JP6407577B2 - Composition for external use - Google Patents
Composition for external use Download PDFInfo
- Publication number
- JP6407577B2 JP6407577B2 JP2014123806A JP2014123806A JP6407577B2 JP 6407577 B2 JP6407577 B2 JP 6407577B2 JP 2014123806 A JP2014123806 A JP 2014123806A JP 2014123806 A JP2014123806 A JP 2014123806A JP 6407577 B2 JP6407577 B2 JP 6407577B2
- Authority
- JP
- Japan
- Prior art keywords
- peg
- composition
- acid
- component
- polyquaternium
- 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.)
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- 239000000203 mixture Substances 0.000 title claims description 126
- 235000014113 dietary fatty acids Nutrition 0.000 claims description 95
- 239000000194 fatty acid Substances 0.000 claims description 95
- 229930195729 fatty acid Natural products 0.000 claims description 95
- -1 polyoxyethylene Polymers 0.000 claims description 80
- 150000004665 fatty acids Chemical class 0.000 claims description 67
- 239000002253 acid Substances 0.000 claims description 45
- 150000003839 salts Chemical class 0.000 claims description 30
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims description 28
- 239000002562 thickening agent Substances 0.000 claims description 26
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 22
- 229920006317 cationic polymer Polymers 0.000 claims description 20
- 150000001413 amino acids Chemical class 0.000 claims description 19
- 230000008719 thickening Effects 0.000 claims description 19
- RMTFNDVZYPHUEF-XZBKPIIZSA-N 3-O-methyl-D-glucose Chemical compound O=C[C@H](O)[C@@H](OC)[C@H](O)[C@H](O)CO RMTFNDVZYPHUEF-XZBKPIIZSA-N 0.000 claims description 15
- IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 claims description 13
- 239000002280 amphoteric surfactant Substances 0.000 claims description 13
- 239000004094 surface-active agent Substances 0.000 claims description 12
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 10
- 238000000034 method Methods 0.000 claims description 9
- 238000005406 washing Methods 0.000 claims description 9
- 229920002907 Guar gum Polymers 0.000 claims description 8
- 235000021355 Stearic acid Nutrition 0.000 claims description 8
- 239000003795 chemical substances by application Substances 0.000 claims description 8
- 239000000665 guar gum Substances 0.000 claims description 8
- 235000010417 guar gum Nutrition 0.000 claims description 8
- 229960002154 guar gum Drugs 0.000 claims description 8
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims description 8
- 239000008117 stearic acid Substances 0.000 claims description 8
- DWANEFRJKWXRSG-UHFFFAOYSA-N 1,2-tetradecanediol Chemical compound CCCCCCCCCCCCC(O)CO DWANEFRJKWXRSG-UHFFFAOYSA-N 0.000 claims description 6
- MQFYRUGXOJAUQK-UHFFFAOYSA-N 2-[2-[2-(2-octadecanoyloxyethoxy)ethoxy]ethoxy]ethyl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCCOCCOCCOCCOC(=O)CCCCCCCCCCCCCCCCC MQFYRUGXOJAUQK-UHFFFAOYSA-N 0.000 claims description 6
- BYBLEWFAAKGYCD-UHFFFAOYSA-N Miconazole Chemical compound ClC1=CC(Cl)=CC=C1COC(C=1C(=CC(Cl)=CC=1)Cl)CN1C=NC=C1 BYBLEWFAAKGYCD-UHFFFAOYSA-N 0.000 claims description 6
- 229960002509 miconazole Drugs 0.000 claims description 6
- ZVUNTIMPQCQCAQ-UHFFFAOYSA-N 2-dodecanoyloxyethyl dodecanoate Chemical compound CCCCCCCCCCCC(=O)OCCOC(=O)CCCCCCCCCCC ZVUNTIMPQCQCAQ-UHFFFAOYSA-N 0.000 claims 2
- RFVNOJDQRGSOEL-UHFFFAOYSA-N 2-hydroxyethyl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCCO RFVNOJDQRGSOEL-UHFFFAOYSA-N 0.000 claims 2
- 229940117924 peg-150 stearate Drugs 0.000 claims 2
- 125000000913 palmityl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000004079 stearyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 239000003240 coconut oil Substances 0.000 description 42
- 235000019864 coconut oil Nutrition 0.000 description 36
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 description 30
- 230000000694 effects Effects 0.000 description 30
- KWIUHFFTVRNATP-UHFFFAOYSA-N Betaine Natural products C[N+](C)(C)CC([O-])=O KWIUHFFTVRNATP-UHFFFAOYSA-N 0.000 description 22
- KWIUHFFTVRNATP-UHFFFAOYSA-O N,N,N-trimethylglycinium Chemical compound C[N+](C)(C)CC(O)=O KWIUHFFTVRNATP-UHFFFAOYSA-O 0.000 description 22
- 229960003237 betaine Drugs 0.000 description 22
- 229940121375 antifungal agent Drugs 0.000 description 21
- 239000003429 antifungal agent Substances 0.000 description 21
- 229940024606 amino acid Drugs 0.000 description 19
- 235000001014 amino acid Nutrition 0.000 description 19
- 238000002360 preparation method Methods 0.000 description 17
- 125000002252 acyl group Chemical group 0.000 description 15
- 239000002736 nonionic surfactant Substances 0.000 description 13
- 239000000047 product Substances 0.000 description 11
- POULHZVOKOAJMA-UHFFFAOYSA-N dodecanoic acid Chemical compound CCCCCCCCCCCC(O)=O POULHZVOKOAJMA-UHFFFAOYSA-N 0.000 description 10
- 238000009472 formulation Methods 0.000 description 10
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 10
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 9
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 description 9
- 239000000126 substance Substances 0.000 description 9
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 8
- 239000003921 oil Substances 0.000 description 8
- 235000019198 oils Nutrition 0.000 description 8
- 229920005989 resin Polymers 0.000 description 8
- 239000011347 resin Substances 0.000 description 8
- 239000002453 shampoo Substances 0.000 description 8
- 239000000344 soap Substances 0.000 description 8
- XOAAWQZATWQOTB-UHFFFAOYSA-N taurine Chemical compound NCCS(O)(=O)=O XOAAWQZATWQOTB-UHFFFAOYSA-N 0.000 description 8
- 239000003814 drug Substances 0.000 description 7
- 238000002156 mixing Methods 0.000 description 7
- 229920000642 polymer Polymers 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 6
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 6
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 6
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 6
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 description 6
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 description 6
- 241000282320 Panthera leo Species 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
- 238000004140 cleaning Methods 0.000 description 6
- 230000000052 comparative effect Effects 0.000 description 6
- SUMDYPCJJOFFON-UHFFFAOYSA-N isethionic acid Chemical compound OCCS(O)(=O)=O SUMDYPCJJOFFON-UHFFFAOYSA-N 0.000 description 6
- MCCACAIVAXEFAL-UHFFFAOYSA-N 1-[2-(2,4-dichlorophenyl)-2-[(2,4-dichlorophenyl)methoxy]ethyl]imidazole;nitric acid Chemical compound O[N+]([O-])=O.ClC1=CC(Cl)=CC=C1COC(C=1C(=CC(Cl)=CC=1)Cl)CN1C=NC=C1 MCCACAIVAXEFAL-UHFFFAOYSA-N 0.000 description 5
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 5
- 229920000289 Polyquaternium Polymers 0.000 description 5
- GSEJCLTVZPLZKY-UHFFFAOYSA-N Triethanolamine Chemical compound OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 description 5
- 239000003945 anionic surfactant Substances 0.000 description 5
- 239000002537 cosmetic Substances 0.000 description 5
- 239000003349 gelling agent Substances 0.000 description 5
- 229960005040 miconazole nitrate Drugs 0.000 description 5
- 239000011593 sulfur Substances 0.000 description 5
- 229910052717 sulfur Inorganic materials 0.000 description 5
- XDOFQFKRPWOURC-UHFFFAOYSA-N 16-methylheptadecanoic acid Chemical compound CC(C)CCCCCCCCCCCCCCC(O)=O XDOFQFKRPWOURC-UHFFFAOYSA-N 0.000 description 4
- GAWIXWVDTYZWAW-UHFFFAOYSA-N C[CH]O Chemical group C[CH]O GAWIXWVDTYZWAW-UHFFFAOYSA-N 0.000 description 4
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 4
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 description 4
- 239000005639 Lauric acid Substances 0.000 description 4
- YTAOBBFIOAEMLL-REQDGWNSSA-N Luliconazole Chemical compound ClC1=CC(Cl)=CC=C1[C@H](CS\1)SC/1=C(\C#N)N1C=NC=C1 YTAOBBFIOAEMLL-REQDGWNSSA-N 0.000 description 4
- 229910019142 PO4 Inorganic materials 0.000 description 4
- 235000019482 Palm oil Nutrition 0.000 description 4
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 4
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 4
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 4
- 208000002474 Tinea Diseases 0.000 description 4
- 241000893966 Trichophyton verrucosum Species 0.000 description 4
- 229960003767 alanine Drugs 0.000 description 4
- 235000004279 alanine Nutrition 0.000 description 4
- 239000002585 base Substances 0.000 description 4
- 125000004432 carbon atom Chemical group C* 0.000 description 4
- 150000001875 compounds Chemical class 0.000 description 4
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 description 4
- 229940079593 drug Drugs 0.000 description 4
- 239000000839 emulsion Substances 0.000 description 4
- 125000005842 heteroatom Chemical group 0.000 description 4
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 4
- 239000007788 liquid Substances 0.000 description 4
- 229960000570 luliconazole Drugs 0.000 description 4
- 229910052757 nitrogen Inorganic materials 0.000 description 4
- 239000003002 pH adjusting agent Substances 0.000 description 4
- 239000002540 palm oil Substances 0.000 description 4
- 239000010452 phosphate Substances 0.000 description 4
- 239000003755 preservative agent Substances 0.000 description 4
- 229960003080 taurine Drugs 0.000 description 4
- 238000012360 testing method Methods 0.000 description 4
- XMAYWYJOQHXEEK-OZXSUGGESA-N (2R,4S)-ketoconazole Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1OC[C@@H]1O[C@@](CN2C=NC=C2)(C=2C(=CC(Cl)=CC=2)Cl)OC1 XMAYWYJOQHXEEK-OZXSUGGESA-N 0.000 description 3
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 description 3
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 description 3
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 description 3
- DCXYFEDJOCDNAF-UHFFFAOYSA-N Asparagine Natural products OC(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-N 0.000 description 3
- 239000001884 Cassia gum Substances 0.000 description 3
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 description 3
- DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 description 3
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 description 3
- 241000047703 Nonion Species 0.000 description 3
- 239000005642 Oleic acid Substances 0.000 description 3
- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 description 3
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- AUNGANRZJHBGPY-SCRDCRAPSA-N Riboflavin Chemical compound OC[C@@H](O)[C@@H](O)[C@@H](O)CN1C=2C=C(C)C(C)=CC=2N=C2C1=NC(=O)NC2=O AUNGANRZJHBGPY-SCRDCRAPSA-N 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- 229920002125 Sokalan® Polymers 0.000 description 3
- AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 description 3
- 239000004473 Threonine Substances 0.000 description 3
- 235000011054 acetic acid Nutrition 0.000 description 3
- 235000010323 ascorbic acid Nutrition 0.000 description 3
- 239000011668 ascorbic acid Substances 0.000 description 3
- 229960005070 ascorbic acid Drugs 0.000 description 3
- 229960001230 asparagine Drugs 0.000 description 3
- 235000009582 asparagine Nutrition 0.000 description 3
- 235000003704 aspartic acid Nutrition 0.000 description 3
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 description 3
- 230000015572 biosynthetic process Effects 0.000 description 3
- 235000019318 cassia gum Nutrition 0.000 description 3
- 229960004022 clotrimazole Drugs 0.000 description 3
- VNFPBHJOKIVQEB-UHFFFAOYSA-N clotrimazole Chemical compound ClC1=CC=CC=C1C(N1C=NC=C1)(C=1C=CC=CC=1)C1=CC=CC=C1 VNFPBHJOKIVQEB-UHFFFAOYSA-N 0.000 description 3
- 150000005690 diesters Chemical class 0.000 description 3
- OVBPIULPVIDEAO-LBPRGKRZSA-N folic acid Chemical compound C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-LBPRGKRZSA-N 0.000 description 3
- 239000000499 gel Substances 0.000 description 3
- 235000013922 glutamic acid Nutrition 0.000 description 3
- 239000004220 glutamic acid Substances 0.000 description 3
- ZDXPYRJPNDTMRX-UHFFFAOYSA-N glutamine Natural products OC(=O)C(N)CCC(N)=O ZDXPYRJPNDTMRX-UHFFFAOYSA-N 0.000 description 3
- 229960002449 glycine Drugs 0.000 description 3
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 description 3
- 229940045996 isethionic acid Drugs 0.000 description 3
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 description 3
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- 125000004433 nitrogen atom Chemical group N* 0.000 description 3
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- 230000002335 preservative effect Effects 0.000 description 3
- 239000008213 purified water Substances 0.000 description 3
- FSYKKLYZXJSNPZ-UHFFFAOYSA-N sarcosine Chemical compound C[NH2+]CC([O-])=O FSYKKLYZXJSNPZ-UHFFFAOYSA-N 0.000 description 3
- 238000003786 synthesis reaction Methods 0.000 description 3
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- IWLROWZYZPNOFC-UHFFFAOYSA-O thiamine triphosphate Chemical compound CC1=C(CCOP(O)(=O)OP(O)(=O)OP(O)(O)=O)SC=[N+]1CC1=CN=C(C)N=C1N IWLROWZYZPNOFC-UHFFFAOYSA-O 0.000 description 3
- GUGWNSHJDUEHNJ-UHFFFAOYSA-N thiamine(1+) monophosphate chloride Chemical compound [Cl-].CC1=C(CCOP(O)(O)=O)SC=[N+]1CC1=CN=C(C)N=C1N GUGWNSHJDUEHNJ-UHFFFAOYSA-N 0.000 description 3
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 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
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 description 2
- AFNXATANNDIXLG-SFHVURJKSA-N 1-[(2r)-2-[(4-chlorophenyl)methylsulfanyl]-2-(2,4-dichlorophenyl)ethyl]imidazole Chemical compound C1=CC(Cl)=CC=C1CS[C@H](C=1C(=CC(Cl)=CC=1)Cl)CN1C=NC=C1 AFNXATANNDIXLG-SFHVURJKSA-N 0.000 description 2
- OCAPBUJLXMYKEJ-UHFFFAOYSA-N 1-[biphenyl-4-yl(phenyl)methyl]imidazole Chemical compound C1=NC=CN1C(C=1C=CC(=CC=1)C=1C=CC=CC=1)C1=CC=CC=C1 OCAPBUJLXMYKEJ-UHFFFAOYSA-N 0.000 description 2
- VHVPQPYKVGDNFY-DFMJLFEVSA-N 2-[(2r)-butan-2-yl]-4-[4-[4-[4-[[(2r,4s)-2-(2,4-dichlorophenyl)-2-(1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-1,2,4-triazol-3-one Chemical compound O=C1N([C@H](C)CC)N=CN1C1=CC=C(N2CCN(CC2)C=2C=CC(OC[C@@H]3O[C@](CN4N=CN=C4)(OC3)C=3C(=CC(Cl)=CC=3)Cl)=CC=2)C=C1 VHVPQPYKVGDNFY-DFMJLFEVSA-N 0.000 description 2
- OSCJHTSDLYVCQC-UHFFFAOYSA-N 2-ethylhexyl 4-[[4-[4-(tert-butylcarbamoyl)anilino]-6-[4-(2-ethylhexoxycarbonyl)anilino]-1,3,5-triazin-2-yl]amino]benzoate Chemical compound C1=CC(C(=O)OCC(CC)CCCC)=CC=C1NC1=NC(NC=2C=CC(=CC=2)C(=O)NC(C)(C)C)=NC(NC=2C=CC(=CC=2)C(=O)OCC(CC)CCCC)=N1 OSCJHTSDLYVCQC-UHFFFAOYSA-N 0.000 description 2
- OYINQIKIQCNQOX-UHFFFAOYSA-M 2-hydroxybutyl(trimethyl)azanium;chloride Chemical compound [Cl-].CCC(O)C[N+](C)(C)C OYINQIKIQCNQOX-UHFFFAOYSA-M 0.000 description 2
- WRMNZCZEMHIOCP-UHFFFAOYSA-N 2-phenylethanol Chemical compound OCCC1=CC=CC=C1 WRMNZCZEMHIOCP-UHFFFAOYSA-N 0.000 description 2
- QGZKDVFQNNGYKY-UHFFFAOYSA-O Ammonium Chemical compound [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 description 2
- 244000303965 Cyamopsis psoralioides Species 0.000 description 2
- RGHNJXZEOKUKBD-SQOUGZDYSA-N D-gluconic acid Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O RGHNJXZEOKUKBD-SQOUGZDYSA-N 0.000 description 2
- SNPLKNRPJHDVJA-ZETCQYMHSA-N D-panthenol Chemical compound OCC(C)(C)[C@@H](O)C(=O)NCCCO SNPLKNRPJHDVJA-ZETCQYMHSA-N 0.000 description 2
- 239000011627 DL-alpha-tocopherol Substances 0.000 description 2
- 235000001815 DL-alpha-tocopherol Nutrition 0.000 description 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 2
- GHJWNRRCRIGGIO-UHFFFAOYSA-N Fosfluconazole Chemical compound C1=NC=NN1CC(C=1C(=CC(F)=CC=1)F)(OP(O)(=O)O)CN1C=NC=N1 GHJWNRRCRIGGIO-UHFFFAOYSA-N 0.000 description 2
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Landscapes
- Medicinal Preparation (AREA)
- Cosmetics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
本発明は、外用組成物に関する。より詳細には、本発明は適度な粘度を有する外用組成物に関する。 The present invention relates to a composition for external use. More specifically, the present invention relates to an external composition having an appropriate viscosity.
