CN1434698A - 毛发生长组合物 - Google Patents
毛发生长组合物 Download PDFInfo
- Publication number
- CN1434698A CN1434698A CN01810823A CN01810823A CN1434698A CN 1434698 A CN1434698 A CN 1434698A CN 01810823 A CN01810823 A CN 01810823A CN 01810823 A CN01810823 A CN 01810823A CN 1434698 A CN1434698 A CN 1434698A
- Authority
- CN
- China
- Prior art keywords
- hair growth
- growth stimulant
- stimulant compositions
- quality
- loniten
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 40
- 229940124563 hair growth stimulant Drugs 0.000 title claims abstract description 27
- ZFMITUMMTDLWHR-UHFFFAOYSA-N Minoxidil Chemical compound NC1=[N+]([O-])C(N)=CC(N2CCCCC2)=N1 ZFMITUMMTDLWHR-UHFFFAOYSA-N 0.000 claims abstract description 36
- 229960003632 minoxidil Drugs 0.000 claims abstract description 36
- 238000002360 preparation method Methods 0.000 claims abstract description 19
- 150000005846 sugar alcohols Polymers 0.000 claims abstract description 14
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 13
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 25
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 claims description 24
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 18
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims description 13
- 229940058015 1,3-butylene glycol Drugs 0.000 claims description 12
- 235000019437 butane-1,3-diol Nutrition 0.000 claims description 12
- 239000003795 chemical substances by application Substances 0.000 claims description 10
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 9
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims description 8
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims description 8
- 239000006210 lotion Substances 0.000 claims description 8
- SZXQTJUDPRGNJN-UHFFFAOYSA-N dipropylene glycol Chemical compound OCCCOCCCO SZXQTJUDPRGNJN-UHFFFAOYSA-N 0.000 claims description 6
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical group CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 claims description 5
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 claims description 5
- 239000002253 acid Substances 0.000 claims description 5
- 235000014655 lactic acid Nutrition 0.000 claims description 5
- 239000004310 lactic acid Substances 0.000 claims description 5
- 229940041616 menthol Drugs 0.000 claims description 5
- -1 pantoyl ethylether Chemical compound 0.000 claims description 5
- 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 description 4
- 230000001476 alcoholic effect Effects 0.000 claims description 4
- 239000004094 surface-active agent Substances 0.000 claims description 3
- TUFYVOCKVJOUIR-UHFFFAOYSA-N 2-hydroxy-3-propan-2-ylcyclohepta-2,4,6-trien-1-one Chemical compound CC(C)C=1C=CC=CC(=O)C=1O TUFYVOCKVJOUIR-UHFFFAOYSA-N 0.000 claims description 2
