WO2001076540A1 - Compositions stimulant la croissance des cheveux - Google Patents
Compositions stimulant la croissance des cheveux Download PDFInfo
- Publication number
- WO2001076540A1 WO2001076540A1 PCT/JP2001/002940 JP0102940W WO0176540A1 WO 2001076540 A1 WO2001076540 A1 WO 2001076540A1 JP 0102940 W JP0102940 W JP 0102940W WO 0176540 A1 WO0176540 A1 WO 0176540A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- composition according
- hair
- polyhydric alcohol
- hair growth
- acid
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 51
- 229940124563 hair growth stimulant Drugs 0.000 title abstract 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims abstract description 47
- ZFMITUMMTDLWHR-UHFFFAOYSA-N Minoxidil Chemical compound NC1=[N+]([O-])C(N)=CC(N2CCCCC2)=N1 ZFMITUMMTDLWHR-UHFFFAOYSA-N 0.000 claims abstract description 33
- 229960003632 minoxidil Drugs 0.000 claims abstract description 33
- MPDGHEJMBKOTSU-YKLVYJNSSA-N 18beta-glycyrrhetic acid Chemical compound C([C@H]1C2=CC(=O)[C@H]34)[C@@](C)(C(O)=O)CC[C@]1(C)CC[C@@]2(C)[C@]4(C)CC[C@@H]1[C@]3(C)CC[C@H](O)C1(C)C MPDGHEJMBKOTSU-YKLVYJNSSA-N 0.000 claims abstract description 32
- FUWUEFKEXZQKKA-UHFFFAOYSA-N beta-thujaplicin Chemical compound CC(C)C=1C=CC=C(O)C(=O)C=1 FUWUEFKEXZQKKA-UHFFFAOYSA-N 0.000 claims abstract description 26
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 23
- 150000005846 sugar alcohols Polymers 0.000 claims abstract description 20
- ZAKOWWREFLAJOT-CEFNRUSXSA-N D-alpha-tocopherylacetate Chemical compound CC(=O)OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C ZAKOWWREFLAJOT-CEFNRUSXSA-N 0.000 claims abstract description 19
- ZAKOWWREFLAJOT-UHFFFAOYSA-N d-alpha-Tocopheryl acetate Natural products CC(=O)OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C ZAKOWWREFLAJOT-UHFFFAOYSA-N 0.000 claims abstract description 19
- 229940042585 tocopherol acetate Drugs 0.000 claims abstract description 19
- CIVCELMLGDGMKZ-UHFFFAOYSA-N 2,4-dichloro-6-methylpyridine-3-carboxylic acid Chemical compound CC1=CC(Cl)=C(C(O)=O)C(Cl)=N1 CIVCELMLGDGMKZ-UHFFFAOYSA-N 0.000 claims abstract description 16
- MPDGHEJMBKOTSU-UHFFFAOYSA-N Glycyrrhetinsaeure Natural products C12C(=O)C=C3C4CC(C)(C(O)=O)CCC4(C)CCC3(C)C1(C)CCC1C2(C)CCC(O)C1(C)C MPDGHEJMBKOTSU-UHFFFAOYSA-N 0.000 claims abstract description 16
- 229960000525 diphenhydramine hydrochloride Drugs 0.000 claims abstract description 16
- 229960003720 enoxolone Drugs 0.000 claims abstract description 16
- MRAMPOPITCOOIN-VIFPVBQESA-N (2r)-n-(3-ethoxypropyl)-2,4-dihydroxy-3,3-dimethylbutanamide Chemical compound CCOCCCNC(=O)[C@H](O)C(C)(C)CO MRAMPOPITCOOIN-VIFPVBQESA-N 0.000 claims abstract description 15
- TUFYVOCKVJOUIR-UHFFFAOYSA-N alpha-Thujaplicin Natural products CC(C)C=1C=CC=CC(=O)C=1O TUFYVOCKVJOUIR-UHFFFAOYSA-N 0.000 claims abstract description 13
- 229930007845 β-thujaplicin Natural products 0.000 claims abstract description 13
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 claims abstract description 12
- 229940041616 menthol Drugs 0.000 claims abstract description 12
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 claims abstract 5
- 230000003779 hair growth Effects 0.000 claims description 30
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 claims description 24
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 16
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims description 16
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims description 14
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims description 13
- 229940058015 1,3-butylene glycol Drugs 0.000 claims description 12
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 12
- 235000019437 butane-1,3-diol Nutrition 0.000 claims description 12
