JP2006524261A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2006524261A5 JP2006524261A5 JP2006513318A JP2006513318A JP2006524261A5 JP 2006524261 A5 JP2006524261 A5 JP 2006524261A5 JP 2006513318 A JP2006513318 A JP 2006513318A JP 2006513318 A JP2006513318 A JP 2006513318A JP 2006524261 A5 JP2006524261 A5 JP 2006524261A5
- Authority
- JP
- Japan
- Prior art keywords
- particles
- core
- dosage form
- sheath
- opioid antagonist
- 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
- 239000002245 particle Substances 0.000 claims 39
- -1 nalolphine Chemical compound 0.000 claims 28
- 239000000203 mixture Substances 0.000 claims 19
- 239000003795 chemical substances by application Substances 0.000 claims 18
- 230000002411 adverse Effects 0.000 claims 15
- 239000003401 opiate antagonist Substances 0.000 claims 15
- 239000002552 dosage form Substances 0.000 claims 10
- 230000002209 hydrophobic effect Effects 0.000 claims 9
- 239000006186 oral dosage form Substances 0.000 claims 9
- OROGSEYTTFOCAN-DNJOTXNNSA-N codeine Chemical compound 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 8
- XYYVYLMBEZUESM-UHFFFAOYSA-N dihydrocodeine Natural products C1C(N(CCC234)C)C2C=CC(=O)C3OC2=C4C1=CC=C2OC XYYVYLMBEZUESM-UHFFFAOYSA-N 0.000 claims 8
- OROGSEYTTFOCAN-UHFFFAOYSA-N hydrocodone Natural products C1C(N(CCC234)C)C2C=CC(O)C3OC2=C4C1=CC=C2OC OROGSEYTTFOCAN-UHFFFAOYSA-N 0.000 claims 8
- 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 8
- 150000003839 salts Chemical class 0.000 claims 8
- 239000003402 opiate agonist Substances 0.000 claims 7
- 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 4
- 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 4
- DEXMFYZAHXMZNM-UHFFFAOYSA-N Narceine Chemical compound OC(=O)C1=C(OC)C(OC)=CC=C1C(=O)CC1=C(CCN(C)C)C=C(OCO2)C2=C1OC DEXMFYZAHXMZNM-UHFFFAOYSA-N 0.000 claims 4
- 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 4
- 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 4
- 239000013543 active substance Substances 0.000 claims 4
- 229960004126 codeine Drugs 0.000 claims 4
- 229960000920 dihydrocodeine Drugs 0.000 claims 4
- 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 4
- 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 4
- 229960000240 hydrocodone Drugs 0.000 claims 4
- 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 4
- 229960001410 hydromorphone Drugs 0.000 claims 4
- 238000004519 manufacturing process Methods 0.000 claims 4
- 239000000463 material Substances 0.000 claims 4
- 229960005181 morphine Drugs 0.000 claims 4
- 229960000805 nalbuphine Drugs 0.000 claims 4
- NETZHAKZCGBWSS-CEDHKZHLSA-N nalbuphine Chemical compound C([C@]12[C@H]3OC=4C(O)=CC=C(C2=4)C[C@@H]2[C@]1(O)CC[C@@H]3O)CN2CC1CCC1 NETZHAKZCGBWSS-CEDHKZHLSA-N 0.000 claims 4
- 229960005297 nalmefene Drugs 0.000 claims 4
- 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 4
- 229960004127 naloxone Drugs 0.000 claims 4
- 229960003086 naltrexone Drugs 0.000 claims 4
- 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 4
- 229960002085 oxycodone Drugs 0.000 claims 4
- 229960005118 oxymorphone Drugs 0.000 claims 4
- 239000000126 substance Substances 0.000 claims 4
- LLPOLZWFYMWNKH-UHFFFAOYSA-N trans-dihydrocodeinone Natural products C1C(N(CCC234)C)C2CCC(=O)C3OC2=C4C1=CC=C2OC LLPOLZWFYMWNKH-UHFFFAOYSA-N 0.000 claims 4
- 239000002775 capsule Substances 0.000 claims 3
- XBRXTUGRUXGBPX-DLBZAZTESA-N cyclazosin Chemical compound N=1C(N)=C2C=C(OC)C(OC)=CC2=NC=1N([C@@H]1CCCC[C@@H]11)CCN1C(=O)C1=CC=CO1 XBRXTUGRUXGBPX-DLBZAZTESA-N 0.000 claims 3
