JPH0460446B2 - - Google Patents
Info
- Publication number
- JPH0460446B2 JPH0460446B2 JP59138985A JP13898584A JPH0460446B2 JP H0460446 B2 JPH0460446 B2 JP H0460446B2 JP 59138985 A JP59138985 A JP 59138985A JP 13898584 A JP13898584 A JP 13898584A JP H0460446 B2 JPH0460446 B2 JP H0460446B2
- Authority
- JP
- Japan
- Prior art keywords
- hair
- acid
- composition
- dandruff
- inhibitory activity
- 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.)
- Expired - Lifetime
Links
- 239000000203 mixture Substances 0.000 claims description 57
- 210000004209 hair Anatomy 0.000 claims description 52
- 235000014113 dietary fatty acids Nutrition 0.000 claims description 29
- 239000000194 fatty acid Substances 0.000 claims description 29
- 229930195729 fatty acid Natural products 0.000 claims description 29
- 150000004665 fatty acids Chemical class 0.000 claims description 29
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 claims description 22
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 claims description 21
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 claims description 21
- 239000005642 Oleic acid Substances 0.000 claims description 21
- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 claims description 21
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 claims description 21
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 claims description 21
- OYHQOLUKZRVURQ-HZJYTTRNSA-N Linoleic acid Chemical compound CCCCC\C=C/C\C=C/CCCCCCCC(O)=O OYHQOLUKZRVURQ-HZJYTTRNSA-N 0.000 claims description 18
- 235000020778 linoleic acid Nutrition 0.000 claims description 18
- OYHQOLUKZRVURQ-IXWMQOLASA-N linoleic acid Natural products CCCCC\C=C/C\C=C\CCCCCCCC(O)=O OYHQOLUKZRVURQ-IXWMQOLASA-N 0.000 claims description 18
- 150000003839 salts Chemical class 0.000 claims description 18
- 238000002156 mixing Methods 0.000 claims description 4
- 230000000694 effects Effects 0.000 description 29
- 230000003779 hair growth Effects 0.000 description 23
- 208000001840 Dandruff Diseases 0.000 description 20
- 208000003251 Pruritus Diseases 0.000 description 20
- 230000002401 inhibitory effect Effects 0.000 description 20
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 19
- 108010066551 Cholestenone 5 alpha-Reductase Proteins 0.000 description 17
- 230000007803 itching Effects 0.000 description 14
- 102000004005 Prostaglandin-endoperoxide synthases Human genes 0.000 description 13
- 108090000459 Prostaglandin-endoperoxide synthases Proteins 0.000 description 13
- MUMGGOZAMZWBJJ-DYKIIFRCSA-N Testostosterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 MUMGGOZAMZWBJJ-DYKIIFRCSA-N 0.000 description 12
- 238000006243 chemical reaction Methods 0.000 description 11
- YZXBAPSDXZZRGB-DOFZRALJSA-N arachidonic acid Chemical compound CCCCC\C=C/C\C=C/C\C=C/C\C=C/CCCC(O)=O YZXBAPSDXZZRGB-DOFZRALJSA-N 0.000 description 10
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 description 10
- 201000004384 Alopecia Diseases 0.000 description 9
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 9
- 230000003676 hair loss Effects 0.000 description 9
- 210000004761 scalp Anatomy 0.000 description 9
- 208000024963 hair loss Diseases 0.000 description 8
- 102000004190 Enzymes Human genes 0.000 description 7
- 108090000790 Enzymes Proteins 0.000 description 7
- 239000004615 ingredient Substances 0.000 description 7
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 6
- 206010061218 Inflammation Diseases 0.000 description 6
- 230000004054 inflammatory process Effects 0.000 description 6
- 238000005259 measurement Methods 0.000 description 6
- 230000007246 mechanism Effects 0.000 description 6
- 229960003604 testosterone Drugs 0.000 description 6
- NVKAWKQGWWIWPM-ABEVXSGRSA-N 17-β-hydroxy-5-α-Androstan-3-one Chemical compound C1C(=O)CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CC[C@H]21 NVKAWKQGWWIWPM-ABEVXSGRSA-N 0.000 description 5
- 235000021314 Palmitic acid Nutrition 0.000 description 5
- 229940114079 arachidonic acid Drugs 0.000 description 5
- 235000021342 arachidonic acid Nutrition 0.000 description 5
- 210000004027 cell Anatomy 0.000 description 5
- 239000012153 distilled water Substances 0.000 description 5
- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 description 5
- 239000000126 substance Substances 0.000 description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
- -1 carboxylic acid compound Chemical class 0.000 description 4
- GHVNFZFCNZKVNT-UHFFFAOYSA-N decanoic acid Chemical compound CCCCCCCCCC(O)=O GHVNFZFCNZKVNT-UHFFFAOYSA-N 0.000 description 4
- POULHZVOKOAJMA-UHFFFAOYSA-N dodecanoic acid Chemical compound CCCCCCCCCCCC(O)=O POULHZVOKOAJMA-UHFFFAOYSA-N 0.000 description 4
- 239000003205 fragrance Substances 0.000 description 4
- 239000000463 material Substances 0.000 description 4
- WWZKQHOCKIZLMA-UHFFFAOYSA-N octanoic acid Chemical compound CCCCCCCC(O)=O WWZKQHOCKIZLMA-UHFFFAOYSA-N 0.000 description 4
- SECPZKHBENQXJG-FPLPWBNLSA-N palmitoleic acid Chemical compound CCCCCC\C=C/CCCCCCCC(O)=O SECPZKHBENQXJG-FPLPWBNLSA-N 0.000 description 4
- IJTNSXPMYKJZPR-UHFFFAOYSA-N parinaric acid Chemical compound CCC=CC=CC=CC=CCCCCCCCC(O)=O IJTNSXPMYKJZPR-UHFFFAOYSA-N 0.000 description 4