- 239000006210 lotion Substances 0.000 claims description 12
- 239000002253 acid Substances 0.000 claims description 8
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims description 8
- SZXQTJUDPRGNJN-UHFFFAOYSA-N dipropylene glycol Chemical compound OCCCOCCCO SZXQTJUDPRGNJN-UHFFFAOYSA-N 0.000 claims description 7
- 235000014655 lactic acid Nutrition 0.000 claims description 7
- 239000004310 lactic acid Substances 0.000 claims description 7
- 229960003511 macrogol Drugs 0.000 claims description 7
- 235000011187 glycerol Nutrition 0.000 claims description 6
- 239000000443 aerosol Substances 0.000 claims description 4
- 239000003002 pH adjusting agent Substances 0.000 claims description 4
- -1 hinokiti Chemical compound 0.000 claims description 3
- 239000004615 ingredient Substances 0.000 claims description 3
- 239000004094 surface-active agent Substances 0.000 claims description 3
- 238000002156 mixing Methods 0.000 claims description 2
- 229940023735 panthenyl ethyl ether Drugs 0.000 claims description 2
- 229940113120 dipropylene glycol Drugs 0.000 claims 2
- 229960005150 glycerol Drugs 0.000 claims 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims 1
- 235000011167 hydrochloric acid Nutrition 0.000 claims 1
- 235000011007 phosphoric acid Nutrition 0.000 claims 1
- 239000011975 tartaric acid Substances 0.000 claims 1
- 235000002906 tartaric acid Nutrition 0.000 claims 1
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 12
- NOOLISFMXDJSKH-KXUCPTDWSA-N (-)-Menthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@H]1O NOOLISFMXDJSKH-KXUCPTDWSA-N 0.000 description 10
- 239000008213 purified water Substances 0.000 description 10
- 230000000052 comparative effect Effects 0.000 description 8
- 230000000694 effects Effects 0.000 description 7
- 239000002904 solvent Substances 0.000 description 7
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 6
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 6
- 238000002360 preparation method Methods 0.000 description 6
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 4
- 239000004480 active ingredient Substances 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- 238000011156 evaluation Methods 0.000 description 3
- LCGLNKUTAGEVQW-UHFFFAOYSA-N Dimethyl ether Chemical compound COC LCGLNKUTAGEVQW-UHFFFAOYSA-N 0.000 description 2
- FWKQNCXZGNBPFD-UHFFFAOYSA-N Guaiazulene Chemical compound CC(C)C1=CC=C(C)C2=CC=C(C)C2=C1 FWKQNCXZGNBPFD-UHFFFAOYSA-N 0.000 description 2
- 235000010323 ascorbic acid Nutrition 0.000 description 2
- 229960005070 ascorbic acid Drugs 0.000 description 2
- 239000011668 ascorbic acid Substances 0.000 description 2
- KVYGGMBOZFWZBQ-UHFFFAOYSA-N benzyl nicotinate Chemical compound C=1C=CN=CC=1C(=O)OCC1=CC=CC=C1 KVYGGMBOZFWZBQ-UHFFFAOYSA-N 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- RMRCNWBMXRMIRW-BYFNXCQMSA-M cyanocobalamin Chemical compound N#C[Co+]N([C@]1([H])[C@H](CC(N)=O)[C@]\2(CCC(=O)NC[C@H](C)OP(O)(=O)OC3[C@H]([C@H](O[C@@H]3CO)N3C4=CC(C)=C(C)C=C4N=C3)O)C)C/2=C(C)\C([C@H](C/2(C)C)CCC(N)=O)=N\C\2=C\C([C@H]([C@@]/2(CC(N)=O)C)CCC(N)=O)=N\C\2=C(C)/C2=N[C@]1(C)[C@@](C)(CC(N)=O)[C@@H]2CCC(N)=O RMRCNWBMXRMIRW-BYFNXCQMSA-M 0.000 description 2
- 239000000284 extract Substances 0.000 description 2
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 description 2
- 229940088594 vitamin Drugs 0.000 description 2
- 229930003231 vitamin Natural products 0.000 description 2
- 235000013343 vitamin Nutrition 0.000 description 2
- 239000011782 vitamin Substances 0.000 description 2
- MPDGHEJMBKOTSU-WFJWTYAKSA-N (2s,4as,6as,6br,10s,12as)-10-hydroxy-2,4a,6a,6b,9,9,12a-heptamethyl-13-oxo-1,2,3,4,4a,5,6,6a,6b,7,8,8a,9,10,11,12,12a,12b,13,14b-icosahydropicene-2-carboxylic acid Chemical compound C12C(=O)C=C3C4C[C@@](C)(C(O)=O)CC[C@]4(C)CC[C@@]3(C)[C@]1(C)CCC1[C@]2(C)CC[C@H](O)C1(C)C MPDGHEJMBKOTSU-WFJWTYAKSA-N 0.000 description 1
