JP2015500273A5 - - Google Patents
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- Publication number
- JP2015500273A5 JP2015500273A5 JP2014545381A JP2014545381A JP2015500273A5 JP 2015500273 A5 JP2015500273 A5 JP 2015500273A5 JP 2014545381 A JP2014545381 A JP 2014545381A JP 2014545381 A JP2014545381 A JP 2014545381A JP 2015500273 A5 JP2015500273 A5 JP 2015500273A5
- Authority
- JP
- Japan
- Prior art keywords
- dosage form
- sustained release
- solid pharmaceutical
- pharmaceutical dosage
- release solid
- 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
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- 238000013268 sustained release Methods 0.000 claims 71
- 239000012730 sustained-release form Substances 0.000 claims 71
- 239000002552 dosage form Substances 0.000 claims 58
- 239000007787 solid Substances 0.000 claims 50
- 239000000203 mixture Substances 0.000 claims 35
- 239000013543 active substance Substances 0.000 claims 22
- 239000011159 matrix material Substances 0.000 claims 22
- 238000009472 formulation Methods 0.000 claims 21
- 239000000014 opioid analgesic Substances 0.000 claims 10
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims 9
- -1 vegitramide Chemical compound 0.000 claims 9
- 238000000034 method Methods 0.000 claims 8
- 239000000463 material Substances 0.000 claims 7
- BQNSLJQRJAJITR-UHFFFAOYSA-N 1,1,2-trichloro-1,2-difluoroethane Chemical compound FC(Cl)C(F)(Cl)Cl BQNSLJQRJAJITR-UHFFFAOYSA-N 0.000 claims 6
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 6
- 229960003617 oxycodone hydrochloride Drugs 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- ZFSXKSSWYSZPGQ-UHFFFAOYSA-N (2-hydroxycyclopentyl)azanium;chloride Chemical group Cl.NC1CCCC1O ZFSXKSSWYSZPGQ-UHFFFAOYSA-N 0.000 claims 5
- 238000003801 milling Methods 0.000 claims 5
- 229960000858 naltrexone hydrochloride Drugs 0.000 claims 5
- 239000008188 pellet Substances 0.000 claims 5
- 229920001610 polycaprolactone Polymers 0.000 claims 5
- 238000005520 cutting process Methods 0.000 claims 4
- 239000012530 fluid Substances 0.000 claims 4
- 230000002496 gastric effect Effects 0.000 claims 4
- OROGSEYTTFOCAN-UHFFFAOYSA-N hydrocodone Natural products C1C(N(CCC234)C)C2C=CC(O)C3OC2=C4C1=CC=C2OC OROGSEYTTFOCAN-UHFFFAOYSA-N 0.000 claims 4
- 238000000338 in vitro Methods 0.000 claims 4
- BQJCRHHNABKAKU-KBQPJGBKSA-N morphine Chemical compound 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 4
- 239000003401 opiate antagonist Substances 0.000 claims 4
- PAPBSGBWRJIAAV-UHFFFAOYSA-N ε-Caprolactone Chemical compound O=C1CCCCCO1 PAPBSGBWRJIAAV-UHFFFAOYSA-N 0.000 claims 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 3
- BRUQQQPBMZOVGD-XFKAJCMBSA-N Oxycodone Chemical compound O=C([C@@H]1O2)CC[C@@]3(O)[C@H]4CC5=CC=C(OC)C2=C5[C@@]13CCN4C BRUQQQPBMZOVGD-XFKAJCMBSA-N 0.000 claims 3
- UQCNKQCJZOAFTQ-ISWURRPUSA-N Oxymorphone Chemical compound O([C@H]1C(CC[C@]23O)=O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O UQCNKQCJZOAFTQ-ISWURRPUSA-N 0.000 claims 3
- BCGJBQBWUGVESK-KCTCKCTRSA-N Oxymorphone hydrochloride Chemical compound Cl.O([C@H]1C(CC[C@]23O)=O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O BCGJBQBWUGVESK-KCTCKCTRSA-N 0.000 claims 3
- 239000012190 activator Substances 0.000 claims 3
- 238000001816 cooling Methods 0.000 claims 3
