JPH0499719A - Application agent for external use - Google Patents
Application agent for external useInfo
- Publication number
- JPH0499719A JPH0499719A JP21838490A JP21838490A JPH0499719A JP H0499719 A JPH0499719 A JP H0499719A JP 21838490 A JP21838490 A JP 21838490A JP 21838490 A JP21838490 A JP 21838490A JP H0499719 A JPH0499719 A JP H0499719A
- Authority
- JP
- Japan
- Prior art keywords
- oil
- external patch
- drug
- parts
- group
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 229940079593 drug Drugs 0.000 claims abstract description 51
- 239000003814 drug Substances 0.000 claims abstract description 51
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 22
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims abstract description 18
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims abstract description 17
- 235000014113 dietary fatty acids Nutrition 0.000 claims abstract description 14
- 239000000194 fatty acid Substances 0.000 claims abstract description 14
- 229930195729 fatty acid Natural products 0.000 claims abstract description 14
- 150000004665 fatty acids Chemical class 0.000 claims abstract description 11
- 241001465754 Metazoa Species 0.000 claims abstract description 8
- 150000005846 sugar alcohols Polymers 0.000 claims abstract description 8
- 235000015112 vegetable and seed oil Nutrition 0.000 claims abstract description 8
- 239000010775 animal oil Substances 0.000 claims abstract description 7
- 239000008158 vegetable oil Substances 0.000 claims abstract description 7
- 239000000043 antiallergic agent Substances 0.000 claims abstract description 6
- 239000002876 beta blocker Substances 0.000 claims abstract description 6
- 229940097320 beta blocking agent Drugs 0.000 claims abstract description 6
- 230000002490 cerebral effect Effects 0.000 claims abstract description 6
- 230000002503 metabolic effect Effects 0.000 claims abstract description 6
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 5
- 239000000730 antalgic agent Substances 0.000 claims abstract description 4
- 239000010642 eucalyptus oil Substances 0.000 claims abstract description 4
- 229940044949 eucalyptus oil Drugs 0.000 claims abstract description 4
- 239000001525 mentha piperita l. herb oil Substances 0.000 claims abstract description 4
- OEIJHBUUFURJLI-UHFFFAOYSA-N octane-1,8-diol Chemical compound OCCCCCCCCO OEIJHBUUFURJLI-UHFFFAOYSA-N 0.000 claims abstract description 4
- 239000004006 olive oil Substances 0.000 claims abstract description 4
- 235000008390 olive oil Nutrition 0.000 claims abstract description 4
- 235000019477 peppermint oil Nutrition 0.000 claims abstract description 4
- 235000019489 Almond oil Nutrition 0.000 claims abstract description 3
- 239000008168 almond oil Substances 0.000 claims abstract description 3
- 239000002585 base Substances 0.000 claims description 26
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 11
- -1 alkali metal salt Chemical class 0.000 claims description 9
- 230000000202 analgesic effect Effects 0.000 claims description 8
- 235000011187 glycerol Nutrition 0.000 claims description 7
- 229940035676 analgesics Drugs 0.000 claims description 6
- 206010000196 Urinary abnormalities Diseases 0.000 claims description 5
- 229940124599 anti-inflammatory drug Drugs 0.000 claims description 5
- CDQSJQSWAWPGKG-UHFFFAOYSA-N butane-1,1-diol Chemical compound CCCC(O)O CDQSJQSWAWPGKG-UHFFFAOYSA-N 0.000 claims description 5
- 229940088597 hormone Drugs 0.000 claims description 5
- TVVTWOGRPVJKDJ-UHFFFAOYSA-N Befunolol hydrochloride Chemical compound [Cl-].CC(C)[NH2+]CC(O)COC1=CC=CC2=C1OC(C(C)=O)=C2 TVVTWOGRPVJKDJ-UHFFFAOYSA-N 0.000 claims description 4
- RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 RJKFOVLPORLFTN-LEKSSAKUSA-N 0.000 claims description 4
- RNGHAJVBYQPLAZ-UHFFFAOYSA-N Terodiline hydrochloride Chemical compound Cl.C=1C=CC=CC=1C(CC(C)NC(C)(C)C)C1=CC=CC=C1 RNGHAJVBYQPLAZ-UHFFFAOYSA-N 0.000 claims description 4
- 229910052783 alkali metal Inorganic materials 0.000 claims description 4
- 229960004374 befunolol Drugs 0.000 claims description 4
- SYTBZMRGLBWNTM-UHFFFAOYSA-N flurbiprofen Chemical compound FC1=CC(C(C(O)=O)C)=CC=C1C1=CC=CC=C1 SYTBZMRGLBWNTM-UHFFFAOYSA-N 0.000 claims description 4
- 229960002390 flurbiprofen Drugs 0.000 claims description 4
- DKYWVDODHFEZIM-UHFFFAOYSA-N ketoprofen Chemical compound OC(=O)C(C)C1=CC=CC(C(=O)C=2C=CC=CC=2)=C1 DKYWVDODHFEZIM-UHFFFAOYSA-N 0.000 claims description 4
- 229960000991 ketoprofen Drugs 0.000 claims description 4
- 239000003921 oil Substances 0.000 claims description 4
- 229960003959 terodiline hydrochloride Drugs 0.000 claims description 4
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 3
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims description 3
- KMISFPIWSMSMJD-GPKQSYPGSA-N Eptazocine hydrobromide Chemical compound Br.C1N(C)CC[C@@]2(C)C3=CC(O)=CC=C3C[C@@H]1C2 KMISFPIWSMSMJD-GPKQSYPGSA-N 0.000 claims description 3
- 239000002202 Polyethylene glycol Substances 0.000 claims description 3
- 235000019198 oils Nutrition 0.000 claims description 3
- 229920001223 polyethylene glycol Polymers 0.000 claims description 3
- 229960002920 sorbitol Drugs 0.000 claims description 3
- JQIYNMYZKRGDFK-RUFWAXPRSA-N Estradiol dipropionate Chemical compound C1CC2=CC(OC(=O)CC)=CC=C2[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CC)[C@@]1(C)CC2 JQIYNMYZKRGDFK-RUFWAXPRSA-N 0.000 claims description 2
- ZJVFLBOZORBYFE-UHFFFAOYSA-N Ibudilast Chemical compound C1=CC=CC2=C(C(=O)C(C)C)C(C(C)C)=NN21 ZJVFLBOZORBYFE-UHFFFAOYSA-N 0.000 claims description 2
- 241000772415 Neovison vison Species 0.000 claims description 2
- 235000019485 Safflower oil Nutrition 0.000 claims description 2
- PDMMFKSKQVNJMI-BLQWBTBKSA-N Testosterone propionate Chemical group C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CC)[C@@]1(C)CC2 PDMMFKSKQVNJMI-BLQWBTBKSA-N 0.000 claims description 2
- 239000002260 anti-inflammatory agent Substances 0.000 claims description 2
- 239000010495 camellia oil Substances 0.000 claims description 2
- 125000004432 carbon atom Chemical group C* 0.000 claims description 2
- FYBXRCFPOTXTJF-UHFFFAOYSA-N carteolol hydrochloride Chemical compound [Cl-].N1C(=O)CCC2=C1C=CC=C2OCC(O)C[NH2+]C(C)(C)C FYBXRCFPOTXTJF-UHFFFAOYSA-N 0.000 claims description 2
- 229960002165 carteolol hydrochloride Drugs 0.000 claims description 2
- 239000004359 castor oil Substances 0.000 claims description 2
- 235000019438 castor oil Nutrition 0.000 claims description 2
- 239000003240 coconut oil Substances 0.000 claims description 2
- 235000019864 coconut oil Nutrition 0.000 claims description 2
- 235000005687 corn oil Nutrition 0.000 claims description 2
- 239000002285 corn oil Substances 0.000 claims description 2
- 235000012343 cottonseed oil Nutrition 0.000 claims description 2
- 239000002385 cottonseed oil Substances 0.000 claims description 2
- 150000002148 esters Chemical class 0.000 claims description 2
- 229950010215 estradiol dipropionate Drugs 0.000 claims description 2
- IVLVTNPOHDFFCJ-UHFFFAOYSA-N fentanyl citrate Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O.C=1C=CC=CC=1N(C(=O)CC)C(CC1)CCN1CCC1=CC=CC=C1 IVLVTNPOHDFFCJ-UHFFFAOYSA-N 0.000 claims description 2
- 229960004207 fentanyl citrate Drugs 0.000 claims description 2
- 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 claims description 2
- 239000005556 hormone Substances 0.000 claims description 2
- 229960002491 ibudilast Drugs 0.000 claims description 2
