JP2004515455A5 - - Google Patents
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- JP2004515455A5 JP2004515455A5 JP2001581910A JP2001581910A JP2004515455A5 JP 2004515455 A5 JP2004515455 A5 JP 2004515455A5 JP 2001581910 A JP2001581910 A JP 2001581910A JP 2001581910 A JP2001581910 A JP 2001581910A JP 2004515455 A5 JP2004515455 A5 JP 2004515455A5
- Authority
- JP
- Japan
- Prior art keywords
- dosage form
- solid oral
- oral dosage
- antagonist
- amount
- 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.)
- Pending
Links
- 239000007787 solid Substances 0.000 description 163
- 239000006186 oral dosage form Substances 0.000 description 136
- 239000005557 antagonist Substances 0.000 description 83
- 239000008194 pharmaceutical composition Substances 0.000 description 58
- 239000002552 dosage form Substances 0.000 description 56
- 239000003401 opiate antagonist Substances 0.000 description 48
- 239000000546 pharmaceutical excipient Substances 0.000 description 29
- 229940124531 pharmaceutical excipient Drugs 0.000 description 29
- 239000003402 opiate agonist Substances 0.000 description 25
- 239000000556 agonist Substances 0.000 description 23
- 239000000758 substrate Substances 0.000 description 18
- 239000011248 coating agent Substances 0.000 description 17
- 238000000576 coating method Methods 0.000 description 17
- 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 description 16
- 239000002775 capsule Substances 0.000 description 14
- 239000012729 immediate-release (IR) formulation Substances 0.000 description 14
- 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 description 11
- 239000007931 coated granule Substances 0.000 description 11
- OROGSEYTTFOCAN-UHFFFAOYSA-N hydrocodone Natural products C1C(N(CCC234)C)C2C=CC(O)C3OC2=C4C1=CC=C2OC OROGSEYTTFOCAN-UHFFFAOYSA-N 0.000 description 11
- 229960005297 nalmefene Drugs 0.000 description 11
- 229960003086 naltrexone Drugs 0.000 description 11
- 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 description 11
- 239000008186 active pharmaceutical agent Substances 0.000 description 10
- 238000011287 therapeutic dose Methods 0.000 description 10
- 239000008187 granular material Substances 0.000 description 9
- 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 description 8
- 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 description 8
- 239000011324 bead Substances 0.000 description 8
- 239000011230 binding agent Substances 0.000 description 8
- 230000009089 cytolysis Effects 0.000 description 8
- XYYVYLMBEZUESM-UHFFFAOYSA-N dihydrocodeine Natural products C1C(N(CCC234)C)C2C=CC(=O)C3OC2=C4C1=CC=C2OC XYYVYLMBEZUESM-UHFFFAOYSA-N 0.000 description 8
- 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 description 8
- 229960000240 hydrocodone Drugs 0.000 description 8
- 239000000203 mixture Substances 0.000 description 8
- 229960005181 morphine Drugs 0.000 description 8
- 229960002085 oxycodone Drugs 0.000 description 8
- 229960004380 tramadol Drugs 0.000 description 8
- TVYLLZQTGLZFBW-GOEBONIOSA-N tramadol Natural products COC1=CC=CC([C@@]2(O)[C@@H](CCCC2)CN(C)C)=C1 TVYLLZQTGLZFBW-GOEBONIOSA-N 0.000 description 8
- LLPOLZWFYMWNKH-UHFFFAOYSA-N trans-dihydrocodeinone Natural products C1C(N(CCC234)C)C2CCC(=O)C3OC2=C4C1=CC=C2OC LLPOLZWFYMWNKH-UHFFFAOYSA-N 0.000 description 8
- 239000008188 pellet Substances 0.000 description 7
- 239000007909 solid dosage form Substances 0.000 description 7
- 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 description 6
- 239000007903 gelatin capsule Substances 0.000 description 6
- 238000004090 dissolution Methods 0.000 description 5
- 239000000725 suspension Substances 0.000 description 5
- 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 description 3
