WO2024142837A1 - Cosmetic - Google Patents
Cosmetic Download PDFInfo
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- WO2024142837A1 WO2024142837A1 PCT/JP2023/043953 JP2023043953W WO2024142837A1 WO 2024142837 A1 WO2024142837 A1 WO 2024142837A1 JP 2023043953 W JP2023043953 W JP 2023043953W WO 2024142837 A1 WO2024142837 A1 WO 2024142837A1
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- 239000002537 cosmetic Substances 0.000 title claims abstract description 57
- 150000001875 compounds Chemical class 0.000 claims abstract description 56
- 235000000346 sugar Nutrition 0.000 claims abstract description 27
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract description 20
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 10
- 125000003277 amino group Chemical group 0.000 claims abstract description 9
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 26
- 238000002360 preparation method Methods 0.000 claims description 26
- 150000004676 glycans Chemical class 0.000 claims description 16
- 229920001282 polysaccharide Polymers 0.000 claims description 16
- 239000005017 polysaccharide Substances 0.000 claims description 16
- 238000002156 mixing Methods 0.000 claims description 14
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 10
- 229960000401 tranexamic acid Drugs 0.000 claims description 9
- GYDJEQRTZSCIOI-LJGSYFOKSA-N tranexamic acid Chemical compound NC[C@H]1CC[C@H](C(O)=O)CC1 GYDJEQRTZSCIOI-LJGSYFOKSA-N 0.000 claims description 9
- DATAGRPVKZEWHA-YFKPBYRVSA-N N(5)-ethyl-L-glutamine Chemical compound CCNC(=O)CC[C@H]([NH3+])C([O-])=O DATAGRPVKZEWHA-YFKPBYRVSA-N 0.000 claims description 8
- YMAWOPBAYDPSLA-UHFFFAOYSA-N glycylglycine Chemical compound [NH3+]CC(=O)NCC([O-])=O YMAWOPBAYDPSLA-UHFFFAOYSA-N 0.000 claims description 8
- 125000000217 alkyl group Chemical group 0.000 claims description 7
- 125000004432 carbon atom Chemical group C* 0.000 claims description 7
- HDTRYLNUVZCQOY-UHFFFAOYSA-N α-D-glucopyranosyl-α-D-glucopyranoside Natural products OC1C(O)C(O)C(CO)OC1OC1C(O)C(O)C(O)C(CO)O1 HDTRYLNUVZCQOY-UHFFFAOYSA-N 0.000 claims description 6
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims description 6
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 4
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims description 4
- 108010016626 Dipeptides Proteins 0.000 claims description 4
- 239000004386 Erythritol Substances 0.000 claims description 4
- UNXHWFMMPAWVPI-UHFFFAOYSA-N Erythritol Natural products OCC(O)C(O)CO UNXHWFMMPAWVPI-UHFFFAOYSA-N 0.000 claims description 4
- 239000005715 Fructose Substances 0.000 claims description 4
- 229930091371 Fructose Natural products 0.000 claims description 4
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 claims description 4
- 108010008488 Glycylglycine Proteins 0.000 claims description 4
- HDTRYLNUVZCQOY-WSWWMNSNSA-N Trehalose Natural products O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-WSWWMNSNSA-N 0.000 claims description 4
- 241000908178 Tremella fuciformis Species 0.000 claims description 4
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims description 4
- HDTRYLNUVZCQOY-LIZSDCNHSA-N alpha,alpha-trehalose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-LIZSDCNHSA-N 0.000 claims description 4
- 150000003862 amino acid derivatives Chemical class 0.000 claims description 4
- 150000001413 amino acids Chemical class 0.000 claims description 4
- 150000004982 aromatic amines Chemical class 0.000 claims description 4
- 235000019414 erythritol Nutrition 0.000 claims description 4
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- 229940043257 glycylglycine Drugs 0.000 claims description 4
- 239000000845 maltitol Substances 0.000 claims description 4
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- 108090000623 proteins and genes Proteins 0.000 claims description 4
- 102000004169 proteins and genes Human genes 0.000 claims description 4
- 239000000600 sorbitol Substances 0.000 claims description 4
- 229940026510 theanine Drugs 0.000 claims description 4
- 229940074410 trehalose Drugs 0.000 claims description 4
- 239000000811 xylitol Substances 0.000 claims description 4
- 235000010447 xylitol Nutrition 0.000 claims description 4
- 229960002675 xylitol Drugs 0.000 claims description 4
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims description 4
- KIUKXJAPPMFGSW-DNGZLQJQSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5S,6R)-3-Acetamido-2-[(2S,3S,4R,5R,6R)-6-[(2R,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 claims description 3
- WCDDVEOXEIYWFB-VXORFPGASA-N (2s,3s,4r,5r,6r)-3-[(2s,3r,5s,6r)-3-acetamido-5-hydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-4,5,6-trihydroxyoxane-2-carboxylic acid Chemical class CC(=O)N[C@@H]1C[C@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](C(O)=O)O[C@@H](O)[C@H](O)[C@H]1O WCDDVEOXEIYWFB-VXORFPGASA-N 0.000 claims description 3
- 229960002737 fructose Drugs 0.000 claims description 3
- 229920002674 hyaluronan Polymers 0.000 claims description 3
- 229960003160 hyaluronic acid Drugs 0.000 claims description 3
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- 150000003839 salts Chemical class 0.000 abstract description 7
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 2
- 239000000126 substance Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 description 29
- -1 acylamino compound Chemical class 0.000 description 24
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- 230000000052 comparative effect Effects 0.000 description 7
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- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 description 3
- 239000002253 acid Substances 0.000 description 3
- 229940024606 amino acid Drugs 0.000 description 3
- 235000001014 amino acid Nutrition 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 239000003205 fragrance Substances 0.000 description 3
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- 230000002087 whitening effect Effects 0.000 description 3
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- 238000004519 manufacturing process Methods 0.000 description 1
- 230000008099 melanin synthesis Effects 0.000 description 1
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- 230000001333 moisturizer Effects 0.000 description 1
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- 235000013923 monosodium glutamate Nutrition 0.000 description 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
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- 229920000435 poly(dimethylsiloxane) Polymers 0.000 description 1
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- 239000003755 preservative agent Substances 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- XOPPYWGGTZVUFP-DLWPFLMGSA-N primeverose Chemical compound O=C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO[C@@H]1OC[C@@H](O)[C@H](O)[C@H]1O XOPPYWGGTZVUFP-DLWPFLMGSA-N 0.000 description 1
- 235000019260 propionic acid Nutrition 0.000 description 1
- 239000001651 pyrus cydonia seed extract Substances 0.000 description 1
- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 description 1
- MUPFEKGTMRGPLJ-ZQSKZDJDSA-N raffinose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO[C@@H]2[C@@H]([C@@H](O)[C@@H](O)[C@@H](CO)O2)O)O1 MUPFEKGTMRGPLJ-ZQSKZDJDSA-N 0.000 description 1
- HEBKCHPVOIAQTA-ZXFHETKHSA-N ribitol Chemical compound OC[C@H](O)[C@H](O)[C@H](O)CO HEBKCHPVOIAQTA-ZXFHETKHSA-N 0.000 description 1
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- 229960001153 serine Drugs 0.000 description 1
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- 229940045898 sodium stearoyl glutamate Drugs 0.000 description 1
- KDHFCTLPQJQDQI-BDQAORGHSA-M sodium;(4s)-4-amino-5-octadecanoyloxy-5-oxopentanoate Chemical compound [Na+].CCCCCCCCCCCCCCCCCC(=O)OC(=O)[C@@H](N)CCC([O-])=O KDHFCTLPQJQDQI-BDQAORGHSA-M 0.000 description 1
- UKSFMDODPANKJI-UHFFFAOYSA-M sodium;2-[methyl(octadecanoyl)amino]ethanesulfonate Chemical compound [Na+].CCCCCCCCCCCCCCCCCC(=O)N(C)CCS([O-])(=O)=O UKSFMDODPANKJI-UHFFFAOYSA-M 0.000 description 1
- XNBZPOHDTUWNMW-QVCHUJKCSA-N solatriose Chemical compound O[C@@H]1[C@H](O)[C@@H](O)[C@H](C)O[C@H]1O[C@@H]1[C@@H](O[C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)[C@@H](O)[C@@H](CO)OC1O XNBZPOHDTUWNMW-QVCHUJKCSA-N 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- PZDOWFGHCNHPQD-VNNZMYODSA-N sophorose Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](C=O)O[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O PZDOWFGHCNHPQD-VNNZMYODSA-N 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- UQZIYBXSHAGNOE-XNSRJBNMSA-N stachyose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO[C@@H]2[C@@H]([C@@H](O)[C@@H](O)[C@@H](CO[C@@H]3[C@@H]([C@@H](O)[C@@H](O)[C@@H](CO)O3)O)O2)O)O1 UQZIYBXSHAGNOE-XNSRJBNMSA-N 0.000 description 1
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- 235000019698 starch Nutrition 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 230000002194 synthesizing effect Effects 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- FGMPLJWBKKVCDB-UHFFFAOYSA-N trans-L-hydroxy-proline Natural products ON1CCCC1C(O)=O FGMPLJWBKKVCDB-UHFFFAOYSA-N 0.000 description 1
- RULSWEULPANCDV-PIXUTMIVSA-N turanose Chemical compound OC[C@@H](O)[C@@H](O)[C@@H](C(=O)CO)O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O RULSWEULPANCDV-PIXUTMIVSA-N 0.000 description 1
- LNRUEZIDUKQGRH-YZUCMPLFSA-N umbelliferose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O[C@@H]2[C@@H]([C@@H](O)[C@@H](O)[C@@H](CO)O2)O)[C@@H](O)[C@@H](O)[C@@H](CO)O1 LNRUEZIDUKQGRH-YZUCMPLFSA-N 0.000 description 1
- FLUADVWHMHPUCG-SWPIJASHSA-N verbascose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO[C@@H]2[C@@H]([C@@H](O)[C@@H](O)[C@@H](CO[C@@H]3[C@@H]([C@@H](O)[C@@H](O)[C@@H](CO[C@@H]4[C@@H]([C@@H](O)[C@@H](O)[C@@H](CO)O4)O)O3)O)O2)O)O1 FLUADVWHMHPUCG-SWPIJASHSA-N 0.000 description 1
- 238000012795 verification Methods 0.000 description 1
- QYNRIDLOTGRNML-ULAALWPKSA-N vicianose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)CO[C@H]1OC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)C(O)O1 QYNRIDLOTGRNML-ULAALWPKSA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/41—Amines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/60—Sugars; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/64—Proteins; Peptides; Derivatives or degradation products thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
Definitions
- the present invention relates to cosmetics.