- JGPMMRGNQUBGND-UHFFFAOYSA-N idebenone Chemical compound COC1=C(OC)C(=O)C(CCCCCCCCCCO)=C(C)C1=O JGPMMRGNQUBGND-UHFFFAOYSA-N 0.000 claims description 2
- 229960004135 idebenone Drugs 0.000 claims description 2
- BWHLPLXXIDYSNW-UHFFFAOYSA-N ketorolac tromethamine Chemical compound OCC(N)(CO)CO.OC(=O)C1CCN2C1=CC=C2C(=O)C1=CC=CC=C1 BWHLPLXXIDYSNW-UHFFFAOYSA-N 0.000 claims description 2
- 229960004384 ketorolac tromethamine Drugs 0.000 claims description 2
- 229960002373 loxoprofen Drugs 0.000 claims description 2
- 150000002763 monocarboxylic acids Chemical class 0.000 claims description 2
- BQJCRHHNABKAKU-KBQPJGBKSA-N morphine Chemical class O([C@H]1[C@H](C=C[C@H]23)O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O BQJCRHHNABKAKU-KBQPJGBKSA-N 0.000 claims description 2
- 229960002508 pindolol Drugs 0.000 claims description 2
- PHUTUTUABXHXLW-UHFFFAOYSA-N pindolol Chemical compound CC(C)NCC(O)COC1=CC=CC2=NC=C[C]12 PHUTUTUABXHXLW-UHFFFAOYSA-N 0.000 claims description 2
- 239000000186 progesterone Substances 0.000 claims description 2
- 229960003387 progesterone Drugs 0.000 claims description 2
- 235000005713 safflower oil Nutrition 0.000 claims description 2
- 239000003813 safflower oil Substances 0.000 claims description 2
- 239000008159 sesame oil Substances 0.000 claims description 2
- 235000011803 sesame oil Nutrition 0.000 claims description 2
- 239000003549 soybean oil Substances 0.000 claims description 2
- 235000012424 soybean oil Nutrition 0.000 claims description 2
- 230000003637 steroidlike Effects 0.000 claims description 2
- 229960001712 testosterone propionate Drugs 0.000 claims description 2
- NZHGWWWHIYHZNX-CSKARUKUSA-N tranilast Chemical compound C1=C(OC)C(OC)=CC=C1\C=C\C(=O)NC1=CC=CC=C1C(O)=O NZHGWWWHIYHZNX-CSKARUKUSA-N 0.000 claims description 2
- 229960005342 tranilast Drugs 0.000 claims description 2
- XIQVNETUBQGFHX-UHFFFAOYSA-N Ditropan Chemical compound C=1C=CC=CC=1C(O)(C(=O)OCC#CCN(CC)CC)C1CCCCC1 XIQVNETUBQGFHX-UHFFFAOYSA-N 0.000 claims 1
- YMBXTVYHTMGZDW-UHFFFAOYSA-N loxoprofen Chemical compound C1=CC(C(C(O)=O)C)=CC=C1CC1C(=O)CCC1 YMBXTVYHTMGZDW-UHFFFAOYSA-N 0.000 claims 1
- 229960005434 oxybutynin Drugs 0.000 claims 1
- 230000000694 effects Effects 0.000 abstract description 9
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 abstract description 4
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 abstract description 4
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 abstract description 4
- WWZKQHOCKIZLMA-UHFFFAOYSA-N Caprylic acid Natural products CCCCCCCC(O)=O WWZKQHOCKIZLMA-UHFFFAOYSA-N 0.000 abstract description 4
- 239000005642 Oleic acid Substances 0.000 abstract description 4
- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 abstract description 4
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 abstract description 4
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 abstract description 4
- 235000021355 Stearic acid Nutrition 0.000 abstract description 3
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 abstract description 3
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 abstract description 3
- 235000021313 oleic acid Nutrition 0.000 abstract description 3
- 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 abstract description 2
- AWQSAIIDOMEEOD-UHFFFAOYSA-N 5,5-Dimethyl-4-(3-oxobutyl)dihydro-2(3H)-furanone Chemical compound CC(=O)CCC1CC(=O)OC1(C)C AWQSAIIDOMEEOD-UHFFFAOYSA-N 0.000 abstract description 2
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 abstract description 2
- GONOPSZTUGRENK-UHFFFAOYSA-N benzyl(trichloro)silane Chemical compound Cl[Si](Cl)(Cl)CC1=CC=CC=C1 GONOPSZTUGRENK-UHFFFAOYSA-N 0.000 abstract description 2
- FUZZWVXGSFPDMH-UHFFFAOYSA-N n-hexanoic acid Natural products CCCCCC(O)=O FUZZWVXGSFPDMH-UHFFFAOYSA-N 0.000 abstract description 2
- DZKXJUASMGQEMA-UHFFFAOYSA-N tetradecyl tetradecanoate Chemical compound CCCCCCCCCCCCCCOC(=O)CCCCCCCCCCCCC DZKXJUASMGQEMA-UHFFFAOYSA-N 0.000 abstract description 2
- SSMSBSWKLKKXGG-UHFFFAOYSA-N 1-(2-chlorophenyl)-2-isopropylaminoethanol Chemical compound CC(C)NCC(O)C1=CC=CC=C1Cl SSMSBSWKLKKXGG-UHFFFAOYSA-N 0.000 abstract 1
- 240000006711 Pistacia vera Species 0.000 abstract 1
- 229950011462 clorprenaline Drugs 0.000 abstract 1
- 159000000000 sodium salts Chemical class 0.000 abstract 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 39
- 230000000052 comparative effect Effects 0.000 description 18
- 239000005995 Aluminium silicate Substances 0.000 description 14
- 235000012211 aluminium silicate Nutrition 0.000 description 14
- NLYAJNPCOHFWQQ-UHFFFAOYSA-N kaolin Chemical compound O.O.O=[Al]O[Si](=O)O[Si](=O)O[Al]=O NLYAJNPCOHFWQQ-UHFFFAOYSA-N 0.000 description 14
- 229920001495 poly(sodium acrylate) polymer Polymers 0.000 description 14
- NNMHYFLPFNGQFZ-UHFFFAOYSA-M sodium polyacrylate Chemical compound [Na+].[O-]C(=O)C=C NNMHYFLPFNGQFZ-UHFFFAOYSA-M 0.000 description 14
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 13
- 239000001768 carboxy methyl cellulose Substances 0.000 description 13
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 13
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 13
- 108010010803 Gelatin Proteins 0.000 description 12
- 229920000159 gelatin Polymers 0.000 description 12
- 239000008273 gelatin Substances 0.000 description 12
- 235000019322 gelatine Nutrition 0.000 description 12
- 235000011852 gelatine desserts Nutrition 0.000 description 12
- 238000004898 kneading Methods 0.000 description 9
- 230000000699 topical effect Effects 0.000 description 9
- 239000000203 mixture Substances 0.000 description 8
- 238000010521 absorption reaction Methods 0.000 description 6
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 5
- 239000011975 tartaric acid Substances 0.000 description 5
- 235000002906 tartaric acid Nutrition 0.000 description 5
- 239000000243 solution Substances 0.000 description 4
- 230000003187 abdominal effect Effects 0.000 description 3
- HMUNWXXNJPVALC-UHFFFAOYSA-N 1-[4-[2-(2,3-dihydro-1H-inden-2-ylamino)pyrimidin-5-yl]piperazin-1-yl]-2-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)ethanone Chemical group C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)N1CCN(CC1)C(CN1CC2=C(CC1)NN=N2)=O HMUNWXXNJPVALC-UHFFFAOYSA-N 0.000 description 2
- VZSRBBMJRBPUNF-UHFFFAOYSA-N 2-(2,3-dihydro-1H-inden-2-ylamino)-N-[3-oxo-3-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)propyl]pyrimidine-5-carboxamide Chemical group C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)C(=O)NCCC(N1CC2=C(CC1)NN=N2)=O VZSRBBMJRBPUNF-UHFFFAOYSA-N 0.000 description 2
- SXAMGRAIZSSWIH-UHFFFAOYSA-N 2-[3-[2-(2,3-dihydro-1H-inden-2-ylamino)pyrimidin-5-yl]-1,2,4-oxadiazol-5-yl]-1-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)ethanone Chemical group C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)C1=NOC(=N1)CC(=O)N1CC2=C(CC1)NN=N2 SXAMGRAIZSSWIH-UHFFFAOYSA-N 0.000 description 2
- YJLUBHOZZTYQIP-UHFFFAOYSA-N 2-[5-[2-(2,3-dihydro-1H-inden-2-ylamino)pyrimidin-5-yl]-1,3,4-oxadiazol-2-yl]-1-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)ethanone Chemical group C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)C1=NN=C(O1)CC(=O)N1CC2=C(CC1)NN=N2 YJLUBHOZZTYQIP-UHFFFAOYSA-N 0.000 description 2
- CONKBQPVFMXDOV-QHCPKHFHSA-N 6-[(5S)-5-[[4-[2-(2,3-dihydro-1H-inden-2-ylamino)pyrimidin-5-yl]piperazin-1-yl]methyl]-2-oxo-1,3-oxazolidin-3-yl]-3H-1,3-benzoxazol-2-one Chemical group C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)N1CCN(CC1)C[C@H]1CN(C(O1)=O)C1=CC2=C(NC(O2)=O)C=C1 CONKBQPVFMXDOV-QHCPKHFHSA-N 0.000 description 2