外用組成物、特に毛髪や皮膚を洗浄するために用いられる外用組成物では、取り扱いの面から、ある程度粘性を備えた組成物であることが好まれている。なぜなら、粘性が殆んど無いサラサラの液体の場合、容器から掌やボディタオル、スポンジ、ブラシ、タワシ等に取り出した外用組成物が零れ落ちてしまい、十分量の外用組成物を皮膚や毛髪に適用し難くなることがあるからである。 The composition for external use, particularly the composition for external use used for washing hair and skin, is preferably a composition having a certain degree of viscosity from the viewpoint of handling. This is because in the case of a smooth liquid with almost no viscosity, the external composition taken out from the container to the palm, body towel, sponge, brush, scrubbing, etc. will spill out, and a sufficient amount of the external composition is applied to the skin and hair. This is because it may be difficult to apply.
そこで従来、例えば増粘剤の配合量を高めることにより、外用組成物の粘度を高める方法等が試みられている。しかし単純に増粘剤の量を高めるだけでは、粘度は高まるものの、ねっとりした使用感や糸引き等を生じる場合もあり、使用感の面で好ましいとは言い難い外用組成物となる場合も多い。また、増粘剤の種類によっては、配合量を高めることにより水馴染みが悪くなって糊のような感触を生じさせることもあり、やはり使用感の面で好ましくないものとなる。また、毛髪や皮膚の洗浄用の外用組成物では、塩類を配合することが多いが、カルボキシビニルポリマー等の外用剤で汎用されている増粘剤は耐塩性が低く、塩類が存在すると粘度低下を引き起こすことも知られている。 Therefore, conventionally, for example, a method for increasing the viscosity of the composition for external use by increasing the blending amount of the thickener has been attempted. However, simply increasing the amount of the thickening agent increases the viscosity, but may result in a moist feeling of use, stringing, etc., often resulting in a composition for external use that is difficult to say in terms of feeling of use. . Also, depending on the type of thickener, increasing the amount of blending may deteriorate the water familiarity and cause a feeling like glue, which is also unfavorable in terms of use feeling. In addition, in external compositions for washing hair and skin, salts are often added, but thickeners commonly used in external preparations such as carboxyvinyl polymer have low salt resistance, and when salts are present, viscosity decreases. It is also known to cause
これまでにも、適度な粘度を有し使用感にも優れた外用洗浄剤組成物を得る試みとして、(A)高級脂肪酸のカリウム塩、(B)両性界面活性剤および/またはノニオン性界面活性剤、(C)メントールをそれぞれ特定の濃度で含有する洗浄剤組成物とすることが提案されている(特許文献1)。また、(A)高級脂肪酸塩と(B)長鎖炭化水素基含有ベタインとをそれぞれ特定の濃度で含有する洗浄剤組成物とすることで、洗浄に適した十分な粘度を保ちながら、使用感にも優れた洗浄剤組成物を調製できることも提案されている(特許文献2)。 Until now, as an attempt to obtain an external detergent composition having an appropriate viscosity and excellent usability, (A) potassium salt of higher fatty acid, (B) amphoteric surfactant and / or nonionic surfactant It has been proposed to use a cleaning composition containing a specific concentration of the agent and (C) menthol (Patent Document 1). In addition, by using a detergent composition containing (A) a higher fatty acid salt and (B) a long-chain hydrocarbon group-containing betaine at a specific concentration, the usability is maintained while maintaining a sufficient viscosity suitable for washing. It has also been proposed that an excellent cleaning composition can be prepared (Patent Document 2).
しかし、外用組成物、特に毛髪や皮膚を洗浄するために用いられる外用組成物に対して適度な粘性を与える更なる有用な他の手段の開発が求められている。 However, there is a need for the development of another useful means for imparting an appropriate viscosity to the external composition, particularly the external composition used for washing hair and skin.
本発明は、上記従来技術に鑑みてなされたものであり、適度な粘度を有する外用組成物、特に毛髪や皮膚の洗浄のための使用に適した粘度を有する外用組成物を提供することを目的とする。 The present invention has been made in view of the above prior art, and an object of the present invention is to provide an external composition having an appropriate viscosity, particularly an external composition having a viscosity suitable for use for washing hair and skin. And
本発明者は、前記課題を解決するために鋭意検討した結果、(A)アゾール系抗真菌剤、(B)カチオン性ポリマー、及び(C)エチレンオキシドの平均付加モル数が50〜300であるポリオキシエチレン付加型の脂肪酸エステル系又は脂肪酸エーテル系のノニオン性増粘剤を組み合わせて配合することにより、適度な粘度を有する外用組成物を調製できることを見出し、本発明を完成するに至った。 As a result of intensive studies to solve the above problems, the present inventor has found that (A) an azole antifungal agent, (B) a cationic polymer, and (C) an ethylene oxide has an average added mole number of 50 to 300. The present inventors have found that an external composition having an appropriate viscosity can be prepared by combining an oxyethylene addition type fatty acid ester-based or fatty acid ether-based nonionic thickener in combination, and the present invention has been completed.
従って、本発明は、以下に掲げる外用組成物を提供する。
[項1] (A)アゾール系抗真菌剤、(B)カチオン性ポリマー、及び(C)エチレンオキシドの平均付加モル数が50〜300であるポリオキシエチレン付加型の脂肪酸エステル系又は脂肪酸エーテル系のノニオン性増粘剤を含有する、外用組成物。
[項2] 前記(A)アゾール系抗真菌剤として、ミコナゾール、ラノコナゾール、ルリコナゾール、イソコナゾール、ケトコナゾール、クロトリマゾール、フルコナゾール、イトラコナゾール、ネチコナゾール、スルコナゾール、ビフホナゾール、ホスフルコナゾール、ボリコナゾール、及びそれらの塩からなる群より選択される少なくとも1種を含む、項1に記載の外用組成物。
[項3] 前記(B)カチオン性ポリマーとして、ポリクオタニウム−10、ポリクオタニウム−7、ポリクオタニウム−2、ポリクオタニウム−4、ポリクオタニウム−5、ポリクオタニウム−6、ポリクオタニウム−11、ポリクオタニウム−16、ポリクオタニウム−22、ポリクオタニウム−24、ポリクオタニウム−28、ポリクオタニウム−30、ポリクオタニウム−32、ポリクオタニウム−33、ポリクオタニウム−37、ポリクオタニウム−39、ポリクオタニウム−43、ポリクオタニウム−44、ポリクオタニウム−46、ポリクオタニウム−47、ポリクオタニウム−49、ポリクオタニウム−51、ポリクオタニウム−52、ポリクオタニウム−53、ポリクオタニウム−54、ポリクオタニウム−55、ポリクオタニウム−56、ポリクオタニウム−57、ポリクオタニウム−61、ポリクオタニウム−64、ポリクオタニウム−65、ポリクオタニウム−68、ポリクオタニウム−92、カチオン化グアーガム、カチオン化カッシアガム、及びカチオン化タラガムからなる群より選択される少なくとも1種を含む、項1又は2に記載の外用組成物。
[項4] 前記(C)成分が、炭素数12〜24の脂肪酸をエステル化又はエーテル化した構造を有するものである、項1〜3のいずれかに記載の外用組成物。
[項5] 前記(C)成分として、ジオレイン酸PEG−120メチルグルコース、トリオレイン酸PEG−120メチルグルコース、トリイソステアリン酸PEG−120メチルグルコース、ジオレイン酸PEG−75、ジステアリン酸PEG−75、ジステアリン酸PEG−140、ジステアリン酸PEG−150、ジステアリン酸PEG−175、ジステアリン酸PEG−190、ジステアリン酸PEG−250、ステアリン酸PEG−75、ステアリン酸PEG−150、ジラウリン酸PEG−75、セテアレス−60ミリスチルグリコール、及びポリオキシエチレンセチルステアリルジエーテルからなる群より選択される少なくとも1種を含む、項1〜4のいずれかに記載の外用組成物。
[項6] 25℃における粘度が300mPa・s以上である、項1〜5のいずれかに記載の外用組成物。
[項7] 前記(A)成分の含有量が、組成物全量に対して0.01重量%以上である、項1〜6のいずれかに記載の外用組成物。
[項8] 前記(B)成分の含有量が、組成物全量に対して0.01重量%以上である、項1〜7のいずれかに記載の外用組成物。
[項9] 前記(C)成分の含有量が、組成物全量に対して0.1重量%以上である、項1〜8のいずれかに記載の外用組成物。
[項10] 毛髪又は皮膚を洗浄するために用いられる、項1〜9のいずれかに記載の外用組成物。
更に本発明は、以下に掲げる組成物の増粘方法を提供する。
[項11] 外用組成物中に、(A)アゾール系抗真菌剤、(B)カチオン性ポリマー、及び(C)エチレンオキシドの平均付加モル数が50〜300であるポリオキシエチレン付加型の脂肪酸エステル系又は脂肪酸エーテル系のノニオン性増粘剤を共存させることで、該外用組成物を増粘する方法。
Therefore, this invention provides the composition for external use hung up below.
[Item 1] (A) an azole antifungal agent, (B) a cationic polymer, and (C) a polyoxyethylene addition type fatty acid ester type or fatty acid ether type having an average addition mole number of ethylene oxide of 50 to 300 An external composition containing a nonionic thickener.
[Item 2] The (A) azole antifungal agent comprises miconazole, ranoconazole, luliconazole, isoconazole, ketoconazole, clotrimazole, fluconazole, itraconazole, neticonazole, sulconazole, bifonazole, phosfluconazole, voriconazole, and salts thereof. Item 2. The external composition according to Item 1, comprising at least one selected from the group.