- 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 description 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Natural products CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims description 2
- 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 description 2
- 239000000084 colloidal system Substances 0.000 claims description 2
- 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 description 2
- 229960003720 enoxolone Drugs 0.000 claims description 2
- 229940035423 ethyl ether Drugs 0.000 claims description 2
- 229940042585 tocopherol acetate Drugs 0.000 claims description 2
- 238000000034 method Methods 0.000 claims 1
- 239000013078 crystal Substances 0.000 abstract 2
- 238000001556 precipitation Methods 0.000 abstract 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 24
- 238000002425 crystallisation Methods 0.000 description 14
- 230000008025 crystallization Effects 0.000 description 14
- 239000002904 solvent Substances 0.000 description 9
- 239000002351 wastewater Substances 0.000 description 8
- HEMHJVSKTPXQMS-UHFFFAOYSA-M sodium hydroxide Inorganic materials [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 7
- 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
- 229920002565 Polyethylene Glycol 400 Polymers 0.000 description 4
- 239000000443 aerosol Substances 0.000 description 4
- 230000003779 hair growth Effects 0.000 description 4
- 239000004615 ingredient Substances 0.000 description 4
- 230000000694 effects Effects 0.000 description 3
- 238000004321 preservation Methods 0.000 description 3
- YBJHBAHKTGYVGT-ZKWXMUAHSA-N (+)-Biotin Chemical compound N1C(=O)N[C@@H]2[C@H](CCCCC(=O)O)SC[C@@H]21 YBJHBAHKTGYVGT-ZKWXMUAHSA-N 0.000 description 2
- GHOKWGTUZJEAQD-ZETCQYMHSA-N (D)-(+)-Pantothenic acid Chemical compound OCC(C)(C)[C@@H](O)C(=O)NCCC(O)=O GHOKWGTUZJEAQD-ZETCQYMHSA-N 0.000 description 2
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 description 2
- 239000004322 Butylated hydroxytoluene Substances 0.000 description 2
- NLZUEZXRPGMBCV-UHFFFAOYSA-N Butylhydroxytoluene Chemical compound CC1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1 NLZUEZXRPGMBCV-UHFFFAOYSA-N 0.000 description 2
- LCGLNKUTAGEVQW-UHFFFAOYSA-N Dimethyl ether Chemical compound COC LCGLNKUTAGEVQW-UHFFFAOYSA-N 0.000 description 2
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-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
- 235000010354 butylated hydroxytoluene Nutrition 0.000 description 2
- 229940095259 butylated hydroxytoluene Drugs 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
- 239000007952 growth promoter Substances 0.000 description 2
- JLFNLZLINWHATN-UHFFFAOYSA-N pentaethylene glycol Chemical compound OCCOCCOCCOCCOCCO JLFNLZLINWHATN-UHFFFAOYSA-N 0.000 description 2
- 239000004033 plastic 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
- 238000003756 stirring Methods 0.000 description 2
- 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