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 2
- OYHQOLUKZRVURQ-HZJYTTRNSA-N Linoleic acid Chemical compound CCCCC\C=C/C\C=C/CCCCCCCC(O)=O OYHQOLUKZRVURQ-HZJYTTRNSA-N 0.000 description 2
- TUNFSRHWOTWDNC-UHFFFAOYSA-N Myristic acid Natural products CCCCCCCCCCCCCC(O)=O TUNFSRHWOTWDNC-UHFFFAOYSA-N 0.000 description 2
- ZOJBYZNEUISWFT-UHFFFAOYSA-N allyl isothiocyanate Chemical compound C=CCN=C=S ZOJBYZNEUISWFT-UHFFFAOYSA-N 0.000 description 2
- POULHZVOKOAJMA-UHFFFAOYSA-N dodecanoic acid Chemical compound CCCCCCCCCCCC(O)=O POULHZVOKOAJMA-UHFFFAOYSA-N 0.000 description 2
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 description 2
- 239000003410 keratolytic agent Substances 0.000 description 2
- 235000020778 linoleic acid Nutrition 0.000 description 2
- OYHQOLUKZRVURQ-IXWMQOLASA-N linoleic acid Natural products CCCCC\C=C/C\C=C\CCCCCCCC(O)=O OYHQOLUKZRVURQ-IXWMQOLASA-N 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 239000008164 mustard oil Substances 0.000 description 2
- FBUKVWPVBMHYJY-UHFFFAOYSA-N nonanoic acid Chemical compound CCCCCCCCC(O)=O FBUKVWPVBMHYJY-UHFFFAOYSA-N 0.000 description 2
- BARWIPMJPCRCTP-UHFFFAOYSA-N oleic acid oleyl ester Natural products CCCCCCCCC=CCCCCCCCCOC(=O)CCCCCCCC=CCCCCCCCC BARWIPMJPCRCTP-UHFFFAOYSA-N 0.000 description 2
- BARWIPMJPCRCTP-CLFAGFIQSA-N oleyl oleate Chemical compound CCCCCCCC\C=C/CCCCCCCCOC(=O)CCCCCCC\C=C/CCCCCCCC BARWIPMJPCRCTP-CLFAGFIQSA-N 0.000 description 2
- PXDJXZJSCPSGGI-UHFFFAOYSA-N palmityl palmitate Chemical compound CCCCCCCCCCCCCCCCOC(=O)CCCCCCCCCCCCCCC PXDJXZJSCPSGGI-UHFFFAOYSA-N 0.000 description 2
- 231100000245 skin permeability Toxicity 0.000 description 2
- 239000011734 sodium Substances 0.000 description 2
- 229910052708 sodium Inorganic materials 0.000 description 2
- GYSCBCSGKXNZRH-UHFFFAOYSA-N 1-benzothiophene-2-carboxamide Chemical compound C1=CC=C2SC(C(=O)N)=CC2=C1 GYSCBCSGKXNZRH-UHFFFAOYSA-N 0.000 description 1
- WZFUQSJFWNHZHM-UHFFFAOYSA-N 2-[4-[2-(2,3-dihydro-1H-inden-2-ylamino)pyrimidin-5-yl]piperazin-1-yl]-1-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)ethanone Chemical group C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)N1CCN(CC1)CC(=O)N1CC2=C(CC1)NN=N2 WZFUQSJFWNHZHM-UHFFFAOYSA-N 0.000 description 1
- GHVNFZFCNZKVNT-UHFFFAOYSA-N Decanoic acid Natural products CCCCCCCCCC(O)=O GHVNFZFCNZKVNT-UHFFFAOYSA-N 0.000 description 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 1
- SNRUBQQJIBEYMU-UHFFFAOYSA-N Dodecane Natural products CCCCCCCCCCCC SNRUBQQJIBEYMU-UHFFFAOYSA-N 0.000 description 1
- 208000010201 Exanthema Diseases 0.000 description 1
- 235000021314 Palmitic acid Nutrition 0.000 description 1
- 240000003296 Petasites japonicus Species 0.000 description 1
- 235000003823 Petasites japonicus Nutrition 0.000 description 1
- 239000004698 Polyethylene Substances 0.000 description 1
- 239000004743 Polypropylene Substances 0.000 description 1
- BCKXLBQYZLBQEK-KVVVOXFISA-M Sodium oleate Chemical compound [Na+].CCCCCCCC\C=C/CCCCCCCC([O-])=O BCKXLBQYZLBQEK-KVVVOXFISA-M 0.000 description 1
- 229920002125 Sokalan® Polymers 0.000 description 1
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 1
- 230000002378 acidificating effect Effects 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 125000003158 alcohol group Chemical group 0.000 description 1
- 125000000217 alkyl group Chemical group 0.000 description 1
- OBETXYAYXDNJHR-UHFFFAOYSA-N alpha-ethylcaproic acid Natural products CCCCC(CC)C(O)=O OBETXYAYXDNJHR-UHFFFAOYSA-N 0.000 description 1
- 239000000440 bentonite Substances 0.000 description 1
- 229910000278 bentonite Inorganic materials 0.000 description 1
- 235000012216 bentonite Nutrition 0.000 description 1
- SVPXDRXYRYOSEX-UHFFFAOYSA-N bentoquatam Chemical compound O.O=[Si]=O.O=[Al]O[Al]=O SVPXDRXYRYOSEX-UHFFFAOYSA-N 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 239000013065 commercial product Substances 0.000 description 1
- 125000002704 decyl group Chemical group [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])* 0.000 description 1
- 238000010586 diagram Methods 0.000 description 1
- 125000003438 dodecyl group Chemical group [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])* 0.000 description 1
- 238000001647 drug administration Methods 0.000 description 1
- 238000012377 drug delivery Methods 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 201000005884 exanthem Diseases 0.000 description 1
- 239000004744 fabric Substances 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- WORCCYVLMMTGFR-UHFFFAOYSA-M loxoprofen sodium Chemical compound [Na+].C1=CC(C(C([O-])=O)C)=CC=C1CC1C(=O)CCC1 WORCCYVLMMTGFR-UHFFFAOYSA-M 0.000 description 1
- 230000014759 maintenance of location Effects 0.000 description 1
- 230000007721 medicinal effect Effects 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 235000010981 methylcellulose Nutrition 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 125000001421 myristyl 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])[H] 0.000 description 1
- 239000004745 nonwoven fabric Substances 0.000 description 1
- 125000002347 octyl 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])[H] 0.000 description 1
- 125000001117 oleyl 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])=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])[H] 0.000 description 1
- 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 description 1
- 239000004584 polyacrylic acid Substances 0.000 description 1
- 229920000728 polyester Polymers 0.000 description 1
- 229920000573 polyethylene Polymers 0.000 description 1
- 229920001155 polypropylene Polymers 0.000 description 1
- 206010037844 rash Diseases 0.000 description 1
- HSFQBFMEWSTNOW-UHFFFAOYSA-N sodium;carbanide Chemical group [CH3-].[Na+] HSFQBFMEWSTNOW-UHFFFAOYSA-N 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 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 description 1
- 238000003756 stirring Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 238000013269 sustained drug release Methods 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 235000010215 titanium dioxide Nutrition 0.000 description 1
- 235000019871 vegetable fat Nutrition 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
【発明の詳細な説明】
（産業上の利用分野）
本発明は外用貼付剤、更に詳しくは外用貼付剤に配合さ
れた薬剤の経皮吸収を充分に高めることができる外用貼
付剤用水性基剤及びこの水性基剤を用いた外用貼付剤に
関するものである。Detailed Description of the Invention (Field of Industrial Application) The present invention provides a topical patch, more specifically, an aqueous base for a topical patch that can sufficiently increase the transdermal absorption of a drug contained in the topical patch. The present invention also relates to an external patch using this aqueous base.
（従来の技術）
近年、効果的薬剤投与経路即ちドラッグデリバリ−シス
テムの概念より、経皮投与経路か注目されている。経皮
投与によると、副作用の強い薬剤や注射による投与が主
に利用されてきた薬剤及び有効血中濃度保持時間か短く
ｌ［］数回の投与か必要な薬剤を、副作用を軽減し且つ
苦痛を伴わずに皮膚から徐々に持続的に吸収させること
ができる。このため、経皮投与は薬剤の徐放化投与方法
として有効である。(Prior Art) In recent years, the concept of an effective drug administration route, that is, a drug delivery system, has attracted attention to the transdermal administration route. Transdermal administration reduces the side effects and pain of drugs that have strong side effects, drugs that have been mainly administered by injection, and drugs that have a short effective blood concentration retention time and require multiple administrations. It can be absorbed gradually and continuously through the skin without any irradiation. Therefore, transdermal administration is effective as a sustained release administration method for drugs.