[Item 3] As the cationic polymer (B), polyquaternium-10, polyquaternium-7, polyquaternium-2, polyquaternium-4, polyquaternium-5, polyquaternium-6, polyquaternium-11, polyquaternium-16, polyquaternium-22, polyquaternium -24, polyquaternium-28, polyquaternium-30, polyquaternium-32, polyquaternium-33, polyquaternium-37, polyquaternium-39, polyquaternium-43, polyquaternium-44, polyquaternium-46, polyquaternium-47, polyquaternium-49, polyquaternium-51 , Polyquaternium-52, Polyquaternium-53, Polyquaternium-54, Polyquaternium-55, Polyqua At least one selected from the group consisting of titanium-56, polyquaternium-57, polyquaternium-61, polyquaternium-64, polyquaternium-65, polyquaternium-68, polyquaternium-92, cationized guar gum, cationized cassia gum, and cationized tara gum. Item 3. The composition for external use according to Item 1 or 2, comprising
[Item 4] The composition for external use according to any one of Items 1 to 3, wherein the component (C) has a structure obtained by esterifying or etherifying a fatty acid having 12 to 24 carbon atoms.
[Item 5] As the component (C), PEG-120 methyl glucose dioleate, PEG-120 methyl glucose trioleate, PEG-120 methyl glucose triisostearate, PEG-75 dioleate, PEG-75 distearate, distearate Acid PEG-140, Distearic acid PEG-150, Distearic acid PEG-175, Distearic acid PEG-190, Distearic acid PEG-250, Stearic acid PEG-75, Stearic acid PEG-150, Dilauric acid PEG-75, Ceteares-60 Item 5. The external composition according to any one of Items 1 to 4, comprising at least one selected from the group consisting of myristyl glycol and polyoxyethylene cetyl stearyl diether.
CLAIM | ITEM 6 The external composition in any one of claim | item 1 -5 whose viscosity in 25 degreeC is 300 mPa * s or more.
CLAIM | ITEM 7 The external composition in any one of claim | item 1 -6 whose content of the said (A) component is 0.01 weight% or more with respect to the composition whole quantity.
CLAIM | ITEM 8 External composition in any one of claim | item 1 -7 whose content of the said (B) component is 0.01 weight% or more with respect to the composition whole quantity.
CLAIM | ITEM 9 The external composition in any one of claim | item 1 -8 whose content of the said (C) component is 0.1 weight% or more with respect to the composition whole quantity.
CLAIM | ITEM 10 External composition in any one of claim | item 1-9 used in order to wash | clean hair or skin.
Furthermore, the present invention provides a method for thickening the composition described below.
[Item 11] In a composition for external use, (A) an azole antifungal agent, (B) a cationic polymer, and (C) a polyoxyethylene addition type fatty acid ester having an average addition mole number of ethylene oxide of 50 to 300 A method of thickening the composition for external use by coexisting a nonionic thickener based on a fatty acid or a fatty acid ether.
本発明により、適度な粘度を有する外用組成物、特に毛髪や皮膚の洗浄への使用に適した適度な粘度を有する外用組成物を提供することができる。 According to the present invention, an external composition having an appropriate viscosity, particularly an external composition having an appropriate viscosity suitable for use in washing hair or skin can be provided.
本発明の外用組成物は、(A)アゾール系抗真菌剤、(B)カチオン性ポリマー、及び(C)エチレンオキシドの平均付加モル数が50〜300であるポリオキシエチレン付加型の脂肪酸エステル系又は脂肪酸エーテル系のノニオン性増粘剤を含有する。 The composition for external use of the present invention comprises (A) an azole antifungal agent, (B) a cationic polymer, and (C) a polyoxyethylene addition type fatty acid ester system having an average addition mole number of ethylene oxide of 50 to 300 or Contains a fatty acid ether-based nonionic thickener.
本発明に用いられる(A)アゾール系抗真菌剤としては、アゾール骨格(1つ以上の窒素原子を含む複素5員環化合物)を共通に有する抗真菌剤として周知の化合物であって、薬学的又は生理学的に許容可能な任意のアゾール系抗真菌剤を使用することができる。アゾール系抗真菌剤としては、例えば、イミダゾール環(2個の窒素原子を含む複素5員環)を有するイミダゾール系抗真菌剤、トリアゾール環(3個の窒素原子を含む複素5員環)を有するトリコナゾール系抗真菌剤等を挙げることができる。より具体的には、ミコナゾール、ラノコナゾール、ルリコナゾール、イソコナゾール、ケトコナゾール、クロトリマゾール、ネチコナゾール、スルコナゾール、ビホナゾール及びこれらの塩等のイミダゾール系抗真菌剤;フルコナゾール、イトラコナゾール、ホスフルコナゾール、ボリコナゾール及びこれらの塩等のトリコナゾール系抗真菌剤を挙げることができ、本発明に好適に使用することができる。特に限定はされないが、より確実に高い本発明の効果が期待できるという観点から、イミダゾール系抗真菌剤が好ましく用いられる。また、より高い増粘効果が期待できるという観点から、芳香環上の少なくとも1個、好ましくは2個以上の水素原子がハロゲン原子(フッ素(F)、塩素(Cl)、臭素(Br)、ヨウ素(I)等)で置換されたハロゲン化アリール構造を有するアゾール系抗真菌剤であることが好ましい。以上のような観点を考慮して、本発明に用いられるアゾール系抗真菌剤としては、好ましくは、ミコナゾール、ラノコナゾール、ルリコナゾール、イソコナゾール、ケトコナゾール、クロトリマゾール、及びこれらの塩であり、より好ましくはミコナゾール及びその塩(例えば、ミコナゾール硝酸塩)が用いられるのがよい。このようなアゾール系抗真菌剤は、合成によって入手してもよく、また市販品を使用することもできる。 The (A) azole antifungal agent used in the present invention is a compound well known as an antifungal agent having a common azole skeleton (a hetero 5-membered ring compound containing one or more nitrogen atoms), Alternatively, any physiologically acceptable azole antifungal agent can be used. As the azole antifungal agent, for example, an imidazole antifungal agent having an imidazole ring (hetero 5-membered ring containing 2 nitrogen atoms) or a triazole ring (hetero 5-membered hetero ring containing 3 nitrogen atoms) is used. A triconazole type antifungal agent etc. can be mentioned. More specifically, imidazole antifungal agents such as miconazole, lanoconazole, luliconazole, isconazole, ketoconazole, clotrimazole, neticoconazole, sulconazole, bifonazole and salts thereof; fluconazole, itraconazole, phosfluconazole, voriconazole and salts thereof, etc. The triconazole type antifungal agent can be mentioned and can be preferably used in the present invention. Although not particularly limited, an imidazole antifungal agent is preferably used from the viewpoint that a higher effect of the present invention can be expected with certainty. From the viewpoint that a higher thickening effect can be expected, at least one, preferably two or more hydrogen atoms on the aromatic ring are halogen atoms (fluorine (F), chlorine (Cl), bromine (Br), iodine). An azole antifungal agent having an aryl halide structure substituted with (I) or the like) is preferred. In view of the above viewpoints, the azole antifungal agent used in the present invention is preferably miconazole, lanoconazole, luliconazole, isconazole, ketoconazole, clotrimazole, and salts thereof, more preferably. Miconazole and its salts (eg, miconazole nitrate) may be used. Such an azole antifungal agent may be obtained by synthesis, or a commercially available product may be used.
なお、本明細書において「塩」とは、例えば、アルカリ金属塩、アルカリ土類金属塩、有機塩基等との塩が例示され、ナトリウム、カリウム、カルシウム、マグネシウム、アンモニウム、またはジエタノールアミン、トリエタノールアミン、エチレンジアミン等との塩が挙げられる。また、例えば、塩酸、臭化水素酸、硫酸、硝酸、リン酸等の無機酸の塩;メタンスルホン酸、ベンゼンスルホン酸、パラトルエンスルホン酸、酢酸、プロピオン酸、酒石酸、フマル酸、マレイン酸、リンゴ酸、シュウ酸、コハク酸、クエン酸、安息香酸、マンデル酸、ケイ皮酸、乳酸、グリコール酸、グルクロン酸、アスコルビン酸、ニコチン酸、サリチル酸等の有機酸との塩;又はアスパラギン酸、グルタミン酸などの酸性アミノ酸との塩なども挙げられる。好ましくは、無機酸の塩であり、より好ましくは硝酸塩である。なお、「塩」には、塩の溶媒和物または水和物を含んでいてもよい。 In the present specification, examples of the “salt” include salts with alkali metal salts, alkaline earth metal salts, organic bases, and the like, such as sodium, potassium, calcium, magnesium, ammonium, diethanolamine, and triethanolamine. And salts with ethylenediamine and the like. In addition, for example, salts of inorganic acids such as hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid; methanesulfonic acid, benzenesulfonic acid, paratoluenesulfonic acid, acetic acid, propionic acid, tartaric acid, fumaric acid, maleic acid, Malic acid, oxalic acid, succinic acid, citric acid, benzoic acid, mandelic acid, cinnamic acid, lactic acid, glycolic acid, glucuronic acid, ascorbic acid, nicotinic acid, salts with organic acids such as salicylic acid; or aspartic acid, glutamic acid And salts with acidic amino acids such as Preferred are inorganic acid salts, and more preferred are nitrates. The “salt” may include a solvate or hydrate of a salt.
本発明の外用組成物中における(A)成分の含有量は、本発明の効果を奏しうる限り特に限定されないが、一例として、組成物全量に対して、約0.01重量%以上、好ましくは約0.05重量%以上、より好ましくは約0.1重量%以上である。(A)成分の含有量の上限もまた、本発明の効果を奏し得る限り特に限定はされないが、組成物全量に対して、一例として約3重量%以下、好ましくは約2重量%以下、より好ましくは約1.5重量%以下とするのがよい。 The content of the component (A) in the composition for external use of the present invention is not particularly limited as long as the effects of the present invention can be achieved. As an example, the content is about 0.01% by weight or more, preferably about 0.05% with respect to the total amount of the composition. % By weight or more, more preferably about 0.1% by weight or more. The upper limit of the content of the component (A) is not particularly limited as long as the effects of the present invention can be obtained, but is about 3% by weight or less, preferably about 2% by weight or less, as an example, based on the total amount of the composition. The amount is preferably about 1.5% by weight or less.
本発明の外用組成物は、上記(A)成分に加えて、更に(B)カチオン性ポリマーを含有する。本発明に用いられるカチオン性ポリマーは、カチオン性を示す任意のポリマーであり得る。カチオン性ポリマーとしては、具体的には、4級アミノ基を側鎖として有する高分子化合物の総称であるポリクオタニウムと称されるポリマーを好適に使用できる。ポリクオタニウムは、FDA(米国食品医薬品局)にも化粧料原料として認められている。そして、ポリクオタニウムに番号をそれぞれ付したものが、PCPC(米国化粧品工業会;旧CTFA)において、INCI(化粧品原料国際命名法)に従ってINCI名として登録されている。また、カチオン性ポリマーとして、天然高分子のカチオン化物も好適に使用することができる。 The composition for external use of the present invention further contains (B) a cationic polymer in addition to the component (A). The cationic polymer used in the present invention can be any polymer that exhibits cationic properties. As the cationic polymer, specifically, a polymer called polyquaternium, which is a general term for polymer compounds having a quaternary amino group as a side chain, can be preferably used. Polyquaternium is also recognized as a cosmetic ingredient by the FDA (Food and Drug Administration). Each of the polyquaterniums numbered is registered as an INCI name in accordance with INCI (International Cosmetic Nomenclature) in PCPC (American Cosmetic Industry Association; former CTFA). Moreover, as a cationic polymer, a cationized natural polymer can also be suitably used.
このようなカチオン性ポリマーとしては、例えば、ポリクオタニウム-10、ポリクオタニウム−6、ポリクオタニウム−7、ポリクオタニウム−2、ポリクオタニウム−4、ポリクオタニウム−5、ポリクオタニウム−11、ポリクオタニウム−16、ポリクオタニウム−22、ポリクオタニウム−24、ポリクオタニウム−28、ポリクオタニウム−30、ポリクオタニウム−32、ポリクオタニウム−33、ポリクオタニウム−37、ポリクオタニウム−39、ポリクオタニウム−43、ポリクオタニウム−44、ポリクオタニウム−46、ポリクオタニウム−47、ポリクオタニウム−49、ポリクオタニウム−51、ポリクオタニウム−52、ポリクオタニウム−53、ポリクオタニウム−54、ポリクオタニウム−55、ポリクオタニウム−56、ポリクオタニウム−57、ポリクオタニウム−61、ポリクオタニウム−64、ポリクオタニウム−65、ポリクオタニウム−68、ポリクオタニウム−92等のようなポリクオタニウム類;カチオン化グアーガム、カチオン化カッシアガム、カチオン化タラガム、カチオン化フェヌグリークガム、カチオン化ローカストビーンガム等のような天然高分子のカチオン化物;等を挙げることができるが、これらに限定されない。より確実に高い増粘効果が期待できるという観点から、好ましくは、ポリクオタニウム-10〔ヒドロキシエチルセルロースに塩化グリシジルトリメチルアンモニウムを付加して得られる4級アンモニウム塩の重合体〕、ポリクオタニウム−6〔塩化ジメチルジアリルアンモニウム重合体〕、ポリクオタニウム−7〔アクリル酸アミドと塩化ジメチルジアリルアンモニウムから得られる4級アンモニウム塩の重合体〕、カチオン化グアーガム〔グアーヒドロキシプロピルトリモニウムクロリド〕、カチオン化カッシアガム〔カッシアヒドロキシプロピルトリモニウムクロリド〕、カチオン化タラガム〔カエサルピニアスピノサヒドロキシプロピルトリモニウムクロリド〕を挙げることができ、より好ましくはポリクオタニウム-10、ポリクオタニウム-7、ポリクオタニウム-6、カチオン化グアーガム、更に好ましくはポリクオタニウム-10、カチオン化グアーガム、特に好ましくはポリクオタニウム-10が用いられる。このようなカチオン性ポリマーは、合成によって入手してもよく、また市販品を使用することもできる。 Examples of such cationic polymers include polyquaternium-10, polyquaternium-6, polyquaternium-7, polyquaternium-2, polyquaternium-4, polyquaternium-5, polyquaternium-11, polyquaternium-16, polyquaternium-22, and polyquaternium-24. , Polyquaternium-28, polyquaternium-30, polyquaternium-32, polyquaternium-33, polyquaternium-37, polyquaternium-39, polyquaternium-43, polyquaternium-44, polyquaternium-46, polyquaternium-47, polyquaternium-49, polyquaternium-51, polyquaternium-51 -52, Polyquaternium-53, Polyquaternium-54, Polyquaternium-55, Polyquaternium-56, Polyquaternium-57, Polyquaternium-61, Polyquat Polyquaterniums such as Titanium-64, Polyquaternium-65, Polyquaternium-68, Polyquaternium-92, etc .; natural highs such as cationized guar gum, cationized cassia gum, cationized tara gum, cationized fenugreek gum, cationized locust bean gum, etc. Examples thereof include, but are not limited to, cationized molecules. From the viewpoint that a higher thickening effect can be expected more reliably, polyquaternium-10 [polymer of quaternary ammonium salt obtained by adding glycidyltrimethylammonium chloride to hydroxyethylcellulose], polyquaternium-6 [dimethyldiallyl chloride] Ammonium polymer], polyquaternium-7 [polymer of quaternary ammonium salt obtained from acrylic acid amide and dimethyldiallylammonium chloride], cationized guar gum [guar hydroxypropyltrimonium chloride], cationized cassia gum [cassia hydroxypropyltrimonium] Chloride) and cationized tara gum [Caesarpinia spinosahydroxypropyltrimonium chloride], more preferably polyquaternium-10, polyquaternium-7 Polyquaternium-6, cationized guar gum, more preferably polyquaternium-10, and cationized guar gum, particularly preferably polyquaternium-10. Such a cationic polymer may be obtained by synthesis, or a commercially available product may be used.
