinose, glucosyltrehalose, cellotriose, mannotriose, gentiobiose, isomaltotriose, isopanose, maltotriose, mannotriose, turanotriose, panose, plantotriose, raffinose, solatriose, umbelliferose, maltosyltrehalose, maltotetraose, stachyose, maltotriosyltrehalose, maltopentaose, verbascose, maltohexaose, etc. can be cited. In addition, the polysaccharides (including polysaccharide bodies) in this specification also include polysaccharide bodies, tremella polysaccharide, etc. derived from one or more selected from starch, plants, seaweeds, and lactic acid bacteria.

[0069] Sugar alcohol is a substance in which the carbonyl group of the above-mentioned monosaccharides and polysaccharides (including polysaccharide bodies), aldose or ketose, is reduced. The sugar alcohol can be a D-form or an L-form, or a mixture of them. The sugar alcohol can be used alone or in appropriate combination of two or more.

[0070] As sugar alcohols, for example, erythritol, xylitol, ribitol, arabinitol, galactitol, sorbitol, inositol, mannitol, paratinit, maltitol, lactitol, isomalt, maltotriitol, maltotetraitol, maltopentaitol, maltohexaitol, etc. can be cited.

[0071] Examples of the mixture include quince seed extract, isomerized sugar, etc. In addition, a mixture of one or more of these mixtures with the above-mentioned monosaccharides, polysaccharides (including polysaccharide bodies), and sugar alcohols can also be used.

[0072] As the sugar (B) in the present invention, in particular, one or more sugars selected from maltitol, sorbitol, fructose, erythritol, trehalose, xylitol, tremella polysaccharide, hyaluronic acid, and hyaluronate can be mentioned.

[0073] "(C) Pyrimidylpyrazole Compounds"

[0074] The component (C) in the cosmetic of the present invention is one or more selected from the compounds represented by the following general formula (1) and their pharmacologically acceptable salts.

[0075]

[0076] (In the general formula (1), R1, R3, R4, and R6 are each independently an alkyl group having 1 to 3 carbon atoms, and R2 and R5 are each independently a hydrogen atom or an alkyl group having 1 to 3 carbon atoms.)

[0077] By mixing the (C) pyrimidylpyrazole compounds in the cosmetic of the present invention, the discoloration caused by the combination of the compound having an amino group (A) and the sugar (B) is suppressed, and a whitening effect is imparted to the cosmetic.

[0078] The alkyl group having 1 to 3 carbon atoms of R1 to R6 can be, for example, methyl, ethyl, n-propyl, isopropyl, or cyclopropyl, and in particular, can be methyl or ethyl, and typically can be methyl.

[0079] In a certain embodiment of the present invention, R1, R3, R4, and R6 in the above general formula (1) are all methyl. In other embodiments of the present invention, R2 and R5 in the above general formula (1) are both hydrogen atoms. In still other embodiments of the present invention, R1, R3, R4, and R6 in the above general formula (1) are all methyl, and R2 and R5 are both hydrogen atoms.

[0080] In a certain embodiment of the present invention, R1, R2, R3, R4, and R6 in the above general formula (1) are all methyl. In other embodiments of the present invention, R5 in the above general formula (1) is a hydrogen atom. In still other embodiments of the present invention, R1, R2, R3, R4, and R6 in the above general formula (1) are all methyl, and R5 is a hydrogen atom.

[0081] In a certain embodiment of the present invention, R2 and R5 in the above general formula (1) are both ethyl groups. In other embodiments of the present invention, R1, R2, R3, R4, and R6 in the above general formula (1) are all methyl groups, and R2 and R5 are both ethyl atoms.

[0082] The component (B) in the present invention can be selected from

[0083] 2-(3,5-dimethylpyrazol-1-yl)-4,6-dimethylpyrimidine,

[0084] 2-(3,5-dimethylpyrazol-1-yl)-4,5,6-trimethylpyrimidine, and

[0085] 5-ethyl-2-(4-ethyl-3,5-dimethylpyrazol-1-yl)-4,6-dimethylpyrimidine, and

[0086] pharmacologically acceptable salts thereof

[0087] one or more compounds selected therefrom.

[0088] The pharmacologically acceptable salts of the compounds represented by the above general formula (1) can be, for example, acid addition salts of the compounds represented by the above general formula (1). The acid in the acid addition salts can be an inorganic acid or an organic acid. The inorganic acid can be, for example, hydrochloric acid, hydrobromic acid, sulfuric acid, phosphoric acid, etc., and the organic acid can be, for example, acetic acid, propionic acid, citric acid, lactic acid, oxalic acid, maleic acid, fumaric acid, succinic acid, tartaric acid, methanesulfonic acid, etc.

[0089] The compounds represented by the above general formula (1) can be synthesized by known methods and can also be obtained as commercially available products. The representative synthesis methods of the compounds represented by the above general formula (1) are disclosed in, for example, the above Patent Document 3.

[0090] "(D) Water"

[0091] The cosmetic of the present invention contains water as a solvent.

[0092] "Other Components"

[0093] The cosmetic of the present invention may further contain other components in addition to the above components (A) to (D).