（発明か解決しようとする課題）
ところが、皮膚は本来外部よりの異物か体内へ侵入する
のを阻止するという性質を有するので、皮膚から投与で
きる薬剤は非常に限られていた。又、エイシン等の角質
溶解剤を用いて薬剤の経皮吸収を高める方法が試みられ
ているが、これらの角質溶解剤は皮膚刺激性か高く、副
作用によるかぶれなとが懸念されるので製剤化は難しい
。(Problem to be Solved by the Invention) However, since the skin originally has the property of preventing foreign substances from entering the body, the drugs that can be administered through the skin are extremely limited. In addition, attempts have been made to increase the transdermal absorption of drugs using keratolytic agents such as Eisin, but these keratolytic agents are highly irritating to the skin, and there are concerns that they may cause rashes as a side effect, so formulations have not been developed. is difficult.
本発明は前記従来技術の問題点を解決するためのもので
ある。本発明の目的は、副作用が少なく安全て且つ外用
貼付剤に配合された薬剤を皮膚から徐々に持続的に効率
良く吸収させることができる外用貼付剤のための水性基
剤及びこの水性基剤を用いた外用貼付剤を提供すること
にある。The present invention is intended to solve the problems of the prior art. The object of the present invention is to provide an aqueous base for a topical patch that is safe with few side effects and allows the drug contained in the topical patch to be absorbed gradually, continuously and efficiently through the skin, and to provide this aqueous base. An object of the present invention is to provide a topical patch using the above-mentioned methods.
（課題を解決するための手段）
本発明の外用貼付側用水性Ｍ：削は、脂肪酸及びその誘
導体及び動植物性油脂からなる群から選ばれた少なくと
も１種と、多価アルコールと、水とからなるという特徴
を有している。(Means for Solving the Problems) The aqueous M for external application of the present invention is made of at least one selected from the group consisting of fatty acids and their derivatives, animal and vegetable oils, polyhydric alcohols, and water. It has the characteristic of becoming.
脂肪酸及びその誘導体は、炭素原ｒ−数５ないし３０の
モノカルボン酸又はそのエステル又はそのアルカリ金属
塩であるのか好ましい。脂肪酸の例は、ヘキサン酸、ヘ
プタン酸、オクタン酸、ノナン酸、デカン酸、ドデカン
酸、テトラデカン酸、ヘキサデカン酸、オクタデカン酸
、オレイン酸、リノール酸である。オクタデカン酸、オ
レイン酸、リノール酸か最も好ましい。The fatty acid and its derivatives are preferably monocarboxylic acids having 5 to 30 carbon atoms, esters thereof, or alkali metal salts thereof. Examples of fatty acids are hexanoic acid, heptanoic acid, octanoic acid, nonanoic acid, decanoic acid, dodecanoic acid, tetradecanoic acid, hexadecanoic acid, octadecanoic acid, oleic acid, linoleic acid. Most preferred are octadecanoic acid, oleic acid, and linoleic acid.
又、脂肪酸エステルは、アルコール残基のアルキル部分
がヘキシル、オクチル、デシル、ドデシル、テトラデシ
ル、ヘキサデシル、オクタデシル、オレイルであるもの
が好ましい。テトラデカン酸テトラデシル、ヘキサデカ
ン酸ヘキサデシル、オレイン酸オレイルか最も好ましい
。Further, the fatty acid ester is preferably one in which the alkyl moiety of the alcohol residue is hexyl, octyl, decyl, dodecyl, tetradecyl, hexadecyl, octadecyl, or oleyl. Most preferred are tetradecyl tetradecanoate, hexadecyl hexadecanoate, and oleyl oleate.
脂肪酸アルカリ金属塩は、脂肪酸ナトリウム塩が最も好
ましい。The fatty acid alkali metal salt is most preferably a fatty acid sodium salt.
動植物性油脂は、アーモンド油、オリーブ油、ツバキ油
、パーシック油、ハツカ油、ゴマ油、ダイズ油、ミンク
油、綿実油、トウモロコシ油、サフラワー油、ヤシ油、
ユーカリ油及びヒマシ油からなる群から選ばれた少なく
とも１種からなるものが好ましい。オリーブ油、ハツカ
油、ユーカリ油が最も好ましい。Animal and vegetable oils include almond oil, olive oil, camellia oil, persic oil, mustard oil, sesame oil, soybean oil, mink oil, cottonseed oil, corn oil, safflower oil, coconut oil,
It is preferable to use at least one selected from the group consisting of eucalyptus oil and castor oil. Most preferred are olive oil, mustard oil, and eucalyptus oil.
府記脂肪酸及びその誘導体及び動植物性油脂は、１種使
用してもよいし又は２種以上を組み合わせて使用しても
よい。又、その使用量は、水性基剤の全重量に対して約
１．０重量％ないし約３０重量％とするのが好ましい。One type of Fuki fatty acids and their derivatives and animal and vegetable fats and oils may be used, or two or more types may be used in combination. The amount used is preferably about 1.0% to about 30% by weight based on the total weight of the aqueous base.
多価アルコールの例は、グリセリン、プロピレングリコ
ール、オクタンジオール、ブタンジオール、ポリエチレ
ングリコール及びＤ−ソルビットである。これらは２種
以上を組み合わせて使用することができる。多価アルコ
ールの使用量は、水性基剤の全重量に対して約１０重量
％ないし約５０重量％とするのが好ましい。Examples of polyhydric alcohols are glycerin, propylene glycol, octanediol, butanediol, polyethylene glycol and D-sorbitol. These can be used in combination of two or more types. Preferably, the amount of polyhydric alcohol used is from about 10% to about 50% by weight, based on the total weight of the aqueous base.
本発明の水性基剤は、前記各成分以外に所望により他の
添加剤例えばセルロース誘導体、ポリアクリル酸アルカ
リ金属塩、ゼラチン、カオリン、ベントナイト、チタン
白等やｐＨ調整剤例えばクエン酸、酒石酸等を所定量含
んていても良い。In addition to the above-mentioned components, the aqueous base of the present invention may optionally contain other additives such as cellulose derivatives, alkali metal salts of polyacrylic acid, gelatin, kaolin, bentonite, titanium white, etc., and pH adjusters such as citric acid, tartaric acid, etc. A predetermined amount may be included.
本発明の水性基剤を使用する場合には、本発明の水性基
剤に外用貼付剤において有効成分として用いる薬剤を所
定量配合する。When using the aqueous base of the present invention, a predetermined amount of a drug used as an active ingredient in the external patch is blended into the aqueous base of the present invention.
即ち、本発明の外用貼付剤は、鎮痛薬、抗アレルギー薬
、脳循環代謝薬、β−遮断薬、ホルモン剤、排尿異常改
善薬及び非ステロイド鎮痛消炎薬からなる群から選ばれ
た少なくとも１種の薬剤と、本発明の外用貼付側用水性
基剤とからなるという特徴を有している。That is, the external patch of the present invention contains at least one selected from the group consisting of analgesics, antiallergic drugs, cerebral circulation metabolic drugs, β-blockers, hormonal drugs, urinary abnormality improving drugs, and nonsteroidal analgesic and antiinflammatory drugs. and the aqueous base for external application of the present invention.
薬剤を、例えば脂肪酸及びその誘導体及び動植物性油脂
からなる群から選ばれた少なくとも１種又は水に溶解し
、これを本発明の水性基剤の他の成分と均一に混練すれ
ば外用貼付剤か得られる。それ故、薬剤は油溶性てあっ
てもよいし又は水溶性であってもよい。更に所望により
、油溶性の薬剤と水溶性の薬剤とを組み合わせて用いる
こともできる。For example, if a drug is dissolved in at least one selected from the group consisting of fatty acids and their derivatives, and animal and vegetable oils or in water, and this is uniformly kneaded with the other components of the aqueous base of the present invention, an external patch can be prepared. can get. Therefore, the drug may be oil-soluble or water-soluble. Furthermore, if desired, an oil-soluble drug and a water-soluble drug can be used in combination.
鎮痛薬は、臭化水素酸ニブタブシン、クエン酸フエンタ
ニール及びモルヒネ塩類からなる群から選ばれた少なく
とも１種からなるものが好ましい。The analgesic is preferably at least one selected from the group consisting of nibutabcin hydrobromide, fentanyl citrate, and morphine salts.
抗アレルギー薬は、塩酸クロルプレナリン、イブジラス
ト及びトラニラストからなる群から選ばれた少なくとも
１種からなるものか好ましい。Preferably, the antiallergic drug is at least one selected from the group consisting of chlorprenaline hydrochloride, ibudilast, and tranilast.