- 238000012360 testing method Methods 0.000 description 4
- OYHQOLUKZRVURQ-NTGFUMLPSA-N (9Z,12Z)-9,10,12,13-tetratritiooctadeca-9,12-dienoic acid Chemical compound C(CCCCCCC\C(=C(/C\C(=C(/CCCCC)\[3H])\[3H])\[3H])\[3H])(=O)O OYHQOLUKZRVURQ-NTGFUMLPSA-N 0.000 description 3
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 3
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 3
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 3
- 241000282414 Homo sapiens Species 0.000 description 3
- 241001465754 Metazoa Species 0.000 description 3
- 238000010521 absorption reaction Methods 0.000 description 3
- 239000004480 active ingredient Substances 0.000 description 3
- 230000001580 bacterial effect Effects 0.000 description 3
- 239000002537 cosmetic Substances 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 239000000284 extract Substances 0.000 description 3
- 230000007794 irritation Effects 0.000 description 3
- 239000006210 lotion Substances 0.000 description 3
- 238000002360 preparation method Methods 0.000 description 3
- SGUKUZOVHSFKPH-YNNPMVKQSA-N prostaglandin G2 Chemical compound C1[C@@H]2OO[C@H]1[C@H](/C=C/[C@@H](OO)CCCCC)[C@H]2C\C=C/CCCC(O)=O SGUKUZOVHSFKPH-YNNPMVKQSA-N 0.000 description 3
- 238000011160 research Methods 0.000 description 3
- 210000001732 sebaceous gland Anatomy 0.000 description 3
- NOOLISFMXDJSKH-KXUCPTDWSA-N (-)-Menthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@H]1O NOOLISFMXDJSKH-KXUCPTDWSA-N 0.000 description 2
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 2
- 108010029908 3-oxo-5-alpha-steroid 4-dehydrogenase Proteins 0.000 description 2
- 102000001779 3-oxo-5-alpha-steroid 4-dehydrogenase Human genes 0.000 description 2
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
- QIVBCDIJIAJPQS-VIFPVBQESA-N L-tryptophane Chemical compound C1=CC=C2C(C[C@H](N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-VIFPVBQESA-N 0.000 description 2
- 239000005639 Lauric acid Substances 0.000 description 2
- 241000283977 Oryctolagus Species 0.000 description 2
- 235000021319 Palmitoleic acid Nutrition 0.000 description 2
- DTOSIQBPPRVQHS-PDBXOOCHSA-N alpha-linolenic acid Chemical compound CC\C=C/C\C=C/C\C=C/CCCCCCCC(O)=O DTOSIQBPPRVQHS-PDBXOOCHSA-N 0.000 description 2
- 235000020661 alpha-linolenic acid Nutrition 0.000 description 2
- IJTNSXPMYKJZPR-WVRBZULHSA-N alpha-parinaric acid Natural products CCC=C/C=C/C=C/C=CCCCCCCCC(=O)O IJTNSXPMYKJZPR-WVRBZULHSA-N 0.000 description 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 2
- 239000003093 cationic surfactant Substances 0.000 description 2
- SECPZKHBENQXJG-UHFFFAOYSA-N cis-palmitoleic acid Natural products CCCCCCC=CCCCCCCCC(O)=O SECPZKHBENQXJG-UHFFFAOYSA-N 0.000 description 2
- 239000006071 cream Substances 0.000 description 2
- 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 2
- 210000003128 head Anatomy 0.000 description 2
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 2
- 229940088597 hormone Drugs 0.000 description 2
- 239000005556 hormone Substances 0.000 description 2
- 230000005764 inhibitory process Effects 0.000 description 2
- 229960004488 linolenic acid Drugs 0.000 description 2
- KQQKGWQCNNTQJW-UHFFFAOYSA-N linolenic acid Natural products CC=CCCC=CCC=CCCCCCCCC(O)=O KQQKGWQCNNTQJW-UHFFFAOYSA-N 0.000 description 2
- 235000019626 lipase activity Nutrition 0.000 description 2
- 239000011159 matrix material Substances 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 210000001589 microsome Anatomy 0.000 description 2
- 235000021313 oleic acid Nutrition 0.000 description 2
- 239000001301 oxygen Substances 0.000 description 2
- 229910052760 oxygen Inorganic materials 0.000 description 2
- CNVZJPUDSLNTQU-SEYXRHQNSA-N petroselinic acid Chemical compound CCCCCCCCCCC\C=C/CCCCC(O)=O CNVZJPUDSLNTQU-SEYXRHQNSA-N 0.000 description 2
- 230000001737 promoting effect Effects 0.000 description 2
- GHMLBKRAJCXXBS-UHFFFAOYSA-N resorcinol Chemical compound OC1=CC=CC(O)=C1 GHMLBKRAJCXXBS-UHFFFAOYSA-N 0.000 description 2
- 210000003491 skin Anatomy 0.000 description 2
- TUNFSRHWOTWDNC-HKGQFRNVSA-N tetradecanoic acid Chemical compound CCCCCCCCCCCCC[14C](O)=O TUNFSRHWOTWDNC-HKGQFRNVSA-N 0.000 description 2
- 229960001295 tocopherol Drugs 0.000 description 2
- 229930003799 tocopherol Natural products 0.000 description 2
- 235000010384 tocopherol Nutrition 0.000 description 2
- 239000011732 tocopherol Substances 0.000 description 2
- 230000001256 tonic effect Effects 0.000 description 2
- 201000010653 vesiculitis Diseases 0.000 description 2
- 229940043810 zinc pyrithione Drugs 0.000 description 2
- PICXIOQBANWBIZ-UHFFFAOYSA-N zinc;1-oxidopyridine-2-thione Chemical compound [Zn+2].[O-]N1C=CC=CC1=S.[O-]N1C=CC=CC1=S PICXIOQBANWBIZ-UHFFFAOYSA-N 0.000 description 2
- 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 2
- BITHHVVYSMSWAG-KTKRTIGZSA-N (11Z)-icos-11-enoic acid Chemical compound CCCCCCCC\C=C/CCCCCCCCCC(O)=O BITHHVVYSMSWAG-KTKRTIGZSA-N 0.000 description 1
- CBMYJHIOYJEBSB-WZDBAGNOSA-N (5s,8r,9s,10s,13s,14s)-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthrene-3,17-diol Chemical compound C1C(O)CC[C@]2(C)[C@H]3CC[C@](C)(C(CC4)O)[C@@H]4[C@@H]3CC[C@H]21 CBMYJHIOYJEBSB-WZDBAGNOSA-N 0.000 description 1