- ZJRHNNNACBPWEB-UHFFFAOYSA-N 2-[2-(dimethylamino)ethoxy]ethyl phenothiazine-10-carboxylate;hydron;chloride Chemical compound Cl.C1=CC=C2N(C(=O)OCCOCCN(C)C)C3=CC=CC=C3SC2=C1 ZJRHNNNACBPWEB-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
- 241000132023 Bellis perennis Species 0.000 description 1
- 235000002566 Capsicum Nutrition 0.000 description 1
- 240000008574 Capsicum frutescens Species 0.000 description 1
- GHOKWGTUZJEAQD-UHFFFAOYSA-N Chick antidermatitis factor Natural products OCC(C)(C)C(O)C(=O)NCCC(O)=O GHOKWGTUZJEAQD-UHFFFAOYSA-N 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
- 229920001287 Chondroitin sulfate Polymers 0.000 description 1
- RGHNJXZEOKUKBD-UHFFFAOYSA-N D-gluconic acid Natural products OCC(O)C(O)C(O)C(O)C(O)=O RGHNJXZEOKUKBD-UHFFFAOYSA-N 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 1
- RGHNJXZEOKUKBD-SQOUGZDYSA-N Gluconic acid Natural products OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O RGHNJXZEOKUKBD-SQOUGZDYSA-N 0.000 description 1
- FWKQNCXZGNBPFD-UHFFFAOYSA-N Guaiazulene Chemical compound CC(C)C1=CC=C(C)C2=CC=C(C)C2=C1 FWKQNCXZGNBPFD-UHFFFAOYSA-N 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 240000005001 Paeonia suffruticosa Species 0.000 description 1
- 235000003889 Paeonia suffruticosa Nutrition 0.000 description 1
- 244000295490 Salvia japonica Species 0.000 description 1
- 235000005794 Salvia japonica Nutrition 0.000 description 1
- 229930003427 Vitamin E Natural products 0.000 description 1
- 230000003213 activating effect Effects 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- VQKFNUFAXTZWDK-UHFFFAOYSA-N alpha-methylfuran Natural products CC1=CC=CO1 VQKFNUFAXTZWDK-UHFFFAOYSA-N 0.000 description 1
- 239000010775 animal oil Substances 0.000 description 1
- 230000000844 anti-bacterial effect Effects 0.000 description 1
- 229940121363 anti-inflammatory agent Drugs 0.000 description 1
- 239000002260 anti-inflammatory agent Substances 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 230000003078 antioxidant effect Effects 0.000 description 1
- 235000006708 antioxidants Nutrition 0.000 description 1
- 229950004580 benzyl nicotinate Drugs 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 229960002685 biotin Drugs 0.000 description 1
- 235000020958 biotin Nutrition 0.000 description 1
- 239000011616 biotin Substances 0.000 description 1
- IMKUQCXMPMOQOI-UHFFFAOYSA-N butanoic acid;n,n-dimethylmethanamine Chemical compound C[NH+](C)C.CCCC([O-])=O IMKUQCXMPMOQOI-UHFFFAOYSA-N 0.000 description 1
- 229940025250 camphora Drugs 0.000 description 1
- 239000010238 camphora Substances 0.000 description 1
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- 235000013877 carbamide Nutrition 0.000 description 1
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- 229960002104 cyanocobalamin Drugs 0.000 description 1