- Patent Document 1 proposes a topical preparation containing tranexamic acid, sugars, and an acylamino compound
- Patent Document 2 proposes a cosmetic preparation containing tranexamic acid, sugars, and an acetophenone derivative, and it is explained that each of these compositions suppresses discoloration due to heat or the passage of time by using a specific blend.
- the inventors have found that discoloration caused by the combination of a compound having an amino group and sugar is suppressed by adding pyrimidylpyrazole compounds. This is presumably because pyrimidylpyrazole compounds have a structure containing many nitrogen-carbon double bonds, and therefore function as antioxidants.
- the component (B) in the cosmetic of the present invention is a sugar.
- examples of the sugar (B) include monosaccharides, polysaccharides (including polysaccharides), sugar alcohols, etc., and may be a mixture containing two or more of these.
- polysaccharides in this specification also include polysaccharides derived from one or more species selected from starch, plants, seaweed, and lactic acid bacteria, Tremella fuciformis polysaccharides, etc.
- the sugar (B) in the present invention may particularly include sugars containing one or more selected from maltitol, sorbitol, fructose, erythritol, trehalose, xylitol, Tremella fuciformis polysaccharide, hyaluronic acid, and hyaluronate salts.
- the alkyl group having 1 to 3 carbon atoms for R 1 to R 6 may be, for example, a methyl group, an ethyl group, an n-propyl group, an isopropyl group, or a cyclopropyl group, in particular a methyl group or an ethyl group, and typically a methyl group.
- R2 and R5 in the above general formula (1) are all ethyl groups.
- R1 , R2 , R3 , R4 , and R6 in the above general formula (1) are all methyl groups, and R2 and R5 are all ethyl atoms.
- the component (B) in the present invention is 2-(3,5-dimethylpyrazol-1-yl)-4,6-dimethylpyrimidine
- the compound may be one or more compounds selected from 2-(3,5-dimethylpyrazol-1-yl)-4,5,6-trimethylpyrimidine, and 5-ethyl-2-(4-ethyl-3,5-dimethylpyrazol-1-yl)-4,6-dimethylpyrimidine, and pharmacologically acceptable salts thereof.
- the pharmacologically acceptable salt of the compound represented by the above general formula (1) may be, for example, an acid addition salt of the compound represented by the above general formula (1).
- the acid in the acid addition salt may be an inorganic acid or an organic acid.
- the inorganic acid may be, for example, hydrochloric acid (hydrochloric acid), hydrobromic acid, sulfuric acid, phosphoric acid, etc.
- the organic acid may be, for example, acetic acid, propionic acid, citric acid, lactic acid, oxalic acid, maleic acid, fumaric acid, succinic acid, tartaric acid, methanesulfonic acid, etc.
- the compound represented by the above general formula (1) can be synthesized by known methods and is also available as a commercial product.
- a representative method for synthesizing the compound represented by the above general formula (1) is disclosed, for example, in the above-mentioned Patent Document 3.
- the cosmetic preparation of the present invention contains water as a solvent.
- the blending amount of the amino compound (A) in the cosmetic of the present invention may be 0.1 mass% or more, 0.5 mass% or more, 1.0 mass% or more, 1.5 mass% or more, or 2.0 mass% or more, and may be 5.0 mass% or less, 4.0 mass% or more, 3.0 mass% or more, or 2.0 mass% or more, based on the total mass of the cosmetic.
- the amount of sugar (B) in the cosmetic of the present invention 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, based on the total mass of the cosmetic, 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 10.0% by mass or less.
- the amount of sugar (B) may be 0.1% by mass or more, 1.0 parts 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, relative to 100 parts by mass of the total of the components (A) to (C). It 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.
- the amount of the pyrimidylpyrazole compounds (C) in the cosmetic of the present invention 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, based on the total mass of the cosmetic, 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.
- the cosmetic of the present invention may be a cosmetic for humans, and can be suitably applied to applications such as skin cosmetics, for example.
- compositions of Comparative Examples a-1 to a-11 and Examples A-1 to A-11 were prepared by blending the components shown in Tables 1 and 2.
- the blend amounts in Tables 1 and 2 are in units of "mass %".
- “Compound (C-1)” in Tables 1 and 2 means "2-(3,5-dimethylpyrazol-1-yl)-4,6-dimethylpyrimidine hydrochloride”.
- the blend amount of ion-exchanged water being the "remainder” means that the blend amount of ion-exchanged water was changed to adjust the total amount of each composition to 100 mass %.
- Example B-1 which contains (A) an amino compound and (B) a sugar as well as (C) pyrimidylpyrazole compounds
- the change in color after storage at 70°C for one week was suppressed and no change in color was observed, compared to the corresponding comparative example, which contains the same type and amount of sugar.
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Birds (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Cosmetics (AREA)
Abstract
A cosmetic including: (A) a compound that has an amino group; (B) a sugar; (C) one or more substances selected from compounds represented by general formula (1) and pharmaceutically acceptable salts thereof (in general formula (1), R1, R3, R4, and R6 each independently represent a C1-3 alkyl group, and R2 and R5 each independently represent a hydrogen atom or a C1-3 alkyl group); and (D) water.
Description
本発明は、化粧料に関する。
The present invention relates to cosmetics.
トラネキサム酸及びその誘導体は、肌荒れの改善作用、美白効果等を有することから、化粧料、香粧品等に配合される成分である。また、糖類は、保湿効果、皮膚コンディショニング効果等を有する他、顧客への訴求力を示すことから、化粧料、香粧品等に配合される成分である。
Tranexamic acid and its derivatives are ingredients that are incorporated into cosmetics, fragrances, and other toiletries, as they have effects such as improving rough skin and whitening the skin. Sugars, in addition to having moisturizing and skin conditioning effects, are also ingredients that are incorporated into cosmetics, fragrances, and other toiletries, as they are appealing to customers.
しかしながら、トラネキサム酸に代表されるアミノ基を有する化合物と、糖とを併用すると、熱又は経時により、変色が生じることがある。
However, when a compound containing an amino group, such as tranexamic acid, is used in combination with sugar, discoloration may occur due to heat or the passage of time.
そこで、従来技術では、上記の変色を抑制する手段が、種々提案されている。
Therefore, various means have been proposed in the prior art to prevent the above-mentioned discoloration.
例えば、特許文献1では、トラネキサム酸、糖類、及びアシルアミノ化合物を含む外用剤が、特許文献2では、トラネキサム酸、糖類、及びアセトフェノン誘導体を含む化粧料が、それぞれ提案されており、それぞれ、所定の配合によって熱又は経時による着色が抑制されると説明されている。
For example, Patent Document 1 proposes a topical preparation containing tranexamic acid, sugars, and an acylamino compound, and Patent Document 2 proposes a cosmetic preparation containing tranexamic acid, sugars, and an acetophenone derivative, and it is explained that each of these compositions suppresses discoloration due to heat or the passage of time by using a specific blend.
ところで、美白効果に優れる皮膚外用剤として、ピリミジルピラゾール化合物が知られている。例えば、特許文献3には、ピリミジルピラゾール化合物が皮膚色素細胞内のメラニン生成を抑制する効果に優れ、美白剤として有用であることが記載されている。
By the way, pyrimidylpyrazole compounds are known as skin topicals with excellent whitening effects. For example, Patent Document 3 describes that pyrimidylpyrazole compounds have excellent effects in suppressing melanin production in skin pigment cells and are useful as whitening agents.
特許文献1及び2で提案された技術は、トラネキサム酸及び糖を併用した場合の熱又は経時による変色の抑制に、一定の効果を有する。
The technologies proposed in Patent Documents 1 and 2 have a certain degree of effectiveness in suppressing discoloration caused by heat or time when tranexamic acid and sugar are used in combination.