- XADCESSVHJOZHK-UHFFFAOYSA-N Meperidine Chemical compound C=1C=CC=CC=1C1(C(=O)OCC)CCN(C)CC1 XADCESSVHJOZHK-UHFFFAOYSA-N 0.000 description 3
- IDBPHNDTYPBSNI-UHFFFAOYSA-N N-(1-(2-(4-Ethyl-5-oxo-2-tetrazolin-1-yl)ethyl)-4-(methoxymethyl)-4-piperidyl)propionanilide Chemical compound C1CN(CCN2C(N(CC)N=N2)=O)CCC1(COC)N(C(=O)CC)C1=CC=CC=C1 IDBPHNDTYPBSNI-UHFFFAOYSA-N 0.000 description 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 description 3
- 229960001391 alfentanil Drugs 0.000 description 3
- 229960004126 codeine Drugs 0.000 description 3
- 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 description 3
- 229960004193 dextropropoxyphene Drugs 0.000 description 3
- 229960002428 fentanyl Drugs 0.000 description 3
- 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 description 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 description 3
- 229960001410 hydromorphone Drugs 0.000 description 3
- 229960001797 methadone Drugs 0.000 description 3
- 229960005118 oxymorphone Drugs 0.000 description 3
- 229960000482 pethidine Drugs 0.000 description 3
- 239000006187 pill Substances 0.000 description 3
- 150000003839 salts Chemical class 0.000 description 3
- 239000007921 spray Substances 0.000 description 3
- 239000003826 tablet Substances 0.000 description 3
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 description 2
- 239000004480 active ingredient Substances 0.000 description 2
- 230000000202 analgesic effect Effects 0.000 description 2
- 230000003110 anti-inflammatory effect Effects 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 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 description 2
- 229960004127 naloxone Drugs 0.000 description 2
- 239000002687 nonaqueous vehicle Substances 0.000 description 2
- 239000004014 plasticizer Substances 0.000 description 2
- 230000003637 steroidlike Effects 0.000 description 2
- 229940111134 coxibs Drugs 0.000 description 1
- 239000003260 cyclooxygenase 1 inhibitor Substances 0.000 description 1
- 239000003255 cyclooxygenase 2 inhibitor Substances 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 239000003887 narcotic antagonist Substances 0.000 description 1
- 229960005489 paracetamol Drugs 0.000 description 1
- 239000008177 pharmaceutical agent Substances 0.000 description 1
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US56607100A | 2000-05-05 | 2000-05-05 | |
| US20222700P | 2000-05-05 | 2000-05-05 | |
| US20226800P | 2000-05-05 | 2000-05-05 | |
| PCT/US2000/012493 WO2000067739A2 (en) | 1999-05-06 | 2000-05-05 | Opioid antagonists containing compositions for enhancing analgesic potency of tramadol and attenuating its adverse side effects |
| US24448200P | 2000-10-30 | 2000-10-30 | |
| US24511000P | 2000-11-01 | 2000-11-01 | |
| US24623500P | 2000-11-02 | 2000-11-02 | |
| US75633101A | 2001-01-08 | 2001-01-08 | |
| PCT/US2001/014377 WO2001085257A2 (en) | 2000-05-05 | 2001-05-04 | Opioid antagonist compositions and dosage forms |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004515455A JP2004515455A (ja) | 2004-05-27 |
| JP2004515455A5 true JP2004515455A5 (enExample) | 2008-06-19 |
Family
ID=38051036
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2001581910A Pending JP2004515455A (ja) | 2000-05-05 | 2001-05-04 | オピオイドアンタゴニスト組成物および投薬形態 |
Country Status (5)
| Country | Link |
|---|---|
| EP (1) | EP1284736A2 (enExample) |
| JP (1) | JP2004515455A (enExample) |
| AU (1) | AU5945801A (enExample) |
| CA (1) | CA2408106A1 (enExample) |
| WO (1) | WO2001085257A2 (enExample) |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6274591B1 (en) | 1997-11-03 | 2001-08-14 | Joseph F. Foss | Use of methylnaltrexone and related compounds |