- 235000014113 dietary fatty acids Nutrition 0.000 claims 3
- 229930195729 fatty acid Natural products 0.000 claims 3
- 239000000194 fatty acid Substances 0.000 claims 3
- 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 2
- 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 2
- 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 2
- 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 2
- OGDVEMNWJVYAJL-UHFFFAOYSA-N Ethylmorphine Natural products C1C(N(CCC234)C)C2C=CC(O)C3OC2=C4C1=CC=C2OCC OGDVEMNWJVYAJL-UHFFFAOYSA-N 0.000 claims 2
- 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 2
- ALFGKMXHOUSVAD-UHFFFAOYSA-N Ketobemidone Chemical compound C=1C=CC(O)=CC=1C1(C(=O)CC)CCN(C)CC1 ALFGKMXHOUSVAD-UHFFFAOYSA-N 0.000 claims 2
- XADCESSVHJOZHK-UHFFFAOYSA-N Meperidine Chemical compound C=1C=CC=CC=1C1(C(=O)OCC)CCN(C)CC1 XADCESSVHJOZHK-UHFFFAOYSA-N 0.000 claims 2
- 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 2
- 239000008896 Opium Substances 0.000 claims 2
- 229960001391 alfentanil Drugs 0.000 claims 2
- 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 2
- 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 2
- 229960001736 buprenorphine Drugs 0.000 claims 2
- 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 2
- 229960001113 butorphanol Drugs 0.000 claims 2
- 229920001577 copolymer Polymers 0.000 claims 2
- LNNWVNGFPYWNQE-GMIGKAJZSA-N desomorphine Chemical compound C1C2=CC=C(O)C3=C2[C@]24CCN(C)[C@H]1[C@@H]2CCC[C@@H]4O3 LNNWVNGFPYWNQE-GMIGKAJZSA-N 0.000 claims 2
- 229950003851 desomorphine Drugs 0.000 claims 2
- 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 2
- 229960003701 dextromoramide Drugs 0.000 claims 2
- 229960004193 dextropropoxyphene Drugs 0.000 claims 2
- 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 2
- 229960003461 dezocine Drugs 0.000 claims 2
- 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 2
- 229960002069 diamorphine Drugs 0.000 claims 2
- 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 2
- 229950011187 dimenoxadol Drugs 0.000 claims 2
- CANBGVXYBPOLRR-UHFFFAOYSA-N dimethylthiambutene Chemical compound C=1C=CSC=1C(=CC(C)N(C)C)C1=CC=CS1 CANBGVXYBPOLRR-UHFFFAOYSA-N 0.000 claims 2
- 229950005563 dimethylthiambutene Drugs 0.000 claims 2
- 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 2
- 229960002500 dipipanone Drugs 0.000 claims 2
- ZOWQTJXNFTWSCS-IAQYHMDHSA-N eptazocine Chemical compound C1N(C)CC[C@@]2(C)C3=CC(O)=CC=C3C[C@@H]1C2 ZOWQTJXNFTWSCS-IAQYHMDHSA-N 0.000 claims 2
- 229950010920 eptazocine Drugs 0.000 claims 2
- 229960004578 ethylmorphine Drugs 0.000 claims 2
- 229960002428 fentanyl Drugs 0.000 claims 2
- 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 2
- 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 2
- 229950009272 isomethadone Drugs 0.000 claims 2
- 229960003029 ketobemidone Drugs 0.000 claims 2
- IMYHGORQCPYVBZ-NLFFAJNJSA-N lofentanil Chemical compound CCC(=O)N([C@@]1([C@@H](CN(CCC=2C=CC=CC=2)CC1)C)C(=O)OC)C1=CC=CC=C1 IMYHGORQCPYVBZ-NLFFAJNJSA-N 0.000 claims 2
- 229950010274 lofentanil Drugs 0.000 claims 2
- YGSVZRIZCHZUHB-COLVAYQJSA-N metazocine Chemical compound C1C2=CC=C(O)C=C2[C@]2(C)CCN(C)[C@@]1([H])[C@@H]2C YGSVZRIZCHZUHB-COLVAYQJSA-N 0.000 claims 2
- 229950009131 metazocine Drugs 0.000 claims 2
- 229960001797 methadone Drugs 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 229960004300 nicomorphine Drugs 0.000 claims 2
- 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 2