脳循環代謝薬は、イデベノン、塩酸ビフェメラン及び塩
酸インデロキサジンからなる群から選ばれた少なくとも
１種からなるものが好ましい。The cerebral circulation metabolic drug is preferably at least one selected from the group consisting of idebenone, biphemeran hydrochloride, and inderoxazine hydrochloride.
β−遮断薬は、塩酸ベフノロール、塩酸カルテオロール
及びピンドロールからなる群から選ばれた少なくとも１
種からなるものが好ましい。The β-blocker is at least one selected from the group consisting of befunolol hydrochloride, carteolol hydrochloride, and pindolol.
Those consisting of seeds are preferred.
ホルモン剤は、プロピオン酸テストステロン、プロピオ
ン酸エストラジオール及びプロゲステロンからなる群か
ら選ばれた少なくとも１種からなるものが好ましい。The hormone agent is preferably at least one selected from the group consisting of testosterone propionate, estradiol propionate, and progesterone.
排尿異常改善薬は、塩酸オギシブチニン、塩酸テロジリ
ン及び塩酸プロピペリンからなる群から選ばれた少なく
とも１種からなるものか好ましい。The urinary abnormality improving drug is preferably at least one selected from the group consisting of ogicibutynin hydrochloride, terodiline hydrochloride, and propiperine hydrochloride.
非ステロイド鎮痛消炎薬は、フルルビプロフェン、ケト
プロフェン、ロキソプロフェンナトリウム及びケトロラ
ックトロメタミンからなる群から選ばれた少なくとも１
種からなるものか好ましい。The nonsteroidal analgesic anti-inflammatory drug is at least one selected from the group consisting of flurbiprofen, ketoprofen, loxoprofen sodium, and ketorolac tromethamine.
Preferably, it consists of seeds.
外用貼付剤中の薬剤濃度は、低すぎると医薬としての作
用が不充分となり、又反対に高すぎてもコスト的に不利
となるなどの不具合を生じる。このため、薬剤濃度は外
用貼付剤の全重量に対して０．０２重量％ないし１０重
量％であるのか良い。If the drug concentration in the external patch is too low, the medicinal effect will be insufficient, and if it is too high, problems such as cost disadvantages will occur. Therefore, the drug concentration is preferably from 0.02% to 10% by weight based on the total weight of the external patch.
このようにして得られた本発明の水性基剤を用いた本発
明の外用貼付剤は、適当な基布例えばネル、不織布等に
展延し、次いて外用貼付剤の露出面にポリエチレン、ポ
リプロピレン、ポリエステル等の剥離用フィルムを貼着
して市販品として供することができる。The external patch of the present invention using the aqueous base of the present invention thus obtained is spread on a suitable base fabric such as flannelette, nonwoven fabric, etc., and then polyethylene, polypropylene, etc. are applied to the exposed surface of the external patch. It can be provided as a commercial product by attaching a peeling film such as polyester or the like.
（作用）
本発明の水性基剤は、皮膚刺激性が高い成分を含まない
ので副作用か少なく、且つ水を含む水性基剤なので皮膚
に対する馴染みがよい。更に、各種成分を適切に配合し
たことにより種々の薬剤とも均質に混合することができ
る。(Function) The aqueous base of the present invention does not contain any components that are highly irritating to the skin, so it has fewer side effects, and since it is an aqueous base that contains water, it is easily compatible with the skin. Furthermore, by appropriately blending various components, it is possible to mix homogeneously with various drugs.
又、上記水性基剤を用いた本発明の外用貼付剤は、種々
の薬剤を皮膚から効率良く且つ徐々に持続的に吸収させ
ることができる。Further, the external patch of the present invention using the above-mentioned aqueous base can efficiently and gradually absorb various drugs through the skin.
（実施例）
以下の実施例及び比較例により、本発明を更に詳細に説
明する。(Example) The present invention will be explained in more detail with the following Examples and Comparative Examples.
実施例１
「フルルビプロフェン」１部をハツカ油４部に溶解し、
これをグリセリン１５部、プロピレングリコール１５部
、カルボキシメチルセルロースナトリウム９部、ポリア
クリル酸ナトリウム７部、ゼラチン４部、水３７部５部
、カオリン７部及びクエン酸０．５部からなる各成分と
均一に混練して、実施例１の外用貼付剤を得た。Example 1 1 part of "flurbiprofen" was dissolved in 4 parts of peppermint oil,
This was uniformly mixed with each component consisting of 15 parts of glycerin, 15 parts of propylene glycol, 9 parts of sodium carboxymethyl cellulose, 7 parts of sodium polyacrylate, 4 parts of gelatin, 37 parts of water, 5 parts of water, 7 parts of kaolin, and 0.5 parts of citric acid. The mixture was kneaded to obtain the external patch of Example 1.
実施例２
「ケトプロフェン」１部をハツカ油４部に溶解し１．こ
れをグリセリン１５部、オクタンジオール１５部、カル
ボキシメチルセルロースナトリウム９部、ポリアクリル
酸ナトリウム７部、ゼラチン４部、水３７．５部、カオ
リン７部及び酒石酸０．５部からなる各成分と均一に混
練して、実施例２の外用貼付剤を得た。Example 2 1 part of "ketoprofen" was dissolved in 4 parts of peppermint oil. This was uniformly mixed with each component consisting of 15 parts of glycerin, 15 parts of octanediol, 9 parts of sodium carboxymethylcellulose, 7 parts of sodium polyacrylate, 4 parts of gelatin, 37.5 parts of water, 7 parts of kaolin, and 0.5 parts of tartaric acid. The mixture was kneaded to obtain the external patch of Example 2.
実施例３
「塩酸テロジリン」１部を水４０．５部に溶解し、これ
をオレイン酸１部、グリセリン１５部、ブタンジオール
１５部、カルボキシメチルセルロースナトリウム９部、
ポリアクリル酸ナトリウム７部、ゼラチン４部、カオリ
ン７部及びクエン酸０．５部からなる各成分と均一に混
練して、実施例３の外用貼付剤を得た。Example 3 1 part of "terodiline hydrochloride" was dissolved in 40.5 parts of water, and this was dissolved in 1 part of oleic acid, 15 parts of glycerin, 15 parts of butanediol, 9 parts of sodium carboxymethylcellulose,
The external patch of Example 3 was obtained by uniformly kneading each component consisting of 7 parts of sodium polyacrylate, 4 parts of gelatin, 7 parts of kaolin, and 0.5 part of citric acid.
実施例４
「塩酸ベフノロール」１部を水４１］、５部に溶解し、
これをリノール酸１部、グリセリン１５部、ポリエチレ
ングリコール１５部、カルホキツメチルセルロースナト
リウム９部、ポリアクリル酸ナトリウム７部、セラチン
４部、ガオリシ７部及びクエン酸０．５部からなる各成
分と均一に混練して、実施例４の外用貼付剤を得た。Example 4 1 part of "Befunolol hydrochloride" was dissolved in 5 parts of water,
This was mixed with each component consisting of 1 part of linoleic acid, 15 parts of glycerin, 15 parts of polyethylene glycol, 9 parts of sodium methyl cellulose, 7 parts of sodium polyacrylate, 4 parts of ceratin, 7 parts of citric acid, and 0.5 parts of citric acid. The mixture was uniformly kneaded to obtain the external patch of Example 4.
実施例５
「塩酸クロルプレナリン」１部を水４０部５部に溶解し
、これをテトラデカン酸テ］・ラデンル１部、グリセリ
ン１５部、Ｄ−ツルヒント・液（Ｄソルビット濃度７０
重量％）１５部、カルボキシメチルセルロースナトリウ
ム９部、ポリアクリル酸ナトリウム７部、ゼラチン４部
、カオリン７部及びクエン酸０．５部からなる各成分と
均一に混練して、実施例５の外用貼付剤を得た。Example 5 1 part of "chlorprenaline hydrochloride" was dissolved in 40 parts and 5 parts of water, and this was dissolved in 1 part of tetradecanoic acid, 1 part of glycerin, and D-Truhinto solution (D sorbitol concentration 70 parts).
% by weight), 9 parts of sodium carboxymethylcellulose, 7 parts of sodium polyacrylate, 4 parts of gelatin, 7 parts of kaolin, and 0.5 parts of citric acid, and the mixture was kneaded uniformly with each component, and the topical patch of Example 5 was prepared. obtained the drug.
実施例６
「ロキソブロフェンナトリウム」１部を水４０．５部に
溶解し、これをオレイン酸オレイル１部、プロピレング
リコール１５部、ブタンジオール１５部、カルボキシメ
チルセルロースナトリウム９部、ポリアクリル酸ナトリ
ウム７部、セラチン４部、カオリン７部及び酒石酸０．
５部からなる各成分と均一に混練して、実施例６の外用
貼付剤を得た。Example 6 1 part of "loxobrofen sodium" was dissolved in 40.5 parts of water, and this was dissolved in 1 part of oleyl oleate, 15 parts of propylene glycol, 15 parts of butanediol, 9 parts of sodium carboxymethyl cellulose, and 7 parts of sodium polyacrylate. part, 4 parts of seratin, 7 parts of kaolin, and 0.0 parts of tartaric acid.