- QKNYBSVHEMOAJP-UHFFFAOYSA-N 2-amino-2-(hydroxymethyl)propane-1,3-diol;hydron;chloride Chemical compound Cl.OCC(N)(CO)CO QKNYBSVHEMOAJP-UHFFFAOYSA-N 0.000 description 1
- 241000894006 Bacteria Species 0.000 description 1
- KWIUHFFTVRNATP-UHFFFAOYSA-N Betaine Natural products C[N+](C)(C)CC([O-])=O KWIUHFFTVRNATP-UHFFFAOYSA-N 0.000 description 1
- XDTMQSROBMDMFD-UHFFFAOYSA-N Cyclohexane Chemical compound C1CCCCC1 XDTMQSROBMDMFD-UHFFFAOYSA-N 0.000 description 1
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 description 1
- 102000001554 Hemoglobins Human genes 0.000 description 1
- 108010054147 Hemoglobins Proteins 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- 239000004166 Lanolin Substances 0.000 description 1
- 239000004367 Lipase Substances 0.000 description 1
- 102000004882 Lipase Human genes 0.000 description 1
- 108090001060 Lipase Proteins 0.000 description 1
- 241000736262 Microbiota Species 0.000 description 1
- KWIUHFFTVRNATP-UHFFFAOYSA-O N,N,N-trimethylglycinium Chemical compound C[N+](C)(C)CC(O)=O KWIUHFFTVRNATP-UHFFFAOYSA-O 0.000 description 1
- ACFIXJIJDZMPPO-NNYOXOHSSA-J NADPH(4-) Chemical compound C1=CCC(C(=O)N)=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](COP([O-])(=O)OP([O-])(=O)OC[C@@H]2[C@H]([C@@H](OP([O-])([O-])=O)[C@@H](O2)N2C3=NC=NC(N)=C3N=C2)O)O1 ACFIXJIJDZMPPO-NNYOXOHSSA-J 0.000 description 1
- 241000283973 Oryctolagus cuniculus Species 0.000 description 1
- 241001494479 Pecora Species 0.000 description 1
- 229920001214 Polysorbate 60 Polymers 0.000 description 1
- 208000012287 Prolapse Diseases 0.000 description 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
- 241000191940 Staphylococcus Species 0.000 description 1
- 241001147736 Staphylococcus capitis Species 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- VBIIFPGSPJYLRR-UHFFFAOYSA-M Stearyltrimethylammonium chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCCCC[N+](C)(C)C VBIIFPGSPJYLRR-UHFFFAOYSA-M 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 230000005856 abnormality Effects 0.000 description 1
- 238000009825 accumulation Methods 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 102000030621 adenylate cyclase Human genes 0.000 description 1
- 108060000200 adenylate cyclase Proteins 0.000 description 1
- 239000000443 aerosol Substances 0.000 description 1
- 150000001298 alcohols Chemical class 0.000 description 1
- 229940024606 amino acid Drugs 0.000 description 1
- 150000001413 amino acids Chemical class 0.000 description 1
- 235000013871 bee wax Nutrition 0.000 description 1
- 239000012166 beeswax Substances 0.000 description 1
- 229960003237 betaine Drugs 0.000 description 1
- 210000004204 blood vessel Anatomy 0.000 description 1
- 230000001680 brushing effect Effects 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 239000004359 castor oil Substances 0.000 description 1
- 235000019438 castor oil Nutrition 0.000 description 1
- 210000000170 cell membrane Anatomy 0.000 description 1
- 229960000541 cetyl alcohol Drugs 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 238000004891 communication Methods 0.000 description 1
- 230000001934 delay Effects 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 230000002500 effect on skin Effects 0.000 description 1
- 229940108623 eicosenoic acid Drugs 0.000 description 1
- BITHHVVYSMSWAG-UHFFFAOYSA-N eicosenoic acid Natural products CCCCCCCCC=CCCCCCCCCCC(O)=O BITHHVVYSMSWAG-UHFFFAOYSA-N 0.000 description 1
- 239000003995 emulsifying agent Substances 0.000 description 1
- 238000000605 extraction Methods 0.000 description 1
- 239000003925 fat Substances 0.000 description 1
- 235000019197 fats Nutrition 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000019634 flavors Nutrition 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 230000002068 genetic effect Effects 0.000 description 1
- 210000004907 gland Anatomy 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 1
- 229940075507 glyceryl monostearate Drugs 0.000 description 1
- 210000003780 hair follicle Anatomy 0.000 description 1
- 230000003054 hormonal effect Effects 0.000 description 1
- 239000003906 humectant Substances 0.000 description 1
- 230000001771 impaired effect Effects 0.000 description 1
- 235000019388 lanolin Nutrition 0.000 description 1
- 229940039717 lanolin Drugs 0.000 description 1
- 229940033355 lauric acid Drugs 0.000 description 1
- 235000019421 lipase Nutrition 0.000 description 1
- 229940057995 liquid paraffin Drugs 0.000 description 1
- 230000010534 mechanism of action Effects 0.000 description 1
- 229940041616 menthol Drugs 0.000 description 1
- 244000005706 microflora Species 0.000 description 1
- 230000003228 microsomal effect Effects 0.000 description 1
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 description 1
- 235000015097 nutrients Nutrition 0.000 description 1
- 235000016709 nutrition Nutrition 0.000 description 1
- 230000035764 nutrition Effects 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 235000014593 oils and fats Nutrition 0.000 description 1
- 229940098695 palmitic acid Drugs 0.000 description 1
- 239000008363 phosphate buffer Substances 0.000 description 1