[0094] Examples of other components include surfactants, thickeners, humectants, defoamers, cooling agents, pH adjusters, chelating agents, preservatives, antioxidants, pigments, fragrances, stabilizers, etc.

[0095] "Mixing Amounts of Each Component"

[0096] The blending amount of the (A) amino compound in the cosmetic of the present invention, based on the total mass of the cosmetic, may be 0.1% by mass or more, 0.5% by mass or more, 1.0% by mass or more, 1.5% by mass or more, or 2.0% by mass or more, and may be 5.0% by mass or less, 4.0% by mass or more, 3.0% by mass or more, or 2.0% by mass or more.

[0097] In addition, the blending amount of the (A) amino compound, relative to 100 parts by mass in total of the components (A) to (C), may be 0.5% by mass or more, 1.0 part by mass or more, 5.0 parts by mass or more, 10 parts by mass or more, 20 parts by mass or more, 30 parts by mass or more, or 35 parts by mass or more, and may be 95% by mass or less, 90 parts by mass or less, 88 parts by mass or less, 85 parts by mass or less, or 80 parts by mass or less.

[0098] The blending amount of the (B) sugar in the cosmetic of the present invention, based on the total mass of the cosmetic, may be 0.001% by mass or more, 0.01% by mass or more, 0.03% by mass or more, 0.05% by mass or more, 0.10% by mass or more, 0.50% by mass or more, 1.0% by mass or more, or 2.0% by mass or more, and may be 10.0% by mass or less, 8.0% by mass or less, 6.0% by mass or less, 5.0% by mass or less, or 4.0% by mass or less.

[0099] In addition, the blending amount of the (B) sugar, relative to 100 parts by mass in total of the components (A) to (C), may be 0.1% by mass or more, 1.0 part by mass or more, 1.5 parts by mass or more, 2.0 parts by mass or more, 3.0 parts by mass or more, 5.0 parts by mass or more, or 10.0 parts by mass or more, and may be 90 parts by mass or less, 80 parts by mass or less, 70 parts by mass or less, 65 parts by mass or less, 60 parts by mass or less, 55 parts by mass or less, or 50 parts by mass or less.

[0100] The blending amount of the (C) pyrimidinylpyrazole compounds in the cosmetic of the present invention, based on the total mass of the cosmetic, may be 0.05% by mass or more, 0.10% by mass or more, 0.15% by mass or more, 0.20% by mass or more, 0.25% by mass or more, or 0.30% by mass or more, and may be 1.00% by mass or less, 0.80% by mass or less, 0.60% by mass or less, 0.50% by mass or less, 0.40% by mass or less, or 0.35% by mass or less.

[0101] In addition, the mixing amount of the pyrimidinylpyrazole compound (C) may be 1.0% by mass or more, 3.0% by mass or more, 3.5% by mass or more, 4.0% by mass or more, 4.5% by mass or more, or 5.0% by mass or more, and may be 40% by mass or less, 35% by mass or less, 30% by mass or less, 35% by mass or less, 20% by mass or less, or 15% by mass or less, based on 100 parts by mass of the total of components (A) to (C).

[0102] Method for Manufacturing Cosmetic

[0103] The cosmetic of the present invention can be produced by mixing the components (A) to (C) and other components to be mixed as needed by an appropriate method.

[0104] Use of Cosmetic

[0105] The cosmetic of the present invention can be a cosmetic for humans, and can be suitably applied, for example, in skin cosmetics and the like.

[0106] Examples

[0107] Confirmation of Effects of the Present Invention

[0108] First, in order to confirm the effects of the present invention, experiments were conducted using a composition with a simplified composition.

[0109] (1) Preparation of Composition

[0110] Compositions of Comparative Examples a-1 to a-11 and Examples A-1 to A-11 were prepared by mixing the components described in Tables 1 and 2. Note that the mixing amounts in Tables 1 and 2 are in units of "% by mass". The so-called "Compound (C-1)" in Tables 1 and 2 refers to "2-(3,5-dimethylpyrazol-1-yl)-4,6-dimethylpyrimidine hydrochloride". In addition, the mixing amount of ion-exchanged water being "balance" means that the mixing amount of ion-exchanged water is changed so that the total amount of each composition adds up to 100% by mass.

[0111] (2) Evaluation of Hue of Composition

[0112] 50 mL of each of the obtained compositions was poured into transparent sample bottles and stored by standing at 70 °C for 1 week (7 days). The sample bottles containing the compositions after 1 week of storage were placed on white paper and visually observed from above to observe the hue of the compositions, and the evaluation was carried out according to the following criteria. The evaluation results are shown in Tables 1 and 2.

[0113] A: The case where the hue has not changed compared to before storage

[0114] B: The case where the hue has slightly changed compared to before storage

[0115] C: The case where the hue has clearly changed compared to before storage

[0116] [Table 1]

[0117]

[0118] [Table 2]

[0119]

[0120] The following is understood from Tables 1 and 2.

[0121] For the compositions of Comparative Examples a-1 to a-11 containing (A) an amino compound and (B) a sugar and not containing (C) pyrimidylpyrazole compounds, a change in hue was observed after storage at 70°C for 1 week.