- 229960004013 normethadone Drugs 0.000 claims 2
- 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 2
- 229950007418 norpipanone Drugs 0.000 claims 2
- 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 2
- 229960001027 opium Drugs 0.000 claims 2
- VOKSWYLNZZRQPF-GDIGMMSISA-N pentazocine Chemical compound C1C2=CC=C(O)C=C2[C@@]2(C)[C@@H](C)[C@@H]1N(CC=C(C)C)CC2 VOKSWYLNZZRQPF-GDIGMMSISA-N 0.000 claims 2
- 229960005301 pentazocine Drugs 0.000 claims 2
- 229960000482 pethidine Drugs 0.000 claims 2
- 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 2
- 229950004345 properidine Drugs 0.000 claims 2
- 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 2
- 229960004739 sufentanil Drugs 0.000 claims 2
- 229960004380 tramadol Drugs 0.000 claims 2
- 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 2
- SMZOUWXMTYCWNB-UHFFFAOYSA-N 2-(2-methoxy-5-methylphenyl)ethanamine Chemical compound COC1=CC=C(C)C=C1CCN SMZOUWXMTYCWNB-UHFFFAOYSA-N 0.000 claims 1
- UZFMOKQJFYMBGY-UHFFFAOYSA-N 4-hydroxy-TEMPO Chemical compound CC1(C)CC(O)CC(C)(C)N1[O] UZFMOKQJFYMBGY-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
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 239000004215 Carbon black (E152) Substances 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
- CERQOIWHTDAKMF-UHFFFAOYSA-N Methacrylic acid Chemical compound CC(=C)C(O)=O CERQOIWHTDAKMF-UHFFFAOYSA-N 0.000 claims 1
- ONBWJWYUHXVEJS-ZTYRTETDSA-N Normorphine Chemical compound C([C@@H](NCC1)[C@@H]2C=C[C@@H]3O)C4=CC=C(O)C5=C4[C@@]21[C@H]3O5 ONBWJWYUHXVEJS-ZTYRTETDSA-N 0.000 claims 1
- 229920013820 alkyl cellulose Polymers 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
- 238000013270 controlled release Methods 0.000 claims 1
- WDEFBBTXULIOBB-WBVHZDCISA-N dextilidine Chemical compound C=1C=CC=CC=1[C@@]1(C(=O)OCC)CCC=C[C@H]1N(C)C WDEFBBTXULIOBB-WBVHZDCISA-N 0.000 claims 1
- QIRAYNIFEOXSPW-UHFFFAOYSA-N dimepheptanol Chemical compound C=1C=CC=CC=1C(CC(C)N(C)C)(C(O)CC)C1=CC=CC=C1 QIRAYNIFEOXSPW-UHFFFAOYSA-N 0.000 claims 1
- 150000004665 fatty acids Chemical class 0.000 claims 1
- 150000002191 fatty alcohols Chemical class 0.000 claims 1
- 229930195733 hydrocarbon Natural products 0.000 claims 1
- 150000002430 hydrocarbons Chemical class 0.000 claims 1
- 229920001477 hydrophilic polymer Polymers 0.000 claims 1
- 229920001600 hydrophobic polymer Polymers 0.000 claims 1
- 238000001727 in vivo Methods 0.000 claims 1
- RCYBMSQOSGJZLO-BGWNEDDSSA-N levophenacylmorphan Chemical compound C([C@]12CCCC[C@H]1[C@H]1CC3=CC=C(C=C32)O)CN1CC(=O)C1=CC=CC=C1 RCYBMSQOSGJZLO-BGWNEDDSSA-N 0.000 claims 1
- 229960003406 levorphanol Drugs 0.000 claims 1
- 229960000365 meptazinol 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
- 229950006134 normorphine Drugs 0.000 claims 1
- 230000002093 peripheral effect Effects 0.000 claims 1
- CFBQYWXPZVQQTN-QPTUXGOLSA-N phenomorphan Chemical compound C([C@]12CCCC[C@H]1[C@H]1CC3=CC=C(C=C32)O)CN1CCC1=CC=CC=C1 CFBQYWXPZVQQTN-QPTUXGOLSA-N 0.000 claims 1
- 229950011496 phenomorphan 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
- 229920000642 polymer Polymers 0.000 claims 1
- 229960001402 tilidine Drugs 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US46429503P | 2003-04-21 | 2003-04-21 | |
| US60/464,295 | 2003-04-21 | ||
| PCT/US2004/012776 WO2004093819A2 (en) | 2003-04-21 | 2004-04-21 | Tamper resistant dosage form comprising co-extruded, adverse agent particles and process of making same |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011084443A Division JP2011157384A (ja) | 2003-04-21 | 2011-04-06 | 同時押出逆作用剤粒子を含有する改変防止剤形およびその製造工程 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2006524261A JP2006524261A (ja) | 2006-10-26 |