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- 229940031578 diisopropyl adipate Drugs 0.000 description 1
- 229960002002 dimethoxanate hydrochloride Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 239000000975 dye Substances 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 239000000284 extract Substances 0.000 description 1
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 description 1
- 239000003349 gelling agent Substances 0.000 description 1
- 235000020710 ginseng extract Nutrition 0.000 description 1
- 239000000174 gluconic acid Substances 0.000 description 1
- 235000012208 gluconic acid Nutrition 0.000 description 1
- 229960002350 guaiazulen Drugs 0.000 description 1
- 229930195733 hydrocarbon Natural products 0.000 description 1
- 150000002430 hydrocarbons Chemical class 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 229960003511 macrogol Drugs 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 239000012046 mixed solvent Substances 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 230000007935 neutral effect Effects 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 229940055726 pantothenic acid Drugs 0.000 description 1
- 235000019161 pantothenic acid Nutrition 0.000 description 1
- 239000011713 pantothenic acid Substances 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
- 210000002826 placenta Anatomy 0.000 description 1
- 230000001737 promoting effect Effects 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
- 229960004889 salicylic acid Drugs 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
- 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
- 235000013599 spices Nutrition 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- UEUXEKPTXMALOB-UHFFFAOYSA-J tetrasodium;2-[2-[bis(carboxylatomethyl)amino]ethyl-(carboxylatomethyl)amino]acetate Chemical compound [Na+].[Na+].[Na+].[Na+].[O-]C(=O)CN(CC([O-])=O)CCN(CC([O-])=O)CC([O-])=O UEUXEKPTXMALOB-UHFFFAOYSA-J 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
- 230000024883 vasodilation Effects 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229940046009 vitamin E Drugs 0.000 description 1
- 235000019165 vitamin E Nutrition 0.000 description 1
- 239000011709 vitamin E Substances 0.000 description 1
- 229920003169 water-soluble polymer Polymers 0.000 description 1
- 239000000080 wetting agent Substances 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
- A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61K8/34—Alcohols
- A61K8/345—Alcohols containing more than one hydroxy group
-
- 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
- A61K8/49—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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Birds (AREA)
- Emergency Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Dermatology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