The external patch of Example 6 was obtained by uniformly kneading the mixture with 5 parts of each component.
実施例７
「臭化水素酸エプタゾシン」１部を水４０．５部に溶解
し、これをオレイン酸ナトリウム１部、プロピレングリ
コール１５部、ブタンジオール１５部、カルボキシメチ
ルセルロースナトリウム９部、ポリアクリル酸ナトリウ
ム７部、セラチン４部、カオリン７部及びクエン酸０．
５部からなる各成分と均一に混練して、実施例７の外用
貼付剤を得た。Example 7 1 part of "eptazocine hydrobromide" was dissolved in 40.5 parts of water, and this was dissolved in 1 part of sodium oleate, 15 parts of propylene glycol, 15 parts of butanediol, 9 parts of sodium carboxymethylcellulose, and sodium polyacrylate. 7 parts, 4 parts of seratin, 7 parts of kaolin, and 0.0 parts of citric acid.
The external patch of Example 7 was obtained by uniformly kneading the mixture with 5 parts of each component.
比較例１
「フルルビプロフェン」１部を水７９．６部に加え、こ
れをカルボキシメチルセルロースナトリウム８部、ポリ
アクリル酸ナトリウム６部、ゼラチン４部、カオリン７
部及びクエン酸０．５部からなる各成分と均一に混練し
て、比較例１の外用貼付剤を得た。Comparative Example 1 1 part of "flurbiprofen" was added to 79.6 parts of water, and this was mixed with 8 parts of sodium carboxymethyl cellulose, 6 parts of sodium polyacrylate, 4 parts of gelatin, and 7 parts of kaolin.
A topical patch of Comparative Example 1 was obtained by uniformly kneading each component consisting of 1 part and 0.5 parts of citric acid.
比較例２
「ケトプロフェン１１部を水７９．６部に加え、これを
カルボキシメチルセルロースナトリウム８部、ポリアク
リル酸ナトリウム６部、ゼラチン４部、カオリン７部及
び酒石酸０．５部からなる各成分と均一に混練して、比
較例２の外用貼付剤を得た。Comparative Example 2 11 parts of ketoprofen was added to 79.6 parts of water, and this was mixed uniformly with each component consisting of 8 parts of sodium carboxymethyl cellulose, 6 parts of sodium polyacrylate, 4 parts of gelatin, 7 parts of kaolin, and 0.5 parts of tartaric acid. The mixture was kneaded to obtain an external patch of Comparative Example 2.
比較例３
「塩酸テロジリン」１部を水７１．５部に溶解し、これ
をカルボキシメチルセルロースナトリウム９部、ポリア
クリル酸ナトリウム７部、ゼラチン４部、カオリン７部
及びクエン酸０．５部からなる各成分と均一に混練して
、比較例３の外用貼付剤を得た。Comparative Example 3 1 part of "terodiline hydrochloride" was dissolved in 71.5 parts of water, and this was dissolved in a solution consisting of 9 parts of sodium carboxymethylcellulose, 7 parts of sodium polyacrylate, 4 parts of gelatin, 7 parts of kaolin, and 0.5 part of citric acid. The external patch of Comparative Example 3 was obtained by uniformly kneading each component.
比較例４
「塩酸ベフノロール１１部を水７１．５部に溶解し、こ
れをカルボキシメチルセルロースナトリウム９部、ポリ
アクリル酸ナトリウム７部、ゼラチン４部、カオリン７
部及びクエン酸０．５部からなる各成分と均一に混練し
て、比較例４の外用貼付剤を得た。Comparative Example 4 ``11 parts of befunolol hydrochloride was dissolved in 71.5 parts of water, and this was dissolved in 9 parts of sodium carboxymethyl cellulose, 7 parts of sodium polyacrylate, 4 parts of gelatin, and 7 parts of kaolin.
A patch for external use of Comparative Example 4 was obtained by uniformly kneading each component consisting of 1 part and 0.5 parts of citric acid.
比較例５
［塩酸クロルプレナリン」１部を水７１．５部に溶解し
、これをカルボキシメチルセルロースナトリウム９部、
ポリアクリル酸ナトリウム７部、ゼラチン４部、カオリ
ン７部及びクエン酸０．５部からなる各成分と均一に混
練して、比較例５の外用貼付剤を得た。Comparative Example 5 1 part of [chlorprenaline hydrochloride] was dissolved in 71.5 parts of water, and this was dissolved in 9 parts of sodium carboxymethylcellulose,
The external patch of Comparative Example 5 was obtained by uniformly kneading each component consisting of 7 parts of sodium polyacrylate, 4 parts of gelatin, 7 parts of kaolin, and 0.5 part of citric acid.
比較例６
「ロキソブロフェンナトリウム」１部を水７１．５部に
溶解し、これをカルボキシメチルセルロースナトリウム
９部、ポリアクリル酸ナトリウム７部、ゼラチン４部、
カオリン７部及び酒石酸０．５部からなる各成分と均一
に混練して、比較例６の外用貼付剤を得た。Comparative Example 6 1 part of "loxobrofen sodium" was dissolved in 71.5 parts of water, and this was dissolved in 9 parts of sodium carboxymethyl cellulose, 7 parts of sodium polyacrylate, 4 parts of gelatin,
The external patch of Comparative Example 6 was obtained by uniformly kneading each component consisting of 7 parts of kaolin and 0.5 parts of tartaric acid.
比較例７
「臭化水素酸エプタゾシン」１部を水７１．５部に溶解
し、これをカルボキシメチルセルロースナトリウム９部
、ポリアクリル酸ナトリウム７部、ゼラチン４部、カオ
リン７部及びクエン酸０．５部からなる各成分と均一に
混練して、比較例７の外用貼付剤を得た。Comparative Example 7 1 part of "eptazocine hydrobromide" was dissolved in 71.5 parts of water, and this was mixed with 9 parts of sodium carboxymethyl cellulose, 7 parts of sodium polyacrylate, 4 parts of gelatin, 7 parts of kaolin, and 0.5 parts of citric acid. A topical patch of Comparative Example 7 was obtained by uniformly kneading each component consisting of 1.
く性能評価試験〉
試験例１ （比較試験）
実施例１〜７及び比較例１〜７の外用貼付剤を用いて、
薬剤の皮膚透過性をインヒドロ試験により評価した。こ
の試験には図に示す吸収セルを用いた。Performance Evaluation Test> Test Example 1 (Comparative Test) Using the external patches of Examples 1 to 7 and Comparative Examples 1 to 7,
The skin permeability of the drug was evaluated by the inhydro test. The absorption cell shown in the figure was used for this test.
固定具１にラット腹部皮膚を挟み、固定具２に試験すべ
き外用貼付剤を貼付してこの外用貼付剤を固定具１のラ
ット腹部皮膚に当接した。The abdominal skin of the rat was held between Fixtures 1, the external patch to be tested was applied to Fixture 2, and this external patch was brought into contact with the rat abdominal skin of Fixture 1.
又、容器３には空気か入らないようにタイロード液５，
１８ｒｎＩを充填した。吸収セルを３７℃のインキュベ
ータ中に置き、攪拌子４てタイロード液５を攪拌しなが
ら、１〜７時間の各時間にタイロード液５を０．５ｍｌ
づつ採取し、このなかの薬剤濃度を測定することにより
試験すべき外用貼付剤中の薬剤（被験薬剤）のラット腹
部皮膚に対する透過速度を求めた。結果を第１表に示す
。Also, put Tyrode's liquid 5, so that no air enters the container 3.
18rnI was loaded. Place the absorption cell in an incubator at 37°C, and while stirring Tyrode's solution 5 with a stirrer 4, add 0.5 ml of Tyrode's solution 5 for each hour from 1 to 7 hours.
The permeation rate of the drug (test drug) in the external patch to be tested through the rat abdominal skin was determined by measuring the concentration of the drug in the sample. The results are shown in Table 1.
第１表 薬剤の透過速度の比較試験結果第１表より、本
発明の水性基剤を用いたことにより薬剤の吸収速度が明
らかに増加したことが分かる。Table 1 Comparative Test Results of Drug Permeation Rate From Table 1, it can be seen that the use of the aqueous base of the present invention clearly increased the drug absorption rate.
試験例２ （ｐＨによる影り
実施例１の外用貼付剤において、クエン酸の添加量を変
えることによりｐ）ｌを５〜９に調整し、試験例１と同
様にして薬剤の透過速度を求めた。結果を第２表に示す
。Test Example 2 (Shadow by pH In the external patch of Example 1, p)l was adjusted to 5 to 9 by changing the amount of citric acid added, and the permeation rate of the drug was determined in the same manner as Test Example 1. Ta. The results are shown in Table 2.
第２表 薬剤の透過速度に対するｐＨの影響第２表から
明らかなように、ｐＨか低い酸性領域において薬剤の透
過速度か増加した。Table 2 Effect of pH on drug permeation rate As is clear from Table 2, drug permeation rate increased in the low acidic pH range.
（発明の効果）
上述の如く、本発明の外用貼付側用水性基剤は、脂肪酸
及びその誘導体及び動植物性油脂からなる群から選ばれ
た少なくとも１種と、多価アルコールと、水とからなる
ため、従来の外用貼付剤用基剤に比へて外用貼付剤に配
合された薬剤の皮膚に対する透過速度か向上した。(Effects of the Invention) As described above, the aqueous base for external application of the present invention comprises at least one selected from the group consisting of fatty acids and their derivatives, animal and vegetable oils, polyhydric alcohols, and water. Therefore, the permeation rate of the drug compounded into the external patch through the skin was improved compared to the conventional base for the external patch.
又、本発明の外用貼付剤は、鎮痛薬、抗アレルギー薬、
脳循環代謝薬、β−遮断薬、ホルモン剤、排尿異常改善
薬及び非ステロイド鎮痛消炎薬からなる群から選ばれた
少なくとも１種の薬剤と、本発明の外用貼付側用水性基
剤とからなるため、薬剤の徐放化に役立ち、副作用が少
なく安全で且つ薬剤を皮膚から徐々に持続的に効率良く
吸収させることかできる。In addition, the external patch of the present invention can be used as an analgesic, an antiallergic drug,
It consists of at least one drug selected from the group consisting of cerebral circulation metabolic drugs, β-blockers, hormonal drugs, urinary abnormality improving drugs, and non-steroidal analgesic and anti-inflammatory drugs, and the aqueous base for external application of the present invention. Therefore, it is useful for sustained drug release, is safe with few side effects, and allows the drug to be absorbed gradually and continuously through the skin efficiently.
図は、外用貼付剤に配合された薬剤の皮膚透過性を評価
するために使用する吸収セルの概略構成図である。
図中、
１．２・−固定具 ３ 容器 ４−攪拌子５−タイ
ロード液The figure is a schematic diagram of an absorption cell used to evaluate the skin permeability of a drug contained in an external patch. In the figure: 1.2 - Fixture 3 Container 4 - Stirrer 5 - Tyrode's liquid
Claims (15)
群から選ばれた少なくとも１種と、多価アルコールと、
水とからなることを特徴とする外用貼付剤用水性基剤。(1) at least one selected from the group consisting of fatty acids and their derivatives and animal and vegetable oils and polyhydric alcohols,
An aqueous base for an external patch, characterized in that it consists of water.
０のモノカルボン酸又はそのエステル又はそのアルカリ
金属塩であることを特徴とする請求項１記載の外用貼付
剤用水性基剤。(2) Fatty acids and derivatives thereof have 5 to 3 carbon atoms.
2. The aqueous base for an external patch according to claim 1, wherein the aqueous base is a monocarboxylic acid or an ester thereof, or an alkali metal salt thereof.
バキ油、パーシック油、ハッカ油、ゴマ油、ダイズ油、
ミンク油、綿実油、トウモロコシ油、サフラワー油、ヤ
シ油、ユーカリ油及びヒマシ油からなる群から選ばれた
少なくとも１種からなることを特徴とする請求項１記載
の外用貼付剤用水性基剤。(3) The animal and vegetable oils include almond oil, olive oil, camellia oil, persic oil, peppermint oil, sesame oil, soybean oil,
2. The aqueous base for an external patch according to claim 1, comprising at least one selected from the group consisting of mink oil, cottonseed oil, corn oil, safflower oil, coconut oil, eucalyptus oil, and castor oil.
コール、オクタンジオール、ブタンジオール、ポリエチ
レングリコール及びＤ−ソルビットからなる群から選ば
れた少なくとも２種からなることを特徴とする請求項１
記載の外用貼付剤用水性基剤。(4) Claim 1 characterized in that the polyhydric alcohol consists of at least two types selected from the group consisting of glycerin, propylene glycol, octanediol, butanediol, polyethylene glycol, and D-sorbitol.
Aqueous base for external patch as described.
断薬、ホルモン剤、排尿異常改善薬及び非ステロイド鎮
痛消炎薬からなる群から選ばれた少なくとも１種の薬剤
と、請求項１記載の外用貼付剤用水性基剤とからなるこ
とを特徴とする外用貼付剤。(5) at least one drug selected from the group consisting of analgesics, antiallergic drugs, cerebral circulation metabolic drugs, β-blockers, hormonal drugs, urinary abnormality improving drugs, and nonsteroidal analgesic and antiinflammatory drugs, and Claim 1 An external patch comprising the aqueous base for an external patch as described above.
５記載の外用貼付剤。(6) The external patch according to claim 5, wherein the drug is an oil-soluble drug.
５記載の外用貼付剤。(7) The external patch according to claim 5, wherein the drug is a water-soluble drug.
らなることを特徴とする請求項５記載の外用貼付剤。(8) The external patch according to claim 5, wherein the drug is a combination of an oil-soluble drug and a water-soluble drug.
ェンタニール及びモルヒネ塩類からなる群から選ばれた
少なくとも１種からなることを特徴とする請求項５記載
の外用貼付剤。(9) The external patch according to claim 5, wherein the analgesic is at least one selected from the group consisting of eptazocine hydrobromide, fentanyl citrate, and morphine salts.
ブジラスト及びトラニラストからなる群から選ばれた少
なくとも１種からなることを特徴とする請求項５記載の
外用貼付剤。(10) The external patch according to claim 5, wherein the antiallergic drug comprises at least one selected from the group consisting of chlorprenaline hydrochloride, ibudilast, and tranilast.
ン及び塩酸インデロキサジンからなる群から選ばれた少
なくとも１種からなることを特徴とする請求項５記載の
外用貼付剤。(11) The external patch according to claim 5, wherein the cerebral circulation metabolic drug is at least one selected from the group consisting of idebenone, biphemeran hydrochloride, and inderoxazine hydrochloride.
オロール及びピンドロールからなる群から選ばれた少な
くとも１種からなることを特徴とする請求項５記載の外
用貼付剤。(12) The external patch according to claim 5, wherein the β-blocker is at least one selected from the group consisting of befunolol hydrochloride, carteolol hydrochloride, and pindolol.
プロピオン酸エストラジオール及びプロゲステロンから
なる群から選ばれた少なくとも１種からなることを特徴
とする請求項５記載の外用貼付剤。(13) The hormone agent is testosterone propionate,
6. The external patch according to claim 5, comprising at least one member selected from the group consisting of estradiol propionate and progesterone.
テロジリン及び塩酸プロピペリンからなる群から選ばれ
た少なくとも１種からなることを特徴とする請求項５記
載の外用貼付剤。(14) The external patch according to claim 5, wherein the urinary abnormality improving drug comprises at least one selected from the group consisting of oxybutynin hydrochloride, terodiline hydrochloride, and propiperine hydrochloride.
ン、ケトプロフェン、ロキソプロフェンナトリウム及び
ケトロラックトロメタミンからなる群から選ばれた少な
くとも１種からなることを特徴とする請求項５記載の外
用貼付剤。(15) The external patch according to claim 5, wherein the non-steroidal analgesic and anti-inflammatory drug is at least one selected from the group consisting of flurbiprofen, ketoprofen, loxoprofen sodium, and ketorolac tromethamine.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP21838490A JP3243564B2 (en) | 1990-08-20 | 1990-08-20 | External patch |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP21838490A JP3243564B2 (en) | 1990-08-20 | 1990-08-20 | External patch |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH0499719A true JPH0499719A (en) | 1992-03-31 |
| JP3243564B2 JP3243564B2 (en) | 2002-01-07 |
Family
ID=16719061
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP21838490A Expired - Lifetime JP3243564B2 (en) | 1990-08-20 | 1990-08-20 | External patch |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP3243564B2 (en) |
Cited By (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1993023025A1 (en) * | 1992-05-13 | 1993-11-25 | Alza Corporation | Transdermal administration of oxybutynin |
| WO1994009777A1 (en) * | 1992-10-30 | 1994-05-11 | Syntex (U.S.A.) Inc. | Transdermal delivery of ketorolac |
| WO1996014069A1 (en) * | 1994-11-04 | 1996-05-17 | Sekisui Kagaku Kogyo Kabushiki Kaisha | Percutaneously absorbable patch |
| WO1996015793A1 (en) * | 1994-11-17 | 1996-05-30 | Toray Industries, Inc. | Percutaneously absorbable preparation |
| WO1997028793A1 (en) * | 1996-02-07 | 1997-08-14 | Lead Chemical Co., Ltd. | External preparation containing tranilast and process for producing the same |
| EP0748629A4 (en) * | 1994-03-11 | 1997-08-20 | Sekisui Chemical Co Ltd | Percutaneously absorbable plaster comprising acid-addition salt of morphine |
| WO1997042952A1 (en) * | 1996-05-13 | 1997-11-20 | Hisamitsu Pharmaceutical Co., Inc. | Percutaneous tape preparation containing fentanyl |
| WO1998008966A1 (en) | 1996-08-26 | 1998-03-05 | Sankyo Company, Limited | Loxoprofen-containing preparation for external use |
| US5807568A (en) * | 1994-12-27 | 1998-09-15 | Mcneil-Ppc, Inc. | Enhanced delivery of topical compositions containing flurbiprofen |
| WO2001003657A1 (en) * | 1999-07-09 | 2001-01-18 | Birgit Neudecker | Topically applied idebenone-containing agent with protective and regenerative effect |
| WO2006121717A3 (en) * | 2005-05-09 | 2006-12-28 | Procter & Gamble | Skin care compositions containing idebenone |
| JP2007517836A (en) * | 2004-01-06 | 2007-07-05 | リポテック，エス．アー． | Use of idebenone in the preparation of topical depigmenting and similar compositions |
| JP2011037903A (en) * | 2010-11-26 | 2011-02-24 | Daiichi Sankyo Co Ltd | Antiinflammatory/analgesic composition for external use |
| JP5230596B2 (en) * | 2007-03-01 | 2013-07-10 | 学校法人日本大学 | Pharmaceutical composition for transdermal absorption |
| JP2015083563A (en) * | 2013-09-18 | 2015-04-30 | 第一三共ヘルスケア株式会社 | Loxoprofen-containing external liquid preparation for skin |
| JPWO2016103999A1 (en) * | 2014-12-26 | 2017-10-05 | ニチバン株式会社 | Packaging for patch and packaging method |
-
1990
- 1990-08-20 JP JP21838490A patent/JP3243564B2/en not_active Expired - Lifetime
Cited By (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5411740A (en) * | 1992-05-13 | 1995-05-02 | Alza Corporation | Transdermal administration of oxybutynin |
| US5500222A (en) * | 1992-05-13 | 1996-03-19 | Alza Corporation | Transdermal administration of oxybutynin |
| WO1993023025A1 (en) * | 1992-05-13 | 1993-11-25 | Alza Corporation | Transdermal administration of oxybutynin |
| WO1994009777A1 (en) * | 1992-10-30 | 1994-05-11 | Syntex (U.S.A.) Inc. | Transdermal delivery of ketorolac |
| EP0748629A4 (en) * | 1994-03-11 | 1997-08-20 | Sekisui Chemical Co Ltd | Percutaneously absorbable plaster comprising acid-addition salt of morphine |
| WO1996014069A1 (en) * | 1994-11-04 | 1996-05-17 | Sekisui Kagaku Kogyo Kabushiki Kaisha | Percutaneously absorbable patch |
| WO1996015793A1 (en) * | 1994-11-17 | 1996-05-30 | Toray Industries, Inc. | Percutaneously absorbable preparation |
| US5854281A (en) * | 1994-11-17 | 1998-12-29 | Toray Industries, Inc. | Preparation for percutaneous absorption |
| JP4024852B2 (en) * | 1994-11-17 | 2007-12-19 | 東レ株式会社 | "Transdermal absorption preparation" |
| US5807568A (en) * | 1994-12-27 | 1998-09-15 | Mcneil-Ppc, Inc. | Enhanced delivery of topical compositions containing flurbiprofen |
| WO1997028793A1 (en) * | 1996-02-07 | 1997-08-14 | Lead Chemical Co., Ltd. | External preparation containing tranilast and process for producing the same |
| CN1081030C (en) * | 1996-02-07 | 2002-03-20 | 立德化学株式会社 | External preparation containing tranilast and process for producing the same |
| WO1997042952A1 (en) * | 1996-05-13 | 1997-11-20 | Hisamitsu Pharmaceutical Co., Inc. | Percutaneous tape preparation containing fentanyl |
| WO1998008966A1 (en) | 1996-08-26 | 1998-03-05 | Sankyo Company, Limited | Loxoprofen-containing preparation for external use |
| US6248350B1 (en) | 1996-08-26 | 2001-06-19 | Lead Chemical Co., Ltd. | External formulation containing loxoprofen |
| JP2008074873A (en) * | 1996-08-26 | 2008-04-03 | Daiichi Sankyo Co Ltd | Hydrous external preparation containing sodium loxoprofen |
| WO2001003657A1 (en) * | 1999-07-09 | 2001-01-18 | Birgit Neudecker | Topically applied idebenone-containing agent with protective and regenerative effect |
| EP1449511A1 (en) * | 1999-07-09 | 2004-08-25 | Birgit Neudecker | Use of Idebenone for the preservation of compositions |
| US6756045B1 (en) | 1999-07-09 | 2004-06-29 | Birgit Neudecker | Topically applied idebenone-containing agent with protective and regenerative effect |
| JP2007517836A (en) * | 2004-01-06 | 2007-07-05 | リポテック，エス．アー． | Use of idebenone in the preparation of topical depigmenting and similar compositions |
| WO2006121717A3 (en) * | 2005-05-09 | 2006-12-28 | Procter & Gamble | Skin care compositions containing idebenone |
| JP5230596B2 (en) * | 2007-03-01 | 2013-07-10 | 学校法人日本大学 | Pharmaceutical composition for transdermal absorption |
| JP2011037903A (en) * | 2010-11-26 | 2011-02-24 | Daiichi Sankyo Co Ltd | Antiinflammatory/analgesic composition for external use |
| JP2015083563A (en) * | 2013-09-18 | 2015-04-30 | 第一三共ヘルスケア株式会社 | Loxoprofen-containing external liquid preparation for skin |
| JPWO2016103999A1 (en) * | 2014-12-26 | 2017-10-05 | ニチバン株式会社 | Packaging for patch and packaging method |
Also Published As
| Publication number | Publication date |
|---|---|
| JP3243564B2 (en) | 2002-01-07 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| DE69430917T2 (en) | 3-L-MENTHOXY-PROPANE-1, 2-DIOL AS SOLUTION AND EXTERNAL PREPARATION THAT CONTAINS THEM | |
| JPH0499719A (en) | Application agent for external use | |
| AU778889B2 (en) | Novel topical oestroprogestational compositions with systemic effect | |
| KR100449939B1 (en) | Tranilast-containing external agent and its production method | |
| US5837735A (en) | Antiinflammatory agent for external use | |
| KR19980703624A (en) | Pharmaceutical composition for subcutaneous administration | |
| AU2023201712A1 (en) | Gel compositions for transdermal delivery to maximize drug concentrations in the stratum corneum and serum and methods of use thereof | |
| JPH0420886B2 (en) | ||
| JPS645579B2 (en) | ||
| JPH1112177A (en) | Stable aspirin-containing preparation for external use | |
| US4263313A (en) | Topical pharmaceutical formulations, carrier compositions therefor, and preparation thereof | |
| JP2007531694A (en) | Topically applied pharmaceutical composition | |
| JPH04266821A (en) | Percutaneous absorption type treating agent for pollakisuria and incontinence of urine | |
| US4837025A (en) | Self-adhesive device for the percutaneous administration of an active ingredient | |
| PT1541137E (en) | Transdermal delivery system of gestodene | |
| WO2005102306A1 (en) | Anti-inflammatory analgesic adhesive patch | |
| JPH0764754B2 (en) | Transdermal absorption enhancer and external preparation for skin containing the same | |
| JPH04217925A (en) | New antipyretic, antiphlogistic and analgesic agent composition | |
| MXPA02001152A (en) | Transdermal delivery of lasofoxifene. | |
| BRPI0417530B1 (en) | Composition for transdermal release of hormones without the need for penetration enhancers, transdermal therapeutic system, and kit | |
| JPH10316560A (en) | Plaster | |
| JP2001048783A (en) | Percutaneously absorbable type therapeutic agent for pollakiuria and incontinence of urine | |
| JP5619363B2 (en) | Transdermal absorption enhancer, skin treatment preparation containing the same, and transdermal absorption preparation | |
| JP4388143B2 (en) | Antifungal persistent external preparation | |
| CA2244679C (en) | Tranilast-containing preparation for external application and method of producing the same |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20081026 Year of fee payment: 7 |
|
| FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20081026 Year of fee payment: 7 |
|
| FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20091026 Year of fee payment: 8 |
|
| FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20091026 Year of fee payment: 8 |
|
| FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20101026 Year of fee payment: 9 |
|
| EXPY | Cancellation because of completion of term |