[0122] In contrast, for the compositions of Examples A-1 to A-11 in which (C) pyrimidylpyrazole compounds were admixed together with (A) an amino compound and (B) a sugar, the change in hue after storage at 70°C for 1 week was suppressed compared to the corresponding Comparative Examples having the same type and amount of sugar admixed.

[0123] The effects of the present invention were confirmed from the above results.

[0124] Verification in Skin Cosmetics

[0125] Next, the effects of the present invention were confirmed assuming the composition of a skin cosmetic.

[0126] (1) Preparation of Compositions

[0127] The components shown in Table 3 were admixed to prepare the compositions of Comparative Example b-a and Example B-1. The amounts of the respective components in Table 3 are in units of "mass%". The so-called "Compound (C-1)" in Table 3 means "2-(3,5-dimethylpyrazol-1-yl)-4,6-dimethylpyrimidine hydrochloride". In addition, the amount of ion-exchanged water admixed being "balance" means that the amount of ion-exchanged water was changed so that the total amount of each composition added up to 100 mass%.

[0128] (2) Evaluation of Hue of Compositions

[0129] Using each of the obtained compositions, the hue was evaluated in the same manner as in Comparative Example a-1, etc. The evaluation results are shown in Table 3.

[0130] [Table 3]

[0131] Table 3

[0132]

[0133] The following is understood from Table 3.

[0134] For the composition of Comparative Example b-1 containing (A) an amino compound and (B) a sugar and not containing (C) pyrimidylpyrazole compounds, a clear change in hue was observed after storage at 70 °C for 1 week.

[0135] In contrast, for the composition of Example B-1 in which (C) pyrimidylpyrazole compounds were admixed together with (A) an amino compound and (B) a sugar, the change in hue after storage at 70 °C for 1 week was suppressed compared to the corresponding comparative example with the same type and blending amount of sugar, and no change in hue was observed.

[0136] From the above results, it was verified that the effects of the present invention are also appropriate assuming the blending in skin cosmetics.

Claims

1. A cosmetic composition comprising: (A) a compound having an amino group; (B) a sugar; (C) one or more selected from the group consisting of compounds represented by the following general formula (1) and pharmaceutically acceptable salts thereof; and (D) water, In general formula (1), R1, R3, R4 and R6 are each independently an alkyl group having 1 to 3 carbon atoms, and R2 and R5 are each independently a hydrogen atom or an alkyl group having 1 to 3 carbon atoms.

2. The cosmetic composition according to claim 1, wherein the component (A) is one or more selected from the group consisting of amino acids, amino acid derivatives, aromatic amines, dipeptides and proteins.

3. The cosmetic composition according to claim 2, wherein the component (A) is one or more selected from the group consisting of tranexamic acid, glycylglycine and L-theanine.

4. The cosmetic composition according to claim 1, wherein the component (B) comprises one or more selected from the group consisting of maltitol, sorbitol, fructose, erythritol, trehalose, xylitol, tremella polysaccharide, hyaluronic acid and hyaluronate.

5. The cosmetic composition according to claim 1, wherein the component (C) is selected from a compound in which R1, R3, R4 and R6 in the general formula (1) are methyl groups and R2 and R5 are hydrogen atoms, a compound in which R1, R2, R3, R4 and R6 in the general formula (1) are methyl groups and R5 is a hydrogen atom, and a compound in which R1, R3, R4 and R6 in the general formula (1) are methyl groups and R2 and R5 are ethyl groups one or more of them.

6. The cosmetic composition according to claim 2, wherein the component (C) is selected from a compound in which R1, R3, R4 and R6 in the general formula (1) are methyl groups and R2 and R5 are hydrogen atoms, a compound in which R1, R2, R3, R4 and R6 in the general formula (1) are methyl groups and R5 is a hydrogen atom, and a compound in which R1, R3, R4 and R6 in the general formula (1) are methyl groups and R2 and R5 are ethyl groups one or more of them.

7. The cosmetic composition according to claim 3, wherein the component (C) is selected from a compound in which R1, R3, R4 and R6 in the general formula (1) are methyl groups and R2 and R5 are hydrogen atoms, a compound in which R1, R2, R3, R4 and R6 in the general formula (1) are methyl groups and R5 is a hydrogen atom, and a compound in which R1, R3, R4 and R6 in the general formula (1) are methyl groups and R2 and R5 are ethyl groups one or more of them.

8. The cosmetic composition according to any one of claims 1 to 7, wherein the mixing amount of the component (A) is 1.0 part by mass or more and 95 parts by mass or less with respect to 100 parts by mass in total of the components (A) to (C).

9. The cosmetic composition according to any one of claims 1 to 7, wherein the mixing amount of the component (B) is 1.0 part by mass or more and 90 parts by mass or less with respect to 100 parts by mass in total of the components (A) to (C).

10. The cosmetic according to any one of claims 1 to 7, wherein the blending amount of the component (C) is 3.0 parts by mass or more and 40 parts by mass or less with respect to 100 parts by mass in total of the components (A) to (C).

11. The cosmetic according to any one of claims 1 to 7, which is a skin cosmetic.

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