- XYYVYLMBEZUESM-UHFFFAOYSA-N dihydrocodeine Natural products C1C(N(CCC234)C)C2C=CC(=O)C3OC2=C4C1=CC=C2OC XYYVYLMBEZUESM-UHFFFAOYSA-N 0.000 claims 3
- 238000004090 dissolution Methods 0.000 claims 3
- WVLOADHCBXTIJK-YNHQPCIGSA-N hydromorphone Chemical compound O([C@H]1C(CC[C@H]23)=O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O WVLOADHCBXTIJK-YNHQPCIGSA-N 0.000 claims 3
- 229960001410 hydromorphone Drugs 0.000 claims 3
- 229960002085 oxycodone Drugs 0.000 claims 3
- 229960005118 oxymorphone Drugs 0.000 claims 3
- 229960005374 oxymorphone hydrochloride Drugs 0.000 claims 3
- 238000005453 pelletization Methods 0.000 claims 3
- 238000002360 preparation method Methods 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- WRRSFOZOETZUPG-FFHNEAJVSA-N (4r,4ar,7s,7ar,12bs)-9-methoxy-3-methyl-2,4,4a,7,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinoline-7-ol;hydrate Chemical compound O.C([C@H]1[C@H](N(CC[C@@]112)C)C3)=C[C@H](O)[C@@H]1OC1=C2C3=CC=C1OC WRRSFOZOETZUPG-FFHNEAJVSA-N 0.000 claims 2
- OKMWKBLSFKFYGZ-UHFFFAOYSA-N 1-behenoylglycerol Chemical group CCCCCCCCCCCCCCCCCCCCCC(=O)OCC(O)CO OKMWKBLSFKFYGZ-UHFFFAOYSA-N 0.000 claims 2
- DYUTXEVRMPFGTH-UHFFFAOYSA-N 4-(2,5-dimethylphenyl)-5-methyl-1,3-thiazol-2-amine Chemical compound S1C(N)=NC(C=2C(=CC=C(C)C=2)C)=C1C DYUTXEVRMPFGTH-UHFFFAOYSA-N 0.000 claims 2
- DJHGAFSJWGLOIV-UHFFFAOYSA-K Arsenate3- Chemical compound [O-][As]([O-])([O-])=O DJHGAFSJWGLOIV-UHFFFAOYSA-K 0.000 claims 2
- 229940000489 arsenate Drugs 0.000 claims 2
- 229960004126 codeine Drugs 0.000 claims 2
- OROGSEYTTFOCAN-DNJOTXNNSA-N codeine Natural products C([C@H]1[C@H](N(CC[C@@]112)C)C3)=C[C@H](O)[C@@H]1OC1=C2C3=CC=C1OC OROGSEYTTFOCAN-DNJOTXNNSA-N 0.000 claims 2
- 235000014113 dietary fatty acids Nutrition 0.000 claims 2
- 238000007907 direct compression Methods 0.000 claims 2
- 238000000605 extraction Methods 0.000 claims 2
- 229930195729 fatty acid Natural products 0.000 claims 2
- 239000000194 fatty acid Substances 0.000 claims 2
- 150000004665 fatty acids Chemical class 0.000 claims 2
- 229940049654 glyceryl behenate Drugs 0.000 claims 2
- 150000004677 hydrates Chemical class 0.000 claims 2
- 229930195733 hydrocarbon Natural products 0.000 claims 2
- 150000002430 hydrocarbons Chemical class 0.000 claims 2
- LLPOLZWFYMWNKH-CMKMFDCUSA-N hydrocodone Chemical compound C([C@H]1[C@H](N(CC[C@@]112)C)C3)CC(=O)[C@@H]1OC1=C2C3=CC=C1OC LLPOLZWFYMWNKH-CMKMFDCUSA-N 0.000 claims 2
- 229960000240 hydrocodone Drugs 0.000 claims 2
- 229960002738 hydromorphone hydrochloride Drugs 0.000 claims 2
- 239000004615 ingredient Substances 0.000 claims 2
- 229960005181 morphine Drugs 0.000 claims 2
- 239000007909 solid dosage form Substances 0.000 claims 2
- LLPOLZWFYMWNKH-UHFFFAOYSA-N trans-dihydrocodeinone Natural products C1C(N(CCC234)C)C2CCC(=O)C3OC2=C4C1=CC=C2OC LLPOLZWFYMWNKH-UHFFFAOYSA-N 0.000 claims 2
- UVITTYOJFDLOGI-UHFFFAOYSA-N (1,2,5-trimethyl-4-phenylpiperidin-4-yl) propanoate Chemical compound C=1C=CC=CC=1C1(OC(=O)CC)CC(C)N(C)CC1C UVITTYOJFDLOGI-UHFFFAOYSA-N 0.000 claims 1
- TVYLLZQTGLZFBW-ZBFHGGJFSA-N (R,R)-tramadol Chemical compound COC1=CC=CC([C@]2(O)[C@H](CCCC2)CN(C)C)=C1 TVYLLZQTGLZFBW-ZBFHGGJFSA-N 0.000 claims 1