- 239000000049 pigment Substances 0.000 description 1
- 235000020777 polyunsaturated fatty acids Nutrition 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000002335 preservative effect Effects 0.000 description 1
- 230000003658 preventing hair loss Effects 0.000 description 1
- 210000005267 prostate cell Anatomy 0.000 description 1
- 210000002374 sebum Anatomy 0.000 description 1
- 210000001625 seminal vesicle Anatomy 0.000 description 1
- 239000002453 shampoo Substances 0.000 description 1
- 239000000741 silica gel Substances 0.000 description 1
- 229910002027 silica gel Inorganic materials 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 150000005846 sugar alcohols Polymers 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 238000004809 thin layer chromatography Methods 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 229960004799 tryptophan Drugs 0.000 description 1
- 229940099259 vaseline Drugs 0.000 description 1
- 239000011782 vitamin 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
- 239000001993 wax Substances 0.000 description 1
Classifications
-
- 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
- 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
- A61K8/36—Carboxylic acids; Salts or anhydrides thereof
- A61K8/361—Carboxylic acids having more than seven carbon atoms in an unbroken chain; Salts or anhydrides 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q5/00—Preparations for care of the hair
- A61Q5/006—Antidandruff preparations
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/74—Biological properties of particular ingredients
- A61K2800/78—Enzyme modulators, e.g. Enzyme agonists
- A61K2800/782—Enzyme inhibitors; Enzyme antagonists
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)
- Emergency Medicine (AREA)
- Cosmetics (AREA)
Description
この発明は、リノール酸成分及びオレイン酸成
分を含有して成り、発毛の促進、脱毛の予防、ふ
け、痒みの抑制等に有効な養毛組成物に関する。
生涯を通じてふさふさした髪を、ということは
人類の共通の願いである。しかして、従来から各
種の養毛組成物が脱毛の予防及び治療、ふけ、痒
みの抑制等に用いられているが、これらの症状の
原因や発生機作が十分には解明されていないこと
もあつて、脱毛を抑制して発毛、養毛を促進し、
さらには、ふけ、痒みを抑制するのに真に有効な
薬剤は未だ見出されていない。
発明者らは、真に有効な養毛組成物を開発すべ
く鋭意研究を行なつた結果、オレイン酸又はその
養毛組成物として許容される塩(以下オレイン酸
成分という)とリノール酸又はその養毛組成物と
して許容される塩(以下リノール酸成分という)
とを含んで成る混合脂肪酸成分がきわめて効果的
な養毛、育毛作用を有し、さらにはふけ、痒みを
も抑制するという驚くべき事実を発見し、この知
見に基きこの発明を完成した。
すなわち、発明者等は、真に科学的な根拠に基
礎づけられた養毛組成物を開発すべく、まず健全
な頭髪を有する者と、ふけ、痒み、異常脱毛等の
健全とは言えない頭髪を有する者とのそれぞれの
頭皮における微生物相を詳細に対比した結果、前
者の頭皮においてはスタフイロコツカス・キヤピ
テイス(Staphylococcus capitia)が単独で大部
分を占めているという全く新しい知見を得、該菌
種の菌体、菌体処理物等を頭皮に適用した場合顕
著な養毛効果が得られ、この効果が該菌が有する
リパーゼ活性及びテストステロン−5α−リダク
ターゼ(テストステロンを5α−ジヒドロテスト
ステロンに還元する酵素、以下、5α−リダクタ
ーゼと略称する)阻害活性と密接な関係を有する
ことを明らかにした(昭和57年第110395号特許出
願明細書)。そして、発明者等は、前記リパーゼ
活性及び5α−リダクターゼ阻害活性と、育毛、
養毛効果との関係を詳細に検討する間に、スタフ
イロコツカス・キヤピテイスの有するリパーゼを
油脂に作用せしめた場合に生成する脂肪酸類を主
成分とする物が強力な5α−リダクターゼ阻害活
性を有し、該脂肪酸類含有物がそれ自体としても
養毛効果を発揮することを見出した(昭和58年第
7463号特許出願明細書)。また、脂肪酸類中の活
性成分を追求した結果、脂肪酸の1種であるリノ
ール酸、オレイン酸、アラキドン酸、n−カプリ
ン酸、n−カプリル酸、ラウリル酸、ミリスチン
酸、パルミチン酸、ステアリン酸、リノレン酸、
パリナリン酸、ペトロセリン酸、もしくはパルミ
トレイン酸、又はこれらの養毛組成物として許容
される塩が強力な5α−リダクターゼ阻害活性を
有すると共に養毛効果を発揮する事を明らかにし
た。(昭和58年第14555号、58−24687号、58−
24686号、58−45292号、及び58−45293号特許出
願明細書)。
発明者らは更に、脂肪酸がフケ、カユミの防止
又は軽減に有効である事から、頭皮部のフケ、カ
ユミの原因である炎症に対して脂肪酸が有効に作
用していると考えた。ある種の脂肪酸は、炎症に
関与すると言われているシクロオキシゲナーゼに
対して阻害作用を示すといわれていることから、
種々の脂肪酸類及びそれらの混合物について、
5α−リダクターゼ阻害活性、シクロオキシゲナ
ーゼ阻害活性、養毛効果、フケ、カユミに対する
効果に関する研究を行なつた結果、オレイン酸又
はその塩(オレイン酸成分)の配合量が80〜99.9
重量%及びリノール酸又はその塩(リノール酸成
分)の配合量が0.1〜20重量%である2種の脂肪
酸又はその塩の混合物及びこの混合物と他種脂肪
酸又はその塩との混合物が最も有効に5α−リダ
クターゼ及びシクロオキシゲナーゼの活性を阻害
し、フケ、カユミの防止又は軽減、養毛効果に有
効である事を見出し、この発明を完成するに至つ
た。
なお、特開昭56−61308号には、ジンクピリチ
オンとカチオン界面活性剤からなる常用のふけ、
かゆみ防止毛髪処理組成物に特定のカルボン酸化
合物を配合して成るふけ、かゆみ防止毛髪処理組
成物が記載されているが、そこにはふけ、かゆみ
を防止する活性成分はジンクピリチオンであり、
カチオン界面活性剤は毛髪を柔軟でしなやかにす
る作用を有し、そしてカルボン酸化合物は、前記
の物質による目や皮膚に対する強い刺激を緩和す
る作用を有する旨記載されているのみであり、脂
肪酸が5α−リダクターゼ阻害活性及びシクロオ
キシゲナーゼ阻害活性を有することはもちろん、
養毛効果を有することはなんら示唆されていな
い。又、特開昭57−502166号には、ベタインと脂
肪族有機酸とを組合わせて含有する毛髪処理が記
載されているが、脂肪族有機酸としてこの発明の
脂肪酸は挙げられておらず、しかもこの毛髪処理
剤は(すでに形成された)毛髪を傷めることな
く、毛髪に良好なブラツシング性を付与する等の
効果を有することが記載されているのみで、養毛
効果についてはなんら記載されていない。
この発明の養毛組成物の活性成分である混合脂
肪酸成分には、前記のオレイン酸成分及びリノー
ル酸成分のほかに、5α−リダクターゼが阻害活
性及びシクロオキシゲナーゼ活性を有する他の脂
肪酸類、例えばn−カプリン酸、n−カプリル
酸、ラウリン酸、ミリスチン酸、パルミチン酸、
リノレン酸、パリナリン酸、ペトロセリン酸、パ
ルミトレイン酸もしくはエイコセン酸又はこれら
の塩、等を任意に含有せしめることができる。
この発明の養毛組成物の活性成分である混合脂
肪酸成分は人体に対して毒性を有しないから、養
毛組成物への配合量は特に限定されず広範囲に選
択することができるが、組成物の全量に対して
0.01〜10重量%の範囲とするのが好ましい。
この発明の養毛組成物に使用する基材として
は、化粧組成物に常用されている任意のものを使
用することができ、例えば、蒸留水、エタノール
等の一価アルコール、グリセリン、エチレングリ
コール等の多価アルコール類、油脂類、界面活性
剤などを使用することができる。
この発明の養毛組成物には、この発明の組成物
の効果を損なわない限りにおいて従来の養毛組成
物や整髪組成物に使用されている公知の諸成分を
含有せしめることができ、これらの成分として
は、例えばホルモン類、ビタミン類、アミノ酸
類、生薬エキス類、感光色素、レゾルシン、メン
トール、湿潤剤、香料等を挙げることができる。
この発明の養毛組成物は、ヘアートニツク、ヘ
アーローシヨン、ヘアークリーム、シヤンプー、
リンス、ポマード、エアーゾル等常用の剤形とす
ることができる。
次に、この発明の効果を、推定作用機作と共に
説明する。なお、以下に簡単に述べるフケ、カユ
ミ、脱毛等の発生機作及びこの発明の養毛組成物
の養毛機作は実験的根拠を伴う推定であるが、仮
りに、フケ、カユミ、脱毛等が他の機作によるも
のであり、又この発明の養毛組成物の養毛効果が
他の機作によるものであつても、それによつてこ
の発明の効果が否定されるものではなく、この発
明の技術的範囲が限定されるものではない。
抜毛、脱毛、ふけ、痒みの原因については、ホ
ルモンのアンバランス説、栄養との関連説、脱漏
説、遺伝説等の種々の説があり、確定していない
が、いずれにしても皮脂腺の発達と高い相関があ
ることは恐らく確実である〔稲葉益巳、毎日ライ
フ、1981年11月号、26〜35頁;最新化粧品科学、
130頁(薬事日報社刊)、昭和55年;アダチ・ケン
ジ等、Biochemical and Biophysical Research
Communication 41(4)884〜890(1970);タ
カヤス・ススム等、Jounal of Investigative
Dermatology74 187〜191頁(1980)〕。すなわ
ち、頭部の皮脂腺が栄養、ホルモン等によつて肥