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Abstract
本发明提供即使在低温下也难以析出结晶而且稳定性高的、配合了高浓度敏乐定的制剂。在配合了10~50质量%的水与3质量%以上的敏乐定的制剂中含有1种以上的多元醇8~30质量%、pH为5.5~6.5的毛发生长组合物,其结晶难以析出,稳定性高。
Description
技术领域
本发明涉及一种以敏乐定为有效成分的毛发生长组合物。更具体来说虽然是高浓度敏乐定(minoxidil),但在低温时也不会产生结晶出现等问题的毛发生长组合物。
背景技术
敏乐定的化学名称是6-(1-哌啶基)-2,4-嘧啶二胺-3-氧化物,据美国专利第4,139,619号中记载适用于生发剂。而且由于敏乐定外用时有更优良的生发、养发作用,所以配合了敏乐定的生发剂(以下叫作“敏乐定制剂”)被广泛采用,销售额也是创记录的。
关于这种制剂,为了提高它的有效性,要求提供敏乐定浓度更高的制剂。如特开昭63-150211号公报中记载的那样,过去3~5质量%浓度的敏乐定制剂容易调制。
发明内容
为了改善毛发生长组合物的性能,当制剂为配合了10~50质量%水的高浓度敏乐定制剂(以下称“高敏乐定制剂”)的时候,在低温状态下长期保存就会发生结晶析出的现象。而且,要使这种析出的结晶再溶解很费事,因此,就明确了在寒冷地区使用毛发生长组合物及在寒冷的场所保管生发剂组合物成为要解决的问题。
本发明的目的是提供一种即使在低温状态长期放置也没有结晶析出、稳定的高敏乐定制剂。
为实现上述目的,本发明对高敏乐定制剂的溶剂组成等进行研究后发现,选择特定浓度的多元醇作为溶剂,把它的pH限定在一定范围,即使在高浓度情况下配合敏乐定及一定量的水也不会出现结晶,而且敏乐定本身也是稳定的,从而完成了本发明。
也就是说本发明提供了在配合了10~50质量%水及3质量%以上敏乐定的制剂中含有1种以上8~30质量%的多元醇、pH为5.5~6.5的毛发生长组合物。实施本发明的最佳形态
本发明的毛发生长组合物中的有效成分敏乐定配合量为3质量%(下面,简单用“%”表示,)以上,优选在3~6%的范围。
溶解这些敏乐定的溶剂是含有多元醇和水的混合溶剂。这种溶剂在最终组合物中,水必须占10~50%、多元醇必须在8~30%的范围内。缺少多元醇或水的任何一方的情况下要防止结晶析出是困难的,而且即使都不缺,如果各自的配合量不在上述范围之内,也难制成使用感优异、并且在低温时能抑制结晶析出的组合物。尤其是因为水配合为18%以上时结晶容易析出,所以本发明的效果明显。多元醇的配合量如前所述,但优选10~20%,更优选15~20%。
在上述溶剂中更优选再加入乙醇。乙醇的配合量优选为在最终的组合物中为70%以下的量。
上述溶剂中使用的多元醇可采用1,3-丁二醇、甘油、一缩二丙二醇、聚乙二醇400、聚乙二醇600等,特别优选是1,3-丁二醇。另外,多元醇优选采用两种以上配合使用。特别优选的多元醇组合有,1,3-丁二醇和甘油,按它们的重量比在10∶1~1∶4的范围组合;还有一缩二丙二醇和甘油,按它们的重量比在10∶1~1∶4的范围组合。
本发明的毛发生长组合物是在上述的含有多元醇和水的溶剂中加入3%以上的有效成分敏乐定和其它必要的活性成分或辅助成分,按常法搅拌、混合制成的,但pH必须维持在5.5~6.5的范围内。也就是说,敏乐定简单地加入水系溶剂中时的液性是中性至弱碱性,但在这种状态下调制高敏乐定制剂时温度下降的情况下结晶容易析出。另一方面,当在pH5以下的酸性情况下,虽然没有结晶析出,相反产生了敏乐定本身容易分解的问题。
本发明的毛发生长组合物的pH调整是按常法进行,pH调整剂优选使用柠檬酸、盐酸、乳酸、磷酸等。
进而,添加、配合到本发明的毛发生长组合物中的优选的药物成分有:由薄荷醇、维生素E乙酸盐、泛酰乙基醚(パントテニルェチルェ一テル)、日扁柏醇、甘草亭酸及盐酸苯海拉明组成的群中选取的成分(下面称为“选择成分”)。选择成分中,作为有效性特别高的可以举出薄荷醇,更优选把薄荷醇作为必需成分添加进去。
这些选择成分的添加量没有特别的限制,可考虑使用感、敏乐定的稳定性或者溶剂系组成等通过实验确定。比如特别优选的选择成分薄荷醇优选配制成在最终组合物中为0.2~0.4%的程度。
本发明的毛发生长剂组合物中除了上述成分以外,还可以在不影响本发明的效果的范围内配合通常使用的成分,比如,用于一般外用剂的各种活性成分和辅助成分,如赋形剂、血管扩张剂、(氯化三甲胺丁酸甲脂、烟酸苄酯、当药提取液、人参提取物、辣椒酊等)、抗组胺剂(盐酸氮异丙嗪等)抗炎症剂(愈创木薁等)、角质溶解剂(尿素、水杨酸等)杀菌剂(葡糖酸洗必泰、异丙甲基酚、季铵盐、ピロクトンオラミン等)、保湿剂(透明质酸钠、硫酸软骨素等)、各种动植物(紫杉、牡丹、甘草、小连翘、五倍子、枇杷、茵陈蒿、雏菊、当归、藏红花、山栀子、迷迭香、鼠尾草、木香、马兜铃、蛇麻草、胎盘等)的提取物、维生素类(乙酸视黄醇酯、盐酸吡哆醇、抗坏血酸、硝酸硫胺素、氰钴胺素、生物素等)、抗氧化剂(二丁羟甲苯、焦亚硫酸钠、维生素E、依地酸钠、抗坏血酸、棓酸异丙酯等)、溶解辅助剂(己二酸二异丙酯、十四烷酸异丙酯、各种植物油、各种动物油、烷基甘油醚、烃类等)、代谢赋活剂(泛酸醇等)、胶凝剂(水溶性高分子等)、粘合剂、香料、清凉剂(薄荷油、樟脑等)、染料等。
但是,添加表面活性剂会影响敏乐定的皮肤吸收,降低其使用感,所以本发明的毛发生长组合物优选是实质上不含表面活性剂。
这样得到的本发明的毛发生长组合物可以作为洗剂、气溶胶剂、滋补剂、乳脂剂、软膏剂、胶剂等适当的外用制剂使用。
实施例
下面以实施例具体说明本发明,但本发明不受这些实施例的限制。
实施例1
把敏乐定3.0g、1,3-丁二醇10.0g、乙醇35g、净化水20g混合、搅拌使之溶解。加入适量柠檬酸,使其液体pH为5.5,再加入净化水,使其成为100mL,得到洗剂(本发明品1)。
实施例2
与实施例1同样,调制出表1和表2所示的本发明产品以及表3所示的比较产品洗剂。
(成分)
表1
本发明品2 | 本发明品3 | 本发明品4 | 本发明品5 | 本发明品6 | 本发明品7 | |
敏乐定 | 3.0g | 5.0g | 5.0g | 3.0g | 3.0g | 5.0g |
1,3-丁二醇 | 10.0g | 20.0g | 30.0g | - | - | 10.0g |
甘油 | - | - | - | - | - | 5.0g |
一缩二丙二醇 | - | - | - | 10.0g | - | - |
聚乙二醇400 | - | - | - | - | 10.0g | - |
乙醇 | 35.0g | 60.0g | 50.0g | 60.0g | 40.0g | 55.0g |