- IYNWSQDZXMGGGI-NUEKZKHPSA-N 3-hydroxymorphinan Chemical compound C1CCC[C@H]2[C@H]3CC4=CC=C(O)C=C4[C@]21CCN3 IYNWSQDZXMGGGI-NUEKZKHPSA-N 0.000 claims 1
- USSIQXCVUWKGNF-UHFFFAOYSA-N 6-(dimethylamino)-4,4-diphenylheptan-3-one Chemical compound C=1C=CC=CC=1C(CC(C)N(C)C)(C(=O)CC)C1=CC=CC=C1 USSIQXCVUWKGNF-UHFFFAOYSA-N 0.000 claims 1
- FERIUCNNQQJTOY-UHFFFAOYSA-M Butyrate Chemical compound CCCC([O-])=O FERIUCNNQQJTOY-UHFFFAOYSA-M 0.000 claims 1
- FERIUCNNQQJTOY-UHFFFAOYSA-N Butyric acid Natural products CCCC(O)=O FERIUCNNQQJTOY-UHFFFAOYSA-N 0.000 claims 1
- 239000004215 Carbon black (E152) Substances 0.000 claims 1
- IJVCSMSMFSCRME-KBQPJGBKSA-N Dihydromorphine Chemical compound O([C@H]1[C@H](CC[C@H]23)O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O IJVCSMSMFSCRME-KBQPJGBKSA-N 0.000 claims 1
- OGDVEMNWJVYAJL-LEPYJNQMSA-N Ethyl morphine Chemical compound C([C@H]1[C@H](N(CC[C@@]112)C)C3)=C[C@H](O)[C@@H]1OC1=C2C3=CC=C1OCC OGDVEMNWJVYAJL-LEPYJNQMSA-N 0.000 claims 1
- OGDVEMNWJVYAJL-UHFFFAOYSA-N Ethylmorphine Natural products C1C(N(CCC234)C)C2C=CC(O)C3OC2=C4C1=CC=C2OCC OGDVEMNWJVYAJL-UHFFFAOYSA-N 0.000 claims 1
- GVGLGOZIDCSQPN-PVHGPHFFSA-N Heroin Chemical compound O([C@H]1[C@H](C=C[C@H]23)OC(C)=O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4OC(C)=O GVGLGOZIDCSQPN-PVHGPHFFSA-N 0.000 claims 1
- ALFGKMXHOUSVAD-UHFFFAOYSA-N Ketobemidone Chemical compound C=1C=CC(O)=CC=1C1(C(=O)CC)CCN(C)CC1 ALFGKMXHOUSVAD-UHFFFAOYSA-N 0.000 claims 1
- JAQUASYNZVUNQP-USXIJHARSA-N Levorphanol Chemical compound C1C2=CC=C(O)C=C2[C@]23CCN(C)[C@H]1[C@@H]2CCCC3 JAQUASYNZVUNQP-USXIJHARSA-N 0.000 claims 1
- XADCESSVHJOZHK-UHFFFAOYSA-N Meperidine Chemical compound C=1C=CC=CC=1C1(C(=O)OCC)CCN(C)CC1 XADCESSVHJOZHK-UHFFFAOYSA-N 0.000 claims 1
- IDBPHNDTYPBSNI-UHFFFAOYSA-N N-(1-(2-(4-Ethyl-5-oxo-2-tetrazolin-1-yl)ethyl)-4-(methoxymethyl)-4-piperidyl)propionanilide Chemical group C1CN(CCN2C(N(CC)N=N2)=O)CCC1(COC)N(C(=O)CC)C1=CC=CC=C1 IDBPHNDTYPBSNI-UHFFFAOYSA-N 0.000 claims 1
- WJBLNOPPDWQMCH-MBPVOVBZSA-N Nalmefene Chemical compound N1([C@@H]2CC3=CC=C(C=4O[C@@H]5[C@](C3=4)([C@]2(CCC5=C)O)CC1)O)CC1CC1 WJBLNOPPDWQMCH-MBPVOVBZSA-N 0.000 claims 1
- 239000008896 Opium Substances 0.000 claims 1
- 229960001391 alfentanil Drugs 0.000 claims 1
- LKYQLAWMNBFNJT-UHFFFAOYSA-N anileridine Chemical compound C1CC(C(=O)OCC)(C=2C=CC=CC=2)CCN1CCC1=CC=C(N)C=C1 LKYQLAWMNBFNJT-UHFFFAOYSA-N 0.000 claims 1
- 229960002512 anileridine Drugs 0.000 claims 1
- 230000003796 beauty Effects 0.000 claims 1
- RDJGWRFTDZZXSM-RNWLQCGYSA-N benzylmorphine Chemical compound O([C@@H]1[C@]23CCN([C@H](C4)[C@@H]3C=C[C@@H]1O)C)C1=C2C4=CC=C1OCC1=CC=CC=C1 RDJGWRFTDZZXSM-RNWLQCGYSA-N 0.000 claims 1
- RMRJXGBAOAMLHD-IHFGGWKQSA-N buprenorphine Chemical compound C([C@]12[C@H]3OC=4C(O)=CC=C(C2=4)C[C@@H]2[C@]11CC[C@]3([C@H](C1)[C@](C)(O)C(C)(C)C)OC)CN2CC1CC1 RMRJXGBAOAMLHD-IHFGGWKQSA-N 0.000 claims 1
- 229960001736 buprenorphine Drugs 0.000 claims 1
- IFKLAQQSCNILHL-QHAWAJNXSA-N butorphanol Chemical compound N1([C@@H]2CC3=CC=C(C=C3[C@@]3([C@]2(CCCC3)O)CC1)O)CC1CCC1 IFKLAQQSCNILHL-QHAWAJNXSA-N 0.000 claims 1
- 229960001113 butorphanol Drugs 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 238000005266 casting Methods 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 238000013270 controlled release Methods 0.000 claims 1