ポリクオタニウム−10は、カチオン化セルロースとも称され、別名、塩化O−[2−ヒドロキシ−3−(トリメチルアンモニオ)プロピル]ヒドロキシエチルセルロース、又は塩化トリメチルアンモニオヒドロキシプロピルヒドロキシエチルセルロースとも呼ばれるカチオン性ポリマーである。ポリクオタニウム-10の市販品としては、例えば、ポイズC-150L(花王)、ポイズC-60H(花王)、ポイズC-80M(花王)、MIRAPOL PQ−10(三晶)、ジェルナー(ダイセル化学工業)、UCARE Polymer(ダウ・ケミカル日本)、カチナールHC−100(東邦化学工業)、カチナールHC-200(東邦化学工業)、カチナールLC−100(東邦化学工業)、カチナールLC-200(東邦化学工業)、Merquat10(ルーブリゾール)、CELQUAT SC-230M(アクゾノーベル)、CELQUAT SC-240C(アクゾノーベル)等を挙げることができる。また、ポリクオタニウム−10を含有する市販の混合原料を使用してもよく、このような混合原料としては、例えば、DNシリコンエマルジョン100000(大日本化成)、レオガードG(ライオン)、レオガードGP(ライオン)、レオガードKGP(ライオン)、レオガードLP(ライオン)、レオガードMGP(ライオン)、レオガードMLP(ライオン)等を挙げることができる。 Polyquaternium-10, also referred to as cationized cellulose, is a cationic polymer, also known as O- [2-hydroxy-3- (trimethylammonio) propyl] hydroxyethylcellulose, or trimethylammoniohydroxypropylhydroxyethylcellulose chloride. . Examples of commercially available products of Polyquaternium-10 include Poise C-150L (Kao), Poise C-60H (Kao), Poise C-80M (Kao), MIRAPOL PQ-10 (Sanshin), and Gerner (Daicel Chemical Industries). , UCARE Polymer (Dow Chemical Japan), Katchinal HC-100 (Toho Chemical Industry), Katchinal HC-200 (Toho Chemical Industry), Katchinal LC-100 (Toho Chemical Industry), Katchinal LC-200 (Toho Chemical Industry), Merquat 10 (Lubrisol), CELQUAT SC-230M (Akzo Nobel), CELQUAT SC-240C (Akzo Nobel) and the like can be mentioned. Commercially available mixed raw materials containing polyquaternium-10 may also be used. Examples of such mixed raw materials include DN silicon emulsion 100000 (Dainippon Kasei), Leoguard G (Lion), Leoguard GP (Lion) , Leo Guard KGP (Lion), Leo Guard LP (Lion), Leo Guard MGP (Lion), Leo Guard MLP (Lion), etc.
本発明に用いられる(B)カチオン性ポリマーの重量平均分子量としては、本発明の効果を奏し得る限り特に限定されず、任意の分子量のものが用いられ得る。一例として、本発明には、分子量1万以上、好ましくは5万以上、より好ましくは10万以上のカチオン性ポリマーが用いられ得る。(C)成分の重量平均分子量の上限値は、特に限定されないが、通常2000万以下、好ましくは1000万以下、より好ましくは500万以下のものを用いることができる。 The weight average molecular weight of the cationic polymer (B) used in the present invention is not particularly limited as long as the effects of the present invention can be obtained, and those having any molecular weight can be used. As an example, a cationic polymer having a molecular weight of 10,000 or more, preferably 50,000 or more, more preferably 100,000 or more can be used in the present invention. Although the upper limit of the weight average molecular weight of (C) component is not specifically limited, Usually, 20 million or less, Preferably it is 10 million or less, More preferably, 5 million or less can be used.
上記(B)成分の窒素含量も、本発明の効果を奏し得る限り特に限定されず、任意の窒素含量のものが用いられ得る。一例として、本発明に用いられる(B)の窒素含量として、0.5〜5%程度のものを挙げることができる。 The nitrogen content of the component (B) is not particularly limited as long as the effects of the present invention can be achieved, and those having any nitrogen content can be used. As an example, the nitrogen content of (B) used in the present invention can be about 0.5 to 5%.
本発明の外用組成物における(B)成分の含有量は、本発明の効果を奏しうる限り特に限定されないが、一例として、組成物全量に対して、約0.01重量%以上、好ましくは約0.05重量%以上、より好ましくは約0.1重量%以上である。(B)成分の含有量の上限もまた、本発明の効果を奏し得る限り特に限定はされないが、組成物全量に対して、一例として約3重量%以下、好ましくは約2重量%以下、より好ましくは約1重量%以下とするのがよい。 The content of the component (B) in the composition for external use of the present invention is not particularly limited as long as the effects of the present invention can be achieved. As an example, the content is about 0.01% by weight or more, preferably about 0.05% by weight based on the total amount of the composition. % Or more, more preferably about 0.1% by weight or more. The upper limit of the content of the component (B) is not particularly limited as long as the effect of the present invention can be obtained, but is about 3% by weight or less, preferably about 2% by weight or less, as an example, based on the total amount of the composition. Preferably it is about 1% by weight or less.
更に本発明の外用組成物において、(A)成分の含有量に対する(B)成分の含有量の比率については、特に制限されないが、より一層効果的に本発明の効果を発揮できるという観点から、一例として、(A)成分の含有量1重量部当たり、(B)成分の含有量が総量で約0.001〜5重量部、好ましくは約0.005〜4重量部、より好ましくは約0.01〜3重量部となる比率が例示される。 Furthermore, in the composition for external use of the present invention, the ratio of the content of the component (B) to the content of the component (A) is not particularly limited, but from the viewpoint that the effect of the present invention can be exhibited more effectively. As an example, the content of component (B) is about 0.001 to 5 parts by weight, preferably about 0.005 to 4 parts by weight, more preferably about 0.01 to 3 parts by weight per part by weight of component (A) The ratio which becomes is illustrated.
本発明の外用組成物は、上記(A)成分及び(B)成分に加えて、更に(C)エチレンオキシドの平均付加モル数が50〜300であるポリオキシエチレン付加型の脂肪酸エステル系又は脂肪酸エーテル系のノニオン性増粘剤を含有する。 In addition to the above components (A) and (B), the composition for external use of the present invention further comprises (C) a polyoxyethylene addition type fatty acid ester or fatty acid ether having an average addition mole number of ethylene oxide of 50 to 300 Contains a nonionic thickener of the system.
本発明で用いられる(C)成分は、エチレンオキシド(「EO」とも称され、ポリエチレングリコールの略称として「PEG」等と称されることもある)を平均付加モル数として50〜300程度付加した高ポリオキシエチレン付加型の脂肪酸エステル又は脂肪酸エーテル構造を有するノニオン性増粘剤として公知の増粘剤である。このようなノニオン性増粘剤は、増粘させるために配合量を著しく増大させると、水馴染みを悪化させ、糊のような不快な使用感を生じさせてしまうことが知られている。 The component (C) used in the present invention has a high added amount of about 50 to 300 as an average addition mole number of ethylene oxide (also referred to as “EO”, which is also referred to as “PEG” as an abbreviation of polyethylene glycol). It is a known thickener as a nonionic thickener having a polyoxyethylene addition type fatty acid ester or fatty acid ether structure. It is known that when such a nonionic thickening agent is remarkably increased in order to increase the viscosity, the familiarity with water deteriorates and an unpleasant feeling of use like glue is generated.
本発明で用いられる(C)成分のノニオン性増粘剤におけるエチレンオキシドの平均付加モル数は、50〜300の範囲内であれば本発明の効果を奏し得る限り特に限定はされないが、上記(A)及び(B)成分の共存による増粘効果をより効果的に発揮させ易いという観点から、好ましくは60〜270程度、より好ましくは75〜250程度、更に好ましくは100〜200程度である。 The average addition mole number of ethylene oxide in the nonionic thickener of component (C) used in the present invention is not particularly limited as long as the effect of the present invention can be obtained as long as it is within the range of 50 to 300. ) And (B) from the viewpoint of easily exerting the thickening effect due to the coexistence of the components, it is preferably about 60 to 270, more preferably about 75 to 250, and still more preferably about 100 to 200.
また、(C)成分を構成する脂肪酸は、本発明の効果を奏し得る限り任意の脂肪酸であり得るが、一般には炭素数12〜24程度、好ましくは炭素数14〜22程度の脂肪酸を挙げることができ、例えば、ラウリン酸、ミリスチン酸、パルミチン酸、オレイン酸、ステアリン酸、イソステアリン酸、ベヘン酸、ヤシ油脂肪酸等を挙げることができるが、これらに限定されない。好ましくは、オレイン酸、ステアリン酸、イソステアリン酸、ラウリン酸であり、より好ましくはオレイン酸、ステアリン酸である。また、脂肪酸エステルは、モノエステル、ジエステル、トリエステル等の任意のエステルであり得るが、好ましくはモノエステル、ジエステルであり、より好ましくはジエステルである。脂肪酸エーテルもまた、モノエーテル、ジエーテル、トリエーテル等の任意のエーテルであってよいが、好ましくはモノエーテル、ジエーテルである。 The fatty acid constituting the component (C) may be any fatty acid as long as the effects of the present invention can be obtained, but generally includes fatty acids having about 12 to 24 carbon atoms, preferably about 14 to 22 carbon atoms. Examples thereof include, but are not limited to, lauric acid, myristic acid, palmitic acid, oleic acid, stearic acid, isostearic acid, behenic acid, coconut oil fatty acid, and the like. Preferred are oleic acid, stearic acid, isostearic acid and lauric acid, and more preferred are oleic acid and stearic acid. The fatty acid ester may be any ester such as a monoester, a diester, or a triester, but is preferably a monoester or a diester, and more preferably a diester. The fatty acid ether may also be any ether such as monoether, diether, and triether, but is preferably monoether or diether.
より具体的には、(C)成分として用いられる高ポリオキシエチレン付加型の脂肪酸エステル又は脂肪酸エーテル系のノニオン性増粘剤として、例えば、ジオレイン酸PEG−120メチルグルコース、トリオレイン酸PEG−120メチルグルコース、トリイソステアリン酸PEG−120メチルグルコース、ジオレイン酸PEG−75、ジステアリン酸PEG−75、ジステアリン酸PEG−140、ジステアリン酸PEG−150、ジステアリン酸PEG−175、ジステアリン酸PEG−190、ジステアリン酸PEG−250、ステアリン酸PEG−75、ステアリン酸PEG−150、ジラウリン酸PEG−75等の高ポリオキシエチレン付加型の脂肪酸エステル系ノニオン性増粘剤;セテアレス−60ミリスチルグリコール、ポリオキシエチレンセチルステアリルジエーテル等の高ポリオキシエチレン付加型の脂肪酸エーテル系ノニオン性増粘剤等を挙げることができるが、これらに限定されない。上記(A)及び(B)成分と組み合わされて一層高い増粘効果を発揮し得るという観点から、好ましくは、脂肪酸エステル系の高ポリオキシエチレン付加型ノニオン性増粘剤であり、より好ましくはジオレイン酸PEG−120メチルグルコース、トリオレイン酸PEG−120メチルグルコース、トリイソステアリン酸PEG−120メチルグルコース、ジステアリン酸PEG−140、ジステアリン酸PEG−150、ジステアリン酸PEG−250、ジステアリン酸PEG−175、ジステアリン酸PEG−190である。 More specifically, examples of the high polyoxyethylene addition type fatty acid ester or fatty acid ether type nonionic thickener used as the component (C) include PEG-120 methyl glucose and PEG-120 trioleate. Methyl glucose, PEG-120 triisostearate, PEG-75 dioleate, PEG-75 distearate, PEG-140 distearate, PEG-150 distearate, PEG-175 distearate, PEG-190 distearate, distearic acid High polyoxyethylene addition type fatty acid ester nonionic thickeners such as PEG-250, stearic acid PEG-75, stearic acid PEG-150, dilauric acid PEG-75; cetealess-60 myristyl glycol; It can be mentioned high-polyoxyethylene-added fatty ether nonionic thickeners such as polyoxyethylene cetyl stearyl diether, without limitation. From the viewpoint of being able to exert a higher thickening effect in combination with the above components (A) and (B), preferably a fatty acid ester-based high polyoxyethylene addition type nonionic thickener, more preferably Dioleic acid PEG-120 methyl glucose, trioleic acid PEG-120 methyl glucose, triisostearic acid PEG-120 methyl glucose, distearic acid PEG-140, distearic acid PEG-150, distearic acid PEG-250, distearic acid PEG-175, Distearic acid PEG-190.