| JP2006524261A5 true JP2006524261A5 (enExample) | 2007-06-07 |
| JP5501553B2 JP5501553B2 (ja) | 2014-05-21 |
Family
ID=33310869
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006513318A Expired - Lifetime JP5501553B2 (ja) | 2003-04-21 | 2004-04-21 | 同時押出逆作用剤粒子を含有する改変防止剤形およびその製造工程 |
| JP2011084443A Withdrawn JP2011157384A (ja) | 2003-04-21 | 2011-04-06 | 同時押出逆作用剤粒子を含有する改変防止剤形およびその製造工程 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011084443A Withdrawn JP2011157384A (ja) | 2003-04-21 | 2011-04-06 | 同時押出逆作用剤粒子を含有する改変防止剤形およびその製造工程 |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US9579286B2 (enExample) |
| EP (1) | EP1615625A4 (enExample) |
| JP (2) | JP5501553B2 (enExample) |
| AU (1) | AU2004232370B2 (enExample) |
| CA (1) | CA2519556C (enExample) |
| MX (1) | MXPA05011071A (enExample) |
| WO (1) | WO2004093819A2 (enExample) |
Families Citing this family (62)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10179130B2 (en) | 1999-10-29 | 2019-01-15 | Purdue Pharma L.P. | Controlled release hydrocodone formulations |
| JP4806507B2 (ja) | 1999-10-29 | 2011-11-02 | ユーロ−セルティーク エス．エイ． | 制御放出ヒドロコドン処方 |
| CN101653411A (zh) | 2000-10-30 | 2010-02-24 | 欧罗赛铁克股份有限公司 | 控释氢可酮制剂 |
| WO2003024430A1 (en) | 2001-09-21 | 2003-03-27 | Egalet A/S | Morphine polymer release system |
| EP2957281A1 (en) | 2001-09-21 | 2015-12-23 | Egalet Ltd. | Polymer release system |
| US7776314B2 (en) | 2002-06-17 | 2010-08-17 | Grunenthal Gmbh | Abuse-proofed dosage system |
| US8877241B2 (en) | 2003-03-26 | 2014-11-04 | Egalet Ltd. | Morphine controlled release system |
| US9579286B2 (en) | 2003-04-21 | 2017-02-28 | Purdue Pharma L.P. | Tamper resistant dosage form comprising co-extruded, sequestered adverse agent particles and process of making same |
| DE10361596A1 (de) | 2003-12-24 | 2005-09-29 | Grünenthal GmbH | Verfahren zur Herstellung einer gegen Missbrauch gesicherten Darreichungsform |
| DE102005005446A1 (de) | 2005-02-04 | 2006-08-10 | Grünenthal GmbH | Bruchfeste Darreichungsformen mit retardierter Freisetzung |
| DE102004032051A1 (de) | 2004-07-01 | 2006-01-19 | Grünenthal GmbH | Verfahren zur Herstellung einer gegen Missbrauch gesicherten, festen Darreichungsform |
| US8075872B2 (en) | 2003-08-06 | 2011-12-13 | Gruenenthal Gmbh | Abuse-proofed dosage form |
| 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 |
| PL1691892T3 (pl) * | 2003-12-09 | 2007-07-31 | Euro Celtique Sa | Odporna na fizyczne manipulowanie, współwytłaczana postać dawkowania zawierająca środek aktywny i środek przeciwdziałający oraz sposób wytwarzania tej postaci |
| US8883204B2 (en) | 2003-12-09 | 2014-11-11 | Purdue Pharma L.P. | Tamper resistant co-extruded dosage form containing an active agent and an adverse agent and process of making same |
| 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 |
| WO2006128471A2 (en) * | 2005-06-03 | 2006-12-07 | Egalet A/S | A solid pharmaceutical composition with a first fraction of a dispersion medium and a second fraction of a matrix, the latter being at least partially first exposed to gastrointestinal fluids |
| WO2007020508A1 (en) * | 2005-08-12 | 2007-02-22 | Ferring International Center S.A. | Method and device for dividing granules |
| US20080119501A1 (en) * | 2006-04-28 | 2008-05-22 | Hein William A | Immediate release oxymorphone compositions and methods of using same |