- INUNXTSAACVKJS-OAQYLSRUSA-N dextromoramide Chemical compound C([C@@H](C)C(C(=O)N1CCCC1)(C=1C=CC=CC=1)C=1C=CC=CC=1)N1CCOCC1 INUNXTSAACVKJS-OAQYLSRUSA-N 0.000 claims 1
- 229960003701 dextromoramide Drugs 0.000 claims 1
- 229960004193 dextropropoxyphene Drugs 0.000 claims 1
- XLMALTXPSGQGBX-GCJKJVERSA-N dextropropoxyphene Chemical compound C([C@](OC(=O)CC)([C@H](C)CN(C)C)C=1C=CC=CC=1)C1=CC=CC=C1 XLMALTXPSGQGBX-GCJKJVERSA-N 0.000 claims 1
- 229960003461 dezocine Drugs 0.000 claims 1
- VTMVHDZWSFQSQP-VBNZEHGJSA-N dezocine Chemical compound C1CCCC[C@H]2CC3=CC=C(O)C=C3[C@]1(C)[C@H]2N VTMVHDZWSFQSQP-VBNZEHGJSA-N 0.000 claims 1
- 229960002069 diamorphine Drugs 0.000 claims 1
- 229950001059 diampromide Drugs 0.000 claims 1
- RXTHKWVSXOIHJS-UHFFFAOYSA-N diampromide Chemical compound C=1C=CC=CC=1N(C(=O)CC)CC(C)N(C)CCC1=CC=CC=C1 RXTHKWVSXOIHJS-UHFFFAOYSA-N 0.000 claims 1
- 229960000920 dihydrocodeine Drugs 0.000 claims 1
- RBOXVHNMENFORY-DNJOTXNNSA-N dihydrocodeine Chemical compound C([C@H]1[C@H](N(CC[C@@]112)C)C3)C[C@H](O)[C@@H]1OC1=C2C3=CC=C1OC RBOXVHNMENFORY-DNJOTXNNSA-N 0.000 claims 1
- RHUWRJWFHUKVED-UHFFFAOYSA-N dimenoxadol Chemical compound C=1C=CC=CC=1C(C(=O)OCCN(C)C)(OCC)C1=CC=CC=C1 RHUWRJWFHUKVED-UHFFFAOYSA-N 0.000 claims 1
- 229950011187 dimenoxadol Drugs 0.000 claims 1
- CANBGVXYBPOLRR-UHFFFAOYSA-N dimethylthiambutene Chemical compound C=1C=CSC=1C(=CC(C)N(C)C)C1=CC=CS1 CANBGVXYBPOLRR-UHFFFAOYSA-N 0.000 claims 1
- 229950005563 dimethylthiambutene Drugs 0.000 claims 1
- SVDHSZFEQYXRDC-UHFFFAOYSA-N dipipanone Chemical compound C=1C=CC=CC=1C(C=1C=CC=CC=1)(C(=O)CC)CC(C)N1CCCCC1 SVDHSZFEQYXRDC-UHFFFAOYSA-N 0.000 claims 1
- 229960002500 dipipanone Drugs 0.000 claims 1
- 238000010828 elution Methods 0.000 claims 1
- MORSAEFGQPDBKM-UHFFFAOYSA-N ethylmethylthiambutene Chemical compound C=1C=CSC=1C(=CC(C)N(C)CC)C1=CC=CS1 MORSAEFGQPDBKM-UHFFFAOYSA-N 0.000 claims 1
- 229950006111 ethylmethylthiambutene Drugs 0.000 claims 1
- 229960004578 ethylmorphine Drugs 0.000 claims 1
- CAHCBJPUTCKATP-FAWZKKEFSA-N etorphine Chemical compound O([C@H]1[C@@]2(OC)C=C[C@@]34C[C@@H]2[C@](C)(O)CCC)C2=C5[C@]41CCN(C)[C@@H]3CC5=CC=C2O CAHCBJPUTCKATP-FAWZKKEFSA-N 0.000 claims 1
- 229950004155 etorphine Drugs 0.000 claims 1
- 238000001125 extrusion Methods 0.000 claims 1
- 150000002191 fatty alcohols Chemical class 0.000 claims 1
- 229960002428 fentanyl Drugs 0.000 claims 1
- PJMPHNIQZUBGLI-UHFFFAOYSA-N fentanyl Chemical compound C=1C=CC=CC=1N(C(=O)CC)C(CC1)CCN1CCC1=CC=CC=C1 PJMPHNIQZUBGLI-UHFFFAOYSA-N 0.000 claims 1
- 125000005908 glyceryl ester group Chemical group 0.000 claims 1
- 238000000227 grinding Methods 0.000 claims 1
- 238000001746 injection moulding Methods 0.000 claims 1
- 229910052500 inorganic mineral Inorganic materials 0.000 claims 1
- IFKPLJWIEQBPGG-UHFFFAOYSA-N isomethadone Chemical compound C=1C=CC=CC=1C(C(C)CN(C)C)(C(=O)CC)C1=CC=CC=C1 IFKPLJWIEQBPGG-UHFFFAOYSA-N 0.000 claims 1
- 229950009272 isomethadone Drugs 0.000 claims 1
- 229960003029 ketobemidone Drugs 0.000 claims 1
- 229960003406 levorphanol Drugs 0.000 claims 1
- JLICHNCFTLFZJN-HNNXBMFYSA-N meptazinol Chemical compound C=1C=CC(O)=CC=1[C@@]1(CC)CCCCN(C)C1 JLICHNCFTLFZJN-HNNXBMFYSA-N 0.000 claims 1
- 229960000365 meptazinol Drugs 0.000 claims 1
- YEOTYALSMRNXLJ-UHFFFAOYSA-N metazosin Chemical compound C1CN(C(=O)C(C)OC)CCN1C1=NC(N)=C(C=C(OC)C(OC)=C2)C2=N1 YEOTYALSMRNXLJ-UHFFFAOYSA-N 0.000 claims 1
- 229960001797 methadone Drugs 0.000 claims 1
- 235000010755 mineral Nutrition 0.000 claims 1
- 239000002480 mineral oil Substances 0.000 claims 1
- 229960005297 nalmefene Drugs 0.000 claims 1
- 229960004127 naloxone Drugs 0.000 claims 1
- UZHSEJADLWPNLE-GRGSLBFTSA-N naloxone Chemical compound O=C([C@@H]1O2)CC[C@@]3(O)[C@H]4CC5=CC=C(O)C2=C5[C@@]13CCN4CC=C UZHSEJADLWPNLE-GRGSLBFTSA-N 0.000 claims 1
- 229960003086 naltrexone Drugs 0.000 claims 1
- DQCKKXVULJGBQN-XFWGSAIBSA-N naltrexone Chemical compound N1([C@@H]2CC3=CC=C(C=4O[C@@H]5[C@](C3=4)([C@]2(CCC5=O)O)CC1)O)CC1CC1 DQCKKXVULJGBQN-XFWGSAIBSA-N 0.000 claims 1
- 229940061390 naltrexone hydrochloride 50 mg Drugs 0.000 claims 1
- 229960004300 nicomorphine Drugs 0.000 claims 1
- HNDXBGYRMHRUFN-CIVUWBIHSA-N nicomorphine Chemical compound O([C@H]1C=C[C@H]2[C@H]3CC=4C5=C(C(=CC=4)OC(=O)C=4C=NC=CC=4)O[C@@H]1[C@]52CCN3C)C(=O)C1=CC=CN=C1 HNDXBGYRMHRUFN-CIVUWBIHSA-N 0.000 claims 1
- 229950011519 norlevorphanol Drugs 0.000 claims 1
- 229960004013 normethadone Drugs 0.000 claims 1
- WCJFBSYALHQBSK-UHFFFAOYSA-N normethadone Chemical compound C=1C=CC=CC=1C(CCN(C)C)(C(=O)CC)C1=CC=CC=C1 WCJFBSYALHQBSK-UHFFFAOYSA-N 0.000 claims 1
- 229950007418 norpipanone Drugs 0.000 claims 1
- WCDSHELZWCOTMI-UHFFFAOYSA-N norpipanone Chemical compound C=1C=CC=CC=1C(C=1C=CC=CC=1)(C(=O)CC)CCN1CCCCC1 WCDSHELZWCOTMI-UHFFFAOYSA-N 0.000 claims 1
- 229960001027 opium Drugs 0.000 claims 1
- 229960000482 pethidine Drugs 0.000 claims 1
- LOXCOAXRHYDLOW-UHFFFAOYSA-N phenadoxone Chemical compound C=1C=CC=CC=1C(C=1C=CC=CC=1)(C(=O)CC)CC(C)N1CCOCC1 LOXCOAXRHYDLOW-UHFFFAOYSA-N 0.000 claims 1
- 229950004540 phenadoxone Drugs 0.000 claims 1
- 229960004315 phenoperidine Drugs 0.000 claims 1
- IPOPQVVNCFQFRK-UHFFFAOYSA-N phenoperidine Chemical compound C1CC(C(=O)OCC)(C=2C=CC=CC=2)CCN1CCC(O)C1=CC=CC=C1 IPOPQVVNCFQFRK-UHFFFAOYSA-N 0.000 claims 1
- OCYSGIYOVXAGKQ-FVGYRXGTSA-N phenylephrine hydrochloride Chemical compound [H+].[Cl-].CNC[C@H](O)C1=CC=CC(O)=C1 OCYSGIYOVXAGKQ-FVGYRXGTSA-N 0.000 claims 1
- 229950004345 properidine Drugs 0.000 claims 1
- XJKQCILVUHXVIQ-UHFFFAOYSA-N properidine Chemical compound C=1C=CC=CC=1C1(C(=O)OC(C)C)CCN(C)CC1 XJKQCILVUHXVIQ-UHFFFAOYSA-N 0.000 claims 1
- 229960004739 sufentanil Drugs 0.000 claims 1
- GGCSSNBKKAUURC-UHFFFAOYSA-N sufentanil Chemical compound C1CN(CCC=2SC=CC=2)CCC1(COC)N(C(=O)CC)C1=CC=CC=C1 GGCSSNBKKAUURC-UHFFFAOYSA-N 0.000 claims 1
- 229960004380 tramadol Drugs 0.000 claims 1
- TVYLLZQTGLZFBW-GOEBONIOSA-N tramadol Natural products COC1=CC=CC([C@@]2(O)[C@@H](CCCC2)CN(C)C)=C1 TVYLLZQTGLZFBW-GOEBONIOSA-N 0.000 claims 1
- 235000015112 vegetable and seed oil Nutrition 0.000 claims 1
- 239000008158 vegetable oil Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161569193P | 2011-12-09 | 2011-12-09 | |
| US61/569,193 | 2011-12-09 | ||
| PCT/IB2012/002681 WO2013084059A1 (en) | 2011-12-09 | 2012-12-07 | Pharmaceutical dosage forms comprising poly (epsilon- caprolactone) and polyethylene oxide |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015500273A JP2015500273A (ja) | 2015-01-05 |
| JP2015500273A5 true JP2015500273A5 (https=) | 2015-12-17 |
| JP6144274B2 JP6144274B2 (ja) | 2017-06-07 |
Family
ID=47522734
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014545381A Active JP6144274B2 (ja) | 2011-12-09 | 2012-12-07 | ポリ（イプシロン−カプロラクトン）およびポリエチレンオキシドを含む医薬剤形 |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US20150265536A1 (https=) |
| EP (1) | EP2787978B1 (https=) |
| JP (1) | JP6144274B2 (https=) |
| CN (2) | CN104010630A (https=) |
| AR (1) | AR089130A1 (https=) |
| AU (1) | AU2012327231B2 (https=) |
| CA (1) | CA2858868C (https=) |
| ES (1) | ES2603278T3 (https=) |
| TW (1) | TW201336529A (https=) |
| WO (1) | WO2013084059A1 (https=) |
Families Citing this family (50)
| Publication number | Priority date | Publication date | Assignee | Title |
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| DE10361596A1 (de) | 2003-12-24 | 2005-09-29 | Grünenthal GmbH | Verfahren zur Herstellung einer gegen Missbrauch gesicherten Darreichungsform |
| US20070048228A1 (en) | 2003-08-06 | 2007-03-01 | Elisabeth Arkenau-Maric | Abuse-proofed dosage form |
| DE10336400A1 (de) | 2003-08-06 | 2005-03-24 | Grünenthal GmbH | Gegen Missbrauch gesicherte Darreichungsform |
| DE102004032049A1 (de) | 2004-07-01 | 2006-01-19 | Grünenthal GmbH | Gegen Missbrauch gesicherte, orale Darreichungsform |
| DE102005005449A1 (de) | 2005-02-04 | 2006-08-10 | Grünenthal GmbH | Verfahren zur Herstellung einer gegen Missbrauch gesicherten Darreichungsform |
| US8821928B2 (en) | 2007-06-04 | 2014-09-02 | Egalet Ltd. | Controlled release pharmaceutical compositions for prolonged effect |
| KR101616246B1 (ko) | 2008-01-25 | 2016-05-02 | 그뤼넨탈 게엠베하 | 약제학적 투여형 |
| AU2009243681B2 (en) | 2008-05-09 | 2013-12-19 | Grunenthal Gmbh | Process for the preparation of an intermediate powder formulation and a final solid dosage form under usage of a spray congealing step |
| CA2751667C (en) | 2009-02-06 | 2016-12-13 | Egalet Ltd. | Immediate release composition resistant to abuse by intake of alcohol |
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| WO2011009602A1 (en) | 2009-07-22 | 2011-01-27 | Grünenthal GmbH | Hot-melt extruded controlled release dosage form |
| TWI473628B (zh) | 2009-07-22 | 2015-02-21 | 用於對氧化敏感之類鴉片藥劑之抗破壞劑型 | |
| WO2012028318A1 (en) | 2010-09-02 | 2012-03-08 | Grünenthal GmbH | Tamper resistant dosage form comprising an anionic polymer |
| CA2808219C (en) | 2010-09-02 | 2019-05-14 | Gruenenthal Gmbh | Tamper resistant dosage form comprising inorganic salt |
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| US20130225697A1 (en) | 2012-02-28 | 2013-08-29 | Grunenthal Gmbh | Tamper-resistant dosage form comprising pharmacologically active compound and anionic polymer |
| PL2838512T3 (pl) | 2012-04-18 | 2018-12-31 | Grünenthal GmbH | Farmaceutyczna postać dawkowania odporna na niewłaściwe użycie i odporna na uderzeniowe uwalnianie dawki |
| US10064945B2 (en) | 2012-05-11 | 2018-09-04 | Gruenenthal Gmbh | Thermoformed, tamper-resistant pharmaceutical dosage form containing zinc |
| AU2013285988A1 (en) | 2012-07-06 | 2015-02-12 | Egalet Ltd. | Abuse deterrent pharmaceutical compositions for controlled release |
| AU2014273227B2 (en) | 2013-05-29 | 2019-08-15 | Grunenthal Gmbh | Tamper-resistant dosage form containing one or more particles |
| JP6466417B2 (ja) | 2013-05-29 | 2019-02-06 | グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング | 二峰性放出プロファイルを有する改変防止（ｔａｍｐｅｒ−ｒｅｓｉｓｔａｎｔ）剤形 |