上記のような(C)高ポリオキシエチレン付加型の脂肪酸エステル又は脂肪酸エーテル系のノニオン性増粘剤は、合成によって入手してもよく、また市販品を用いることもできる。市販品としては、特に限定されないが、グルカメートDOE-120(ルーブリゾール)、イオネットDS-4000(三洋化成工業)、エマルミン862(三洋化成工業)、ノニオンDS-40HN(日本油脂)、ブラウノンDS-6000F(青木油脂工業)、ブラウノンDS-10000F(青木油脂工業)、エマノーン3299V(花王)、エマノーン3299RV(花王)、NIKKOL CDS-6000P(日光ケミカルズ)、EMALEX6300di-ST(日本エマルジョン)、アキュリン60(ローム・アンド・ハース・ジャパン)、ノイゲンDS-601(第一工業製薬)等を挙げることができる。 The (C) high polyoxyethylene addition type fatty acid ester or fatty acid ether type nonionic thickener as described above may be obtained by synthesis, or a commercially available product may be used. Although it is not particularly limited as a commercial product, Glucamate DOE-120 (Lubrisol), Ionette DS-4000 (Sanyo Chemical Industries), Emarumin 862 (Sanyo Chemical Industries), Nonion DS-40HN (Nippon Yushi), Braunon DS-6000F (Aoki Yushi Kogyo), Braunon DS-10000F (Aoki Yushi Kogyo), Emanon 3299V (Kao), Emanon 3299RV (Kao), NIKKOL CDS-6000P (Nikko Chemicals), EMALEX6300di-ST (Nihon Emulsion), Aculine 60 (Rohm) And Haas Japan) and Neugen DS-601 (Daiichi Kogyo Seiyaku).
本発明の外用組成物における(C)成分の含有量は、本発明の効果を奏しうる限り特に限定されないが、一例として、組成物全量に対して、約0.1重量%以上、好ましくは約0.3重量%以上、より好ましくは約0.5重量%以上である。(C)成分の含有量の上限もまた、本発明の効果を奏し得る限り特に限定はされないが、組成物全量に対して、一例として約10重量%以下、好ましくは約8重量%以下、より好ましくは約5重量%以下とするのがよい。 The content of the component (C) in the composition for external use of the present invention is not particularly limited as long as the effects of the present invention can be achieved. As an example, the content is about 0.1% by weight or more, preferably about 0.3% by weight based on the total amount of the composition. % Or more, more preferably about 0.5% by weight or more. The upper limit of the content of the component (C) is not particularly limited as long as the effects of the present invention can be achieved, but as an example, it is about 10% by weight or less, preferably about 8% by weight or less, based on the total amount of the composition. Preferably it is about 5% by weight or less.
更に本発明の外用組成物において、(A)成分の含有量に対する(C)成分の含有量の比率については、特に制限されないが、より一層効果的に本発明の効果を発揮できるという観点から、一例として、(A)成分の含有量1重量部当たり、(C)成分の含有量が総量で約0.01〜10重量部、好ましくは約0.05〜8重量部、より好ましくは約0.1〜5重量部となる比率が例示される。 Furthermore, in the composition for external use of the present invention, the ratio of the content of the component (C) to the content of the component (A) is not particularly limited, but from the viewpoint that the effect of the present invention can be exhibited more effectively. As an example, the content of component (C) is about 0.01 to 10 parts by weight, preferably about 0.05 to 8 parts by weight, more preferably about 0.1 to 5 parts by weight per part by weight of component (A) The ratio which becomes is illustrated.
本発明の外用組成物には、更にアミノ酸系の界面活性剤を配合してもよい。アミノ酸系の界面活性剤とは、界面活性剤の構造の一部にアミノ酸類(例えば、アミノ酸、含硫アミノ酸又はその由来物、及びそれらの炭素数1〜4程度のアルキル化誘導体)を含む界面活性剤をいう。アミノ酸系界面活性剤は一般に、皮膚に対して低刺激性であるため好まれるが、石油等に由来する合成系界面活性剤に比べて、粘性を高めた製剤を調製し難い傾向があることが分かっている。然るに、本発明によれば、上記(A)〜(C)の三成分を組み合わせて使用することにより適度な粘度を有する外用組成物を調製することができる。従って、本発明は、一般に高粘度の製剤を調製し難い傾向があるアミノ酸系界面活性剤を含有する外用組成物の調製において好適に用いられ得る。 The composition for external use of the present invention may further contain an amino acid surfactant. An amino acid-based surfactant is an interface containing amino acids (for example, amino acids, sulfur-containing amino acids or their derivatives, and alkylated derivatives having about 1 to 4 carbon atoms thereof) as part of the surfactant structure. An activator. Amino acid surfactants are generally preferred because they are less irritating to the skin, but they tend to be difficult to prepare formulations with increased viscosity compared to synthetic surfactants derived from petroleum or the like. I know. However, according to the present invention, an external composition having an appropriate viscosity can be prepared by using the three components (A) to (C) in combination. Therefore, the present invention can be suitably used in the preparation of a composition for external use containing an amino acid surfactant that generally tends to be difficult to prepare a highly viscous preparation.
本発明の外用組成物に配合してもよいアミノ酸系界面活性剤としては、特に限定はされないが、例えば、ヤシ油脂肪酸アシルグルタミン酸(ココイルグルタミン酸ともいう)、ヤシ油脂肪酸アシルアスパラギン酸(ココイルアスパラギン酸ともいう)、ヤシ油脂肪酸アシルグリシン(ココイルグリシンともいう)、ヤシ油脂肪酸アシルグルタミン(ココイルグルタミンともいう)、ヤシ油脂肪酸アシルアスパラギン(ココイルアスパラギンともいう)、ヤシ油脂肪酸アシルアラニン(ココイルアラニンともいう)、ヤシ油脂肪酸アシルトレオニン(ココイルトレオニンともいう)及びこれらの塩等のヤシ油脂肪酸とアミノ酸とのアシル化物であるアニオン性界面活性剤;ヤシ油脂肪酸アシルサルコシン(ココイルサルコシンともいう)、ヤシ油脂肪酸アシルメチルアラニン(ココイルメチルアラニンともいう)及びこれらの塩等のヤシ油脂肪酸と炭素数1〜4アルキル化アミノ酸とのアシル化物であるアニオン性界面活性剤;ヤシ油脂肪酸アシルタウリン(ココイルタウリンともいう)、ヤシ油脂肪酸アシルイセチオン酸(ココイルイセチオン酸)及びこれらの塩等のヤシ油脂肪酸と含流硫アミノ酸由来物とのアシル化物であるアニオン性界面活性剤;並びに、ヤシ油脂肪酸アシルメチルタウリン(ココイルメチルタウリンともいう)及びこれらの塩等のヤシ油脂肪酸と炭素数1〜4アルキル化含流硫アミノ酸由来物とのアシル化物であるアニオン性界面活性剤;等を挙げることができる。好ましくは、ヤシ油脂肪酸とアミノ酸とのアシル化物であるアニオン性界面活性剤が用いられであり、より好ましくは、ヤシ油脂肪酸アシルグルタミン酸、ヤシ油脂肪酸アシルアスパラギン酸、ヤシ油脂肪酸アシルグリシン、ヤシ油脂肪酸アシルグルタミン、ヤシ油脂肪酸アシルアスパラギン、ヤシ油脂肪酸アシルアラニン、ヤシ油脂肪酸アシルトレオニン、及びこれらの塩が用いられ、更に好ましくはヤシ油脂肪酸アシルグルタミン酸、ヤシ油脂肪酸アシルアスパラギン酸、ヤシ油脂肪酸アシルアラニン、及びこれらの塩(例えば、ヤシ油脂肪酸アシルグルタミン酸ナトリウム、ヤシ油脂肪酸アシルアラニントリエタノールアミン等)が用いられる。なお、ここで、含硫アミノ酸由来物とは、含硫アミノ酸(例えば、メチオニンあるいはシステイン)から合成され得る物質で、カルボキシル基を有さず、スルホン基を有する化合物をいう。特には、アミノ酸様の、タウリンあるいはイセチオン酸等をさす。 The amino acid-based surfactant that may be blended in the composition for external use of the present invention is not particularly limited, and examples thereof include coconut oil fatty acid acylglutamic acid (also referred to as cocoylglutamic acid), coconut oil fatty acid acylaspartic acid (cocoylaspartic acid). Coconut oil fatty acid acyl glycine (also referred to as cocoyl glycine), coconut oil fatty acid acyl glutamine (also referred to as cocoyl glutamine), coconut oil fatty acid acyl asparagine (also referred to as cocoyl asparagine), coconut oil fatty acid acyl alanine (also referred to as cocoyl alanine). ), Palm oil fatty acid acyl threonine (also referred to as cocoyl threonine) and anionic surfactants that are acylated products of coconut oil fatty acid and amino acids such as salts thereof; coconut oil fatty acid acyl sarcosine (also referred to as cocoyl sarcosine), Anionic surfactants that are acylated products of fatty acid acylmethylalanine (also referred to as cocoylmethylalanine) and coconut oil fatty acids and C1-C4 alkylated amino acids such as salts thereof; coconut oil fatty acid acyl taurine (also referred to as cocoyl taurine) An anionic surfactant which is an acylated product of a coconut oil fatty acid and a product containing a sulfur-containing sulfur amino acid such as coconut oil fatty acid acyl isethionic acid (cocoyl isethionic acid) and salts thereof; and coconut oil fatty acid acylmethyl taurine (Also referred to as cocoyl methyl taurine) and anionic surfactants that are acylated products of coconut oil fatty acids such as salts thereof and derivatives derived from a C1-C4 alkylated sulfur-containing amino acid. Preferably, an anionic surfactant that is an acylated product of coconut oil fatty acid and amino acid is used, and more preferably, coconut oil fatty acid acylglutamic acid, coconut oil fatty acid acylaspartic acid, coconut oil fatty acid acylglycine, coconut oil Fatty acid acyl glutamine, coconut oil fatty acid acyl asparagine, coconut oil fatty acid acyl alanine, coconut oil fatty acid acyl threonine, and salts thereof are used, more preferably coconut oil fatty acid acyl glutamic acid, coconut oil fatty acid acyl aspartic acid, coconut oil fatty acid acyl. Alanine and salts thereof (for example, coconut oil fatty acid acyl glutamate sodium, coconut oil fatty acid acylalanine triethanolamine, etc.) are used. Here, the sulfur-containing amino acid-derived material refers to a compound that can be synthesized from a sulfur-containing amino acid (for example, methionine or cysteine) and does not have a carboxyl group but has a sulfone group. In particular, it refers to amino acid-like taurine or isethionic acid.
本発明の外用組成物におけるアミノ酸系界面活性剤の含有量は、本発明の効果を奏しうる限り特に限定されないが、一例として、組成物全量に対して、0.1〜50重量%程度、好ましくは0.5〜45重量%程度、より好ましくは1〜40重量%程度とするのがよい。 The content of the amino acid surfactant in the composition for external use of the present invention is not particularly limited as long as the effects of the present invention can be achieved. As an example, the content is about 0.1 to 50% by weight, preferably 0.5% with respect to the total amount of the composition. About 45% by weight, more preferably about 1-40% by weight.
本発明の外用組成物には、更に両性界面活性剤を含有してもよい。両性界面活性剤を配合することにより、より一層高い本発明の効果が得られると共に、起泡性や洗浄力にも優れた外用組成物とすることができる。 The external composition of the present invention may further contain an amphoteric surfactant. By blending an amphoteric surfactant, it is possible to obtain a composition for external use that has a higher effect of the present invention and is also excellent in foamability and detergency.
本発明の外用組成物に配合してもよい両性界面活性剤としては、特に限定はされないが、例えば、ベタイン型両性界面活性剤が好ましい。ベタイン型両性界面活性剤としては、例えば、ヤシ油脂肪酸アミドプロピルジメチルベタイン、ラウリルアミドプロピルジメチルベタイン、オレイルアミドプロピルジメチルベタイン、ヤシ油脂肪酸アミドプロピルジ(ヒドロキシエチル)ベタイン、ラウリルアミドプロピルジ(ヒドロキシエチル)ベタイン、オレイルアミドプロピルジ(ヒドロキシエチル)ベタイン、ヤシ油脂肪酸アミドプロピルベタイン等のアミドプロピルベタイン型両性界面活性剤;N−ラウリル−N,N−ジメチルアミノ酢酸ベタイン、N−ヤシアルキル−N,N−ジメチルアミノ酢酸ベタイン、N−ステアリル−N,N−ジメチルアミノ酢酸ベタイン、N−オレイル−N,N−ジメチルアミノ酢酸ベタイン、N−ラウリル−N,N−ジ(ヒドロキシエチル)アミノ酢酸ベタイン、N−ヤシアルキル−N,N−ジ(ヒドロキシエチル)アミノ酢酸ベタイン、N−ステアリル−N,N−ジ(ヒドロキシエチル)アミノ酢酸ベタイン、N−オレイル−N,N−ジ(ヒドロキシエチル)アミノ酢酸ベタイン等のアミノ酢酸ベタイン型両性界面活性剤;2−アルキル(C11〜21)−N−カルボキシメチル−N−ヒドロキシエチルイミダゾリニウムベタイン等のイミダゾリウムベタイン型両性界面活性剤;等を挙げることができる。好ましくは、アミドプロピルベタイン型両性界面活性剤であり、より好ましくは、ヤシ油脂肪酸アミドプロピルベタイン、ヤシ油脂肪酸アミドプロピルジメチルベタイン、ヤシ油脂肪酸アミドプロピルジ(ヒドロキシエチル)ベタインであり、特に好ましくはヤシ油脂肪酸アミドプロピルベタインである。 Although it does not specifically limit as an amphoteric surfactant which may be mix | blended with the composition for external use of this invention, For example, a betaine type | mold amphoteric surfactant is preferable. Examples of betaine-type amphoteric surfactants include coconut oil fatty acid amidopropyl dimethyl betaine, lauryl amidopropyl dimethyl betaine, oleyl amidopropyl dimethyl betaine, coconut oil fatty acid amidopropyl di (hydroxyethyl) betaine, lauryl amidopropyl di (hydroxyethyl). ) Amidopropyl betaine-type amphoteric surfactants such as betaine, oleylamidopropyldi (hydroxyethyl) betaine, coconut oil fatty acid amidopropyl betaine; N-lauryl-N, N-dimethylaminoacetic acid betaine, N-coconut alkyl-N, N -Dimethylaminoacetic acid betaine, N-stearyl-N, N-dimethylaminoacetic acid betaine, N-oleyl-N, N-dimethylaminoacetic acid betaine, N-lauryl-N, N-di (hydroxyethyl) amino Acid betaine, N-coconut alkyl-N, N-di (hydroxyethyl) aminoacetic acid betaine, N-stearyl-N, N-di (hydroxyethyl) aminoacetic acid betaine, N-oleyl-N, N-di (hydroxyethyl) Aminoacetic acid betaine-type amphoteric surfactants such as aminoacetic acid betaine; imidazolium betaine-type amphoteric surfactants such as 2-alkyl (C11-21) -N-carboxymethyl-N-hydroxyethylimidazolinium betaine; be able to. Preferred are amidopropyl betaine type amphoteric surfactants, more preferred are coconut oil fatty acid amidopropyl betaine, coconut oil fatty acid amidopropyl dimethyl betaine, and coconut oil fatty acid amidopropyl di (hydroxyethyl) betaine, particularly preferred It is a coconut oil fatty acid amidopropyl betaine.