上記のような状況のもと、本発明は、アミノ基を有する化合物及び糖を含みながら、熱又は経時による変色が抑制されており、かつ、変色抑制の目的で配合される成分によって化粧料として更なる価値が付与されている、化粧料を提供することを目的とする。
Under the circumstances described above, the present invention aims to provide a cosmetic that contains a compound having an amino group and a sugar, while being inhibited from discoloring due to heat or the passage of time, and that is endowed with additional value as a cosmetic by ingredients that are blended for the purpose of inhibiting discoloration.
本発明は、以下のとおりである。
The present invention is as follows:
《態様1》(A)アミノ基を有する化合物、
(B)糖、
(C)下記一般式(1):
(一般式(1)中、R1、R3、R4、及びR6は、それぞれ独立して、炭素数1~3のアルキル基であり、R2及びR5は、それぞれ独立して、水素原子又は炭素数1~3のアルキル基である。)
で表される化合物及びその薬理学的に許容される塩から選択される1種又は2種以上、並びに
(D)水
を含む、化粧料。
《態様2》前記(A)成分が、アミノ酸、アミノ酸誘導体、芳香族アミン、ジペプチド、及びタンパク質から選択される1種又は2種以上である、態様1に記載の化粧料。
《態様3》
前記(A)成分が、トラネキサム酸、グリシルグリシン、及びテアニンから選択される1種又は2種以上である、態様2に記載の化粧料。
《態様4》前記(B)成分が、マルチトール、ソルビトール、フルクトース、エリスリトール、トレハロース、キシリトール、シロキクラゲ多糖体、ヒアルロン酸、及びヒアルロン酸塩から選択される1種又は2種以上を含む、態様1に記載の化粧料。
《態様5》前記(C)成分が、
前記一般式(1)におけるR1、R3、R4、及びR6がメチル基であり、かつ、R2及びR5が水素原子である化合物、
前記一般式(1)におけるR1、R2、R3、R4、及びR6がメチル基であり、かつ、R5が水素原子である化合物、並びに
前記一般式(1)におけるR1、R3、R4、及びR6がメチル基であり、かつ、R2及びR5がエチル基である化合物
から選択される、1種又は2種以上である、態様1に記載の化粧料。
《態様6》前記(C)成分が、
前記一般式(1)におけるR1、R3、R4、及びR6がメチル基であり、かつ、R2及びR5が水素原子である化合物、
前記一般式(1)におけるR1、R2、R3、R4、及びR6がメチル基であり、かつ、R5が水素原子である化合物、並びに
前記一般式(1)におけるR1、R3、R4、及びR6がメチル基であり、かつ、R2及びR5がエチル基である化合物
から選択される、1種又は2種以上である、態様2に記載の化粧料。
《態様7》前記(C)成分が、
前記一般式(1)におけるR1、R3、R4、及びR6がメチル基であり、かつ、R2及びR5が水素原子である化合物、
前記一般式(1)におけるR1、R2、R3、R4、及びR6がメチル基であり、かつ、R5が水素原子である化合物、並びに
前記一般式(1)におけるR1、R3、R4、及びR6がメチル基であり、かつ、R2及びR5がエチル基である化合物
から選択される、1種又は2種以上である、態様3に記載の化粧料。
《態様8》前記(A)成分の配合量が、前記(A)~(C)成分の合計100質量部に対して、1.0質量部以上95質量部以下である、態様1~7のいずれか一項に記載の化粧料。
《態様9》前記(B)成分の配合量が、前記(A)~(C)成分の合計100質量部に対して、1.0質量部以上90質量部以下である、態様1~7のいずれか一項に記載の化粧料。
《態様10》前記(C)成分の配合量が、前記(A)~(C)成分の合計100質量部に対して、3.0質量部以上40質量部以下である、態様1~7のいずれか一項に記載の化粧料。
《態様11》皮膚化粧料である、態様1~7のいずれか一項に記載の化粧料。 <<Aspect 1>> (A) a compound having an amino group,
(B) sugar,
(C) a compound represented by the following general formula (1):
(In general formula (1), R 1 , R 3 , R 4 , and R 6 are each independently an alkyl group having 1 to 3 carbon atoms, and R 2 and R 5 are each independently a hydrogen atom or an alkyl group having 1 to 3 carbon atoms.)
and (D) water.
<<Aspect 2>> The cosmetic preparation according to aspect 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.
Aspect 3
A cosmetic preparation according to aspect 2, wherein the component (A) is one or more selected from tranexamic acid, glycylglycine, and theanine.
<<Aspect 4>> The cosmetic preparation according to aspect 1, wherein the component (B) comprises one or more selected from maltitol, sorbitol, fructose, erythritol, trehalose, xylitol, tremella fuciformis polysaccharide, hyaluronic acid, and hyaluronate salts.
<Embodiment 5> The component (C) is
A compound in which R 1 , R 3 , R 4 , and R 6 in the general formula (1) are methyl groups, and R 2 and R 5 are hydrogen atoms;
The cosmetic preparation according to aspect 1 , which is one or more selected from a compound in which R 1 , R 2 , R 3 , R 4 , and R 6 in the general formula (1) are methyl groups and R 5 is a hydrogen atom, and a compound in which R 1 , R 3 , R 4 , and R 6 in the general formula (1) are methyl groups and R 2 and R 5 are ethyl groups.
<Embodiment 6> The component (C) is,
A compound in which R 1 , R 3 , R 4 , and R 6 in the general formula (1) are methyl groups, and R 2 and R 5 are hydrogen atoms;
The cosmetic preparation according to aspect 2, which is one or more selected from a compound in which R 1 , R 2 , R 3 , R 4 , and R 6 in the general formula (1) are methyl groups and R 5 is a hydrogen atom, and a compound in which R 1 , R 3 , R 4 , and R 6 in the general formula (1) are methyl groups and R 2 and R 5 are ethyl groups.
<Embodiment 7> The component (C) is,
A compound in which R 1 , R 3 , R 4 , and R 6 in the general formula (1) are methyl groups, and R 2 and R 5 are hydrogen atoms;
The cosmetic preparation according to aspect 3, which is one or more selected from a compound in which R 1 , R 2 , R 3 , R 4 , and R 6 in the general formula (1) are methyl groups and R 5 is a hydrogen atom, and a compound in which R 1 , R 3 , R 4 , and R 6 in the general formula (1) are methyl groups and R 2 and R 5 are ethyl groups.
<Aspect 8> The cosmetic preparation according to any one of aspects 1 to 7, wherein the blending amount of the component (A) is equal to or greater than 1.0 part by mass and equal to or less than 95 parts by mass, per 100 parts by mass of the combined total of the components (A) to (C).
<Aspect 9> The cosmetic preparation according to any one of aspects 1 to 7, wherein the blending amount of the component (B) is 1.0 part by mass or more and 90 parts by mass or less, per 100 parts by mass of the total of the components (A) to (C).
<Aspect 10> The cosmetic preparation according to any one of aspects 1 to 7, wherein the blending amount of the component (C) is equal to or greater than 3.0 parts by mass and equal to or less than 40 parts by mass, per 100 parts by mass of the combined total of the components (A) to (C).
Aspect 11: The cosmetic preparation according to any one of Aspects 1 to 7, which is a skin cosmetic preparation.
(B)糖、
(C)下記一般式(1):
で表される化合物及びその薬理学的に許容される塩から選択される1種又は2種以上、並びに
(D)水
を含む、化粧料。
《態様2》前記(A)成分が、アミノ酸、アミノ酸誘導体、芳香族アミン、ジペプチド、及びタンパク質から選択される1種又は2種以上である、態様1に記載の化粧料。
《態様3》
前記(A)成分が、トラネキサム酸、グリシルグリシン、及びテアニンから選択される1種又は2種以上である、態様2に記載の化粧料。
《態様4》前記(B)成分が、マルチトール、ソルビトール、フルクトース、エリスリトール、トレハロース、キシリトール、シロキクラゲ多糖体、ヒアルロン酸、及びヒアルロン酸塩から選択される1種又は2種以上を含む、態様1に記載の化粧料。
《態様5》前記(C)成分が、
前記一般式(1)におけるR1、R3、R4、及びR6がメチル基であり、かつ、R2及びR5が水素原子である化合物、
前記一般式(1)におけるR1、R2、R3、R4、及びR6がメチル基であり、かつ、R5が水素原子である化合物、並びに
前記一般式(1)におけるR1、R3、R4、及びR6がメチル基であり、かつ、R2及びR5がエチル基である化合物
から選択される、1種又は2種以上である、態様1に記載の化粧料。
《態様6》前記(C)成分が、
前記一般式(1)におけるR1、R3、R4、及びR6がメチル基であり、かつ、R2及びR5が水素原子である化合物、
前記一般式(1)におけるR1、R2、R3、R4、及びR6がメチル基であり、かつ、R5が水素原子である化合物、並びに
前記一般式(1)におけるR1、R3、R4、及びR6がメチル基であり、かつ、R2及びR5がエチル基である化合物
から選択される、1種又は2種以上である、態様2に記載の化粧料。
《態様7》前記(C)成分が、
前記一般式(1)におけるR1、R3、R4、及びR6がメチル基であり、かつ、R2及びR5が水素原子である化合物、
前記一般式(1)におけるR1、R2、R3、R4、及びR6がメチル基であり、かつ、R5が水素原子である化合物、並びに
前記一般式(1)におけるR1、R3、R4、及びR6がメチル基であり、かつ、R2及びR5がエチル基である化合物
から選択される、1種又は2種以上である、態様3に記載の化粧料。
《態様8》前記(A)成分の配合量が、前記(A)~(C)成分の合計100質量部に対して、1.0質量部以上95質量部以下である、態様1~7のいずれか一項に記載の化粧料。
《態様9》前記(B)成分の配合量が、前記(A)~(C)成分の合計100質量部に対して、1.0質量部以上90質量部以下である、態様1~7のいずれか一項に記載の化粧料。
《態様10》前記(C)成分の配合量が、前記(A)~(C)成分の合計100質量部に対して、3.0質量部以上40質量部以下である、態様1~7のいずれか一項に記載の化粧料。
《態様11》皮膚化粧料である、態様1~7のいずれか一項に記載の化粧料。 <<Aspect 1>> (A) a compound having an amino group,
(B) sugar,
(C) a compound represented by the following general formula (1):
and (D) water.
<<Aspect 2>> The cosmetic preparation according to aspect 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.
Aspect 3
A cosmetic preparation according to aspect 2, wherein the component (A) is one or more selected from tranexamic acid, glycylglycine, and theanine.
<<Aspect 4>> The cosmetic preparation according to aspect 1, wherein the component (B) comprises one or more selected from maltitol, sorbitol, fructose, erythritol, trehalose, xylitol, tremella fuciformis polysaccharide, hyaluronic acid, and hyaluronate salts.
<Embodiment 5> The component (C) is
A compound in which R 1 , R 3 , R 4 , and R 6 in the general formula (1) are methyl groups, and R 2 and R 5 are hydrogen atoms;
The cosmetic preparation according to aspect 1 , which is one or more selected from a compound in which R 1 , R 2 , R 3 , R 4 , and R 6 in the general formula (1) are methyl groups and R 5 is a hydrogen atom, and a compound in which R 1 , R 3 , R 4 , and R 6 in the general formula (1) are methyl groups and R 2 and R 5 are ethyl groups.
<Embodiment 6> The component (C) is,
A compound in which R 1 , R 3 , R 4 , and R 6 in the general formula (1) are methyl groups, and R 2 and R 5 are hydrogen atoms;
The cosmetic preparation according to aspect 2, which is one or more selected from a compound in which R 1 , R 2 , R 3 , R 4 , and R 6 in the general formula (1) are methyl groups and R 5 is a hydrogen atom, and a compound in which R 1 , R 3 , R 4 , and R 6 in the general formula (1) are methyl groups and R 2 and R 5 are ethyl groups.
<Embodiment 7> The component (C) is,
A compound in which R 1 , R 3 , R 4 , and R 6 in the general formula (1) are methyl groups, and R 2 and R 5 are hydrogen atoms;
The cosmetic preparation according to aspect 3, which is one or more selected from a compound in which R 1 , R 2 , R 3 , R 4 , and R 6 in the general formula (1) are methyl groups and R 5 is a hydrogen atom, and a compound in which R 1 , R 3 , R 4 , and R 6 in the general formula (1) are methyl groups and R 2 and R 5 are ethyl groups.
<Aspect 8> The cosmetic preparation according to any one of aspects 1 to 7, wherein the blending amount of the component (A) is equal to or greater than 1.0 part by mass and equal to or less than 95 parts by mass, per 100 parts by mass of the combined total of the components (A) to (C).
<Aspect 9> The cosmetic preparation according to any one of aspects 1 to 7, wherein the blending amount of the component (B) is 1.0 part by mass or more and 90 parts by mass or less, per 100 parts by mass of the total of the components (A) to (C).
<Aspect 10> The cosmetic preparation according to any one of aspects 1 to 7, wherein the blending amount of the component (C) is equal to or greater than 3.0 parts by mass and equal to or less than 40 parts by mass, per 100 parts by mass of the combined total of the components (A) to (C).
Aspect 11: The cosmetic preparation according to any one of Aspects 1 to 7, which is a skin cosmetic preparation.
本発明によると、アミノ基を有する化合物及び糖を含みながら、熱又は経時による変色が抑制されており、かつ、変色抑制の目的で配合される成分によって化粧料として更なる価値が付与されている、化粧料が提供される。
The present invention provides a cosmetic that contains a compound having an amino group and a sugar, while being inhibited from discoloring due to heat or over time, and that is further enhanced in value as a cosmetic by the components that are blended in for the purpose of inhibiting discoloration.
《化粧料》
本発明の化粧料は、
(A)アミノ基を有する化合物(アミノ化合物)、
(B)糖、
(C)上記一般式(1)で表される化合物及びその薬理学的に許容される塩から選択される1種又は2種以上(以下、これらをまとめて「ピリミジルピラゾール化合物類」ということがある。)、並びに
(D)水
を含む。 Cosmetics
The cosmetic composition of the present invention comprises:
(A) a compound having an amino group (amino compound),
(B) sugar,
(C) one or more compounds selected from the group consisting of compounds represented by the above general formula (1) and pharmacologically acceptable salts thereof (hereinafter, these may be collectively referred to as "pyrimidylpyrazole compounds"), and (D) water.
本発明の化粧料は、
(A)アミノ基を有する化合物(アミノ化合物)、
(B)糖、
(C)上記一般式(1)で表される化合物及びその薬理学的に許容される塩から選択される1種又は2種以上(以下、これらをまとめて「ピリミジルピラゾール化合物類」ということがある。)、並びに
(D)水
を含む。 Cosmetics
The cosmetic composition of the present invention comprises:
(A) a compound having an amino group (amino compound),
(B) sugar,
(C) one or more compounds selected from the group consisting of compounds represented by the above general formula (1) and pharmacologically acceptable salts thereof (hereinafter, these may be collectively referred to as "pyrimidylpyrazole compounds"), and (D) water.
本発明者らは、アミノ基を有する化合物及び糖の組合せによる変色が、ピリミジルピラゾール化合物類の配合によって、抑制されることを見出した。これは、ピリミジルピラゾール化合物類が、窒素炭素二重結合を多く含む構造を有することによって、酸化防止剤として機能することによると推察される。
The inventors have found that discoloration caused by the combination of a compound having an amino group and sugar is suppressed by adding pyrimidylpyrazole compounds. This is presumably because pyrimidylpyrazole compounds have a structure containing many nitrogen-carbon double bonds, and therefore function as antioxidants.
本発明は、上記のような知見に基づいてなされたものである。なお、本発明は、特定の理論に拘束されない。
The present invention has been made based on the above findings. However, the present invention is not bound by any particular theory.
以下、本発明の化粧料を構成する要素について、順に説明する。
The components that make up the cosmetic of the present invention will be explained below in order.
《(A)アミノ化合物》
本発明の化粧料における(A)成分は、アミノ化合物である。 (A) Amino compound
The component (A) in the cosmetic of the present invention is an amino compound.
本発明の化粧料における(A)成分は、アミノ化合物である。 (A) Amino compound
The component (A) in the cosmetic of the present invention is an amino compound.
(A)アミノ化合物としては、例えば、アミノ酸、アミノ酸誘導体、芳香族アミン、ジペプチド、タンパク質等を例示することができる他、これらの概念に包含されない他の化合物が挙げられる。
(A) Examples of amino compounds include amino acids, amino acid derivatives, aromatic amines, dipeptides, proteins, etc., as well as other compounds not encompassed by these concepts.
アミノ酸は、例えば、エクトイン、グリシン、システイン、テアニン、セリン、ヒドロキシプロリン、アスパラギン酸、トラネキサム酸等であってよく;
アミノ酸誘導体は、例えば、グルタミン酸Na、システインHCl、ステアロイルグルタミン酸Na、ココイルグルタミン酸K、ヤシ脂肪酸アルギニン等であってよく;
芳香族アミンは、例えば、硫酸4,4’-ジアミノジフェニルアミン等であってよく;
ジペプチドは、例えば、グリシルグリシン、アスパラギン酸アルギニン等であってよく;
タンパク質は、例えば、セリシン等であってよく;
他の化合物は、例えば、アラントイン、ステアロイルメチルタウリンナトリウム、アモジメチコン、ベタイン等であってよい。 The amino acid may be, for example, ectoine, glycine, cysteine, theanine, serine, hydroxyproline, aspartic acid, tranexamic acid, etc.;
The amino acid derivative may be, for example, sodium glutamate, cysteine HCl, sodium stearoyl glutamate, potassium cocoyl glutamate, coconut fatty acid arginine, etc.;
The aromatic amine may be, for example, 4,4'-diaminodiphenylamine sulfate, and the like;
The dipeptide may be, for example, glycylglycine, arginine aspartate, etc.;
The protein may be, for example, sericin;
Other compounds may be, for example, allantoin, sodium methyl stearoyl taurate, amodimethicone, betaine, and the like.