| JP6449871B2 (ja) | 2013-07-12 | 2019-01-09 | グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング | エチレン−酢酸ビニルポリマーを含有する改変防止剤形 |
| CA3042642A1 (en) | 2013-08-12 | 2015-02-19 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded immediate release abuse deterrent pill |
| EP3073994A1 (en) | 2013-11-26 | 2016-10-05 | Grünenthal GmbH | Preparation of a powdery pharmaceutical composition by means of cryo-milling |
| US10172797B2 (en) | 2013-12-17 | 2019-01-08 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded extended release abuse deterrent pill |
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| EP3142646A1 (en) | 2014-05-12 | 2017-03-22 | Grünenthal GmbH | Tamper resistant immediate release capsule formulation comprising tapentadol |
| EA201692388A1 (ru) | 2014-05-26 | 2017-05-31 | Грюненталь Гмбх | Лекарственная форма в виде множества частиц, защищенная от вызываемого этанолом сброса дозы |
| CA2955229C (en) | 2014-07-17 | 2020-03-10 | Pharmaceutical Manufacturing Research Services, Inc. | Immediate release abuse deterrent liquid fill dosage form |
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| WO2016064873A1 (en) | 2014-10-20 | 2016-04-28 | Pharmaceutical Manufacturing Research Services, Inc. | Extended release abuse deterrent liquid fill dosage form |
| EP3229785A2 (de) * | 2014-12-08 | 2017-10-18 | Develco Pharma Schweiz AG | Naloxon-monopräparat und mehrschichttablette |
| BR112017021475A2 (pt) | 2015-04-24 | 2018-07-10 | Gruenenthal Gmbh | forma de dosagem resistente à adulteração (tamper) com liberação imediata e resistência contra extração de solvente |
| WO2017042325A1 (en) | 2015-09-10 | 2017-03-16 | Grünenthal GmbH | Protecting oral overdose with abuse deterrent immediate release formulations |
| HK1258050A1 (zh) | 2015-10-23 | 2019-11-01 | Lyndra Therapeutics, Inc. | 用於治疗剂缓释的胃驻留系统及其使用方法 |
| EP3386488B1 (en) | 2015-12-08 | 2023-09-06 | Lyndra Therapeutics, Inc. | Geometric configurations for gastric residence systems |
| EP3181124A1 (en) * | 2015-12-16 | 2017-06-21 | Universität Basel | Abuse deterrent pharmaceutical dosage forms |
| AU2017268840B2 (en) | 2016-05-27 | 2022-02-10 | Nortiva Bio, Inc. | Materials architecture for gastric residence systems |
| US11576866B2 (en) | 2016-09-30 | 2023-02-14 | Lyndra Therapeutics, Inc. | Gastric residence systems for sustained delivery of adamantane-class drugs |
| US12023406B2 (en) | 2017-06-09 | 2024-07-02 | Lyndra Therapeutics, Inc. | Gastric residence systems with release rate-modulating films |
| AU2018390826B2 (en) | 2017-12-20 | 2024-09-12 | Purdue Pharma L.P. | Abuse deterrent morphine sulfate dosage forms |
| CA3166250A1 (en) | 2020-02-05 | 2021-08-12 | Gregory G. Plucinski | Drug products for intranasal administration and uses thereof |
| WO2023145869A1 (ja) * | 2022-01-31 | 2023-08-03 | 住友精化株式会社 | 製剤用組成物の製造方法及び製剤の製造方法 |
| WO2023145871A1 (ja) * | 2022-01-31 | 2023-08-03 | 住友精化株式会社 | 製剤用組成物の製造方法及び製剤の製造方法 |
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| FR2557459B1 (fr) * | 1984-01-02 | 1986-05-30 | Lhd Lab Hygiene Dietetique | Matrice inerte a base de polycaprolactone pour administration orale d'un medicament, et procede de preparation de la forme galenique comprenant cette matrice |
| FR2701152B1 (fr) | 1993-02-03 | 1995-03-10 | Digipress Sa | Procédé de fabrication d'un disque maître pour la réalisation d'une matrice de pressage notamment de disques optiques, matrice de pressage obtenue par ce procédé et disque optique obtenu à partir de cette matrice de pressage. |
| CA2270362C (en) * | 1996-11-05 | 2011-12-13 | Novamont S.P.A. | Biodegradable polymeric compositions comprising starch and a thermoplastic polymer |
| EP2092936B1 (en) * | 2000-02-08 | 2013-03-20 | Euro-Celtique S.A. | Tamper-resistant oral opioid agonist formulations |
| US20020007013A1 (en) * | 2000-05-16 | 2002-01-17 | Cohen Gordon Mark | Compositions containing elastomeric ethylene or (meth)acrylic ester copolymers |
| JP2006516969A (ja) * | 2003-01-23 | 2006-07-13 | アモレパシフィック コーポレーション | 徐放性製剤及びその製造方法 |
| WO2004082615A2 (en) * | 2003-03-14 | 2004-09-30 | Nirmal Mulye | A process for preparing sustained release tablets |
| US20060165790A1 (en) * | 2003-06-27 | 2006-07-27 | Malcolm Walden | Multiparticulates |
| DE102005005446A1 (de) * | 2005-02-04 | 2006-08-10 | Grünenthal GmbH | Bruchfeste Darreichungsformen mit retardierter Freisetzung |
| US20070014846A1 (en) * | 2003-10-10 | 2007-01-18 | Lifecycle Pharma A/S | Pharmaceutical compositions comprising fenofibrate and atorvastatin |
| HRP20090363T1 (hr) * | 2004-02-23 | 2009-08-31 | Euro-Celtique S.A. | Transdermalni injektor opioida rezistentan na zlouporabu |
| TWI365880B (en) | 2004-03-30 | 2012-06-11 | Euro Celtique Sa | Process for preparing oxycodone hydrochloride having less than 25 ppm 14-hydroxycodeinone and oxycodone hydrochloride composition,pharmaceutical dosage form,sustained release oeal dosage form and pharmaceutically acceptable package having less than 25 pp |
| AU2006244214A1 (en) * | 2005-05-10 | 2006-11-16 | Novartis Ag | Modified release famciclovir pharmaceutical compositions |
| BRPI0619806A2 (pt) * | 2005-12-13 | 2011-10-18 | Biodelivery Sciences Int Inc | dispositivo para fornecimento de fármacos transmucosal resistente ao abuso |
| SA07280459B1 (ar) * | 2006-08-25 | 2011-07-20 | بيورديو فارما إل. بي. | أشكال جرعة صيدلانية للتناول عن طريق الفم مقاومة للعبث تشتمل على مسكن شبه أفيوني |
| BRPI0913724B8 (pt) * | 2008-09-18 | 2021-05-25 | Purdue Pharma Lp | formas farmacêuticas de liberação prolongada compreendendo naltrexona e poli (e-caprolactona) e seu preparo |
-
2012
- 2012-12-07 AU AU2012327231A patent/AU2012327231B2/en active Active
- 2012-12-07 TW TW101146199A patent/TW201336529A/zh unknown
- 2012-12-07 CN CN201280059890.2A patent/CN104010630A/zh active Pending
- 2012-12-07 JP JP2014545381A patent/JP6144274B2/ja active Active
- 2012-12-07 ES ES12813099.4T patent/ES2603278T3/es active Active
- 2012-12-07 US US14/363,004 patent/US20150265536A1/en not_active Abandoned
- 2012-12-07 CN CN201710933357.9A patent/CN107854434A/zh active Pending
- 2012-12-07 CA CA2858868A patent/CA2858868C/en active Active
- 2012-12-07 EP EP12813099.4A patent/EP2787978B1/en active Active
- 2012-12-07 WO PCT/IB2012/002681 patent/WO2013084059A1/en not_active Ceased
- 2012-12-10 AR ARP120104624A patent/AR089130A1/es not_active Application Discontinuation
-
2019
- 2019-10-08 US US16/596,136 patent/US20200170954A1/en not_active Abandoned
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