柠檬酸 | - | - | - | - | - | 适量 |
乳酸 | 适量 | - | - | - | - | - |
磷酸 | - | 适量 | - | - | 适量 | - |
盐酸 | - | - | 适量 | 1.0g | - | - |
氢氧化钠 | - | - | - | 适量 | - | - |
净化水(总量) | 100mL | 100mL | 100mL | 100mL | 100mL | 100mL |
pH | 5.5 | 6.5 | 6.1 | 6.5 | 6.0 | 6.0 |
表2
本发明品8 | 本发明品9 | 本发明品10 | 本发明品11 | 本发明品12 | 本发明品13 | 本发明品14 | 本发明品15 | |
敏乐定 | 3.0g | 5.0g | 3.0g | 3.0g | 5.0g | 3.0g | 3.0g | 5.0g |
1,3-丁二醇 | 7.0g | - | 5.0g | 8.0g | - | - | - | - |
甘油 | 3.0g | 15.0g | 5.0g | 2.0g | - | - | 3.0g | 5.0g |
一缩二丙二醇 | - | 15.0g | - | - | 20.0g | - | 7.0g | 10.0g |
聚乙二醇400 | - | - | - | - | - | 10.0g | - | - |
乙醇 | 60.0g | 40.0g | 60.0g | 60.0g | 50.0g | 70.0g | 60.0g | 55.0g |
柠檬酸 | - | - | - | 1.0g | - | - | 适量 | - |
乳酸 | 适量 | - | - | - | - | - | - | - |
磷酸 | - | 适量 | - | - | 适量 | - | - | - |
盐酸 | - | - | 适量 | - | - | 1.0g | - | 适量 |
氢氧化钠 | - | - | - | 适量 | - | 适量 | - | - |
净化水(总量) | 100mL | 100mL | 100mL | 100mL | 100mL | 100mL | 100mL | 100mL |
pH | 5.5 | 6.5 | 6.1 | 5.8 | 5.6 | 6.5 | 5.5 | 6.0 |
表3
比较品1 | 比较品2 | |
敏乐定 | 3.0g | 5.0g |
1,3-丁二醇 | 5.0g | 10.0g |
甘油 | - | 5.0g |
一缩二丙二醇 | - | - |
聚乙二醇400 | - | - |
乙醇 | 45.0g | 55.0g |
柠檬酸 | - | - |
乳酸 | - | - |
磷酸 | - | - |
盐酸 | - | - |
氢氧化钠 | - | - |
净化水(总量) | 100mL | 100mL |
pH | 8.8 | 9.3 |
把本发明品和比较品在-10℃的条件下保存一周,观察结晶的析出程度,本发明品中敏乐定的浓度虽高,但没有发现结晶析出,而比较品的情况就不同,有结晶析出。
实施例3
把实施例1调制的洗剂30mL充填到气溶胶罐中,再加入二甲醚70mL,制成气溶胶剂。另外,用实施例2的洗剂也可以同样的制成气溶胶剂。
试验例1
同实施例1一样,调整表4所示的本发明品16及比较品3的洗剂。用一周时间观察它们按下述条件保存时的结晶析出性。其结果如表5中所示。
保存条件
保存温度:-10℃
容器:35mL塑料瓶
充填量:30mL
各观察时间的N数:8支
表4
本发明品16 | 比较品3 | |
敏乐定 | 5.0g | 5.0g |
1,3-丁二醇 | 10.0g | 5.0g |
乙醇 | 64.34g | 64.34g |
磷酸 | 0.5mL | 0.5mL |
二丁羟甲苯 | 0.05g | 0.05g |
净化水(总量) | 100mL | 100mL |
制剂中的含水率(W/W)% | 18 | 18 |
pH | 6.0 | 6.0 |
表5
析出的支数 | ||||
当时 | 1天后 | 4天后 | 7天后 | |
本发明品16 | 0支 | 0支 | 0支 | 0支 |
比较品3 | 0支 | 0支 | 3支 | 3支 |
试验例2
同实施例1一样,调整表6所示的本发明品17~20及表7所示的比较品4~8的洗剂。把用一周时间观察它们按下述的条件保存时的结晶析出性。其结果如表8所示。
保存条件
保存温度:-10~-16℃
容器:35mL塑料瓶
充填量:30mL
各观察时间的N数:8支
表6
本发明品17 | 本发明品18 | 本发明品19 | 本发明品20 | |
敏乐定 | 5.0g | 5.0g | 5.0g | 5.0g |
1,3-丁二醇 | 10.0g | 20.0g | 30.0g | 40.0g |
乙醇 | 49.0g | 41.0g | 33.0g | 24.0g |
磷酸 | 0.5mL | 0.5mL | 0.5mL | 0.5mL |
净化水(总量) | 100mL | 100mL | 100mL | 100mL |
制剂中的含水率(W/W%) | 32 | 32 | 31 | 32 |
pH | 5.7 | 5.7 | 5.7 | 5.7 |
表7
比较品4 | 比较品5 | 比较品6 | 比较品7 | 比较品8 | |
敏乐定 | 5.0g | 5.0g | 5.0g | 5.0g | 5.0g |
1,3-丁二醇 | 5.0g | 10.0g | - | - | - |
甘油 | - | 5.0g | - | - | - |
一缩二丙二醇 | - | - | 5.0g | 5.0g | 5.0g |
乙醇 | 53.0g | 55.0g | 40.0g | 60.0g | 60.0g |
磷酸 | 0.5mL | - | 0.5mL | 0.05mL | 0.2mL |
净化水(总量) | 100mL | 100mL | 100mL | 100mL | 100mL |
制剂中的含水率(W/W%) | 33 | 24 | 53 | 28 | 28 |
pH | 5.7 | 9.3 | 5.5 | 7.0 | 6.4 |
表8
析出支数 | ||||
当时 | 1天后 | 4天后 | 7天后 | |
本发明品17本发明品18本发明品19本发明品20比较品4比较品5比较品6比较品7比较品8 | 0支0支0支0支0支0支0支0支0支 | 0支0支0支0支0支1支1支1支0支 | 0支0支0支0支1支1支1支1支1支 | 0支0支0支0支1支1支1支1支1支 |
Claims (13)
1.一种毛发生长组合物,其特征在于,在配合了10~50质量%的水与3质量%以上的敏乐定的制剂中含有多元醇8~30质量%,pH为5.5~6.5。