アミノ酸誘導体は、例えば、グルタミン酸Na、システインHCl、ステアロイルグルタミン酸Na、ココイルグルタミン酸K、ヤシ脂肪酸アルギニン等であってよく;
芳香族アミンは、例えば、硫酸4,4’-ジアミノジフェニルアミン等であってよく;
ジペプチドは、例えば、グリシルグリシン、アスパラギン酸アルギニン等であってよく;
タンパク質は、例えば、セリシン等であってよく;
他の化合物は、例えば、アラントイン、ステアロイルメチルタウリンナトリウム、アモジメチコン、ベタイン等であってよい。 The amino acid may be, for example, ectoine, glycine, cysteine, theanine, serine, hydroxyproline, aspartic acid, tranexamic acid, etc.;
The amino acid derivative may be, for example, sodium glutamate, cysteine HCl, sodium stearoyl glutamate, potassium cocoyl glutamate, coconut fatty acid arginine, etc.;
The aromatic amine may be, for example, 4,4'-diaminodiphenylamine sulfate, and the like;
The dipeptide may be, for example, glycylglycine, arginine aspartate, etc.;
The protein may be, for example, sericin;
Other compounds may be, for example, allantoin, sodium methyl stearoyl taurate, amodimethicone, betaine, and the like.
本発明における(A)アミノ化合物としては、特に、トラネキサム酸、グリシルグリシン、及びテアニンから選択される1種又は2種以上が挙げられる。
The amino compound (A) in the present invention may in particular be one or more selected from tranexamic acid, glycylglycine, and theanine.
《(B)糖》
本発明の化粧料における(B)成分は、糖である。この(B)糖としては、単糖類、多糖類(多糖体を含む)、糖アルコール等が挙げられ、これらのうちの2種以上を含む混合物であってもよい。 (B) Sugar
The component (B) in the cosmetic of the present invention is a sugar. Examples of the sugar (B) include monosaccharides, polysaccharides (including polysaccharides), sugar alcohols, etc., and may be a mixture containing two or more of these.
本発明の化粧料における(B)成分は、糖である。この(B)糖としては、単糖類、多糖類(多糖体を含む)、糖アルコール等が挙げられ、これらのうちの2種以上を含む混合物であってもよい。 (B) Sugar
The component (B) in the cosmetic of the present invention is a sugar. Examples of the sugar (B) include monosaccharides, polysaccharides (including polysaccharides), sugar alcohols, etc., and may be a mixture containing two or more of these.
単糖類としては、例えば、エリツルロース、エリトロース、トレオース、アラビノース、キシロース、リキソース、リボース、キシルロース、リブロース、ガラクトース、グルコース、タロース、マンノース、ソルボース、タガトース、プシコース、フルクトース、アピオース、ハマメロース等が挙げられる。
Examples of monosaccharides include erythrulose, erythrose, threose, arabinose, xylose, lyxose, ribose, xylulose, ribulose, galactose, glucose, talose, mannose, sorbose, tagatose, psicose, fructose, apiose, and hamamelose.
多糖類(多糖体を含む)としては、例えば、キシロビオース、アガロビオース、 カラビオース、マルトース、イソマルトース、ソホロース、セロビオース、トレハロース 、ネオトレハロース、イソトレハロース、イヌロビオース、ビシアノース、イソプリメベ ロース、サンブビオース、プリメベロース、ソラビオース、メリビオース、ラクトース、 リコビオース、エピセロビオース、スクロース、ツラノース、マルツロース、ラクツロー ス、エピゲンチビオース、ロビノビオース、シラノビオース、ルチノース、グルコシルトレハロース、セロトリオース、カコトリオース、ゲンチ アノース、イソマルトトリオース、イソパノース、マルトトリオース、マンニノトリオー ス、メレンジトース、パノース、プランテオース、ラフィノース、ソラトリオース、ウン ベリフェロース、マルトシルトレハロース、マルトテ トラオース、スタキオース、マルトトリオシルトレハ ロース、マルトペンタオース、ベルバスコース、マルトヘキサオース等が挙げられる他、本明細書における多糖類(多糖体を含む)は、デンプン、植物、海藻、及び乳酸菌から選択される1種又は2種以上に由来する多糖体、シロキクラゲ多糖体等も包含する。
Examples of polysaccharides (including polysaccharides) include xylobiose, agarobiose, carabiose, maltose, isomaltose, sophorose, cellobiose, trehalose, neotrehalose, isotrehalose, inulobiose, vicianose, isoprimeverose, sambubiose, primeverose, sorabioses, melibiose, lactose, lycobiose, epicellobiose, sucrose, turanose, maltulose, lactulose, epigentibiose, robinobiose, cylanobiose, rutinose, glucosyltrehalose, cellotriose, cacosyl. Examples of such polysaccharides include maltotriose, gentianose, isomaltotriose, isopanose, maltotriose, manninotriose, melenitose, panose, planteose, raffinose, solatriose, umbelliferose, maltosyltrehalose, maltotetraose, stachyose, maltotriosyltrehalose, maltopentaose, verbascose, and maltohexaose. In addition, the polysaccharides (including polysaccharides) in this specification also include polysaccharides derived from one or more species selected from starch, plants, seaweed, and lactic acid bacteria, Tremella fuciformis polysaccharides, etc.
糖アルコールは、前記の単糖類及び多糖類(多糖体含む)のうちの、アルドース又はケトースのカルボニル基が還元されたものである。糖アルコールは、D体若しくはL体、又はこれらの混合物であってよい。糖アルコールは、1種単独で、又は2種以上を適宜組み合わせて使用することができる。
Sugar alcohols are those obtained by reducing the carbonyl group of aldose or ketose from the above-mentioned monosaccharides and polysaccharides (including polysaccharides). The sugar alcohols may be D- or L-isomers, or a mixture of these. The sugar alcohols may be used alone or in appropriate combination of two or more kinds.
糖アルコールとしては、例えば、エリスリトール、キシリトール、リビトール、アラビトール、ガラクチトール、ソルビトール、イノシトール、マンニトール、パラチニット、マルチトール、ラクチトール、イソマルトース、マルトトリイトール、マルトテトライトール、マルトペンタイトール、マルトヘキサトリイトール等が挙げられる。
Examples of sugar alcohols include erythritol, xylitol, ribitol, arabitol, galactitol, sorbitol, inositol, mannitol, palatinite, maltitol, lactitol, isomaltose, maltotriitol, maltotetriitol, maltopentaitol, and maltohexatriitol.
混合物としては、例えば、クインスシードエキス、異性化糖等が挙げられる。また、これらの混合物と、上記の単糖類、多糖類(多糖体を含む)、及び糖アルコールのうちの1種又は2種以上との混合物を使用してもよい。
Examples of mixtures include quince seed extract, isomerized sugar, etc. Also, mixtures of these with one or more of the above-mentioned monosaccharides, polysaccharides (including polysaccharides), and sugar alcohols may be used.
本発明における(B)糖としては、特に、マルチトール、ソルビトール、フルクトース、エリスリトール、トレハロース、キシリトール、シロキクラゲ多糖体、ヒアルロン酸、及びヒアルロン酸塩から選択される1種又は2種以上を含む糖が挙げられる。
The sugar (B) in the present invention may particularly include sugars containing one or more selected from maltitol, sorbitol, fructose, erythritol, trehalose, xylitol, Tremella fuciformis polysaccharide, hyaluronic acid, and hyaluronate salts.
《(C)ピリミジルピラゾール化合物類》
本発明の化粧料における(C)成分は、下記一般式(1):
(一般式(1)中、R1、R3、R4、及びR6は、それぞれ独立して、炭素数1~3のアルキル基であり、R2及びR5は、それぞれ独立して、水素原子又は炭素数1~3のアルキル基である。)
で表される化合物及びその薬理学的に許容される塩から選択される1種又は2種以上である。 (C) Pyrimidylpyrazole compounds
The component (C) in the cosmetic of the present invention is a compound represented by the following general formula (1):
(In general formula (1), R 1 , R 3 , R 4 , and R 6 are each independently an alkyl group having 1 to 3 carbon atoms, and R 2 and R 5 are each independently a hydrogen atom or an alkyl group having 1 to 3 carbon atoms.)
and pharmacologically acceptable salts thereof.
本発明の化粧料における(C)成分は、下記一般式(1):
で表される化合物及びその薬理学的に許容される塩から選択される1種又は2種以上である。 (C) Pyrimidylpyrazole compounds
The component (C) in the cosmetic of the present invention is a compound represented by the following general formula (1):
and pharmacologically acceptable salts thereof.
本発明の化粧料に、この(C)ピリミジルピラゾール化合物類が配合されることにより、(A)アミノ基を有する化合物と、(B)糖との組合せによる変色が抑制されるとともに、化粧料に美白効果が付与される。
By blending the (C) pyrimidylpyrazole compounds in the cosmetic of the present invention, discoloration caused by the combination of (A) a compound having an amino group and (B) a sugar is suppressed, and a whitening effect is imparted to the cosmetic.
R1~R6の炭素数1~3のアルキル基は、例えば、メチル基、エチル基、n-プロピル基、イソプロピル基、又はシクロプロピル基であってよく、特にメチル基又はエチル基であってよく、典型的にはメチル基であってよい。
The alkyl group having 1 to 3 carbon atoms for R 1 to R 6 may be, for example, a methyl group, an ethyl group, an n-propyl group, an isopropyl group, or a cyclopropyl group, in particular a methyl group or an ethyl group, and typically a methyl group.
本発明のある実施態様では、上記一般式(1)におけるR1、R3、R4、及びR6が、いずれもメチル基である。本発明の別の実施態様では、上記一般式(1)におけるR2及びR5が、いずれも水素原子である。本発明の更に別の実施態様では、上記一般式(1)におけるR1、R3、R4、及びR6が、いずれもメチル基であり、かつ、R2及びR5が、いずれも水素原子である。
In one embodiment of the present invention, R 1 , R 3 , R 4 , and R 6 in the above general formula (1) are all methyl groups. In another embodiment of the present invention, R 2 and R 5 in the above general formula (1) are all hydrogen atoms. In yet another embodiment of the present invention, R 1 , R 3 , R 4 , and R 6 in the above general formula (1) are all methyl groups, and R 2 and R 5 are all hydrogen atoms.
本発明のある実施態様では、上記一般式(1)におけるR1、R2、R3、R4、及びR6が、いずれもメチル基である。本発明の別の実施態様では、上記一般式(1)におけるR5が水素原子である。本発明の更に別の実施態様では、上記一般式(1)におけるR1、R2、R3、R4、及びR6が、いずれもメチル基であり、かつ、R5が水素原子である。
In one embodiment of the present invention, R 1 , R 2 , R 3 , R 4 , and R 6 in the above general formula (1) are all methyl groups. In another embodiment of the present invention, R 5 in the above general formula (1) is a hydrogen atom. In yet another embodiment of the present invention, R 1 , R 2 , R 3 , R 4 , and R 6 in the above general formula (1) are all methyl groups, and R 5 is a hydrogen atom.
本発明のある実施態様では、上記一般式(1)におけるR2及びR5が、いずれもエチル基である。本発明の別の実施態様では、上記一般式(1)におけるR1、R2、R3、R4、及びR6が、いずれもメチル基であり、かつ、R2及びR5が、いずれもエチル原子である。
In one embodiment of the present invention, R2 and R5 in the above general formula (1) are all ethyl groups. In another embodiment 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 all ethyl atoms.
本発明における(B)成分は、
2-(3,5-ジメチルピラゾール-1-イル)-4,6-ジメチルピリミジン、
2-(3,5-ジメチルピラゾール-1-イル)-4,5,6-トリメチルピリミジン、及び
5-エチル-2-(4-エチル-3,5-ジメチルピラゾール-1-イル)-4,6-ジメチルピリミジン、並びに
薬理学的に許容されるこれらの塩
から選択される、1種又は2種以上の化合物であってよい。 The component (B) in the present invention is
2-(3,5-dimethylpyrazol-1-yl)-4,6-dimethylpyrimidine,
The compound may be one or more compounds selected from 2-(3,5-dimethylpyrazol-1-yl)-4,5,6-trimethylpyrimidine, and 5-ethyl-2-(4-ethyl-3,5-dimethylpyrazol-1-yl)-4,6-dimethylpyrimidine, and pharmacologically acceptable salts thereof.
2-(3,5-ジメチルピラゾール-1-イル)-4,6-ジメチルピリミジン、
2-(3,5-ジメチルピラゾール-1-イル)-4,5,6-トリメチルピリミジン、及び
5-エチル-2-(4-エチル-3,5-ジメチルピラゾール-1-イル)-4,6-ジメチルピリミジン、並びに
薬理学的に許容されるこれらの塩
から選択される、1種又は2種以上の化合物であってよい。 The component (B) in the present invention is
2-(3,5-dimethylpyrazol-1-yl)-4,6-dimethylpyrimidine,
The compound may be one or more compounds selected from 2-(3,5-dimethylpyrazol-1-yl)-4,5,6-trimethylpyrimidine, and 5-ethyl-2-(4-ethyl-3,5-dimethylpyrazol-1-yl)-4,6-dimethylpyrimidine, and pharmacologically acceptable salts thereof.
上記一般式(1)で表される化合物の薬理学的に許容される塩は、例えば、上記一般式(1)で表される化合物の酸付加塩でであってよい、酸付加塩における酸は、無機酸でも有機酸でもよい。無機酸は、例えば、塩化水素酸(塩酸)、臭化水素酸、硫酸、リン酸等であってよく、有機酸は、例えば、酢酸、プロピオン酸、クエン酸、乳酸、シュウ酸、マレイン酸、フマル酸、コハク酸、酒石酸、メタンスルホン酸等であってよい。
The pharmacologically acceptable salt of the compound represented by the above general formula (1) may be, for example, an acid addition salt of the compound represented by the above general formula (1). The acid in the acid addition salt may be an inorganic acid or an organic acid. The inorganic acid may be, for example, hydrochloric acid (hydrochloric acid), hydrobromic acid, sulfuric acid, phosphoric acid, etc., and the organic acid may be, for example, acetic acid, propionic acid, citric acid, lactic acid, oxalic acid, maleic acid, fumaric acid, succinic acid, tartaric acid, methanesulfonic acid, etc.
上記一般式(1)で表される化合物は、公知の方法によって合成することができ、市販品として入手することも可能である。上記一般式(1)で表される化合物の代表的な合成方法は、例えば、上述の特許文献3に開示されている。
The compound represented by the above general formula (1) can be synthesized by known methods and is also available as a commercial product. A representative method for synthesizing the compound represented by the above general formula (1) is disclosed, for example, in the above-mentioned Patent Document 3.
《(D)水》
本発明の化粧料は、溶媒として水を含む。 (D) Water
The cosmetic preparation of the present invention contains water as a solvent.
本発明の化粧料は、溶媒として水を含む。 (D) Water
The cosmetic preparation of the present invention contains water as a solvent.
《その他の成分》
本発明の化粧料は、上述の(A)~(D)成分の他に、その他の成分を更に含んでいてもよい。 Other Ingredients
The cosmetic preparation of the present invention may further contain other components in addition to the above-mentioned components (A) to (D).
本発明の化粧料は、上述の(A)~(D)成分の他に、その他の成分を更に含んでいてもよい。 Other Ingredients
The cosmetic preparation of the present invention may further contain other components in addition to the above-mentioned components (A) to (D).
その他の成分としては、例えば、界面活性剤、(増粘剤、保湿剤、消泡剤、清涼化剤、pH調整剤、キレート化剤、防腐剤、酸化防止剤、色素、香料、安定化剤等が挙げられる。
Other ingredients include, for example, surfactants, thickeners, moisturizers, defoamers, cooling agents, pH adjusters, chelating agents, preservatives, antioxidants, colorants, fragrances, stabilizers, etc.
《各成分の配合量》
本発明の化粧料における(A)アミノ化合物の配合量は、化粧料の全質量を基準として、0.1質量%以上、0.5質量%以上、1.0質量%以上、1.5質量%以上、又は2.0質量%以上であってよく、5.0質量%以下、4.0質量%以上、3.0質量%以上、又は2.0質量%以上であってよい。 《Amount of each ingredient》
The blending amount of the amino compound (A) in the cosmetic of the present invention may be 0.1 mass% or more, 0.5 mass% or more, 1.0 mass% or more, 1.5 mass% or more, or 2.0 mass% or more, and may be 5.0 mass% or less, 4.0 mass% or more, 3.0 mass% or more, or 2.0 mass% or more, based on the total mass of the cosmetic.
本発明の化粧料における(A)アミノ化合物の配合量は、化粧料の全質量を基準として、0.1質量%以上、0.5質量%以上、1.0質量%以上、1.5質量%以上、又は2.0質量%以上であってよく、5.0質量%以下、4.0質量%以上、3.0質量%以上、又は2.0質量%以上であってよい。 《Amount of each ingredient》
The blending amount of the amino compound (A) in the cosmetic of the present invention may be 0.1 mass% or more, 0.5 mass% or more, 1.0 mass% or more, 1.5 mass% or more, or 2.0 mass% or more, and may be 5.0 mass% or less, 4.0 mass% or more, 3.0 mass% or more, or 2.0 mass% or more, based on the total mass of the cosmetic.
また、(A)アミノ化合物の配合量は、(A)~(C)成分の合計100質量部に対して、0.5質量%以上、1.0質量部以上、5.0質量部以上、10質量部以上、20質量部以上、30質量部以上、又は35質量部以上であってよく、95質量%以下、90質量部以下、88質量部以下、85質量部以下、又は80質量部以下であってよい。
The amount of the amino compound (A) may be 0.5% by mass or more, 1.0 parts 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, relative to 100 parts by mass of the total of the components (A) to (C).
It 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.
本発明の化粧料における(B)糖の配合量は、化粧料の全質量を基準として、0.001質量%以上、0.01質量%以上、0.03質量%以上、0.05質量%以上、0.10質量%以上、0.50質量%以上、1.0質量%以上、又は2.0質量%以上であってよく、10.0質量%以下、8.0質量%以下、6.0質量%以下、5.0質量%以下、又は質量%以下であってよい。
The amount of sugar (B) in the cosmetic of the present invention 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, based on the total mass of the cosmetic, 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 10.0% by mass or less.
また、(B)糖の配合量は、(A)~(C)成分の合計100質量部に対して、0.1質量%以上、1.0質量部以上、1.5質量部以上、2.0質量部以上、3.0質量部以上、5.0質量部以上、又は10.0質量部以上であってよく、90質量部以下、80質量部以下、70質量部以下、65質量部以下、60質量部以下、55質量部以下、又は50質量部以下であってよい。
The amount of sugar (B) may be 0.1% by mass or more, 1.0 parts 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, relative to 100 parts by mass of the total of the components (A) to (C). It 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.