大してくると、該腺中に存在する5α−リダクタ
ーゼによりテストステロンがより強力な5α−ジ
ヒドロテストステロンに変換され、これが血管を
介して毛乳頭へ移行し、毛母細胞におけるアデニ
ルサイクラーゼの活性を抑制して毛母細胞の分裂
を遅らせ、その結果毛包が次第に退縮し、このた
めに毛が細かくウブ毛化し、禿が発するに至ると
されている。
更に、何らかの刺激によつて炎症が生じ、フ
ケ、カユミが発生すると考えられ、皮脂腺より分
泌された皮脂の頭皮部への蓄積も刺激の原因と考
えられる。炎症はアラキドン酸カスケードにより
生産される物質が関与していると考えられてい
る。細胞内では刺激によつて細胞膜から遊離した
アラキドン酸が、シクロオキシゲナーゼによつて
プロスタグランデインG2となり、更にエンドパ
ーオキシダーゼによつてプロスタグランデイン
H2となるが、この時生じたヒドロキシラジカル
がが炎症の原因となると考えられる。また、プロ
スタグランデインG2自体も炎症の原因となつて
いると言われている(藤村 一、最近医学、第38
巻、2226〜2232頁、1983年)。
このようなフケ、カユミ、脱毛等の発生機作を
基礎にして考えた場合、5α−リダクターゼ阻害
活性及びシクロオキシゲナーゼ阻害活性は養毛組
成物が有すべき重要な属性であり、且つ養毛組成
物の効果を科学的に評価する場合の一つの基準と
なるものである。
この発明の養毛組成物であるオレイン酸及びリ
ノール酸の二種の脂肪酸又はそれらの塩、の混合
物あるいはこれと他種脂肪酸類又はその塩との混
合物は前記のごとく強力な5α−リダクターゼ阻
害作用及びシクロオキシゲナーゼ阻害作用を有し
ており、この発明の養毛組成物が強力なフケ、カ
ユミの抑制作用及び養毛効果を発揮するのは前記
のような機作によるものと考えられるが、更にこ
の発明の二種の脂肪酸又はそれらの塩の混合物、
あるいはこれと他種脂肪酸類又はその塩との混合
物は頭皮の微生物相を良好な状態に制御し、これ
らが総合され又は相乗して強力なフケ、カユミの
抑制作用、養毛効果を発揮するものと考えられ
る。
この発明の養毛組成物をヒトの頭皮又は動物の
皮膚に適用した場合、強力な養毛効果を発揮す
る。すなわち、この発明の組成物を頭皮に適用し
た場合、抜毛、脱毛が抑制され、うぶ毛化した頭
髪が健全化し、又毛の伸長速度が顕著に上昇す
る。又ふけの発生が抑制され、痒みが防止され
る。さらに、この発明の化粧料を動物に適用した
場合、毛の伸長速度が顕著に上昇する。
この発明の養毛組成物は、ヒト及び動物に対す
る安全性について全く問題がない。すなわちこの
発明の脂肪酸及びその複数の塩をそれぞれ別々の
基剤(アルコール水溶液)に分散せしめて、これ
らを5頭ずつの家兎に1日1回ずつ3日間にわた
り塗布し、基材のみを塗布した対照と比較した結
果、異常は全く認められなかつた。
なお、本発明において、5α−リダクターゼ阻
害活性及びシクロオキシゲナーゼ阻害活性は次の
方法により測定した。
1 5α−リダクターゼ阻害活性の測定
ラツトの前立腺細胞を破砕し、この破砕液から
ミクロゾームを分離してテストステロン5α−リ
ダクターゼの標品を作る。この酵素標品によるテ
ストステロンから5α−ジヒドロテストステロン
への変換を、ラジオアイソトープでラベルされた
テストステロンを用いて追跡する。反応終了後、
酢酸エチルで抽出し、シリカゲル薄層クロマトグ
ラフイー(溶媒系ジクロロメタン:シクロヘキサ
ン:アセトン=15:4:1)により二重展開し、
5α−ジヒドロテストステロン及び5α−アンドロ
スタン−3,17−ジオール(以下アデオールと略
す)の量を放射能強度から求める。
(反応)
0.05M燐酸緩衝液(PH6.6)30μ、酵素標品
1.6unit(1unitは1時間に1pmolのテストステロン
を還元する酵素量)、ラベルドテストステロン
8.5pmol、還元型NADP50nmol、及び測定試料
を混合して全量を50μとする。これを25℃にて
60分間反応せしめる。反応終了後、反応液に酢酸
エチル100μを加えて抽出し、抽出液を上記の
如く展開した後、生成した5α−ジヒドロテスト
ステロン及びアデオールの量をシンチレーシヨン
カウンターによるラジオアイソトープ量の測定に
より求める。
上記の測定をオレイン酸及びリノール酸から成
る種々の混合比の二種の脂肪酸混合物試料の種々
の濃度について行ない、5α−リダクターゼ阻害
活性をID50として求める。
2 シクロオキシゲナーゼ阻害活性の測定
酵素は、ヒツジ精嚢腺ミクロゾーム酵素(メー
カーコード,A−3,イスラエル・RANケミカ
ル社)を使用した。
シクロオキシゲナーゼ活性は、以下に述べる酸
素吸収法により測定した。反応液の酵素吸収は、
DG−G−5型酵素電極(石川製作所,東京)を
備えた3.2ml容反応槽(同製作所)を用いて測定
した。反応槽は、恒温循環槽(ネスラブ社,エン
ドカルRTE−9)により30℃に保つ。反応液
(3.2ml)は、トリス−塩酸緩衝液(0.1M,PH8.0)
3.1ml、ヒツジ精嚢腺ミクロゾーム1mg、ヘモグ
ロビン(0.25μM)、L−トリプトフアン
(10mM)及びアラキドン酸(21.8μM)を含む。
反応は、アラキドン酸の添加により開始する。テ
スト標品は、50μのエタノールに溶かして、反
応開始の5分前に添加した。記録紙上の酸素吸収
カーブの直線部分より初発速度を求める。
上記の測定を種々の混合比の二種の脂肪酸混合
物試料の種々の濃度について行ない、シクロオキ
シゲナーゼ阻害活性をID50として求めた。
The present invention relates to a hair growth composition containing a linoleic acid component and an oleic acid component, which is effective in promoting hair growth, preventing hair loss, suppressing dandruff, itching, and the like. It is a common desire of all human beings to have thick hair throughout their lives. Although various hair nourishing compositions have been used to prevent and treat hair loss, suppress dandruff, and itching, the causes and mechanisms behind these symptoms are not fully understood. It suppresses hair loss and promotes hair growth and nourishment.
Furthermore, no drug has yet been found that is truly effective in suppressing dandruff and itching. As a result of intensive research to develop a truly effective hair nourishing composition, the inventors discovered that oleic acid or a salt thereof acceptable as a hair nourishing composition (hereinafter referred to as the oleic acid component) and linoleic acid or its salt. Salts acceptable as hair nourishing compositions (hereinafter referred to as linoleic acid components)
The present inventors have discovered the surprising fact that a mixed fatty acid component comprising the following has an extremely effective hair-nourishing and hair-growth effect, and also suppresses dandruff and itching, and based on this knowledge, they have completed this invention. In other words, in order to develop a hair nourishing composition based on truly scientific evidence, the inventors first focused on those with healthy hair, and those with less-than-healthy hair, such as those with dandruff, itching, or abnormal hair loss. As a result of a detailed comparison of the microbiota in the scalps of individuals with the former's scalp, we obtained a completely new finding that Staphylococcus capitia alone accounts for the majority of the scalp of the former. When applied to the scalp, the bacterial cells of the bacterial species, the treated bacterial cells, etc. have a remarkable hair-nourishing effect, and this effect is due to the lipase activity and testosterone-5α-reductase (reducing testosterone to 5α-dihydrotestosterone) of the bacteria. 5α-reductase (hereinafter abbreviated as 5α-reductase) has a close relationship with the inhibitory activity of 5α-reductase (Patent Application No. 110395, 1982). The inventors have discovered that the lipase activity and 5α-reductase inhibitory activity, hair growth,
While examining in detail the relationship with the hair-nourishing effect, we found that a substance whose main component is fatty acids produced when the lipase of Staphylococcus capitis acts on fats and oils has a strong 5α-reductase inhibitory activity. It was discovered that the fatty acid-containing substance itself also exerts a hair-nurturing effect (1981).
7463 patent application specification). In addition, as a result of pursuing the active ingredients in fatty acids, we found that linoleic acid, oleic acid, arachidonic acid, n-capric acid, n-caprylic acid, lauric acid, myristic acid, palmitic acid, stearic acid, linolenic acid,
It has been revealed that parinaric acid, petroselic acid, palmitoleic acid, or salts thereof that are acceptable as hair-growth compositions have strong 5α-reductase inhibitory activity and exhibit hair-growth effects. (1981 No. 14555, 58-24687, 58-
No. 24686, No. 58-45292, and No. 58-45293 patent application specifications). The inventors further considered that since fatty acids are effective in preventing or alleviating dandruff and itching, fatty acids act effectively against inflammation that causes dandruff and itching in the scalp. Certain fatty acids are said to have an inhibitory effect on cyclooxygenase, which is said to be involved in inflammation.
Regarding various fatty acids and mixtures thereof,
As a result of research on 5α-reductase inhibitory activity, cyclooxygenase inhibitory activity, hair growth effect, dandruff, and anti-itch effect, we found that the amount of oleic acid or its salt (oleic acid component) is 80 to 99.9%.
A mixture of two types of fatty acids or their salts in which the amount of linoleic acid or its salt (linoleic acid component) is 0.1 to 20% by weight, and a mixture of this mixture and other types of fatty acids or their salts are most effective. The present invention was completed based on the discovery that it inhibits the activities of 5α-reductase and cyclooxygenase, and is effective in preventing or alleviating dandruff and itching, and in promoting hair growth. In addition, JP-A-56-61308 discloses a commonly used dandruff, which is made of zinc pyrithione and a cationic surfactant.
An anti-dandruff and itch-preventing hair treatment composition is described in which a specific carboxylic acid compound is blended into the itch-preventing hair treatment composition, and the active ingredient for preventing dandruff and itch is zinc pyrithione;
Cationic surfactants have the effect of making hair soft and supple, and carboxylic acid compounds are only described as having the effect of alleviating the strong irritation to the eyes and skin caused by the above substances, and fatty acids are It not only has 5α-reductase inhibitory activity and cyclooxygenase inhibitory activity, but also
There is no suggestion that it has a hair-nourishing effect. Further, JP-A-57-502166 describes a hair treatment containing a combination of betaine and an aliphatic organic acid, but the fatty acid of this invention is not mentioned as the aliphatic organic acid. Moreover, it is only stated that this hair treatment agent has the effect of imparting good brushing properties to the hair without damaging the hair (that has already been formed), and there is no mention of any effect on hair growth. do not have. In addition to the above-mentioned oleic acid component and linoleic acid component, the mixed fatty acid component that is the active component of the hair nourishing composition of this invention includes other fatty acids that have 5α-reductase inhibitory activity and cyclooxygenase activity, such as n- Capric acid, n-caprylic acid, lauric acid, myristic acid, palmitic acid,
Linolenic acid, parinaric acid, petroselic acid, palmitoleic acid or eicosenoic acid, or salts thereof, etc. can be optionally contained. Since the mixed fatty acid component which is the active ingredient of the hair nourishing composition of this invention is not toxic to the human body, the amount to be added to the hair nourishing composition is not particularly limited and can be selected from a wide range. for the total amount of
It is preferably in the range of 0.01 to 10% by weight. As the base material used in the hair growth composition of this invention, any base material commonly used in cosmetic compositions can be used, such as distilled water, monohydric alcohols such as ethanol, glycerin, ethylene glycol, etc. Polyhydric alcohols, oils and fats, surfactants, etc. can be used. The hair nourishing composition of the present invention may contain various known ingredients used in conventional hair nourishing compositions and hair styling compositions, as long as the effects of the composition of the present invention are not impaired. Examples of the ingredients include hormones, vitamins, amino acids, crude drug extracts, photosensitive pigments, resorcinol, menthol, humectants, fragrances, and the like. The hair nourishing composition of this invention includes hair tonic, hair lotion, hair cream, shampoo,
It can be in conventional dosage forms such as rinses, pomades, aerosols, etc. Next, the effects of this invention will be explained together with the estimated mechanism of action. The mechanisms of occurrence of dandruff, itching, hair loss, etc., and the hair growth mechanism of the hair growth composition of this invention, which will be briefly described below, are estimates based on experimental evidence. Even if the hair growth effect of the hair growth composition of this invention is due to other mechanisms, this does not negate the effects of this invention. The technical scope of the invention is not limited. There are various theories regarding the causes of hair loss, hair loss, dandruff, and itching, including hormonal imbalance theory, nutrition-related theory, prolapse theory, and genetic theory.Although it is not confirmed, in any case, it is related to the development of sebaceous glands. [Masumi Inaba, Mainichi Life, November 1981 issue, pp. 26-35; Latest Cosmetic Science,
130 pages (published by Yakuji Nippo), 1981; Kenji Adachi et al., Biochemical and Biophysical Research
Communication 41 (4) 884-890 (1970); Susumu Takayasu et al., Journal of Investigative
Dermatology 74 pp. 187-191 (1980)]. In other words, when the sebaceous glands on the head become enlarged due to nutrients, hormones, etc., the 5α-reductase present in the glands converts testosterone into the more powerful 5α-dihydrotestosterone, which is then transferred to the dermal papilla via blood vessels. It inhibits the activity of adenyl cyclase in hair matrix cells and delays the division of hair matrix cells, resulting in gradual regression of hair follicles, which causes the hair to become fine and unkempt, leading to baldness. has been done. Furthermore, it is thought that inflammation occurs due to some kind of irritation, resulting in dandruff and itching, and the accumulation of sebum secreted by sebaceous glands on the scalp is also thought to be a cause of irritation. Inflammation is thought to involve substances produced by the arachidonic acid cascade. In the cell, arachidonic acid released from the cell membrane due to stimulation is converted to prostaglandin G2 by cyclooxygenase, and further converted to prostaglandin G2 by endoperoxidase.
The hydroxyl radicals generated at this time are considered to be the cause of inflammation. In addition, prostaglandin G2 itself is said to be a cause of inflammation (Hajime Fujimura, Recent Medicine, Vol. 38).