本発明の外用組成物における両性界面活性剤の含有量は、本発明の効果を奏しうる限り特に限定されないが、一例として、組成物全量に対して、0.001〜50重量%程度、好ましくは0.01〜40重量%程度、より好ましくは0.05〜30重量%程度とするのがよい。 The content of the amphoteric surfactant in the composition for external use of the present invention is not particularly limited as long as the effects of the present invention can be achieved, but as an example, about 0.001 to 50% by weight, preferably 0.01 to about the total amount of the composition About 40% by weight, more preferably about 0.05 to 30% by weight.
本発明の外用組成物には更に、ノニオン性界面活性剤を配合してもよい。上記(C)成分は、ノニオン性界面活性剤としての作用を有するものがあるが、本発明には上記(C)成分以外のノニオン性界面活性剤を配合することもできる。具体的には、上記(C)成分以外のノニオン性界面活性剤として、エチレンオキシドの平均付加モル数が50未満又は300よりも多いポリオキシエチレン付加型の脂肪酸エステル系又は脂肪酸エステル系のノニオン性界面活性剤;ポリオキシエチレン構造を含まないノニオン性界面活性剤;脂肪酸エステル又は脂肪酸エーテル構造を含まないノニオン性界面活性剤;等を挙げることができる。 The composition for external use of the present invention may further contain a nonionic surfactant. Although the component (C) has a function as a nonionic surfactant, a nonionic surfactant other than the component (C) can be blended in the present invention. Specifically, as the nonionic surfactant other than the component (C), the polyoxyethylene addition type fatty acid ester type or fatty acid ester type nonionic interface having an average addition mole number of ethylene oxide of less than 50 or more than 300 Nonionic surfactant which does not contain polyoxyethylene structure; Nonionic surfactant which does not contain fatty acid ester or fatty acid ether structure;
上記のような(C)成分以外のノニオン性界面活性剤として、具体的には、ヤシ油脂肪酸ジエタノールアミド、ラウリン酸モノエタノールアミド、N−ポリヒドロキシアルキル脂肪酸アミド等のモノ又はジエタノールアミド系のノニオン性界面活性剤;モノイソステアリン酸ソルビタン、モノオレイン酸ソルビタン等のソルビタン脂肪酸エステル系のノニオン性界面活性剤;ラウリン酸ショ糖エステル、ショ糖モノステアレート等のショ糖脂肪酸エステル系のノニオン性界面活性剤;セスキオレイン酸グリセリン等のグリセリン系のノニオン性界面活性剤;等を挙げることができる。好ましくは、モノ又はジエタノールアミド系のノニオン性界面活性剤であり、より好ましくは、ヤシ油脂肪酸ジエタノールアミドである。 Specific examples of nonionic surfactants other than the component (C) include mono- or diethanolamide-based nonions such as coconut oil fatty acid diethanolamide, lauric acid monoethanolamide, and N-polyhydroxyalkyl fatty acid amide. Nonionic surfactants of sorbitan fatty acid esters such as sorbitan monoisostearate and sorbitan monooleate; Nonionic surfactants of sucrose fatty acid esters such as lauric sucrose ester and sucrose monostearate Agents; glycerin-based nonionic surfactants such as glyceryl sesquioleate; and the like. Preferred are mono- or diethanolamide-based nonionic surfactants, and more preferred is coconut oil fatty acid diethanolamide.
本発明の外用組成物における(C)成分以外のノニオン性界面活性剤の含有量は、本発明の効果を奏しうる限り特に限定されないが、一例として、組成物全量に対して、0.01〜20重量%程度、好ましくは0.05〜15重量%程度、より好ましくは0.1〜10重量%程度とするのがよい。 The content of the nonionic surfactant other than the component (C) in the composition for external use of the present invention is not particularly limited as long as the effect of the present invention can be exerted, but as an example, 0.01 to 20 wt. %, Preferably about 0.05 to 15% by weight, more preferably about 0.1 to 10% by weight.
本発明の外用組成物には、他の有効成分(例えば、局所麻酔剤、ビタミン剤、殺菌剤、鎮痒成分等)を配合してもよい。 You may mix | blend other active ingredients (For example, a local anesthetic, a vitamin agent, a disinfectant, an antipruritic component, etc.) with the composition for external use of this invention.
局所麻酔剤としては、例えば、プロカイン、テトラカイン、リドカイン、ジブカイン、ブピバカイン、メピバカイン、ロピバカイン、レボブピバカイン、およびそれらの薬学的に許容される塩、およびアミノ安息香酸エチルからなる群より選択される1種または2種以上であることが好ましい。 Examples of the local anesthetic include 1 selected from the group consisting of procaine, tetracaine, lidocaine, dibucaine, bupivacaine, mepivacaine, ropivacaine, levobupivacaine, and pharmaceutically acceptable salts thereof, and ethyl aminobenzoate. It is preferable that it is a seed | species or 2 or more types.
ビタミン剤としては、dl−α−トコフェロール、酢酸dl−α−トコフェロール、コハク酸dl−α−トコフェロール、コハク酸dl−α−トコフェロールカルシウム等のビタミンE類、ユビキノン誘導体およびその生理学的又は薬理学的に許容される塩、リボフラビン、フラビンモノヌクレオチド、フラビンアデニンジヌクレオチド、リボフラビン酪酸エステル、リボフラビンテトラ酪酸エステル、リボフラビン5’−リン酸エステルナトリウム、リボフラビンテトラニコチン酸エステル、ニコチン酸dl−α−トコフェロール、ニコチン酸ベンジル、ニコチン酸メチル、ニコチン酸β−ブトキシエチル、ニコチン酸1−(4−メチルフェニル)エチル、アスコルビゲン−A、アスコルビン酸ステアリン酸エステル、アスコルビン酸パルミチン酸エステル、ジパルミチン酸L−アスコルビル、メチルヘスペリジン、エルゴカルシフェロール、コレカルシフェロール、フィロキノン、ファルノキノン、γ−オリザノール、ジベンゾイルチアミン、ジベンゾイルチアミン塩酸塩、チアミン塩酸塩、チアミンセチル塩酸塩、チアミンチオシアン酸塩、チアミンラウリル塩酸塩、チアミン硝酸塩、チアミンモノリン酸塩、チアミンリジン塩、チアミントリリン酸塩、チアミンモノリン酸エステルリン酸塩、チアミンモノリン酸エステル、チアミンジリン酸エステル、チアミンジリン酸エステル塩酸塩、チアミントリリン酸エステル、チアミントリリン酸エステルモノリン酸塩、塩酸ピリドキシン、酢酸ピリドキシン、塩酸ピリドキサール、5’−リン酸ピリドキサール、塩酸ピリドキサミン、シアノコバラミン、ヒドロキソコバラミン、デオキシアデノシルコバラミン、葉酸、プテロイルグルタミン酸、ニコチン酸、ニコチン酸アミド、パントテン酸、パントテン酸カルシウム、パントテニルアルコール(パンテノール)、D−パンテサイン、D−パンテチン、補酵素A、パントテニルエチルエーテル等のパントテン酸類、ビオチン、ビオチシン、アスコルビン酸、アスコルビン酸ナトリウム、デヒドロアスコルビン酸、アスコルビン酸リン酸エステルナトリウム、アスコルビン酸リン酸エステルマグネシウム、カルニチン、フェルラ酸、α−リポ酸、オロット酸、ヘスペリジン、γ−オリザノール、オロチン酸、ルチン、エリオシトリンおよびその薬理学的に許容される塩からなる群より選択される1種または2種以上であることが好ましい。 Vitamins such as dl-α-tocopherol, dl-α-tocopherol acetate, dl-α-tocopherol succinate, dl-α-tocopherol calcium succinate, ubiquinone derivatives and their physiological or pharmacological properties Acceptable salts, riboflavin, flavin mononucleotide, flavin adenine dinucleotide, riboflavin butyrate, riboflavin tetrabutyrate, riboflavin sodium 5'-phosphate, riboflavin tetranicotinate, nicotinic acid dl-α-tocopherol, nicotine Benzyl acid, methyl nicotinate, β-butoxyethyl nicotinate, 1- (4-methylphenyl) ethyl nicotinate, ascorbigen-A, ascorbic acid stearate, palmitic ascorbic acid Acid ester, L-ascorbyl dipalmitate, methyl hesperidin, ergocalciferol, cholecalciferol, phylloquinone, farnoquinone, γ-oryzanol, dibenzoylthiamine, dibenzoylthiamine hydrochloride, thiamine hydrochloride, thiaminecetyl hydrochloride, thiamine thiocyanate Acid salt, thiamine lauryl hydrochloride, thiamine nitrate, thiamine monophosphate, thiamine lysine salt, thiamine triphosphate, thiamine monophosphate phosphate, thiamine monophosphate, thiamine diphosphate, thiamine diphosphate hydrochloride, Thiamine triphosphate, thiamine triphosphate monophosphate, pyridoxine hydrochloride, pyridoxine acetate, pyridoxal hydrochloride, 5'-pyridoxal phosphate, pyridoxamine hydrochloride, Cyanocobalamin, hydroxocobalamin, deoxyadenosylcobalamin, folic acid, pteroylglutamic acid, nicotinic acid, nicotinic acid amide, pantothenic acid, calcium pantothenate, pantothenyl alcohol (panthenol), D-panthecin, D-panthetin, coenzyme A Pantothenic acids such as pantothenyl ethyl ether, biotin, bioticin, ascorbic acid, sodium ascorbate, dehydroascorbic acid, sodium ascorbate phosphate, magnesium ascorbate phosphate, carnitine, ferulic acid, α-lipoic acid, orot It may be one or more selected from the group consisting of acid, hesperidin, γ-oryzanol, orotic acid, rutin, eriocitrin and pharmacologically acceptable salts thereof. preferable.
殺菌剤としては、イソプロピルメチルフェノール、塩化デカリニウム、塩化ベンザルコニウム、塩化ベンゼトニウム、塩酸クロルへキシジン、グルコン酸クロルヘキシジン、塩酸アルキルジアミノエチルグリシン、塩化セチルピリジニウム、安息香酸ナトリウム、エタノール、クロロブタノール、ソルビン酸、ソルビン酸カリウム、デヒドロ酢酸ナトリウム、パラオキシ安息香酸メチル、パラオキシ安息香酸エチル、パラオキシ安息香酸プロピル、パラオキシ安息香酸ブチル、硫酸オキシキノリン、フェネチルアルコール、ベンジルアルコール、およびビグアニド化合物からなる群より選択される1種または2種以上であることが好ましい。 Disinfectants include isopropylmethylphenol, decalinium chloride, benzalkonium chloride, benzethonium chloride, chlorhexidine hydrochloride, chlorhexidine gluconate, alkyldiaminoethylglycine hydrochloride, cetylpyridinium chloride, sodium benzoate, ethanol, chlorobutanol, sorbic acid 1 selected from the group consisting of potassium sorbate, sodium dehydroacetate, methyl paraoxybenzoate, ethyl paraoxybenzoate, propyl paraoxybenzoate, butyl paraoxybenzoate, oxyquinoline sulfate, phenethyl alcohol, benzyl alcohol, and biguanide compounds It is preferable to be a seed or two or more.
鎮痒成分としては、クロタミトン、イクタモール、モクタモール、チモール酸およびその薬理学的に許容される塩からなる群より選択される1種または2種以上であることが好ましい。 The antipruritic component is preferably one or more selected from the group consisting of crotamiton, ictamol, moctamol, thymolic acid and pharmacologically acceptable salts thereof.
本発明の外用組成物は、医薬品、医薬部外品等として幅広く利用可能な任意の形態で提供される。好ましくは、皮膚及び/又は毛髪用の外用剤として利用可能な製剤として提供される。 The composition for external use of the present invention is provided in any form that can be widely used as a pharmaceutical, a quasi-drug, and the like. Preferably, it is provided as a preparation that can be used as an external preparation for skin and / or hair.