2.根据权利要求1所述的毛发生长组合物,其中多元醇是1,3-丁二醇。
3.根据权利要求1所述的毛发生长组合物,其中所述的多元醇是1,3-丁二醇及甘油,它们的组成质量比是10∶1~1∶4。
4.根据权利要求1所述的毛发生长组合物,其中所述的多元醇是一缩二丙二醇及甘油,它们的组成质量比是10∶1~1∶4。
5.根据权利要求1~4任何一项所述的毛发生长组合物,其中所述的敏乐定的配合量是3~6质量%。
6.根据权利要求1~5任何一项所述的毛发生长组合物,为进一步含有乙醇的洗剂。
7.根据权利要求1~5任何一项所述的毛发生长组合物,为进一步含有乙醇的胶剂。
8.根据权利要求1~7任何一项所述的毛发生长组合物,其中所述的乙醇的含有量为70质量%以下。
9.根据权利要求1~8任何一项所述的毛发生长组合物,其中所述的水的配合量为18~50质量%。
10.根据权利要求1~9任何一项所述的毛发生长组合物,其中实质上不含表面活性剂。
11.根据权利要求1~10任何一项所述的毛发生长组合物,其中配合作为pH调整剂的柠檬酸、盐酸、乳酸或磷酸。
12.根据权利要求1~11任何一项所述的毛发生长组合物,其中进一步含有选自薄荷醇、维生素E乙酸盐、泛酰乙基醚、日扁柏醇、甘草亭酸及盐酸苯海拉明的1种或2种以上成分。
13.防止析出的方法,其中,在配合了10~50质量%的水与3质量%以上的敏乐定的制剂中,配合8~30质量%多元醇,使pH调整为5.5~6.5。
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JPS63145217A (ja) * | 1986-12-09 | 1988-06-17 | Taisho Pharmaceut Co Ltd | 経皮投与組成物 |
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2001
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- 2001-04-05 DE DE60113822T patent/DE60113822T2/de not_active Expired - Fee Related
- 2001-04-05 AU AU4473101A patent/AU4473101A/xx active Pending
- 2001-04-05 CN CNB018108237A patent/CN100361644C/zh not_active Expired - Fee Related
- 2001-04-05 HU HU0300417A patent/HUP0300417A2/hu unknown
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- 2001-04-05 AU AU2001244731A patent/AU2001244731B2/en not_active Ceased
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- 2001-04-05 WO PCT/JP2001/002942 patent/WO2001076541A1/ja active IP Right Grant
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- 2001-04-06 TW TW090108237A patent/TWI289459B/zh not_active IP Right Cessation
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- 2004-01-27 HK HK04100543A patent/HK1057708A1/xx not_active IP Right Cessation
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CN104487048A (zh) * | 2012-07-27 | 2015-04-01 | 大正制药株式会社 | 外用剂组合物 |
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AU4473101A (en) | 2001-10-23 |
HUP0300417A2 (hu) | 2003-08-28 |
EP1269973A1 (en) | 2003-01-02 |
US20030108500A1 (en) | 2003-06-12 |
KR20020081600A (ko) | 2002-10-28 |
TWI289459B (en) | 2007-11-11 |
HK1057708A1 (en) | 2004-04-16 |
RU2002126557A (ru) | 2004-03-20 |
JP5527787B2 (ja) | 2014-06-25 |
JP5561264B2 (ja) | 2014-07-30 |
KR100774074B1 (ko) | 2007-11-06 |
NZ521830A (en) | 2004-07-30 |
BR0110146A (pt) | 2003-12-30 |
EP1269973B1 (en) | 2005-10-05 |
ATE305765T1 (de) | 2005-10-15 |
JP2012025770A (ja) | 2012-02-09 |
ES2245980T3 (es) | 2006-02-01 |
CN100361644C (zh) | 2008-01-16 |
DE60113822T2 (de) | 2006-08-03 |
CA2405452A1 (en) | 2001-10-18 |
JPWO2001076541A1 (ja) | 2004-01-08 |
ZA200208013B (en) | 2003-07-24 |
DE60113822D1 (de) | 2006-02-16 |
WO2001076541A1 (fr) | 2001-10-18 |
AU2001244731B2 (en) | 2005-02-17 |
EP1269973A4 (en) | 2003-07-09 |
RU2274440C2 (ru) | 2006-04-20 |
US20040204433A1 (en) | 2004-10-14 |
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