- DSSYKIVIOFKYAU-XCBNKYQSSA-N (R)-camphor Chemical compound C1C[C@@]2(C)C(=O)C[C@@H]1C2(C)C DSSYKIVIOFKYAU-XCBNKYQSSA-N 0.000 description 1
- SPSPIUSUWPLVKD-UHFFFAOYSA-N 2,3-dibutyl-6-methylphenol Chemical compound CCCCC1=CC=C(C)C(O)=C1CCCC SPSPIUSUWPLVKD-UHFFFAOYSA-N 0.000 description 1
- IJALWSVNUBBQRA-UHFFFAOYSA-N 4-Isopropyl-3-methylphenol Chemical compound CC(C)C1=CC=C(O)C=C1C IJALWSVNUBBQRA-UHFFFAOYSA-N 0.000 description 1
- HBTAOSGHCXUEKI-UHFFFAOYSA-N 4-chloro-n,n-dimethyl-3-nitrobenzenesulfonamide Chemical compound CN(C)S(=O)(=O)C1=CC=C(Cl)C([N+]([O-])=O)=C1 HBTAOSGHCXUEKI-UHFFFAOYSA-N 0.000 description 1
- HIQIXEFWDLTDED-UHFFFAOYSA-N 4-hydroxy-1-piperidin-4-ylpyrrolidin-2-one Chemical compound O=C1CC(O)CN1C1CCNCC1 HIQIXEFWDLTDED-UHFFFAOYSA-N 0.000 description 1
- SQDAZGGFXASXDW-UHFFFAOYSA-N 5-bromo-2-(trifluoromethoxy)pyridine Chemical compound FC(F)(F)OC1=CC=C(Br)C=N1 SQDAZGGFXASXDW-UHFFFAOYSA-N 0.000 description 1
- 235000016068 Berberis vulgaris Nutrition 0.000 description 1
- 241000335053 Beta vulgaris Species 0.000 description 1
- 241000700199 Cavia porcellus Species 0.000 description 1
- GHXZTYHSJHQHIJ-UHFFFAOYSA-N Chlorhexidine Chemical compound C=1C=C(Cl)C=CC=1NC(N)=NC(N)=NCCCCCCN=C(N)N=C(N)NC1=CC=C(Cl)C=C1 GHXZTYHSJHQHIJ-UHFFFAOYSA-N 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 1
- 229920001287 Chondroitin sulfate Polymers 0.000 description 1
- 241000723346 Cinnamomum camphora Species 0.000 description 1
- 235000015655 Crocus sativus Nutrition 0.000 description 1
- 244000124209 Crocus sativus Species 0.000 description 1
- SNPLKNRPJHDVJA-ZETCQYMHSA-N D-panthenol Chemical compound OCC(C)(C)[C@@H](O)C(=O)NCCCO SNPLKNRPJHDVJA-ZETCQYMHSA-N 0.000 description 1
- ZGTMUACCHSMWAC-UHFFFAOYSA-L EDTA disodium salt (anhydrous) Chemical compound [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 235000008694 Humulus lupulus Nutrition 0.000 description 1
- 229940124091 Keratolytic Drugs 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 240000004371 Panax ginseng Species 0.000 description 1
- 235000002789 Panax ginseng Nutrition 0.000 description 1
- 241001529742 Rosmarinus Species 0.000 description 1
- 229920002385 Sodium hyaluronate Polymers 0.000 description 1
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 1
- 230000002378 acidificating effect Effects 0.000 description 1
- 239000012190 activator Substances 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 230000000996 additive effect Effects 0.000 description 1
- 239000000853 adhesive Substances 0.000 description 1
- 230000001070 adhesive effect Effects 0.000 description 1
- 239000010775 animal oil Substances 0.000 description 1
- 229940121363 anti-inflammatory agent Drugs 0.000 description 1
- 239000002260 anti-inflammatory agent Substances 0.000 description 1
- 229940125715 antihistaminic agent Drugs 0.000 description 1
- 239000000739 antihistaminic agent Substances 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 235000006708 antioxidants Nutrition 0.000 description 1
- 229950004580 benzyl nicotinate Drugs 0.000 description 1
- 235000010354 butylated hydroxytoluene Nutrition 0.000 description 1
- 229960000846 camphor Drugs 0.000 description 1
- 229930008380 camphor Natural products 0.000 description 1
- 239000004202 carbamide Substances 0.000 description 1
- 229960003260 chlorhexidine Drugs 0.000 description 1
- 229940059329 chondroitin sulfate Drugs 0.000 description 1
- 235000009508 confectionery Nutrition 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- 229960002104 cyanocobalamin Drugs 0.000 description 1
- 235000000639 cyanocobalamin Nutrition 0.000 description 1
- 239000011666 cyanocobalamin Substances 0.000 description 1
- GVJHHUAWPYXKBD-UHFFFAOYSA-N d-alpha-tocopherol Natural products OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 description 1
- 229940031578 diisopropyl adipate Drugs 0.000 description 1
- 239000000975 dye Substances 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 239000000417 fungicide Substances 0.000 description 1
- 239000003349 gelling agent Substances 0.000 description 1
- 235000008434 ginseng Nutrition 0.000 description 1
- 229960002350 guaiazulen Drugs 0.000 description 1
- 230000003700 hair damage Effects 0.000 description 1
- 239000003676 hair preparation Substances 0.000 description 1
- 239000003906 humectant Substances 0.000 description 1
- 229930195733 hydrocarbon Natural products 0.000 description 1
- 150000002430 hydrocarbons Chemical class 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical compound [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- NFIDBGJMFKNGGQ-UHFFFAOYSA-N isopropylmethylphenol Natural products CC(C)CC1=CC=CC=C1O NFIDBGJMFKNGGQ-UHFFFAOYSA-N 0.000 description 1
- 230000001530 keratinolytic effect Effects 0.000 description 1
- 239000003410 keratolytic agent Substances 0.000 description 1
- 239000002932 luster Substances 0.000 description 1
- 230000002503 metabolic effect Effects 0.000 description 1
- 235000001968 nicotinic acid Nutrition 0.000 description 1
- 239000011664 nicotinic acid Substances 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 235000019198 oils Nutrition 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 238000010979 pH adjustment Methods 0.000 description 1
- 229940101267 panthenol Drugs 0.000 description 1
- 235000020957 pantothenol Nutrition 0.000 description 1
- 239000011619 pantothenol Substances 0.000 description 1
- 125000001232 pantothenyl group Chemical group C(CCNC([C@H](O)C(C)(C)CO)=O)(=O)* 0.000 description 1
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 description 1
- TXGSOSAONMOPDL-UHFFFAOYSA-N propan-2-yl 3,4,5-trihydroxybenzoate Chemical compound CC(C)OC(=O)C1=CC(O)=C(O)C(O)=C1 TXGSOSAONMOPDL-UHFFFAOYSA-N 0.000 description 1
- ZUFQODAHGAHPFQ-UHFFFAOYSA-N pyridoxine hydrochloride Chemical compound Cl.CC1=NC=C(CO)C(CO)=C1O ZUFQODAHGAHPFQ-UHFFFAOYSA-N 0.000 description 1
- 229960004172 pyridoxine hydrochloride Drugs 0.000 description 1
- 235000019171 pyridoxine hydrochloride Nutrition 0.000 description 1
- 239000011764 pyridoxine hydrochloride Substances 0.000 description 1
- 150000003242 quaternary ammonium salts Chemical class 0.000 description 1
- 229960000342 retinol acetate Drugs 0.000 description 1
- QGNJRVVDBSJHIZ-QHLGVNSISA-N retinyl acetate Chemical compound CC(=O)OC\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C QGNJRVVDBSJHIZ-QHLGVNSISA-N 0.000 description 1
- 235000019173 retinyl acetate Nutrition 0.000 description 1
- 239000011770 retinyl acetate Substances 0.000 description 1
- 235000013974 saffron Nutrition 0.000 description 1
- 239000004248 saffron Substances 0.000 description 1
- 229960004889 salicylic acid Drugs 0.000 description 1
- 230000001953 sensory effect Effects 0.000 description 1
- 230000037384 skin absorption Effects 0.000 description 1
- 231100000274 skin absorption Toxicity 0.000 description 1
- HRZFUMHJMZEROT-UHFFFAOYSA-L sodium disulfite Chemical compound [Na+].[Na+].[O-]S(=O)S([O-])(=O)=O HRZFUMHJMZEROT-UHFFFAOYSA-L 0.000 description 1
- 229940037001 sodium edetate Drugs 0.000 description 1
- 229940010747 sodium hyaluronate Drugs 0.000 description 1
- 235000010262 sodium metabisulphite Nutrition 0.000 description 1
- YWIVKILSMZOHHF-QJZPQSOGSA-N sodium;(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- Chemical compound [Na+].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 YWIVKILSMZOHHF-QJZPQSOGSA-N 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- UIERGBJEBXXIGO-UHFFFAOYSA-N thiamine mononitrate Chemical compound [O-][N+]([O-])=O.CC1=C(CCO)SC=[N+]1CC1=CN=C(C)N=C1N UIERGBJEBXXIGO-UHFFFAOYSA-N 0.000 description 1
- 229940098465 tincture Drugs 0.000 description 1
- 229930003799 tocopherol Natural products 0.000 description 1
- 235000010384 tocopherol Nutrition 0.000 description 1
- 229960001295 tocopherol Drugs 0.000 description 1
- 239000011732 tocopherol Substances 0.000 description 1
- 230000001256 tonic effect Effects 0.000 description 1
- 229940124549 vasodilator Drugs 0.000 description 1
- 239000003071 vasodilator agent Substances 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 150000003722 vitamin derivatives Chemical class 0.000 description 1
- 229920003169 water-soluble polymer Polymers 0.000 description 1
- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-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
- A61K8/42—Amides
-
- 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
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/34—Alcohols
-
- 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
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/35—Ketones, e.g. benzophenone
-
- 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
- A61K8/494—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
- A61K8/4953—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom containing pyrimidine ring derivatives, e.g. minoxidil
-
- 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
- A61K8/63—Steroids; 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
- A61K8/67—Vitamins
- A61K8/671—Vitamin A; Derivatives thereof, e.g. ester of vitamin A acid, ester of retinol, retinol, retinal
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q7/00—Preparations for affecting hair growth
Definitions
- the present invention relates to a hair restoration composition containing minoxidil as an active ingredient, and more particularly, to a hair restoration composition having an improved feeling in use.
- Minoxidil has the chemical name 6- (1-piperidinyl) -1,2,4-pyrimidinediamine-13-oxide, and its application as a hair restorer is described in U.S. Patent No. 4,139,619. I have. Minoxidil has excellent hair-growth and hair-growth effects when applied externally, so hair growth agents containing minoxidil (hereinafter referred to as “minoxidil preparations”) have been widely accepted and their sales have been record-setting.
- minoxidil preparations are used daily for a long period of time on the head, preparations with excellent feeling in use are required.
- the feeling of use is important for a hair restorer with an increased concentration of minoxydil.
- an object of the present invention is to provide a minoxidil-containing hair growth composition having a higher feeling of use than the currently provided minoxidil preparations. Disclosure of the invention
- the present inventors have conducted intensive studies on the solvent composition and additive compounds of the minoxidil formulation in order to solve the above problems, and as a result, selected a polyvalent alcohol / ethanol / water ternary system as the solvent. By selecting and adding a specific compound to this, when minoxidil is blended at a high concentration, Nevertheless, they have found that a stable and excellent feeling in use can be obtained, and the present invention has been completed.
- the present invention relates to a group comprising 1 to 6% by mass of minoxidil, polyhydric alcohol, ethanol and water, and further comprising menthol, vitamin E acetate, pantothenyl ethyl ether, hinokitiol, glycyrrhetinic acid and diphenhydramine hydrochloride.
- An object of the present invention is to provide a hair growth composition comprising one or more selected components.
- the present invention comprises 1 to 6% by mass of minoxidil, polyhydric alcohol, ethanol, menthol and water, and further comprises a group consisting of vitamin E acetate, pantothenylethyl ether, hinokitiol, glycyrrhetinic acid and diphenhydramine hydrochloride.
- An object of the present invention is to provide a hair growth composition comprising one or more selected components.
- the present invention provides a group comprising 1 to 6% by mass of minoxidil, polyhydric alcohol, ethanol, vitamin E acetate and water, and further comprising menthol, panthenylethyl ether, hinokitiol, glycyrrhetinic acid and diphenhydramine hydrochloride.
- An object of the present invention is to provide a hair growth composition comprising one or more components selected from the group consisting of:
- the present invention comprises 1 to 6% by mass of minoxidil, polyhydric alcohol, ethanol, pantothenyl ethyl ether and water, and further contains menthol, vitamin E acetate, hinokitiol, glycyrrhetinic acid and diphenhydric hydrochloride.
- Another object of the present invention is to provide a hair growth composition comprising one or more components selected from the group consisting of dramin.
- the content of minoxidil as an active ingredient is in the range of 1 to 6% by mass (hereinafter, simply indicated by “%”).
- the effect of the present invention is remarkable in a hair growth composition containing 2% or more.
- the solvent system for dissolving this minoxidil is a ternary system composed of polyhydric alcohol, ethanol and water.
- the amount of each component of the solvent system is not particularly limited, but the amount of ethanol is about 25 to 75% and the amount of water is about 5 to 30% in the final composition. Is preferred.
- the polyhydric alcohol is preferably used as a solubilizer in an amount of 5 to 30%, and more preferably 8 to 20% in terms of usability.
- polyhydric alcohol 1,3-butylendalcol, glycerin, dipropylene glycol, macrogol 300, macrogol 400, macrogol 600, etc.
- glycerin 1,3-butylendalcol, glycerin, dipropylene glycol, macrogol 300, macrogol 400, macrogol 600, etc.
- the components to be added to and mixed with the hair growth composition of the present invention were selected from the group consisting of menthol, vitamin E acetate, pantothenylethyl ether, hinokitiol, glycyrrhetinic acid and diphenhydramine hydrochloride.
- Ingredients hereinafter, referred to as “selected ingredients”.
- selected ingredients those having particularly high effectiveness include menthol, vitamin E acetate and pantothenyl ethyl ether, and it is more preferable to add these as essential components.
- the amount of the selective active ingredient to be added is not particularly limited, and can be determined experimentally in consideration of the stability of minoxidil used or the composition of the solvent system.
- menthol which is a particularly preferred selection component, is preferably blended in an amount of about 0.2 to 0.4% in the final composition.
- vitamin E acetate is 0.016 to 0.15%
- pantothenyl ethyl ether is 0.5 to 1.5%
- hinokitiol is 0.02 to 0.08%
- glycyrrhetinic acid is 0.08%.
- various components used in general external preparations for example, excipients, vasodilators (capium chloride, dimethyl nicotinate, benzyl nicotinate, Extracts, Panax ginseng extract, Toragarachi tincture, etc., antihistamines (isotipendyl hydrochloride, etc.), anti-inflammatory agents (guaiazulene, etc.), keratolytics (urea, salicylic acid, etc.), fungicides (chlorhexidine dalconate, isopropylmethylphenol) , Quaternary ammonium salt, pyroctone laminate, etc.), humectant (sodium hyaluronate, chondroitin sulfate, etc.), various animals and plants (yew, buttonamp, kanzo, guinea pig, batsushi, beet, power Wara
- the hair growth composition of the present invention be substantially free of a surfactant.
- the hair growth composition of the present invention is prepared by blending the above components according to a conventional method.
- the pH of the hair growth composition is about 5.5 to 9.5. It is more preferable to set the temperature in the range of about 5.5 to 6.5, which is particularly weakly acidic.
- an appropriate acid and / or base can be used as a pH adjuster.
- a pH adjuster examples include citric acid, hydrochloric acid, lactic acid, and phosphoric acid. be able to.
- the hair growth composition of the present invention thus obtained can be used as a suitable external preparation such as a lotion, an aerosol, a tonic, a cream, an ointment, a gel and the like.
- Example 1 Example 1
- the present invention 2 The present invention 3
- the present invention 4 The present invention 5
- the present invention 6 The present invention 7
- the present invention 8 The present invention 9
- Invention product 23 Invention product 24 Invention product 25 Invention product 26 Invention product 27 Invention product 28
- 1,3-butylene glycol 5.0 g 1 0.0 g chryselino 1 5.0 g 5.0 g 3.0 g
- the feeling of use of the hair growth lotion shown in Table 9 and Table 10 was evaluated by a sensory test by four expert panelists in their 20s to 40s.
- the evaluation was performed by a left-right paired comparison using a half head.
- the right side of the head is the non-administration site, and the left side is the lotion application site, applying 1 mL twice a day for 3 weeks, and evaluating the hair condition every week according to the evaluation criteria in Table 11 did.
- Table 12 shows the average scores of the four panelists.
- Table 9 Inventive product 47 Inventive product 48 Inventive product 49 Minoxidil 1.0 g 1.0 g 1.0 g
- Vitamin E acetate 0.08 g
- Important elements of beautiful and healthy hair include firmness, shine, and moistness.
- the effect of the hair growth lotion of the present invention on these factors was determined by a 3-week usability test.
- the hair growth lotion of the example showed a higher effect from an earlier stage than the hair growth lotion of the comparative example. Furthermore, it has been found that an unprecedented feeling of use is obtained by combining a plurality of selected components. In addition, the effect of improving the usability was obtained in a well-balanced manner for all three factors, and it was found that the composition had an overall effect of improving the usability as a hair preparation. that's all
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Abstract
Compositions stimulant la croissance des cheveux et présentant un confort d'utilisation amélioré. Ces compositions contiennent 1 à 6 % en masse de minoxidil, un alcool polyhydrique, éthanol et de l'eau, ainsi qu'au moins un constituant sélectionné dans le groupe constitué par menthol, vitamine E acétate, pantothényléthyléther, hinokitiol, acide glycyrrhétinique et hydrochlorure de diphenhydramine.
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU2001244729A AU2001244729A1 (en) | 2000-04-07 | 2001-04-05 | Hair growth stimulant compositions |
| JP2001574059A JPWO2001076540A1 (ja) | 2000-04-07 | 2001-04-05 | 育毛組成物 |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2000106497 | 2000-04-07 | ||
| JP2000-106497 | 2000-04-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO2001076540A1 true WO2001076540A1 (fr) | 2001-10-18 |
Family
ID=18619655
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/JP2001/002940 WO2001076540A1 (fr) | 2000-04-07 | 2001-04-05 | Compositions stimulant la croissance des cheveux |
Country Status (3)
| Country | Link |
|---|---|
| JP (1) | JPWO2001076540A1 (fr) |
| AU (1) | AU2001244729A1 (fr) |
| WO (1) | WO2001076540A1 (fr) |
Cited By (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2006342090A (ja) * | 2005-06-08 | 2006-12-21 | Taisho Pharmaceut Co Ltd | エアゾール剤 |
| ES2315115A1 (es) * | 2006-07-31 | 2009-03-16 | Jose Ignacio Navarro Sanchez | Solucion concentrada de minoxidil al 20%. |
| JP2013056882A (ja) * | 2012-09-28 | 2013-03-28 | Taisho Pharmaceutical Co Ltd | エアゾール剤 |
| JP2016138094A (ja) * | 2015-01-23 | 2016-08-04 | 大正製薬株式会社 | 外用組成物 |
| JP2016145179A (ja) * | 2015-02-06 | 2016-08-12 | ダイヤ製薬株式会社 | ミノキシジル含有外用液剤および外用液剤の製造方法 |
| JP2020023467A (ja) * | 2018-01-19 | 2020-02-13 | ロート製薬株式会社 | 外用製剤、液切れ性を改善する方法、および、液切れ性改善剤 |
| JP2020105217A (ja) * | 2015-03-27 | 2020-07-09 | 大正製薬株式会社 | ローション剤 |
| JP2021014416A (ja) * | 2019-07-10 | 2021-02-12 | ロート製薬株式会社 | 外用製剤 |
| JP2021165305A (ja) * | 2016-09-15 | 2021-10-14 | 大正製薬株式会社 | 外用組成物 |
Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH054908A (ja) * | 1990-09-28 | 1993-01-14 | Taisho Pharmaceut Co Ltd | ミノキシジル含有育毛剤 |
| JPH06211681A (ja) * | 1993-01-12 | 1994-08-02 | Taisho Pharmaceut Co Ltd | テストステロン−５α−リダクターゼ阻害剤 |
| JPH08277209A (ja) * | 1995-04-07 | 1996-10-22 | Taisho Pharmaceut Co Ltd | 育毛剤 |
| JPH09188620A (ja) * | 1996-01-05 | 1997-07-22 | Taisho Pharmaceut Co Ltd | ヒノキチオール含有組成物 |
| EP0970683A1 (fr) * | 1997-01-23 | 2000-01-12 | Taisho Pharmaceutical Co. Ltd | Tonique capillaire persistant |
| JP2000198719A (ja) * | 1998-10-29 | 2000-07-18 | Taisho Pharmaceut Co Ltd | 発毛剤 |
-
2001
- 2001-04-05 JP JP2001574059A patent/JPWO2001076540A1/ja not_active Withdrawn
- 2001-04-05 AU AU2001244729A patent/AU2001244729A1/en not_active Abandoned
- 2001-04-05 WO PCT/JP2001/002940 patent/WO2001076540A1/fr active Application Filing
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH054908A (ja) * | 1990-09-28 | 1993-01-14 | Taisho Pharmaceut Co Ltd | ミノキシジル含有育毛剤 |
| JPH06211681A (ja) * | 1993-01-12 | 1994-08-02 | Taisho Pharmaceut Co Ltd | テストステロン−５α−リダクターゼ阻害剤 |
| JPH08277209A (ja) * | 1995-04-07 | 1996-10-22 | Taisho Pharmaceut Co Ltd | 育毛剤 |
| JPH09188620A (ja) * | 1996-01-05 | 1997-07-22 | Taisho Pharmaceut Co Ltd | ヒノキチオール含有組成物 |
| EP0970683A1 (fr) * | 1997-01-23 | 2000-01-12 | Taisho Pharmaceutical Co. Ltd | Tonique capillaire persistant |
| JP2000198719A (ja) * | 1998-10-29 | 2000-07-18 | Taisho Pharmaceut Co Ltd | 発毛剤 |
Cited By (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2006342090A (ja) * | 2005-06-08 | 2006-12-21 | Taisho Pharmaceut Co Ltd | エアゾール剤 |
| ES2315115A1 (es) * | 2006-07-31 | 2009-03-16 | Jose Ignacio Navarro Sanchez | Solucion concentrada de minoxidil al 20%. |
| JP2013056882A (ja) * | 2012-09-28 | 2013-03-28 | Taisho Pharmaceutical Co Ltd | エアゾール剤 |
| JP2016138094A (ja) * | 2015-01-23 | 2016-08-04 | 大正製薬株式会社 | 外用組成物 |
| JP2016145179A (ja) * | 2015-02-06 | 2016-08-12 | ダイヤ製薬株式会社 | ミノキシジル含有外用液剤および外用液剤の製造方法 |
| JP2020105217A (ja) * | 2015-03-27 | 2020-07-09 | 大正製薬株式会社 | ローション剤 |
| JP7067581B2 (ja) | 2015-03-27 | 2022-05-16 | 大正製薬株式会社 | ローション剤 |
| JP2021165305A (ja) * | 2016-09-15 | 2021-10-14 | 大正製薬株式会社 | 外用組成物 |
| JP2020023467A (ja) * | 2018-01-19 | 2020-02-13 | ロート製薬株式会社 | 外用製剤、液切れ性を改善する方法、および、液切れ性改善剤 |
| JP2021014416A (ja) * | 2019-07-10 | 2021-02-12 | ロート製薬株式会社 | 外用製剤 |
| JP7488634B2 (ja) | 2019-07-10 | 2024-05-22 | ロート製薬株式会社 | 外用製剤 |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2001244729A1 (en) | 2001-10-23 |
| JPWO2001076540A1 (ja) | 2004-01-08 |
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