本発明の(A)アゾール系抗真菌剤、(B)カチオン性ポリマー、及び(C)エチレンオキシドの平均付加モル数が50〜300であるポリオキシエチレン付加型の脂肪酸エステル系又は脂肪酸エーテル系のノニオン性増粘剤を含有する外用組成物は、医薬品、医薬部外品、化粧品等として、皮膚および/または毛髪用外用剤の形態で使用され得る。これらの外用剤形態においては、(A)成分、(B)成分、および(C)成分に加えて、さらに、本発明の効果を損なわない範囲で、皮膚及び/又は毛髪用外用剤(医薬部外品、医薬品、化粧品等)に添加される公知の基剤又は担体を混合して使用できる。更に例えば、経皮吸収促進剤、他の界面活性剤、油分、アルコール類、親水性ゲル化剤、親油性ゲル化剤、保湿剤、増粘剤、防腐剤、酸化防止剤、キレート剤、保存剤、pH調整剤、安定化剤、分散剤、香料、着色剤、色素、パール光沢付与剤、血行促進成分、保湿成分、紫外線吸収成分、紫外線散乱成分、洗浄成分、収斂成分、ペプチド、アミノ酸類、角質柔軟成分、細胞賦活化成分、溶解補助剤、水等を配合することができる。添加剤は、1種を単独で、又は2種以上を組み合わせて使用できる。 (A) azole antifungal agent of the present invention, (B) cationic polymer, and (C) polyoxyethylene addition type fatty acid ester type or fatty acid ether type nonion whose average addition mole number of ethylene oxide is 50 to 300 The composition for external use containing a natural thickener can be used in the form of an external preparation for skin and / or hair as a pharmaceutical, a quasi-drug, a cosmetic and the like. In these external preparation forms, in addition to the component (A), the component (B), and the component (C), the external preparation for skin and / or hair (pharmaceutical department) within the range not impairing the effects of the present invention. A known base or carrier added to external products, pharmaceuticals, cosmetics, etc.) can be used by mixing. Furthermore, for example, transdermal absorption accelerators, other surfactants, oils, alcohols, hydrophilic gelling agents, lipophilic gelling agents, moisturizers, thickeners, preservatives, antioxidants, chelating agents, storage Agent, pH adjuster, stabilizer, dispersant, fragrance, colorant, dye, pearl luster imparting agent, blood circulation promoting component, moisturizing component, UV absorbing component, UV scattering component, cleaning component, astringent component, peptide, amino acids , Keratin soft component, cell activation component, solubilizing agent, water and the like can be blended. An additive can be used individually by 1 type or in combination of 2 or more types.
本発明で使用できる油分としては、鉱物性油(流動ワセリン)、植物性油(カリテバターの液状留分、ヒマワリ油)、動物性油(ペルヒドロスクアレン)、合成油(プルセリン油)、シリコーン油又はロウ(シクロメチコーン)、及びフッ化油(ペルフルオロポリエーテル)、ミツロウ、カルナウバロウ又はパラフィンロウなどが挙げられる。 Oils that can be used in the present invention include mineral oil (fluid petroleum jelly), vegetable oil (liquid fraction of karite butter, sunflower oil), animal oil (perhydrosqualene), synthetic oil (purserine oil), silicone oil or Examples include wax (cyclomethicone), fluorinated oil (perfluoropolyether), beeswax, carnauba wax, and paraffin wax.
本発明においてはさらに他の界面活性剤を併用することもできる。 In the present invention, other surfactants can be used in combination.
本発明で使用できるアルコール類は、低級アルコールが好ましく、特にエタノール、イソプロパノール、及びプロピレングリコールが好ましい。 The alcohol that can be used in the present invention is preferably a lower alcohol, particularly ethanol, isopropanol, or propylene glycol.
本発明で使用できる親水性のゲル化剤としては、カルボキシビニルポリマー、アクリルコポリマー、例えばアクリラート/アクリル酸アルキルのコポリマー、ポリアクリルアミド、多糖類、例えばヒドロキシプロピルセルロース、天然ガム及びクレーを挙げることができる。本発明で使用できる親油性のゲル化剤としては、変性クレー類、例えばベントーン、脂肪酸の金属塩、例えばステアリン酸アルミニウム、及び疎水性シリカ、エチルセルロース及びポリエチレンを挙げることができる。 Hydrophilic gelling agents that can be used in the present invention can include carboxyvinyl polymers, acrylic copolymers such as acrylate / alkyl acrylate copolymers, polyacrylamides, polysaccharides such as hydroxypropylcellulose, natural gums and clays. . The lipophilic gelling agent that can be used in the present invention includes modified clays such as bentone, metal salts of fatty acids such as aluminum stearate, and hydrophobic silica, ethylcellulose and polyethylene.
その他の基剤又は担体としては、流動パラフィン;パルミチン酸イソプロピル;カルボキシビニルポリマー;水などの水系基剤などが挙げられる。 Other bases or carriers include liquid paraffin; isopropyl palmitate; carboxyvinyl polymer; aqueous bases such as water.
pH調整剤としては、有機酸(クエン酸、乳酸、酢酸、酒石酸、リンゴ酸、コハク酸、シュウ酸、グルコン酸、フマル酸、プロピオン酸、酢酸、アスパラギン酸、イプシロン−アミノカプロン酸、グルタミン酸、アミノエチルスルホン酸等);無機酸(塩酸、硫酸、リン酸、ポリリン酸、ホウ酸等);有機塩基(モノエタノールアミン、トリエタノールアミン、ジイソプロパノールアミン、トリイソプロパノールアミン、リジン等);無機塩基(炭酸水素ナトリウム、炭酸ナトリウム、水酸化カリウム、水酸化ナトリウム、水酸化カルシウム、水酸化マグネシウム等);等を挙げることができる。 pH adjusters include organic acids (citric acid, lactic acid, acetic acid, tartaric acid, malic acid, succinic acid, oxalic acid, gluconic acid, fumaric acid, propionic acid, acetic acid, aspartic acid, epsilon-aminocaproic acid, glutamic acid, aminoethyl Inorganic acids (hydrochloric acid, sulfuric acid, phosphoric acid, polyphosphoric acid, boric acid, etc.); organic bases (monoethanolamine, triethanolamine, diisopropanolamine, triisopropanolamine, lysine, etc.); inorganic bases (carbonic acid) Sodium hydrogen, sodium carbonate, potassium hydroxide, sodium hydroxide, calcium hydroxide, magnesium hydroxide, etc.).
アルコール類などの溶媒、ゲル化剤、基剤又は担体は、1種を単独で、又は2種以上を組み合わせて使用できる。 Solvents such as alcohols, gelling agents, bases or carriers can be used singly or in combination of two or more.
本発明の外用組成物である薬剤は、医薬品、医薬部外品又は化粧品等の公知の形態として、例えば、毛髪や皮膚への使用に適した任意の剤形であり得る。本発明の外用組成物は、使用後で洗い流す形態の洗浄用組成物であってもよいし、使用後に洗い流さないリーブオン型の外用組成物であってもよい。本発明により、ある程度の粘性を備えた外用組成物に調製できるという点を考慮すると、使用時に適度な粘度を備えることが望まれる洗浄用組成物として用いられることが好ましい。洗浄用の外用組成物の形態は特に限定されないが、例えば、シャンプー(頭髪用シャンプー、ドライシャンプー、リンスインシャンプー等)、石鹸(液体石鹸、泡状石鹸、ボディソープ(ボディシャンプーともいう)、ハンドソープ等、クレンジングフォーム等であり得る。さらに、リンス、コンディショナーなどの形態であってもよい。これらの中でも、適度な粘性を備えることが望まれることも多いシャンプー、リンス、ボディソープ、ハンドソープ、液体石鹸が好ましく、とりわけ、シャンプーが好ましい。また、本発明の外用組成物は、例えば、ローション、ジェル、ムース、液剤、懸濁剤、乳剤、クリーム剤、軟膏剤、ゲル剤、リニメント剤等としても提供され得る。中でも、液剤、懸濁剤、乳剤、クリーム剤、軟膏剤、ゲル剤の形態で用いられることが好ましい。 The medicine which is the composition for external use of the present invention can be any dosage form suitable for use on, for example, hair and skin, as a known form such as pharmaceuticals, quasi drugs or cosmetics. The composition for external use of the present invention may be a cleaning composition that is washed away after use, or may be a leave-on external composition that is not washed off after use. In view of the fact that the present invention can be prepared into an external composition having a certain degree of viscosity, it is preferably used as a cleaning composition that is desired to have an appropriate viscosity at the time of use. The form of the external composition for cleaning is not particularly limited. For example, shampoo (hair shampoo, dry shampoo, rinse-in shampoo, etc.), soap (liquid soap, foam soap, body soap (also called body shampoo), hand soap It may be in the form of a rinse, a conditioner, etc. Among these, shampoos, rinses, body soaps, hand soaps, liquids that are often desired to have an appropriate viscosity Soaps are preferred, and shampoos are particularly preferred, and the composition for external use of the present invention can be used, for example, as a lotion, gel, mousse, solution, suspension, emulsion, cream, ointment, gel, liniment, etc. Among them, solutions, suspensions, emulsions, creams, ointments, gels It is preferably used in state.
本発明の外用組成物は、任意の容器に入れて提供され得る。容器の形状は特に限定されず、ボトル形状であってもよいし、ノズルを備えたポンプ形状であってもよい。更に容器の材質も特に限定されず、一例として、ポリエチレン樹脂、ポリプロピレン樹脂、ポリエステル樹脂(例えば、ポリエチレンテレフタレート樹脂、ポリブチレンテレフタレート樹脂、ポリトリメチレンテレフタレート樹脂、ポリ(1,4−シクロヘキシルジメチレンテレフタレート)樹脂、ポリエチレンナフタレート樹脂、ポリブチレンナフタレート樹脂等)、及びこれらの混合樹脂等で少なくとも一部(例えば、容器内壁の少なくとも一部)が構成される容器であり得る。 The external composition of the present invention can be provided in any container. The shape of the container is not particularly limited, and may be a bottle shape or a pump shape provided with a nozzle. Further, the material of the container is not particularly limited. For example, polyethylene resin, polypropylene resin, polyester resin (for example, polyethylene terephthalate resin, polybutylene terephthalate resin, polytrimethylene terephthalate resin, poly (1,4-cyclohexyldimethylene terephthalate)) Resin, polyethylene naphthalate resin, polybutylene naphthalate resin, and the like), and mixed resins thereof, and the like.
本発明の外用組成物は、外用組成物、特に毛髪や皮膚を洗浄するために用いられる外用組成物の使用の際に望まれる適度な粘性を備えた外用組成物として調製することができる。本発明の外用組成物の粘度は、特に限定はされないが、例えば、B型粘度計を用いて25℃で測定した場合の粘度が通常300〜2000000mPa・s程度、好ましくは400〜1000000mPa・s程度、より好ましくは500〜100000mPa・s程度である。 The external composition of the present invention can be prepared as an external composition having an appropriate viscosity desired when using an external composition, particularly an external composition used for washing hair and skin. The viscosity of the composition for external use of the present invention is not particularly limited. For example, the viscosity when measured at 25 ° C. using a B-type viscometer is usually about 300 to 2000000 mPa · s, preferably about 400 to 100000 mPa · s. More preferably, it is about 500 to 100,000 mPa · s.
また、本発明の外用組成物のpHは、本発明の効果を奏し得る限り特に限定はされないが、一例としてpH3〜9程度を例示することができる。一般に増粘剤による増粘作用は製剤のpHが中性に近づくにつれて弱くなる傾向があるが、本発明によれば中性付近であっても適度な増粘効果を得ることができる。かかる観点に鑑みれば、本発明は好ましくはpH4〜8程度、より好ましくはpH5〜7程度(例えば、pH5.5〜6.5程度)の外用組成物を調製する際に好適に使用され得る。 Moreover, the pH of the composition for external use of the present invention is not particularly limited as long as the effects of the present invention can be obtained, but an example of about pH 3 to 9 can be exemplified. In general, the thickening action by a thickener tends to weaken as the pH of the preparation approaches neutrality. However, according to the present invention, an appropriate thickening effect can be obtained even in the vicinity of neutrality. In view of such a viewpoint, the present invention is preferably used when preparing an external composition having a pH of about 4 to 8, more preferably about 5 to 7 (for example, about pH 5.5 to 6.5).
本発明の外用組成物は、アゾール系抗真菌剤を含有するので、抗真菌効果を発揮することが望まれる任意の場面で使用され得る。例えば、本発明の外用組成物は、頭皮湿疹、フケ症、白癬(例えば、足白癬、体部白癬、股部白癬)、カンジダ症(例えば、指間びらん症、間擦疹)、癜風等の治療、予防及び/又は改善のために好適に用いられる。本発明の外用組成物は、真菌を原因とする症状が気になる皮膚や毛髪に塗布して使用することができ、また真菌を原因とする症状が気になる皮膚や毛髪に塗布して洗浄後に水分等で洗い流して使用することもできる。好ましくは、本発明の外用組成物は、毛髪や皮膚を洗浄するために用いられる。用法は、特に限定されず、シャンプーであれば、1日1回程度の使用でもよい。あるいは、1日数回(例えば、朝、昼、晩の3回)定期的に使用してもよく、または必要に応じて適時使用してもよい。皮膚及び/又は毛髪用の外用剤形態の場合には、適量(例えば、0.1〜10g程度)を、皮膚及び/又は毛髪に塗布、塗擦または噴霧することにより適用することができる。 Since the composition for external use of the present invention contains an azole antifungal agent, it can be used in any scene where it is desired to exert an antifungal effect. For example, the composition for external use of the present invention has scalp eczema, dandruff, ringworm (for example, foot ringworm, body ringworm, hip ringworm), candidiasis (for example, finger erosion, rash), folding screen, etc. It is suitably used for the treatment, prevention and / or improvement. The composition for external use of the present invention can be applied to skin and hair where the symptoms caused by fungi are anxious, and is applied to the skin and hair where symptoms caused by fungi are anxious. It can also be used after being washed away with moisture or the like. Preferably, the composition for external use of the present invention is used for washing hair and skin. The usage is not particularly limited, and may be used about once a day as long as it is a shampoo. Alternatively, it may be used regularly several times a day (for example, three times in the morning, noon, and evening), or may be used in a timely manner as necessary. In the case of an external preparation for skin and / or hair, an appropriate amount (for example, about 0.1 to 10 g) can be applied by applying, rubbing or spraying to the skin and / or hair.