Vol., pp. 2226-2232, 1983). Considering the mechanisms of occurrence of dandruff, itching, hair loss, etc., 5α-reductase inhibitory activity and cyclooxygenase inhibitory activity are important attributes that a hair nourishing composition should have. It serves as a standard for scientifically evaluating the effects of The hair nourishing composition of this invention, which is a mixture of two types of fatty acids, oleic acid and linoleic acid, or their salts, or a mixture of this with other types of fatty acids or their salts has a strong 5α-reductase inhibitory effect as described above. The hair-growth composition of the present invention has a strong dandruff and itch-suppressing effect and a hair-growth effect, which is thought to be due to the above-mentioned mechanism. A mixture of two fatty acids or their salts according to the invention,
Alternatively, a mixture of this and other types of fatty acids or their salts can control the microflora of the scalp in a good condition, and when these are combined or synergized, they exert a strong dandruff and itch control effect and a hair-nourishing effect. it is conceivable that. When the hair growth composition of this invention is applied to human scalp or animal skin, it exhibits a strong hair growth effect. That is, when the composition of the present invention is applied to the scalp, hair pulling and hair loss are suppressed, downy hair becomes healthy, and the rate of hair growth is significantly increased. Also, the occurrence of dandruff is suppressed and itching is prevented. Furthermore, when the cosmetic of the present invention is applied to animals, the rate of hair growth increases significantly. The hair growth composition of this invention has no safety problems for humans and animals. That is, the fatty acid and its plurality of salts of the present invention were each dispersed in separate base materials (aqueous alcohol solutions), and these were applied to five domestic rabbits once a day for three days, and only the base material was applied. As a result of comparison with the control, no abnormalities were observed. In the present invention, 5α-reductase inhibitory activity and cyclooxygenase inhibitory activity were measured by the following method. 1 Measurement of 5α-reductase inhibitory activity Rat prostate cells are disrupted and microsomes are separated from the disrupted solution to prepare a specimen of testosterone 5α-reductase. The conversion of testosterone to 5α-dihydrotestosterone by this enzyme preparation is monitored using radioisotope-labeled testosterone. After the reaction is complete,
Extract with ethyl acetate, double develop using silica gel thin layer chromatography (solvent system dichloromethane: cyclohexane: acetone = 15:4:1),
The amounts of 5α-dihydrotestosterone and 5α-androstane-3,17-diol (hereinafter abbreviated as Adeol) are determined from the radioactivity intensity. (Reaction) 0.05M phosphate buffer (PH6.6) 30μ, enzyme preparation
1.6 unit (1 unit is the amount of enzyme that reduces 1 pmol of testosterone per hour), labeled testosterone
Mix 8.5 pmol, reduced NADP, 50 nmol, and the measurement sample to make a total volume of 50μ. This at 25℃
Allow to react for 60 minutes. After the reaction is completed, 100 μl of ethyl acetate is added to the reaction solution for extraction, the extract is developed as described above, and the amount of 5α-dihydrotestosterone and adéol produced is determined by measuring the amount of radioisotope using a scintillation counter. The above measurements are performed on various concentrations of two fatty acid mixture samples of oleic acid and linoleic acid at various mixing ratios, and the 5α-reductase inhibitory activity is determined as ID 50 . 2 Measurement of cyclooxygenase inhibitory activity As the enzyme, sheep seminal vesicle gland microsomal enzyme (manufacturer code: A-3, RAN Chemical Company, Israel) was used. Cyclooxygenase activity was measured by the oxygen absorption method described below. Enzyme absorption of the reaction solution is
The measurement was carried out using a 3.2 ml reaction tank (Ishikawa Seisakusho, Tokyo) equipped with a DG-G-5 type enzyme electrode (Ishikawa Seisakusho, Tokyo). The reaction tank is maintained at 30°C using a constant temperature circulation tank (Neslab, Endocal RTE-9). The reaction solution (3.2ml) was Tris-HCl buffer (0.1M, PH8.0)
3.1 ml, containing 1 mg of ovine seminal vesicle microsomes, hemoglobin (0.25 μM), L-tryptophan (10 mM) and arachidonic acid (21.8 μM).
The reaction is initiated by the addition of arachidonic acid. The test preparation was dissolved in 50μ of ethanol and added 5 minutes before the start of the reaction. The initial velocity is determined from the straight line part of the oxygen absorption curve on the recording paper. The above measurements were performed on various concentrations of two types of fatty acid mixture samples with various mixing ratios, and the cyclooxygenase inhibitory activity was determined as ID50 .
【表】
以上の結果から明らかな通り、オレイン酸とリ
ノール酸とを上記の比率の範囲内で混合した場
合、5α−リダクターゼの阻害はこれらの脂肪酸
単独の場合と同等、又はそれ以上である。シクロ
オキシゲナーゼの阻害はリノール酸単独の場合が
最も強力であり、オレイン酸単独の場合は弱い。
しかしながら、リノール酸は多価不飽和脂肪酸で
あるため酸化されやすく、脂肪酸成分としてこれ
のみを使用した場合、養毛組成物を長期間保存す
ることが困難となる場合がある。従つてこれをオ
レイン酸と混合し、混合脂肪酸組分物全体に対す
るリノール酸の量を20重量%以下にするのが好ま
しい。又前記の通りオレイン酸のシクロオキシゲ
ナーゼ阻害活性は弱いため、混合脂肪酸組成物全
体に対するリノール酸の量を0.1%以上とするの
が好ましい。
次に、この発明の養毛組成物及びその効果を説
明するために実施例を記載する。
実施例1 (養毛組成物の配合例)
次の組成を有する養毛組成物を調製した。
(1) ヘアートニツク 成 分 含 量
オレイン酸 98重量%
リノール酸 2 〃 混合物 0.5g
l−メントール 0.1g
95%エタノール 74ml
蒸留水 全体を100mlとする
(2) ヘアーローシヨン 成 分 含 量
オレイン酸
リノール酸
パルミチン酸98重量%
2 〃
1 〃 混合物 0.2g
プロピレングリコール 3g
トコフエロール 0.05g
香 料 適量
95%エタノール 50ml
蒸留水 全体を100mlとする。
(3) ヘアークリーム 成 分 含 量
オレイン酸 99重量%
リノール酸 1 〃 混合物 0.5g
流動パラフイン 45g
ミツロウ 5g
ラノリン 3g
ワセリン 5g
乳化剤(ポリオキシエチレンソルビタンセスキ
オレート) 2g
プロピレングリコール 5g
香 料 適量
蒸留水 全体を100mlとする。
(4) ポマード 成 分 含 量
オレイン酸
リノール酸
パルミチン酸 98重量%
1 〃
1 〃 混合物 0.5g
モクロウ 12g
ヒマシ油 87.5g
トコフエロール 0.1g
香 料 適量
(5) リンス 成 分 含 量
オレイン酸 99重量%
リノール酸 1 〃 混合物 0.2g
塩化ステアリルトリメチルアンモニウム 2g
セチルアルコール 1g
モノステアリン酸グリセリン 0.5g
プロピレングリコール 5.5g
香料・防腐剤 適量
蒸留水 80ml
実施例2 (使用例)
実施例1で調整したヘアートニツクをフケ、カ
ユミ、抜毛の多い不健全な頭髪状態の男子(年令
24才〜49才)各11名ずつについて、1日1〜2
回、4週間にわたり、頭部に適量塗擦したとこ
ろ、次の結果を得た。[Table] As is clear from the above results, when oleic acid and linoleic acid are mixed within the above ratio range, the inhibition of 5α-reductase is equal to or greater than when these fatty acids are used alone. Inhibition of cyclooxygenase is most potent with linoleic acid alone and weaker with oleic acid alone.