本発明の化粧料における(C)ピリミジルピラゾール化合物類の配合量は、化粧料の全質量を基準として、0.05質量%以上、0.10質量%以上、0.15質量%以上、0.20質量%以上、0.25質量%以上、又は0.30質量%以上であってよく、1.00質量%以下、0.80質量%以下、0.60質量%以下、0.50質量%以下、0.40質量%以下、又は0.35質量%以下であってよい。
The amount of the pyrimidylpyrazole compounds (C) in the cosmetic of the present invention 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, based on the total mass of the cosmetic, 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.
また、(C)ピリミジルピラゾール化合物類の配合量は、(A)~(C)成分の合計100質量部に対して、1.0質量%以上、3.0質量部以上、3.5質量部以上、4.0質量部以上、4.5質量部以上、又は5.0質量部以上であってよく、40質量部以下、35質量部以下、30質量部以下、35質量部以下、20質量部以下、又は15質量部以下であってよい。
The amount of the pyrimidylpyrazole compounds (C) blended may be 1.0% by mass or more, 3.0 parts by mass or more, 3.5 parts by mass or more, 4.0 parts by mass or more, 4.5 parts by mass or more, or 5.0 parts by mass or more, and may be 40 parts by mass or less, 35 parts by mass or less, 30 parts by mass or less, 35 parts by mass or less, 20 parts by mass or less, or 15 parts by mass or less, based on 100 parts by mass of the total of the components (A) to (C).
《化粧料の製造方法》
本発明の化粧料は、(A)~(C)の各成分、及び必要に応じて配合されるその他の成分を、適宜の方法によって混合することによって製造されてよい。 <<Production method of cosmetics>>
The cosmetic of the present invention may be produced by mixing the components (A) to (C) and other components that are blended as necessary, by an appropriate method.
本発明の化粧料は、(A)~(C)の各成分、及び必要に応じて配合されるその他の成分を、適宜の方法によって混合することによって製造されてよい。 <<Production method of cosmetics>>
The cosmetic of the present invention may be produced by mixing the components (A) to (C) and other components that are blended as necessary, by an appropriate method.
《化粧料の用途》
本発明の化粧料は、人の化粧料であってよく、例えば、皮膚化粧料等の用途に、好適に適用できる。 <Use of cosmetics>
The cosmetic of the present invention may be a cosmetic for humans, and can be suitably applied to applications such as skin cosmetics, for example.
本発明の化粧料は、人の化粧料であってよく、例えば、皮膚化粧料等の用途に、好適に適用できる。 <Use of cosmetics>
The cosmetic of the present invention may be a cosmetic for humans, and can be suitably applied to applications such as skin cosmetics, for example.
《本発明の作用効果の確認》
先ず、本発明の効果を確認するために、組成を単純化した組成物を用いて実験を行った。 <Confirmation of the Effects of the Present Invention>
First, in order to confirm the effect of the present invention, an experiment was carried out using a simplified composition.
先ず、本発明の効果を確認するために、組成を単純化した組成物を用いて実験を行った。 <Confirmation of the Effects of the Present Invention>
First, in order to confirm the effect of the present invention, an experiment was carried out using a simplified composition.
(1)組成物の調製
表1及び2に記載の成分を配合して、比較例a-1~a-11及び実施例A-1~A-11の組成物を調製した。なお、表1及び2における配合量は、「質量%」単位である。表1及び表2における「化合物(C-1)」とは、「2-(3,5-ジメチルピラゾール-1-イル)-4,6-ジメチルピリミジン塩酸塩」を意味する。また、イオン交換水の配合量が「残余」であるとは、イオン交換水の配合量を変量して、各組成物の全量を100質量%に合わせたことを意味する。 (1) Preparation of Compositions The compositions of Comparative Examples a-1 to a-11 and Examples A-1 to A-11 were prepared by blending the components shown in Tables 1 and 2. The blend amounts in Tables 1 and 2 are in units of "mass %". "Compound (C-1)" in Tables 1 and 2 means "2-(3,5-dimethylpyrazol-1-yl)-4,6-dimethylpyrimidine hydrochloride". The blend amount of ion-exchanged water being the "remainder" means that the blend amount of ion-exchanged water was changed to adjust the total amount of each composition to 100 mass %.
表1及び2に記載の成分を配合して、比較例a-1~a-11及び実施例A-1~A-11の組成物を調製した。なお、表1及び2における配合量は、「質量%」単位である。表1及び表2における「化合物(C-1)」とは、「2-(3,5-ジメチルピラゾール-1-イル)-4,6-ジメチルピリミジン塩酸塩」を意味する。また、イオン交換水の配合量が「残余」であるとは、イオン交換水の配合量を変量して、各組成物の全量を100質量%に合わせたことを意味する。 (1) Preparation of Compositions The compositions of Comparative Examples a-1 to a-11 and Examples A-1 to A-11 were prepared by blending the components shown in Tables 1 and 2. The blend amounts in Tables 1 and 2 are in units of "mass %". "Compound (C-1)" in Tables 1 and 2 means "2-(3,5-dimethylpyrazol-1-yl)-4,6-dimethylpyrimidine hydrochloride". The blend amount of ion-exchanged water being the "remainder" means that the blend amount of ion-exchanged water was changed to adjust the total amount of each composition to 100 mass %.
(2)組成物の色調の評価
得られた組成物を、透明のサンプル瓶に50mLずつ注入して、70℃において1週間(7日間)静置して保管した。1週間保管後の、組成物が入ったサンプル瓶を白色の紙の上に静置して、上方から目視することにより、組成物の色調を観察し、以下の基準で評価した。評価結果を表1及び2に示す。
A:保管前と比較して、色調に変化がなかった場合
B:保管前と比較して、色調がわずかに変化した場合
C:保管前と比較して、色調が明確に変化した場合 (2) Evaluation of color tone of composition 50 mL of the obtained composition was poured into a transparent sample bottle and stored at 70° C. for one week (7 days). After one week of storage, the sample bottle containing the composition was placed on a white paper and visually observed from above to observe the color tone of the composition and evaluate it according to the following criteria. The evaluation results are shown in Tables 1 and 2.
A: There was no change in color tone compared to before storage. B: There was a slight change in color tone compared to before storage. C: There was a clear change in color tone compared to before storage.
得られた組成物を、透明のサンプル瓶に50mLずつ注入して、70℃において1週間(7日間)静置して保管した。1週間保管後の、組成物が入ったサンプル瓶を白色の紙の上に静置して、上方から目視することにより、組成物の色調を観察し、以下の基準で評価した。評価結果を表1及び2に示す。
A:保管前と比較して、色調に変化がなかった場合
B:保管前と比較して、色調がわずかに変化した場合
C:保管前と比較して、色調が明確に変化した場合 (2) Evaluation of color tone of composition 50 mL of the obtained composition was poured into a transparent sample bottle and stored at 70° C. for one week (7 days). After one week of storage, the sample bottle containing the composition was placed on a white paper and visually observed from above to observe the color tone of the composition and evaluate it according to the following criteria. The evaluation results are shown in Tables 1 and 2.
A: There was no change in color tone compared to before storage. B: There was a slight change in color tone compared to before storage. C: There was a clear change in color tone compared to before storage.
表1及び2から、以下のことが理解される。
The following can be understood from Tables 1 and 2:
(A)アミノ化合物及び(B)糖を含み、かつ(C)ピリミジルピラゾール化合物類を含まない、比較例a-1~a~11の組成物では、70℃、1週間の保管後に、色調の変化が観察された。
In the compositions of Comparative Examples a-1 to a-11, which contain (A) an amino compound and (B) a sugar, but do not contain (C) pyrimidylpyrazole compounds, a change in color was observed after storage at 70°C for one week.
これらに対して、(A)アミノ化合物及び(B)糖とともに、(C)ピリミジルピラゾール化合物類を配合した、実施例A-1~A-11の組成物では、糖の種類及び配合量を同じくする対応の比較例に比べて、70℃、1週間保管後の色調の変化が抑制されていた。
In contrast, the compositions of Examples A-1 to A-11, which contain (A) an amino compound and (B) a sugar as well as (C) pyrimidylpyrazole compounds, showed less change in color after storage at 70°C for one week than the corresponding comparative examples, which contained the same type and amount of sugar.
以上の結果から、本発明の作用効果が確認された。
The above results confirm the effectiveness of the present invention.
《皮膚化粧料における検証》
次に、皮膚化粧料を想定した組成において、本発明の効果を確認した。 <Verification in skin cosmetics>
Next, the effects of the present invention were confirmed in a composition intended as a skin cosmetic.
次に、皮膚化粧料を想定した組成において、本発明の効果を確認した。 <Verification in skin cosmetics>
Next, the effects of the present invention were confirmed in a composition intended as a skin cosmetic.
(1)組成物の調製
表3に記載の成分を配合することにより、比較例b-a及び実施例B-1の組成物を調製した。表3における各成分の配合量は、「質量%」単位である。表3における「化合物(C-1)」とは、「2-(3,5-ジメチルピラゾール-1-イル)-4,6-ジメチルピリミジン塩酸塩」を意味する。また、イオン交換水の配合量が「残余」であるとは、イオン交換水の配合量を変量して、各組成物の全量を100質量%に合わせたことを意味する。 (1) Preparation of Compositions Compositions of Comparative Example b-a and Example B-1 were prepared by blending the components shown in Table 3. The blending amount of each component in Table 3 is in "mass %". "Compound (C-1)" in Table 3 means "2-(3,5-dimethylpyrazol-1-yl)-4,6-dimethylpyrimidine hydrochloride". Furthermore, the blending amount of ion-exchanged water being the "remainder" means that the blending amount of ion-exchanged water was changed to adjust the total amount of each composition to 100 mass %.
表3に記載の成分を配合することにより、比較例b-a及び実施例B-1の組成物を調製した。表3における各成分の配合量は、「質量%」単位である。表3における「化合物(C-1)」とは、「2-(3,5-ジメチルピラゾール-1-イル)-4,6-ジメチルピリミジン塩酸塩」を意味する。また、イオン交換水の配合量が「残余」であるとは、イオン交換水の配合量を変量して、各組成物の全量を100質量%に合わせたことを意味する。 (1) Preparation of Compositions Compositions of Comparative Example b-a and Example B-1 were prepared by blending the components shown in Table 3. The blending amount of each component in Table 3 is in "mass %". "Compound (C-1)" in Table 3 means "2-(3,5-dimethylpyrazol-1-yl)-4,6-dimethylpyrimidine hydrochloride". Furthermore, the blending amount of ion-exchanged water being the "remainder" means that the blending amount of ion-exchanged water was changed to adjust the total amount of each composition to 100 mass %.
(2)組成物の色調の評価
得られた各組成物を用いて、比較例a-1等と同様にして、色調の評価を行った。評価結果を表3に示す。 (2) Evaluation of Color Tone of Composition Using each of the obtained compositions, evaluation of color tone was carried out in the same manner as in Comparative Example a-1, etc. The evaluation results are shown in Table 3.
得られた各組成物を用いて、比較例a-1等と同様にして、色調の評価を行った。評価結果を表3に示す。 (2) Evaluation of Color Tone of Composition Using each of the obtained compositions, evaluation of color tone was carried out in the same manner as in Comparative Example a-1, etc. The evaluation results are shown in Table 3.
表3から、以下のことが理解される。
The following can be understood from Table 3:
(A)アミノ化合物及び(B)糖を含み、かつ(C)ピリミジルピラゾール化合物類を含まない、比較例b-1の組成物では、70℃、1週間の保管後に、色調の明確な変化が観察された。
In the composition of Comparative Example b-1, which contains (A) an amino compound and (B) a sugar, but does not contain (C) pyrimidylpyrazole compounds, a clear change in color was observed after storage at 70°C for one week.
これに対して、(A)アミノ化合物及び(B)糖とともに、(C)ピリミジルピラゾール化合物類を配合した、実施例B-1の組成物では、糖の種類及び配合量を同じくする対応の比較例に比べて、70℃、1週間保管後の色調の変化が抑制され、色調の変化が観察されなかった。
In contrast, in the composition of Example B-1, which contains (A) an amino compound and (B) a sugar as well as (C) pyrimidylpyrazole compounds, the change in color after storage at 70°C for one week was suppressed and no change in color was observed, compared to the corresponding comparative example, which contains the same type and amount of sugar.
以上の結果から、本発明の効果は、皮膚化粧料を想定した配合においても妥当することが検証された。
These results demonstrate that the effects of the present invention are also valid for formulations intended for skin cosmetics.
Claims (11)
- (A)アミノ基を有する化合物、
(B)糖、
(C)下記一般式(1):
で表される化合物及びその薬理学的に許容される塩から選択される1種又は2種以上、並びに
(D)水
を含む、化粧料。 (A) a compound having an amino group,
(B) sugar,
(C) a compound represented by the following general formula (1):
and (D) water. - 前記(A)成分が、アミノ酸、アミノ酸誘導体、芳香族アミン、ジペプチド、及びタンパク質から選択される1種又は2種以上である、請求項1に記載の化粧料。 The cosmetic preparation 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.
- 前記(A)成分が、トラネキサム酸、グリシルグリシン、及びテアニンから選択される1種又は2種以上である、請求項2に記載の化粧料。 The cosmetic preparation according to claim 2, wherein the component (A) is one or more selected from tranexamic acid, glycylglycine, and theanine.
- 前記(B)成分が、マルチトール、ソルビトール、フルクトース、エリスリトール、トレハロース、キシリトール、シロキクラゲ多糖体、ヒアルロン酸、及びヒアルロン酸塩から選択される1種又は2種以上を含む、請求項1に記載の化粧料。 The cosmetic preparation according to claim 1, wherein the component (B) contains one or more selected from maltitol, sorbitol, fructose, erythritol, trehalose, xylitol, Tremella fuciformis polysaccharide, hyaluronic acid, and hyaluronate salts.
- 前記(C)成分が、
前記一般式(1)におけるR1、R3、R4、及びR6がメチル基であり、かつ、R2及びR5が水素原子である化合物、
前記一般式(1)におけるR1、R2、R3、R4、及びR6がメチル基であり、かつ、R5が水素原子である化合物、並びに
前記一般式(1)におけるR1、R3、R4、及びR6がメチル基であり、かつ、R2及びR5がエチル基である化合物
から選択される、1種又は2種以上である、請求項1に記載の化粧料。 The component (C) is
A compound in which R 1 , R 3 , R 4 , and R 6 in the general formula (1) are methyl groups, and R 2 and R 5 are hydrogen atoms;
The cosmetic preparation according to claim 1, which is one or more selected from the group consisting of a compound in which R 1 , R 2 , R 3 , R 4 , and R 6 in the general formula (1) are methyl groups and R 5 is a hydrogen atom, and a compound in which R 1 , R 3 , R 4 , and R 6 in the general formula (1) are methyl groups and R 2 and R 5 are ethyl groups. - 前記(C)成分が、
前記一般式(1)におけるR1、R3、R4、及びR6がメチル基であり、かつ、R2及びR5が水素原子である化合物、
前記一般式(1)におけるR1、R2、R3、R4、及びR6がメチル基であり、かつ、R5が水素原子である化合物、並びに
前記一般式(1)におけるR1、R3、R4、及びR6がメチル基であり、かつ、R2及びR5がエチル基である化合物
から選択される、1種又は2種以上である、請求項2に記載の化粧料。 The component (C) is
A compound in which R 1 , R 3 , R 4 , and R 6 in the general formula (1) are methyl groups, and R 2 and R 5 are hydrogen atoms;
The cosmetic preparation according to claim 2, which is one or more selected from the group consisting of a compound in which R 1 , R 2 , R 3 , R 4 , and R 6 in the general formula (1) are methyl groups and R 5 is a hydrogen atom, and a compound in which R 1 , R 3 , R 4 , and R 6 in the general formula (1) are methyl groups and R 2 and R 5 are ethyl groups. - 前記(C)成分が、
前記一般式(1)におけるR1、R3、R4、及びR6がメチル基であり、かつ、R2及びR5が水素原子である化合物、
前記一般式(1)におけるR1、R2、R3、R4、及びR6がメチル基であり、かつ、R5が水素原子である化合物、並びに
前記一般式(1)におけるR1、R3、R4、及びR6がメチル基であり、かつ、R2及びR5がエチル基である化合物
から選択される、1種又は2種以上である、請求項3に記載の化粧料。 The component (C) is
A compound in which R 1 , R 3 , R 4 , and R 6 in the general formula (1) are methyl groups, and R 2 and R 5 are hydrogen atoms;
The cosmetic preparation according to claim 3, which is one or more selected from the group consisting of a compound in which R 1 , R 2 , R 3 , R 4 , and R 6 in the general formula (1) are methyl groups and R 5 is a hydrogen atom, and a compound in which R 1 , R 3 , R 4 , and R 6 in the general formula (1) are methyl groups and R 2 and R 5 are ethyl groups. - 前記(A)成分の配合量が、前記(A)~(C)成分の合計100質量部に対して、1.0質量部以上95質量部以下である、請求項1~7のいずれか一項に記載の化粧料。 The cosmetic preparation according to any one of claims 1 to 7, wherein the blending amount of the (A) component is 1.0 part by mass or more and 95 parts by mass or less per 100 parts by mass of the total of the (A) to (C) components.
- 前記(B)成分の配合量が、前記(A)~(C)成分の合計100質量部に対して、1.0質量部以上90質量部以下である、請求項1~7のいずれか一項に記載の化粧料。 The cosmetic preparation according to any one of claims 1 to 7, wherein the blending amount of the (B) component is 1.0 part by mass or more and 90 parts by mass or less per 100 parts by mass of the total of the (A) to (C) components.
- 前記(C)成分の配合量が、前記(A)~(C)成分の合計100質量部に対して、3.0質量部以上40質量部以下である、請求項1~7のいずれか一項に記載の化粧料。 The cosmetic preparation according to any one of claims 1 to 7, wherein the blending amount of the (C) component is 3.0 parts by mass or more and 40 parts by mass or less per 100 parts by mass of the total of the (A) to (C) components.
- 皮膚化粧料である、請求項1~7のいずれか一項に記載の化粧料。 The cosmetic according to any one of claims 1 to 7, which is a skin cosmetic.
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WO2009099192A1 (en) * | 2008-02-08 | 2009-08-13 | Shiseido Company Ltd. | Skin whitening agent and external preparation for the skin |
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WO2012124436A1 (en) * | 2011-03-17 | 2012-09-20 | 株式会社 資生堂 | Skin cosmetic |
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