| US20080069891A1 (en) | 2006-09-15 | 2008-03-20 | Cima Labs, Inc. | Abuse resistant drug formulation |
| US20080075771A1 (en) * | 2006-07-21 | 2008-03-27 | Vaughn Jason M | Hydrophilic opioid abuse deterrent delivery system using opioid antagonists |
| 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 |
| US8445018B2 (en) | 2006-09-15 | 2013-05-21 | Cima Labs Inc. | Abuse resistant drug formulation |
| DE102007011485A1 (de) | 2007-03-07 | 2008-09-11 | Grünenthal GmbH | Darreichungsform mit erschwertem Missbrauch |
| NZ580972A (en) | 2007-06-04 | 2012-02-24 | Egalet Ltd | Controlled release pharmaceutical compositions for prolonged effect |
| JP5730572B2 (ja) * | 2007-09-13 | 2015-06-10 | シマ ラブス インク． | 濫用抵抗性製剤 |
| CA2709905A1 (en) * | 2007-12-17 | 2009-06-25 | Alfred Liang | Abuse-resistant oxycodone composition |
| JP5774853B2 (ja) | 2008-01-25 | 2015-09-09 | 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 | 医薬投薬形 |
| US9226907B2 (en) | 2008-02-01 | 2016-01-05 | Abbvie Inc. | Extended release hydrocodone acetaminophen and related methods and uses thereof |
| MX2010012039A (es) | 2008-05-09 | 2010-11-30 | Gruenenthal Gmbh | Proceso para la preparacion de una formulacion de polvo intermedia y una forma de dosificacion solida final bajo el uso de un paso de congelacion por rocio. |
| ES2414856T3 (es) * | 2008-12-12 | 2013-07-23 | Paladin Labs Inc. | Formulaciones de fármaco narcótico con potencial de adicción disminuido |
| WO2010089132A1 (en) | 2009-02-06 | 2010-08-12 | Egalet A/S | Immediate release composition resistant to abuse by intake of alcohol |
| WO2010088911A1 (en) | 2009-02-06 | 2010-08-12 | Egalet A/S | Pharmaceutical compositions resistant to abuse |
| EP2445487A2 (en) | 2009-06-24 | 2012-05-02 | Egalet Ltd. | Controlled release formulations |
| BR112012001547A2 (pt) | 2009-07-22 | 2016-03-08 | Gruenenthal Gmbh | forma de dosagem farmacêutica extrusada por fusão a quente |
| ES2428938T3 (es) | 2009-07-22 | 2013-11-12 | Grünenthal GmbH | Forma de dosificación resistente a la manipulación y estabilizada frente a la oxidación |
| WO2011143120A1 (en) | 2010-05-11 | 2011-11-17 | Cima Labs Inc. | Alcoholres i stant metoprolol - containing extended - release oral dosage forms |
| CA2808219C (en) | 2010-09-02 | 2019-05-14 | Gruenenthal Gmbh | Tamper resistant dosage form comprising inorganic salt |
| CN103179954A (zh) | 2010-09-02 | 2013-06-26 | 格吕伦塔尔有限公司 | 包含阴离子聚合物的抗破碎剂型 |
| PL2736497T3 (pl) | 2011-07-29 | 2018-01-31 | Gruenenthal Gmbh | Tabletka odporna na ingerencję, zapewniająca natychmiastowe uwalnianie leku |
| CA2839123A1 (en) | 2011-07-29 | 2013-02-07 | Grunenthal Gmbh | Tamper-resistant tablet providing immediate drug release |
| MX356421B (es) | 2012-02-28 | 2018-05-29 | Gruenenthal Gmbh | Forma de dosificacion resistente a la manipulacion indebida que comprende un compuesto farmacologicamente activo y un polimero anionico. |
| 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 |
| BR112015000150A2 (pt) | 2012-07-06 | 2017-06-27 | Egalet Ltd | composições farmacêuticas dissuasoras de abuso de liberação controlada |
| MX371432B (es) | 2013-05-29 | 2020-01-30 | Gruenenthal Gmbh | Forma de dosificacion resistente al uso indebido que contiene una o mas particulas. |
| WO2014191396A1 (en) | 2013-05-29 | 2014-12-04 | Grünenthal GmbH | Tamper resistant dosage form with bimodal release profile |
| US10624862B2 (en) | 2013-07-12 | 2020-04-21 | Grünenthal GmbH | Tamper-resistant dosage form containing ethylene-vinyl acetate polymer |
| WO2015065547A1 (en) | 2013-10-31 | 2015-05-07 | Cima Labs Inc. | Immediate release abuse-deterrent granulated dosage forms |
| WO2015078891A1 (en) | 2013-11-26 | 2015-06-04 | Farmaceutici Formenti S.P.A. | Preparation of a powdery pharmaceutical composition by means of cryo-milling |
| US20150320690A1 (en) | 2014-05-12 | 2015-11-12 | Grünenthal GmbH | Tamper resistant immediate release capsule formulation comprising tapentadol |
| EP3148512A1 (en) | 2014-05-26 | 2017-04-05 | Grünenthal GmbH | Multiparticles safeguarded against ethanolic dose-dumping |
| 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 |
| AU2016319203A1 (en) | 2015-09-10 | 2018-02-22 | Grünenthal GmbH | Protecting oral overdose with abuse deterrent immediate release formulations |
| US10583089B2 (en) * | 2016-07-19 | 2020-03-10 | Johnson & Johnson Consumer Inc. | Tablets having discontinuous coated regions |
| US12161754B2 (en) | 2017-12-20 | 2024-12-10 | Purdue Pharma L.P. | Abuse deterrent morphine sulfate dosage forms |
| WO2020225773A1 (en) | 2019-05-07 | 2020-11-12 | Clexio Biosciences Ltd. | Abuse-deterrent dosage forms containing esketamine |
| US20220062200A1 (en) | 2019-05-07 | 2022-03-03 | Clexio Biosciences Ltd. | Abuse-deterrent dosage forms containing esketamine |
| AU2022202053A1 (en) * | 2021-09-17 | 2023-04-06 | Biocorrx, Inc. | Biodegradable implant including naltrexone |
| US12303604B1 (en) | 2024-10-16 | 2025-05-20 | Currax Pharmaceuticals Llc | Pharmaceutical formulations comprising naltrexone and/or bupropion |
Family Cites Families (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3493657A (en) | 1961-03-14 | 1970-02-03 | Mozes Juda Lewenstein | Therapeutic compositions of n-allyl-14-hydroxy - dihydronormorphinane and morphine |
| US3773955A (en) | 1970-08-03 | 1973-11-20 | Bristol Myers Co | Analgetic compositions |
| US3966940A (en) | 1973-11-09 | 1976-06-29 | Bristol-Myers Company | Analgetic compositions |
| US4457933A (en) | 1980-01-24 | 1984-07-03 | Bristol-Myers Company | Prevention of analgesic abuse |
| GB8332556D0 (en) | 1983-12-06 | 1984-01-11 | Reckitt & Colmann Prod Ltd | Analgesic compositions |
| US4673565A (en) * | 1985-05-03 | 1987-06-16 | E. I. Du Pont De Nemours And Company | Pharmaceutical compositions containing hollow fine tubular drug delivery systems |
| US5316759A (en) | 1986-03-17 | 1994-05-31 | Robert J. Schaap | Agonist-antagonist combination to reduce the use of nicotine and other drugs |
| DE3612211A1 (de) | 1986-04-11 | 1987-10-15 | Basf Ag | Kontinuierliches verfahren zum tablettieren |
| US4970075A (en) | 1986-07-18 | 1990-11-13 | Euroceltique, S.A. | Controlled release bases for pharmaceuticals |
| GB8626098D0 (en) | 1986-10-31 | 1986-12-03 | Euro Celtique Sa | Controlled release hydromorphone composition |
| US5200193A (en) | 1987-04-22 | 1993-04-06 | Mcneilab, Inc. | Pharmaceutical sustained release matrix and process |
| DE3812567A1 (de) | 1988-04-15 | 1989-10-26 | Basf Ag | Verfahren zur herstellung pharmazeutischer mischungen |
| DE3830353A1 (de) | 1988-09-07 | 1990-03-15 | Basf Ag | Verfahren zur kontinuierlichen herstellung von festen pharmazeutischen formen |
| US4880535A (en) * | 1989-02-21 | 1989-11-14 | Burrows Bruce D | Water supply station with multiple water storage reservoirs |
| FR2677886B1 (fr) | 1991-06-18 | 1995-03-31 | Adir | Comprime matriciel permettant la liberation prolongee d'indapamide apres administration par voie orale. |
| US5266331A (en) | 1991-11-27 | 1993-11-30 | Euroceltique, S.A. | Controlled release oxycodone compositions |
| US5656295A (en) | 1991-11-27 | 1997-08-12 | Euro-Celtique, S.A. | Controlled release oxycodone compositions |
| US5968551A (en) | 1991-12-24 | 1999-10-19 | Purdue Pharma L.P. | Orally administrable opioid formulations having extended duration of effect |
| US5478577A (en) | 1993-11-23 | 1995-12-26 | Euroceltique, S.A. | Method of treating pain by administering 24 hour oral opioid formulations exhibiting rapid rate of initial rise of plasma drug level |
| US5472712A (en) | 1991-12-24 | 1995-12-05 | Euroceltique, S.A. | Controlled-release formulations coated with aqueous dispersions of ethylcellulose |
| US5324351A (en) | 1992-08-13 | 1994-06-28 | Euroceltique | Aqueous dispersions of zein and preparation thereof |
| US5879705A (en) | 1993-07-27 | 1999-03-09 | Euro-Celtique S.A. | Sustained release compositions of morphine and a method of preparing pharmaceutical compositions |
| US5492692A (en) | 1993-08-17 | 1996-02-20 | University Of Kentucky Research Foundation | Coated products with potent anti-HIV and antimicrobial properties |
| US5451409A (en) | 1993-11-22 | 1995-09-19 | Rencher; William F. | Sustained release matrix system using hydroxyethyl cellulose and hydroxypropyl cellulose polymer blends |
| US5965161A (en) | 1994-11-04 | 1999-10-12 | Euro-Celtique, S.A. | Extruded multi-particulates |
| US6007843A (en) | 1995-09-29 | 1999-12-28 | Lam Pharmaceuticals Corp. | Sustained release delivery system |
| AUPN605795A0 (en) | 1995-10-19 | 1995-11-09 | F.H. Faulding & Co. Limited | Analgesic pharmaceutical composition |
| DE19539361A1 (de) * | 1995-10-23 | 1997-04-24 | Basf Ag | Verfahren zur Herstellung von mehrschichtigen, festen Arzneiformen zur oralen oder rektalen Verabreichung |
| DE19710008A1 (de) | 1997-03-12 | 1998-09-17 | Basf Ag | Feste, mindestens zweiphasige Zubereitungsformen eines Opioid-Analgeticums mit verzögerter Freisetzung |
| IN183097B (enExample) | 1997-03-27 | 1999-09-04 | Rajiv Indravadan Dr Modi | |
| EP2266564B1 (en) * | 1997-12-22 | 2013-03-13 | Euro-Celtique S.A. | Pharmaceutical oral dosage form comprising a combination of an opioid agonist and an opioid antagonist |
| BR9813826A (pt) | 1997-12-22 | 2000-10-10 | Euro Celtique Sa | Potencial de uso abusivo de administração oral de opióide analgésico |
| DE19812688A1 (de) | 1998-03-23 | 1999-09-30 | Basf Ag | Verfahren zur Herstellung von festen Dosierungsformen |
| FR2795326B1 (fr) | 1999-06-28 | 2001-08-31 | Adir | Composition pharmaceutique solide thermoformable a liberation controlee |
| JP4806507B2 (ja) * | 1999-10-29 | 2011-11-02 | ユーロ−セルティーク エス．エイ． | 制御放出ヒドロコドン処方 |
| EP2517710B1 (en) * | 2000-02-08 | 2015-03-25 | Euro-Celtique S.A. | Tamper-resistant oral opioid agonist formulations |
| EP1213014B1 (en) | 2000-12-07 | 2005-04-20 | Warner-Lambert Company LLC | Process and system for uniform release drug delivery |
| CA2778114A1 (en) * | 2001-05-11 | 2002-11-21 | Endo Pharmaceuticals, Inc. | Abuse-resistant opioid dosage form |
| US20030157168A1 (en) * | 2001-08-06 | 2003-08-21 | Christopher Breder | Sequestered antagonist formulations |
| US7144587B2 (en) | 2001-08-06 | 2006-12-05 | Euro-Celtique S.A. | Pharmaceutical formulation containing opioid agonist, opioid antagonist and bittering agent |
| WO2003013479A1 (en) * | 2001-08-06 | 2003-02-20 | Euro-Celtique S.A. | Compositions and methods to prevent abuse of opioids |
| US20030044458A1 (en) * | 2001-08-06 | 2003-03-06 | Curtis Wright | Oral dosage form comprising a therapeutic agent and an adverse-effect agent |
| MXPA04001210A (es) * | 2001-08-06 | 2004-07-08 | Euro Celtique Sa | Formulaciones de agonista opioide con antagonista liberable y aislado. |
| JP4790219B2 (ja) | 2002-03-26 | 2011-10-12 | ユーロ−セルティーク エス．エイ． | 徐放性ゲルコーティング組成物 |
| SI1551372T1 (en) | 2002-09-20 | 2018-08-31 | Alpharma Pharmaceuticals Llc | SUBVENCATION DATA AND RELATED CONSTRUCTIONS AND PROCEDURES |
| US9579286B2 (en) | 2003-04-21 | 2017-02-28 | Purdue Pharma L.P. | Tamper resistant dosage form comprising co-extruded, sequestered adverse agent particles and process of making same |
| PL1691892T3 (pl) | 2003-12-09 | 2007-07-31 | Euro Celtique Sa | Odporna na fizyczne manipulowanie, współwytłaczana postać dawkowania zawierająca środek aktywny i środek przeciwdziałający oraz sposób wytwarzania tej postaci |
-
2004
- 2004-04-21 US US10/554,157 patent/US9579286B2/en active Active
- 2004-04-21 EP EP04760176A patent/EP1615625A4/en not_active Withdrawn
- 2004-04-21 AU AU2004232370A patent/AU2004232370B2/en not_active Expired
- 2004-04-21 CA CA2519556A patent/CA2519556C/en not_active Expired - Lifetime
- 2004-04-21 MX MXPA05011071A patent/MXPA05011071A/es active IP Right Grant
- 2004-04-21 WO PCT/US2004/012776 patent/WO2004093819A2/en not_active Ceased
- 2004-04-21 JP JP2006513318A patent/JP5501553B2/ja not_active Expired - Lifetime
-
2011
- 2011-04-06 JP JP2011084443A patent/JP2011157384A/ja not_active Withdrawn
-
2017
- 2017-01-30 US US15/419,486 patent/US10039720B2/en not_active Expired - Lifetime
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2006524261A5 (enExample) | ||
| CA2519556A1 (en) | Tamper resistant dosage form comprising co-extruded, adverse agent particles and process of making same | |
| JP2011126895A5 (enExample) | ||
| HRP20100289T1 (hr) | Proizvodi otporni na miješanje za opioidnu primjenu | |
| CA2557839A1 (en) | Tamper resistant dosage form comprising an adsorbent and an adverse agent | |
| AU2003234395B2 (en) | Abuse-resistant opioid solid dosage form | |
| US5149538A (en) | Misuse-resistive transdermal opioid dosage form | |
| JP2006524249A5 (enExample) | ||
| JP2024015430A5 (enExample) | ||
| CA2699172C (en) | Compositions and methods for delivery of poorly soluble drugs | |
| JP2010189403A5 (enExample) | ||
| JP2008528534A5 (enExample) | ||
| RU2011135568A (ru) | Защищенная от применения не по назначению экструдированная из расплава композиция с уменьшенным взаимодействием со спиртом | |
| JP2011515495A5 (enExample) | ||
| HRP20150835T1 (hr) | Farmaceutski oblici doziranja s kontroliranim oslobađanjem | |
| RU2009101082A (ru) | Фармацевтические композиции | |
| KR960703004A (ko) | 혈장 약물 농도의 신속한 초기 증가량을 시현하는 24시간 경구용 오피오이드 제형을 투여함으로써 통증을 치료하는 방법 | |
| CA2547334A1 (en) | Methods and compositions for deterring abuse of opioid containing dosage forms | |
| HRP20120641T1 (hr) | Oralni farmaceutski oblici doziranja otporni na neovlašteno korištenje koji sadrže opioidni analgetik | |
| CA2654700A1 (en) | Transdermal patch | |
| JP2012519675A5 (enExample) | ||
| WO2007088489A2 (en) | Pharmaceutical composition containing a central opioid agonist, a central opioid antagonist, and a peripheral opioid antagonist, and method for making the same | |
| EP2670400A1 (en) | Pharmaceutical composition comprising opioid agonist and sequestered antagonist | |
| RU2017112301A (ru) | Стойкие к злоупотреблению фармацевтические композиции | |
| CA2652981A1 (en) | Robust sustained release formulations |