However, since linoleic acid is a polyunsaturated fatty acid, it is easily oxidized, and if it is used alone as a fatty acid component, it may be difficult to store the hair nourishing composition for a long period of time. Therefore, it is preferable to mix this with oleic acid so that the amount of linoleic acid is 20% by weight or less based on the entire mixed fatty acid composition. Further, as mentioned above, since the cyclooxygenase inhibitory activity of oleic acid is weak, it is preferable that the amount of linoleic acid is 0.1% or more based on the entire mixed fatty acid composition. Next, Examples will be described to explain the hair growth composition of the present invention and its effects. Example 1 (Example of formulation of hair nourishing composition) A hair nourishing composition having the following composition was prepared. (1) Hair lotion ingredients Contents Oleic acid 98% by weight Linoleic acid 2 Mixture 0.5g L-menthol 0.1g 95% ethanol 74ml Distilled water Total volume is 100ml (2) Hair lotion ingredients Contents Oleic acid Linoleic acid Palmitic acid 98% by weight 2 〃 1 〃 Mixture 0.2g Propylene glycol 3g Tocopherol 0.05g Flavor Appropriate amount 95% ethanol 50ml Distilled water Make the total volume 100ml. (3) Hair cream ingredients Contents Oleic acid 99% by weight Linoleic acid 1 Mixture 0.5g Liquid paraffin 45g Beeswax 5g Lanolin 3g Vaseline 5g Emulsifier (polyoxyethylene sorbitan sesquiolate) 2g Propylene glycol 5g Fragrance Appropriate amount of distilled water The volume should be 100ml. (4) Pomade ingredients Contents Oleic acid Linoleic acid Palmitic acid 98% by weight 1 〃 1 〃 Mixture 0.5g Japanese wax 12g Castor oil 87.5g Tocopherol 0.1g Fragrance Appropriate amount (5) Rinse ingredients Content Oleic acid 99% by weight Linole Acid 1 Mixture 0.2g Stearyltrimethylammonium chloride 2g Cetyl alcohol 1g Glyceryl monostearate 0.5g Propylene glycol 5.5g Fragrance/preservative Appropriate amount of distilled water 80ml Example 2 (Example of use) Use the hair tonic prepared in Example 1 to treat dandruff and itching. , boys with unhealthy hair that pulls out a lot (age
24 years old to 49 years old) 1 to 2 times per day for each 11 people
When an appropriate amount of the product was rubbed on the head twice for 4 weeks, the following results were obtained.
【表】
実施例3 (家兎に対する効果)
雄の家兎(2ケ月令)の背部の毛を剃り取り、
この部分にオレイン酸98重量%、リノール酸1重
量%、パルミチン酸1重量%の混合物の0.2%エ
タノール溶液を1日2回、少量を滴下し、指先で
軽くすり込み、3週間に伸長した毛の長さを測定
した。対象として脂肪酸を含有しないエタノール
溶液を使用した。この結果を下表に示す。
なお、表中の付号は
a:対照側毛長平均値(mm)±標準偏差
a′:試験側毛長平均値(mm)±標準偏差
b:試験側毛長平均値一対照側毛長平均値
(mm)
※1:対照側毛長平均値の平均
※2:試験側毛長平均値の平均
を意味する。[Table] Example 3 (Effect on domestic rabbits) The hair on the back of a male rabbit (2 months old) was shaved off,
Twice a day, drop a small amount of a 0.2% ethanol solution of a mixture of 98% oleic acid, 1% linoleic acid, and 1% palmitic acid in this area and rub it in with your fingertips. The length was measured. An ethanol solution containing no fatty acids was used as a control. The results are shown in the table below. The numbers in the table are a: Average hair length on the control side (mm) ± standard deviation a': Average hair length on the test side (mm) ± standard deviation b: Average hair length on the test side - Hair length on the control side Average value (mm) *1: Average of the average hair length on the control side *2: Means the average hair length on the test side.
【表】【table】
Claims (1)
れる塩とリノール酸又はその養毛組成物として許
容される塩とを含んで成る混合脂肪酸成分を含有
し、該混合脂肪酸成分に対する前記オレイン酸又
はその塩の配合量が80〜99.9重量%でありそして
リノール酸又はその塩の配合量が0.1〜20重量%
であることを特徴とする養毛組成物。 2 前記混合脂肪酸成分の総量が養毛組成物の総
量に対して0.01〜10重量%である特許請求の範囲
第1項記載の養毛組成物。[Scope of Claims] 1. A mixed fatty acid component comprising oleic acid or a salt thereof acceptable as a hair nourishing composition and linoleic acid or a salt thereof acceptable as a hair nourishing composition; The blending amount of the oleic acid or its salt is 80 to 99.9% by weight, and the blending amount of linoleic acid or its salt is 0.1 to 20% by weight.
A hair nourishing composition characterized by: 2. The hair nourishing composition according to claim 1, wherein the total amount of the mixed fatty acid component is 0.01 to 10% by weight based on the total amount of the hair nourishing composition.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP13898584A JPS6118709A (en) | 1984-07-06 | 1984-07-06 | Hair tonic composition containing mixed fatty acid |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP13898584A JPS6118709A (en) | 1984-07-06 | 1984-07-06 | Hair tonic composition containing mixed fatty acid |
Publications (2)
Publication Number | Publication Date |
---|---|
JPS6118709A JPS6118709A (en) | 1986-01-27 |
JPH0460446B2 true JPH0460446B2 (en) | 1992-09-28 |
Family
ID=15234781
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP13898584A Granted JPS6118709A (en) | 1984-07-06 | 1984-07-06 | Hair tonic composition containing mixed fatty acid |
Country Status (1)
Country | Link |
---|---|
JP (1) | JPS6118709A (en) |
Families Citing this family (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2820951B2 (en) * | 1989-03-30 | 1998-11-05 | マツダ株式会社 | Rear body structure of vehicle |
DE19728832A1 (en) * | 1997-07-05 | 1999-01-07 | Wella Ag | Means for increasing the shine of hair |
JP6453546B2 (en) * | 2014-02-19 | 2019-01-16 | 株式会社サロン・ド・リジュー | Hair growth composition |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS5051986A (en) * | 1972-11-03 | 1975-05-09 |
-
1984
- 1984-07-06 JP JP13898584A patent/JPS6118709A/en active Granted
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS5051986A (en) * | 1972-11-03 | 1975-05-09 |
Also Published As
Publication number | Publication date |
---|---|
JPS6118709A (en) | 1986-01-27 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
US4885289A (en) | Alteration of character of male beard growth | |
EP0116439A2 (en) | Fatty acid containing hair tonic composition | |
US3729560A (en) | Treatment of hair and scalp with compositions containing estriol | |
CA2212127A1 (en) | Formulations and methods for reducing skin irritation | |
JP3049593B2 (en) | Hair restorer | |
US20110236503A1 (en) | Topical Skincare Composition | |
JP3223404B2 (en) | Hair restorer | |
AU584070B2 (en) | Hair growth modification | |
JPH11286423A (en) | Composition for suppressing body odor | |
JPS59172411A (en) | Hair tonic composition containing fatty acid | |
JPH0460446B2 (en) | ||
JPH0853327A (en) | Hair tonic composed of allantoin or its derivative | |
US4272508A (en) | Cosmetics for treatment of hair and skin | |
JPS59152308A (en) | Hair tonic composition containing oleic acid | |
JPS5910323B2 (en) | Cosmetics that suppress skin and mucous membrane irritation | |
JPH07267830A (en) | Hair-growing hair-tonic agent | |
JPH02311411A (en) | Hair-culturing agent | |
JP3227378B2 (en) | Epidermal keratinization promoter | |
JPS59152307A (en) | Hair tonic composition containing arachidonic acid | |
JPS59141514A (en) | Hair tonic composition containing linoleic acid | |
JPH0112725B2 (en) | ||
JP3014215B2 (en) | Hair restoration cosmetics | |
JPH0465044B2 (en) | ||
JPH0552802B2 (en) | ||
JPH0227965B2 (en) | YOMORYO |