更に本発明は別の観点から、外用組成物中に、(A)アゾール系抗真菌剤、(B)カチオン性ポリマー、及び(C)エチレンオキシドの平均付加モル数が50〜300であるポリオキシエチレン付加型の脂肪酸エステル系又は脂肪酸エーテル系のノニオン性増粘剤を共存させることで、該外用組成物を増粘する方法をも提供する。本方法の一態様として、本発明は、(B)カチオン性ポリマー、及び(C)エチレンオキシドの平均付加モル数が50〜300であるポリオキシエチレン付加型の脂肪酸エステル系又は脂肪酸エーテル系のノニオン性増粘剤を含有する組成物に、(A)アゾール系抗真菌剤を配合することにより、該組成物を増粘する方法、を提供する。
これらの増粘方法における(A)〜(C)成分の種類や配合量、その他に配合し得る成分やその配合量等は、上記で外用組成物について詳述したものと同様である。
Furthermore, from another viewpoint, the present invention provides polyoxyethylene in which the average addition mole number of (A) azole antifungal agent, (B) cationic polymer, and (C) ethylene oxide is 50 to 300 in the composition for external use. The present invention also provides a method for thickening the composition for external use by allowing an addition-type fatty acid ester-based or fatty acid ether-based nonionic thickener to coexist. As an embodiment of the present method, the present invention provides (B) a cationic polymer, and (C) a polyoxyethylene addition type fatty acid ester type or fatty acid ether type nonionic property having an average addition mole number of ethylene oxide of 50 to 300. Provided is a method for thickening the composition by adding (A) an azole antifungal agent to the composition containing the thickener.
The types and blending amounts of the components (A) to (C) in these thickening methods, other components that can be blended, blending amounts thereof, and the like are the same as those described above in detail for the external composition.
以下に、実施例に基づいて本発明を詳細に説明するが、本発明はこれらの実施例によって限定されるものではない。 EXAMPLES The present invention will be described in detail below based on examples, but the present invention is not limited to these examples.
(試験例1.粘度評価(1))
下記表1に示す処方を常法に従って調製した。具体的には、各成分を100mlガラスバイアルに量り取り、蒸留水で合計量が100重量%となるように添加して、約80℃で保温しながら攪拌し均一な製剤を得た。次いで、各比較例及び実施例の製剤の粘度(25℃:mPa・s)をB型回転粘度計(東機産業株式会社製)で測定した。この結果を、下記表1の最下欄に併せて示す。
The formulation shown in Table 1 below was prepared according to a conventional method. Specifically, each component was weighed into a 100 ml glass vial, added with distilled water to a total amount of 100% by weight, and stirred while keeping the temperature at about 80 ° C. to obtain a uniform preparation. Subsequently, the viscosity (25 degreeC: mPa * s) of the formulation of each comparative example and an Example was measured with the B type rotational viscometer (made by Toki Sangyo Co., Ltd.). The results are also shown in the bottom column of Table 1 below.
上記結果に示されるように、(B)カチオン性ポリマーも(C)高ポリオキシエチレン付加型の脂肪酸エステル又は脂肪酸エーテル構造を有するノニオン性増粘剤も含まない比較例1の製剤は非常に粘度が低い。また、比較例1の製剤に、上記(B)成分又は(C)成分をそれぞれ単独で添加した比較例2、3の製剤では、多少は粘度が高められたものの、本試験で用いた添加濃度では増粘効果はまだ不十分である。そして、(A)ミコナゾール硝酸塩を配合せずに上記(B)成分及び(C)成分を比較例2又は3と同量添加した比較例4の製剤でも増粘効果は不十分であった。しかしながら、本発明の(A)〜(C)成分を組み合わせて配合した実施例1では、単独では増粘効果を発揮するに不十分な量の(B)又は(C)成分との組合せでありながら、増粘効果が著しく高められることが明らかとなった。これまでに、ミコナゾール硝酸塩を配合することによる増粘効果は知られておらず、本結果は全く予想外の結果であった。そして、実施例1の製剤は水馴染みもよく、ねっとりとした使用感や糸引き等も生じておらず、使用感にも優れた外用組成物であった。 As shown in the above results, the preparation of Comparative Example 1 containing neither (B) a cationic polymer nor (C) a nonionic thickener having a fatty acid ester or fatty acid ether structure of high polyoxyethylene addition type is very viscous. Is low. Further, in the preparations of Comparative Examples 2 and 3 in which the above-mentioned component (B) or (C) component was added to the preparation of Comparative Example 1 respectively, the addition concentration used in this test was somewhat increased in viscosity. Then the thickening effect is still insufficient. And the thickening effect was inadequate also in the formulation of the comparative example 4 which added the said (B) component and the (C) component in the same amount as the comparative example 2 or 3 without mix | blending (A) miconazole nitrate. However, in Example 1 in which the components (A) to (C) of the present invention are combined and combined, it is a combination with an amount of the component (B) or (C) that is insufficient to exhibit a thickening effect alone. However, it became clear that the thickening effect was remarkably enhanced. So far, the thickening effect by adding miconazole nitrate has not been known, and this result was completely unexpected. The formulation of Example 1 was a composition for external use that was well-familiar with water, did not cause a sticky feeling or stringing, and had an excellent feeling of use.
(試験例2.粘度評価(2))
下記表2に示す処方を常法に従って調製した。具体的には、各成分を100mlガラスバイアルに量り取り、蒸留水で合計量が100重量%となるように添加して、約80℃で保温しながら攪拌し均一な製剤を得た。次いで、上記試験例1と同様の手順により、各製剤の粘度(25℃:mPa・s)を測定した。この結果を、下記表2の最下欄に併せて示す。
The formulation shown in Table 2 below was prepared according to a conventional method. Specifically, each component was weighed into a 100 ml glass vial, added with distilled water to a total amount of 100% by weight, and stirred while keeping the temperature at about 80 ° C. to obtain a uniform preparation. Subsequently, the viscosity (25 ° C .: mPa · s) of each preparation was measured by the same procedure as in Test Example 1. The results are also shown in the bottom column of Table 2 below.
上記結果に示されるように、(C)高ポリオキシエチレン付加型の脂肪酸エステル系ノニオン性増粘剤として、ジステアリン酸PEG−150を使用した場合にも、本発明の(A)〜(C)の三成分を組み合わせて配合することにより、25℃における粘度が1000mPa・sを超える程度になり、増粘効果が著しく高められることが明らかとなった。 As shown in the above results, when (C) distearic acid PEG-150 is used as the high polyoxyethylene addition type fatty acid ester nonionic thickener, (A) to (C) of the present invention. It was clarified that the viscosity at 25 ° C. exceeds 1000 mPa · s, and the thickening effect is remarkably enhanced by combining these three components.
以下、本発明の製剤処方例を示す。 Hereinafter, formulation examples of the present invention will be shown.
(製剤処方例1)
ミコナゾール硝酸塩 1.0重量%
ポリクオタニウム-10 0.3重量%
ジオレイン酸PEG-120メチルグルコース 0.8重量%
N-ヤシ油脂肪酸アシル-DL-アラニントリエタノールアミン液 20.0重量%
N-ヤシ油脂肪酸アシル-L-グルタミン酸ナトリウム液 10.0重量%
ヤシ油脂肪酸アミドプロピルベタイン 15.0重量%
ヤシ油脂肪酸ジエタノールアミド 3.0重量%
pH調整剤 適量
防腐剤 適量
油剤 適量
精製水 残量
(Formulation Formulation Example 1)
Miconazole nitrate 1.0% by weight
Polyquaternium-10 0.3 wt%
Dioleic acid PEG-120 methyl glucose 0.8 wt%
N-coconut oil fatty acid acyl-DL-alanine triethanolamine solution 20.0% by weight
N-coconut oil fatty acid acyl-L-sodium glutamate solution 10.0% by weight
Palm oil fatty acid amidopropyl betaine 15.0% by weight
Coconut oil fatty acid diethanolamide 3.0% by weight
pH adjuster appropriate amount preservative appropriate amount oil agent appropriate amount purified water remaining
(製剤処方例2)
ミコナゾール硝酸塩 1.0重量%
グアーヒドロキシプロピルトリモニウムクロリド 0.5重量%
ジステアリン酸PEG-150 2.0重量%
N-ヤシ油脂肪酸アシル-DL-アラニントリエタノールアミン液 10.0重量%
N-ヤシ油脂肪酸アシル-L-アスパラギン酸ナトリウム 3.0重量%
ラウリン酸アミドプロピルベタイン液 10.0重量%
ヤシ油脂肪酸ジエタノールアミド 1.0重量%
pH調整剤 適量
防腐剤 適量
油剤 適量
精製水 残量
(Preparation Example 2)
Miconazole nitrate 1.0% by weight
Guar hydroxypropyltrimonium chloride 0.5% by weight
PEG-150 distearate 2.0% by weight
N-coconut oil fatty acid acyl-DL-alanine triethanolamine solution 10.0% by weight
N-coconut oil fatty acid acyl-L-sodium aspartate 3.0% by weight
Lauric acid amidopropyl betaine solution 10.0% by weight
Palm oil fatty acid diethanolamide 1.0 wt%
pH adjuster appropriate amount preservative appropriate amount oil agent appropriate amount purified water remaining
(製剤処方例3)
ルリコナゾール 1.0重量%
ポリクオタニウム-10 0.5重量%
セテアレス-60ミリスチルグリコール 2.5重量%
N-ヤシ油脂肪酸アシルメチルタウリンナトリウム液 10.0重量%
N-ヤシ油脂肪酸アシル-L-グルタミン酸ナトリウム液 15.0重量%
ラウリン酸アミドプロピルベタイン液 5.0重量%
ヤシ油脂肪酸ジエタノールアミド 1.5重量%
pH調整剤 適量
防腐剤 適量
油剤 適量
精製水 残量
(Prescription Formulation Example 3)
Luliconazole 1.0% by weight
Polyquaternium-10 0.5% by weight
CETEARETH-60 myristyl glycol 2.5% by weight
N-coconut oil fatty acid acylmethyl taurine sodium solution 10.0% by weight
N-coconut oil fatty acid acyl-L-sodium glutamate solution 15.0% by weight
Lauric acid amidopropyl betaine solution 5.0% by weight
Palm oil fatty acid diethanolamide 1.5% by weight
pH adjuster appropriate amount preservative appropriate amount oil agent appropriate amount purified water remaining
Claims (11)
該(B)成分として、ポリクオタニウム−10、ポリクオタニウム−7、ポリクオタニウム−6、カチオン化グアーガムからなる群より選択される少なくとも1種を含み、及び、
該(C)成分として、ジオレイン酸PEG−120メチルグルコース、トリオレイン酸PEG−120メチルグルコース、トリイソステアリン酸PEG−120メチルグルコース、ジオレイン酸PEG−75、ジステアリン酸PEG−75、ジステアリン酸PEG−140、ジステアリン酸PEG−150、ジステアリン酸PEG−175、ジステアリン酸PEG−190、ジステアリン酸PEG−250、ステアリン酸PEG−75、ステアリン酸PEG−150、ジラウリン酸PEG−75、セテアレス−60ミリスチルグリコール、及びポリオキシエチレンセチルステアリルジエーテルからなる群より選択される少なくとも1種を含む、外用組成物。 (A) miconazole and / or salt thereof, (B) cationic polymer, (C) polyoxyethylene addition type fatty acid ester type or fatty acid ether type nonionic thickening having an average addition mole number of ethylene oxide of 50 to 300 An external composition comprising an agent, and (D) an amino acid surfactant and / or an amphoteric surfactant ,
The component (B) includes at least one selected from the group consisting of polyquaternium-10, polyquaternium-7, polyquaternium-6, and cationized guar gum; and
As the component (C), dioleic acid PEG-120 methyl glucose, trioleic acid PEG-120 methyl glucose, triisostearic acid PEG-120 methyl glucose, dioleic acid PEG-75, distearic acid PEG-75, distearic acid PEG-140 PEG-150 distearate, PEG-175 distearate, PEG-190 distearate, PEG-250 distearate, PEG-75 stearate, PEG-150 stearate, PEG-75 dilaurate, ceteares-60 myristyl glycol, and An external composition comprising at least one selected from the group consisting of polyoxyethylene cetyl stearyl diether.
該(B)成分として、ポリクオタニウム−10、ポリクオタニウム−7、ポリクオタニウム−6、カチオン化グアーガムからなる群より選択される少なくとも1種を含み、及び、
該(C)成分として、ジオレイン酸PEG−120メチルグルコース、トリオレイン酸PEG−120メチルグルコース、トリイソステアリン酸PEG−120メチルグルコース、ジオレイン酸PEG−75、ジステアリン酸PEG−75、ジステアリン酸PEG−140、ジステアリン酸PEG−150、ジステアリン酸PEG−175、ジステアリン酸PEG−190、ジステアリン酸PEG−250、ステアリン酸PEG−75、ステアリン酸PEG−150、ジラウリン酸PEG−75、セテアレス−60ミリスチルグリコール、及びポリオキシエチレンセチルステアリルジエーテルからなる群より選択される少なくとも1種を含む、該外用組成物を増粘する方法。 In the composition for external use, (A) miconazole and / or salt thereof, (B) cationic polymer, (C) polyoxyethylene addition type fatty acid ester or fatty acid ether having an average addition mole number of ethylene oxide of 50 to 300 A nonionic thickening agent of the system, and (D) an amino acid surfactant and / or an amphoteric surfactant to coexist, thereby thickening the composition for external use ,
The component (B) includes at least one selected from the group consisting of polyquaternium-10, polyquaternium-7, polyquaternium-6, and cationized guar gum; and
As the component (C), dioleic acid PEG-120 methyl glucose, trioleic acid PEG-120 methyl glucose, triisostearic acid PEG-120 methyl glucose, dioleic acid PEG-75, distearic acid PEG-75, distearic acid PEG-140 PEG-150 distearate, PEG-175 distearate, PEG-190 distearate, PEG-250 distearate, PEG-75 stearate, PEG-150 stearate, PEG-75 dilaurate, ceteares-60 myristyl glycol, and The method to thicken this external composition containing at least 1 sort (s) selected from the group which consists of polyoxyethylene cetyl stearyl diether.
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Free format text: JAPANESE INTERMEDIATE CODE: R250 |
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R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
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R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |