JPH11505264A - オキシブチニンを含んで成る剤形 - Google Patents
オキシブチニンを含んで成る剤形Info
- Publication number
- JPH11505264A JPH11505264A JP8535714A JP53571496A JPH11505264A JP H11505264 A JPH11505264 A JP H11505264A JP 8535714 A JP8535714 A JP 8535714A JP 53571496 A JP53571496 A JP 53571496A JP H11505264 A JPH11505264 A JP H11505264A
- Authority
- JP
- Japan
- Prior art keywords
- oxybutynin
- molecular weight
- layer
- osmagent
- permeable
- 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.)
- Withdrawn
Links
- XIQVNETUBQGFHX-UHFFFAOYSA-N Ditropan Chemical compound C=1C=CC=CC=1C(O)(C(=O)OCC#CCN(CC)CC)C1CCCCC1 XIQVNETUBQGFHX-UHFFFAOYSA-N 0.000 title claims abstract description 116
- 229960005434 oxybutynin Drugs 0.000 title claims abstract description 113
- 239000002552 dosage form Substances 0.000 title description 33
- 239000000203 mixture Substances 0.000 claims abstract description 70
- 230000001225 therapeutic effect Effects 0.000 claims description 27
- 239000012530 fluid Substances 0.000 claims description 19
- 239000000314 lubricant Substances 0.000 claims description 18
- 229920000233 poly(alkylene oxides) Polymers 0.000 claims description 18
- 150000003839 salts Chemical class 0.000 claims description 18
- 239000003814 drug Substances 0.000 claims description 14
- 229940079593 drug Drugs 0.000 claims description 13
- -1 Pamoate Chemical compound 0.000 claims description 11
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 11
- 239000003963 antioxidant agent Substances 0.000 claims description 8
- 230000003078 antioxidant effect Effects 0.000 claims description 8
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims description 8
- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims description 6
- 239000002253 acid Substances 0.000 claims description 6
- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims description 6
- 239000008112 carboxymethyl-cellulose Substances 0.000 claims description 6
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 6
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims description 5
- GHOKWGTUZJEAQD-ZETCQYMHSA-N (D)-(+)-Pantothenic acid Chemical compound OCC(C)(C)[C@@H](O)C(=O)NCCC(O)=O GHOKWGTUZJEAQD-ZETCQYMHSA-N 0.000 claims description 3
- FEWJPZIEWOKRBE-UHFFFAOYSA-M 3-carboxy-2,3-dihydroxypropanoate Chemical compound OC(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-M 0.000 claims description 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims description 3
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 claims description 3
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims description 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 3
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims description 3
- JVTAAEKCZFNVCJ-UHFFFAOYSA-M Lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 claims description 3
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims description 3
- 229910002651 NO3 Inorganic materials 0.000 claims description 3
- NHNBFGGVMKEFGY-UHFFFAOYSA-N Nitrate Chemical compound [O-][N+]([O-])=O NHNBFGGVMKEFGY-UHFFFAOYSA-N 0.000 claims description 3
- 229910019142 PO4 Inorganic materials 0.000 claims description 3
- 229920002253 Tannate Polymers 0.000 claims description 3
- SXDBWCPKPHAZSM-UHFFFAOYSA-M bromate Inorganic materials [O-]Br(=O)=O SXDBWCPKPHAZSM-UHFFFAOYSA-M 0.000 claims description 3
- SXDBWCPKPHAZSM-UHFFFAOYSA-N bromic acid Chemical compound OBr(=O)=O SXDBWCPKPHAZSM-UHFFFAOYSA-N 0.000 claims description 3
- 229940009662 edetate Drugs 0.000 claims description 3
- CCIVGXIOQKPBKL-UHFFFAOYSA-M ethanesulfonate Chemical compound CCS([O-])(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-M 0.000 claims description 3
- 229960001731 gluceptate Drugs 0.000 claims description 3
- KWMLJOLKUYYJFJ-VFUOTHLCSA-N glucoheptonic acid Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)[C@@H](O)C(O)=O KWMLJOLKUYYJFJ-VFUOTHLCSA-N 0.000 claims description 3
- 229930195712 glutamate Natural products 0.000 claims description 3
- 229940049920 malate Drugs 0.000 claims description 3
- BJEPYKJPYRNKOW-UHFFFAOYSA-N malic acid Chemical compound OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims description 3
- LRMHVVPPGGOAJQ-UHFFFAOYSA-N methyl nitrate Chemical compound CO[N+]([O-])=O LRMHVVPPGGOAJQ-UHFFFAOYSA-N 0.000 claims description 3
- 229940014662 pantothenate Drugs 0.000 claims description 3
- 235000019161 pantothenic acid Nutrition 0.000 claims description 3
- 239000011713 pantothenic acid Substances 0.000 claims description 3
- 239000010452 phosphate Substances 0.000 claims description 3
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 3
- 239000003380 propellant Substances 0.000 claims description 3
- YGSDEFSMJLZEOE-UHFFFAOYSA-M salicylate Chemical compound OC1=CC=CC=C1C([O-])=O YGSDEFSMJLZEOE-UHFFFAOYSA-M 0.000 claims description 3
- 229960001860 salicylate Drugs 0.000 claims description 3
- RGHNJXZEOKUKBD-SQOUGZDYSA-N D-gluconic acid Chemical class OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O RGHNJXZEOKUKBD-SQOUGZDYSA-N 0.000 claims description 2
- 229920002675 Polyoxyl Polymers 0.000 claims description 2
- 229920013821 hydroxy alkyl cellulose Polymers 0.000 claims description 2
- 150000003467 sulfuric acid derivatives Chemical class 0.000 claims description 2
- 150000003892 tartrate salts Chemical class 0.000 claims description 2
- 239000003513 alkali Substances 0.000 claims 1
- 239000002981 blocking agent Substances 0.000 claims 1
- 125000004106 butoxy group Chemical group [*]OC([H])([H])C([H])([H])C(C([H])([H])[H])([H])[H] 0.000 claims 1
- 238000011282 treatment Methods 0.000 abstract description 11
- 238000000034 method Methods 0.000 description 29
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 26
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 20
- 239000000017 hydrogel Substances 0.000 description 18
- 210000003932 urinary bladder Anatomy 0.000 description 18
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 14
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 14
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 14
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 14
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 14
- 235000019359 magnesium stearate Nutrition 0.000 description 13
- 206010021639 Incontinence Diseases 0.000 description 12
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 12
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 11
- 238000002156 mixing Methods 0.000 description 11
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 10
- 230000003204 osmotic effect Effects 0.000 description 10
- 239000011780 sodium chloride Substances 0.000 description 10
- 239000007787 solid Substances 0.000 description 9
- 239000002904 solvent Substances 0.000 description 9
- 239000008187 granular material Substances 0.000 description 8
- UQSXHKLRYXJYBZ-UHFFFAOYSA-N iron oxide Inorganic materials [Fe]=O UQSXHKLRYXJYBZ-UHFFFAOYSA-N 0.000 description 7
- 238000004519 manufacturing process Methods 0.000 description 7
- NDLPOXTZKUMGOV-UHFFFAOYSA-N oxo(oxoferriooxy)iron hydrate Chemical compound O.O=[Fe]O[Fe]=O NDLPOXTZKUMGOV-UHFFFAOYSA-N 0.000 description 7
- 239000000725 suspension Substances 0.000 description 7
- 239000004322 Butylated hydroxytoluene Substances 0.000 description 6
- NLZUEZXRPGMBCV-UHFFFAOYSA-N Butylhydroxytoluene Chemical compound CC1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1 NLZUEZXRPGMBCV-UHFFFAOYSA-N 0.000 description 6
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 6
- 235000006708 antioxidants Nutrition 0.000 description 6
- 235000010354 butylated hydroxytoluene Nutrition 0.000 description 6
- 229940095259 butylated hydroxytoluene Drugs 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
- 235000014113 dietary fatty acids Nutrition 0.000 description 6
- 239000000194 fatty acid Substances 0.000 description 6
- 229930195729 fatty acid Natural products 0.000 description 6
- 150000004665 fatty acids Chemical class 0.000 description 6
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 6
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 6
- 239000003826 tablet Substances 0.000 description 6
- TWRXJAOTZQYOKJ-UHFFFAOYSA-L Magnesium chloride Chemical compound [Mg+2].[Cl-].[Cl-] TWRXJAOTZQYOKJ-UHFFFAOYSA-L 0.000 description 5
- 206010046543 Urinary incontinence Diseases 0.000 description 5
- 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 5
- 125000002723 alicyclic group Chemical group 0.000 description 5
- 229920002678 cellulose Polymers 0.000 description 5
- 239000001913 cellulose Substances 0.000 description 5
- 238000000576 coating method Methods 0.000 description 5
- 230000000694 effects Effects 0.000 description 5
- 238000005469 granulation Methods 0.000 description 5
- 230000003179 granulation Effects 0.000 description 5
- 239000000463 material Substances 0.000 description 5
- 210000003205 muscle Anatomy 0.000 description 5
- 229920000642 polymer Polymers 0.000 description 5
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 5
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 5
- 210000003708 urethra Anatomy 0.000 description 5
- 210000002700 urine Anatomy 0.000 description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 4
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 4
- CSNNHWWHGAXBCP-UHFFFAOYSA-L Magnesium sulfate Chemical compound [Mg+2].[O-][S+2]([O-])([O-])[O-] CSNNHWWHGAXBCP-UHFFFAOYSA-L 0.000 description 4
- 239000002202 Polyethylene glycol Substances 0.000 description 4
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 description 4
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 4
- 229920002301 cellulose acetate Polymers 0.000 description 4
- 239000011248 coating agent Substances 0.000 description 4
- 239000006184 cosolvent Substances 0.000 description 4
- 235000019441 ethanol Nutrition 0.000 description 4
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical class CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 description 4
- 229920001223 polyethylene glycol Polymers 0.000 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 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 description 3
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 3
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 3
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 3
- 235000021355 Stearic acid Nutrition 0.000 description 3
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 3
- 159000000032 aromatic acids Chemical class 0.000 description 3
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 3
- 230000008602 contraction Effects 0.000 description 3
- 238000013270 controlled release Methods 0.000 description 3
- 239000011928 denatured alcohol Substances 0.000 description 3
- SWXVUIWOUIDPGS-UHFFFAOYSA-N diacetone alcohol Chemical compound CC(=O)CC(C)(C)O SWXVUIWOUIDPGS-UHFFFAOYSA-N 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 239000012633 leachable Substances 0.000 description 3
- 230000027939 micturition Effects 0.000 description 3
- 238000003801 milling Methods 0.000 description 3
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Chemical class CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 3
- 239000000600 sorbitol Substances 0.000 description 3
- 238000005507 spraying Methods 0.000 description 3
- 239000008117 stearic acid Chemical class 0.000 description 3
- KAKVFSYQVNHFBS-UHFFFAOYSA-N (5-hydroxycyclopenten-1-yl)-phenylmethanone Chemical compound OC1CCC=C1C(=O)C1=CC=CC=C1 KAKVFSYQVNHFBS-UHFFFAOYSA-N 0.000 description 2
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Chemical class CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 description 2
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 description 2
- QPFMBZIOSGYJDE-UHFFFAOYSA-N 1,1,2,2-tetrachloroethane Chemical compound ClC(Cl)C(Cl)Cl QPFMBZIOSGYJDE-UHFFFAOYSA-N 0.000 description 2
- WSLDOOZREJYCGB-UHFFFAOYSA-N 1,2-Dichloroethane Chemical compound ClCCCl WSLDOOZREJYCGB-UHFFFAOYSA-N 0.000 description 2
- HZAXFHJVJLSVMW-UHFFFAOYSA-N 2-Aminoethan-1-ol Chemical compound NCCO HZAXFHJVJLSVMW-UHFFFAOYSA-N 0.000 description 2
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Chemical class CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 description 2
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Chemical class CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 description 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
- SQUHHTBVTRBESD-UHFFFAOYSA-N Hexa-Ac-myo-Inositol Natural products CC(=O)OC1C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C1OC(C)=O SQUHHTBVTRBESD-UHFFFAOYSA-N 0.000 description 2
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 description 2
- 208000000693 Neurogenic Urinary Bladder Diseases 0.000 description 2
- 206010029279 Neurogenic bladder Diseases 0.000 description 2
- 239000005642 Oleic acid Chemical class 0.000 description 2
- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Chemical class CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 description 2
- 235000021314 Palmitic acid Nutrition 0.000 description 2
- ZTHYODDOHIVTJV-UHFFFAOYSA-N Propyl gallate Chemical compound CCCOC(=O)C1=CC(O)=C(O)C(O)=C1 ZTHYODDOHIVTJV-UHFFFAOYSA-N 0.000 description 2
- MUPFEKGTMRGPLJ-RMMQSMQOSA-N Raffinose Natural products O(C[C@H]1[C@@H](O)[C@H](O)[C@@H](O)[C@@H](O[C@@]2(CO)[C@H](O)[C@@H](O)[C@@H](CO)O2)O1)[C@@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1 MUPFEKGTMRGPLJ-RMMQSMQOSA-N 0.000 description 2
- 206010066218 Stress Urinary Incontinence Diseases 0.000 description 2
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 2
- 229930006000 Sucrose Natural products 0.000 description 2
- 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 2
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 2
- MUPFEKGTMRGPLJ-UHFFFAOYSA-N UNPD196149 Natural products OC1C(O)C(CO)OC1(CO)OC1C(O)C(O)C(O)C(COC2C(C(O)C(O)C(CO)O2)O)O1 MUPFEKGTMRGPLJ-UHFFFAOYSA-N 0.000 description 2
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 description 2
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- 238000000498 ball milling Methods 0.000 description 2
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- DKPFZGUDAPQIHT-UHFFFAOYSA-N butyl acetate Chemical compound CCCCOC(C)=O DKPFZGUDAPQIHT-UHFFFAOYSA-N 0.000 description 2
- CZBZUDVBLSSABA-UHFFFAOYSA-N butylated hydroxyanisole Chemical compound COC1=CC=C(O)C(C(C)(C)C)=C1.COC1=CC=C(O)C=C1C(C)(C)C CZBZUDVBLSSABA-UHFFFAOYSA-N 0.000 description 2
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 description 2
- 239000008116 calcium stearate Substances 0.000 description 2
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- 239000004202 carbamide Substances 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- SDWYUQHONRZPMW-UHFFFAOYSA-L disodium;octanedioate Chemical compound [Na+].[Na+].[O-]C(=O)CCCCCCC([O-])=O SDWYUQHONRZPMW-UHFFFAOYSA-L 0.000 description 2
- 238000012377 drug delivery Methods 0.000 description 2
- VFPFQHQNJCMNBZ-UHFFFAOYSA-N ethyl gallate Chemical compound CCOC(=O)C1=CC(O)=C(O)C(O)=C1 VFPFQHQNJCMNBZ-UHFFFAOYSA-N 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 239000003049 inorganic solvent Substances 0.000 description 2
- CDAISMWEOUEBRE-GPIVLXJGSA-N inositol Chemical compound O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O)[C@@H]1O CDAISMWEOUEBRE-GPIVLXJGSA-N 0.000 description 2
- 229960000367 inositol Drugs 0.000 description 2
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Chemical class CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 description 2
- 239000007942 layered tablet Substances 0.000 description 2
- 238000002386 leaching Methods 0.000 description 2
- 229910001629 magnesium chloride Inorganic materials 0.000 description 2
- 229910052943 magnesium sulfate Inorganic materials 0.000 description 2
- 235000019341 magnesium sulphate Nutrition 0.000 description 2
- AXLHVTKGDPVANO-UHFFFAOYSA-N methyl 2-amino-3-[(2-methylpropan-2-yl)oxycarbonylamino]propanoate Chemical compound COC(=O)C(N)CNC(=O)OC(C)(C)C AXLHVTKGDPVANO-UHFFFAOYSA-N 0.000 description 2
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 description 2
- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Chemical class CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 description 2
- 206010029446 nocturia Diseases 0.000 description 2
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical class CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 2
- 235000021313 oleic acid Nutrition 0.000 description 2
- 239000003960 organic solvent Substances 0.000 description 2
- XNLICIUVMPYHGG-UHFFFAOYSA-N pentan-2-one Chemical compound CCCC(C)=O XNLICIUVMPYHGG-UHFFFAOYSA-N 0.000 description 2
- 239000008196 pharmacological composition Substances 0.000 description 2
- 238000011458 pharmacological treatment Methods 0.000 description 2
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- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
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Landscapes
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.オキシブチニン1ng乃至450mg、分子量200,000乃至300 ,000のポリアルキレンオキシド40mg乃至250mg、分子量9,000 乃至150,000のヒドロキシプロピルアルキルセルロース1mg乃至25m g及び滑剤0.01mg乃至5mgを含んで成る治療用組成物。 2.オキシブチニンが酢酸塩、二酒石酸塩、クエン酸塩、エデト酸塩、エジシ レート、エストレート、エシレート、フマル酸塩、グルセプテート、グルコン酸 塩、グルタミン酸塩、臭酸塩、塩酸塩、乳酸塩、リンゴ酸塩、マレイン酸塩、マ ンデル酸塩、メシレート、メチル硝酸塩、ムチン酸塩、ナプシレート、硝酸塩、 パモエート、パントテン酸塩、リン酸塩、サリチル酸塩、ステアリン酸塩、琥珀 酸塩、硫酸塩、タンニン酸塩及び酒石酸塩より成る群から選ばれる治療上許容で きる塩である、請求の範囲第1項に記載の治療用組成物。 3.オキシブチニン1ng乃至450mg、分子量200,000乃至300 ,000のポリアルキレンオキシド40mg乃至450mg、分子量9,000 乃至150,000のヒドロキシプロピルアルキルセルロース1mg乃至25m g及び滑剤0.01mg乃至5mgを含んで成る治療用層を、分子量3,000 ,000乃至8,000,000のポリアルキレンオキシド40mg乃至250 mg、オスマジェント10mg乃至50mg、分子量9,000乃至225,0 00のヒドロキシプロピルアルキルセルロース0.1mg乃至20mg、酸化防 止剤0.0ng乃至1.5mg及び滑剤0.2mg乃至7mgを含んで成るヒド ロゲル層と接触して含んで成る二層化錠剤。 4.オキシブチニン1ng乃至450mg、分子量200,000のポリアル キレンオキシド40mg乃至250mg、分子量9,000乃至150,000 のヒドロキシプロピルアルキルセルロース1mg乃至25mg及び滑剤0.01 mg乃至5mgを含んで成る治療用層を含む二層化錠剤にして、該層が分子量1 0,000乃至6,000,000のアルカリ・カルボキシメチルセルロース4 0mg乃至250mg、オスマジェント10mg乃至50mg、分子量9,00 0乃至225,000のヒドロキシプロピルアルキルセルロース0.1mg乃至 20mg、分子量7,500乃至175,000のヒドロキシアルキルセルロー ス0.1mg乃至30mg、酸化防止剤0.0ng乃至1.5mg及び滑剤0. 2mg乃至7mgを含んで成る推進層と接触している、上記の二層化錠剤。 5.オキシブチニン1ng乃至450mg、分子量200,000乃至300 ,000のポリアルキレンオキシド40mg乃至250mg、分子量9,000 乃至250,000のヒドロキシプロピルアルキルセルロース1mg乃至25m g及びオスマジェント1mg乃至50mgを含んで成る層と、オスモポリマー4 0mg乃至250mg及びオスマジェント10mg乃至50mgを含んで成る接 触層;それら層を包囲している、流体の通過に対しては透過性であるが、オキシ ブチニンの通過に対しては不透過性である半透過性の壁と、該半透過性壁を貫通 する、オキシブチニンを患者に時間の経過に対して制御された速度で投与するた めの出口;を含んで成る、オキシブチニンを必要としている患者にオキシブチニ ンを投与するためのデリバリーディバイス。 6.オキシブチニン1ng乃至450mg、分子量200,000乃至300 ,000のポリアルキレンオキシド40mg乃至250mg、分子量9,000 乃至250,000のヒドロキシプロピルアルキルセルロース1mg乃至25m g、オスマジェント1mg乃至50mgを含んで成る薬物層と、分子量10,0 00乃至6,000,000のカルボキシメチルセルロース40mg乃至250 mg及びオスマジェント10mg乃至50mgを含んで成る接触置換層;それら 層を包囲している、流体の通過に対しては透過性であるが、オキシブチニンの通 過に対しては不透過性である半透過性の壁と、該半透過性壁を貫通する、オキシ ブチニンを患者に時間の経過に対して制御された速度で投与するための出口;を 含んで成る、オキシブチニンを必要としている患者にオキシブチニンを投与する ためのデリバリーディバイス。 7.オキシブチニン1ng乃至450mg、分子量200,000乃至300 ,000のポリアルキレンオキシド40mg乃至250mg、分子量9,000 乃至250,000のヒドロキシプロピルアルキルセルロース1mg乃至25m g、オスマジェント1mg乃至50mgを含んで成る薬物層と、分子量3,00 0,000乃至8,000,000のポリアルキレンオキシド40mg乃至25 0 mg及びオスマジェント10mg乃至50mgを含んで成る収縮性置換層;その 層を包囲している、流体の通過に対しては透過性であるが、オキシブチニンの通 過に対しては不透過性である半透過性の壁と、該半透過性壁を貫通する、オキシ ブチニンを患者に時間の経過に対して制御された速度で投与するための出口;を 含んで成る、オキシブチニンを必要としている患者にオキシブチニンを投与する ためのデリバリーディバイス。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US08/445,849 US5674895A (en) | 1995-05-22 | 1995-05-22 | Dosage form comprising oxybutynin |
US08/445,849 | 1995-05-22 | ||
PCT/US1996/006639 WO1996037202A1 (en) | 1995-05-22 | 1996-05-08 | Dosage form comprising oxybutynin |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2007122013A Division JP2007197462A (ja) | 1995-05-22 | 2007-05-07 | オキシブチニンを含んで成る剤形 |
Publications (1)
Publication Number | Publication Date |
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JPH11505264A true JPH11505264A (ja) | 1999-05-18 |
Family
ID=23770440
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP8535714A Withdrawn JPH11505264A (ja) | 1995-05-22 | 1996-05-08 | オキシブチニンを含んで成る剤形 |
JP2007122013A Pending JP2007197462A (ja) | 1995-05-22 | 2007-05-07 | オキシブチニンを含んで成る剤形 |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2007122013A Pending JP2007197462A (ja) | 1995-05-22 | 2007-05-07 | オキシブチニンを含んで成る剤形 |
Country Status (14)
Country | Link |
---|---|
US (2) | US5674895A (ja) |
JP (2) | JPH11505264A (ja) |
KR (1) | KR100404954B1 (ja) |
AU (2) | AU695194B2 (ja) |
BE (1) | BE1009462A3 (ja) |
CA (2) | CA2218714C (ja) |
CH (1) | CH690955A5 (ja) |
DE (1) | DE19681389B3 (ja) |
FR (1) | FR2734483B1 (ja) |
GB (1) | GB2318055B (ja) |
IT (1) | IT1285345B1 (ja) |
NL (1) | NL1003185C2 (ja) |
NZ (1) | NZ307116A (ja) |
WO (1) | WO1996037202A1 (ja) |
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JP2003527404A (ja) * | 2000-03-21 | 2003-09-16 | エンハンス ファーマシューティカルズ,インコーポレイティド | 女性の尿失禁を治療するための用具および方法 |
US7943176B2 (en) | 2001-10-09 | 2011-05-17 | Apogepha Arzneimittel Gmbh | Oral dosage form for propiverine or its pharmaceutically acceptable salts with an extended release of the active ingredient |
Also Published As
Publication number | Publication date |
---|---|
FR2734483A1 (fr) | 1996-11-29 |
AU695194B2 (en) | 1998-08-06 |
NZ307116A (en) | 1999-03-29 |
CH690955A5 (de) | 2001-03-15 |
CA2218714C (en) | 2005-08-23 |
FR2734483B1 (fr) | 1997-07-11 |
AU5639296A (en) | 1996-12-11 |
MX9709013A (es) | 1998-03-31 |
IT1285345B1 (it) | 1998-06-03 |
DE19681389T1 (de) | 1998-04-23 |
WO1996037202A1 (en) | 1996-11-28 |
GB2318055B (en) | 1999-07-21 |
ITTO960427A0 (it) | 1996-05-21 |
NL1003185C2 (nl) | 1996-12-03 |
CA2218714A1 (en) | 1996-11-28 |
BE1009462A3 (fr) | 1997-04-01 |
GB2318055A (en) | 1998-04-15 |
CA2510391A1 (en) | 1996-11-28 |
GB9723081D0 (en) | 1998-01-07 |
JP2007197462A (ja) | 2007-08-09 |
NL1003185A1 (nl) | 1996-11-25 |
AU9052298A (en) | 1999-01-14 |
AU718849B2 (en) | 2000-04-20 |
KR100404954B1 (ko) | 2004-04-28 |
US5840754A (en) | 1998-11-24 |
US5674895A (en) | 1997-10-07 |
DE19681389B3 (de) | 2015-12-10 |
KR19990021879A (ko) | 1999-03-25 |
ITTO960427A1 (it) | 1997-11-21 |
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