| 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 |
| EP2517710B1 (en) | 2000-02-08 | 2015-03-25 | Euro-Celtique S.A. | Tamper-resistant oral opioid agonist formulations |
| JP4522652B2 (ja) | 2001-05-11 | 2010-08-11 | エンドー ファーマシューティカルズ， インコーポレイティド | 乱用防止制御放出オピオイド投薬形態 |
| US7968119B2 (en) | 2001-06-26 | 2011-06-28 | Farrell John J | Tamper-proof narcotic delivery system |
| CA2454328C (en) | 2001-07-18 | 2008-03-18 | Christopher D. Breder | Pharmaceutical combinations of oxycodone and naloxone |
| US20030157168A1 (en) | 2001-08-06 | 2003-08-21 | Christopher Breder | Sequestered antagonist formulations |
| MXPA04001210A (es) | 2001-08-06 | 2004-07-08 | Euro Celtique Sa | Formulaciones de agonista opioide con antagonista liberable y aislado. |
| US8128957B1 (en) | 2002-02-21 | 2012-03-06 | Valeant International (Barbados) Srl | Modified release compositions of at least one form of tramadol |
| JP4683842B2 (ja) * | 2002-03-14 | 2011-05-18 | ユーロ−セルティーク エス．エイ． | 塩酸ナルトレキソン組成物 |
| LT2425824T (lt) | 2002-04-05 | 2017-07-25 | Euro-Celtique S.A. | Farmacinis preparatas, turintis oksikodono ir naloksono |
| PT1894562E (pt) * | 2002-08-15 | 2011-01-14 | Euro Celtique Sa | Composições farmacêuticas que compreendem um antagonista opióide |
| SI1551372T1 (en) | 2002-09-20 | 2018-08-31 | Alpharma Pharmaceuticals Llc | SUBVENCATION DATA AND RELATED CONSTRUCTIONS AND PROCEDURES |
| ES2528669T3 (es) | 2003-04-08 | 2015-02-11 | Progenics Pharmaceuticals, Inc. | Formulaciones farmacéuticas que contienen metilnaltrexona |
| MY135852A (en) | 2003-04-21 | 2008-07-31 | Euro Celtique Sa | Pharmaceutical products |
| RU2350327C2 (ru) | 2003-04-29 | 2009-03-27 | Ориксиджен Серапьютикс, Инкорпорэйтд | Составы, вызывающие потерю веса |
| EP1702558A1 (en) | 2005-02-28 | 2006-09-20 | Euro-Celtique S.A. | Method and device for the assessment of bowel function |
| WO2006096626A2 (en) | 2005-03-07 | 2006-09-14 | The University Of Chicago | Use of opioid antagonists to attenuate endothelial cell proliferation and migration |
| US8524731B2 (en) | 2005-03-07 | 2013-09-03 | The University Of Chicago | Use of opioid antagonists to attenuate endothelial cell proliferation and migration |
| US8518962B2 (en) | 2005-03-07 | 2013-08-27 | The University Of Chicago | Use of opioid antagonists |
| US9662325B2 (en) | 2005-03-07 | 2017-05-30 | The University Of Chicago | Use of opioid antagonists to attenuate endothelial cell proliferation and migration |
| WO2006126529A1 (ja) | 2005-05-25 | 2006-11-30 | Shionogi & Co., Ltd. | ６，７－不飽和－７－カルバモイル置換モルヒナン誘導体 |
| AR057325A1 (es) | 2005-05-25 | 2007-11-28 | Progenics Pharm Inc | Sintesis de (s)-n-metilnaltrexona, composiciones farmaceuticas y usos |
| AR057035A1 (es) | 2005-05-25 | 2007-11-14 | Progenics Pharm Inc | SíNTESIS DE (R)-N-METILNALTREXONA, COMPOSICIONES FARMACÉUTICAS Y USOS |
| EP1951212A2 (en) | 2005-11-22 | 2008-08-06 | Orexigen Therapeutics, Inc. | Compositions and methods for increasing insulin sensitivity |
| AU2006326377B2 (en) | 2005-12-13 | 2010-10-07 | Biodelivery Sciences International, Inc. | Abuse resistant transmucosal drug delivery device |
| US8916195B2 (en) | 2006-06-05 | 2014-12-23 | Orexigen Therapeutics, Inc. | Sustained release formulation of naltrexone |
| EP2719378B1 (en) | 2006-06-19 | 2016-08-31 | Alpharma Pharmaceuticals LLC | Pharmaceutical compositions |
| SI2054031T1 (sl) | 2006-07-21 | 2016-09-30 | Biodelivery Sciences International, Inc. | Transmukozne naprave za administracijo z izboljšanim vnosom |
| TWI489984B (zh) | 2006-08-04 | 2015-07-01 | Wyeth Corp | 用於非經腸道傳輸化合物之配方及其用途 |
| CA2668885C (en) | 2006-11-09 | 2016-08-02 | Orexigen Therapeutics, Inc. | Methods for administering weight loss medications |
| PE20090700A1 (es) | 2007-03-29 | 2009-07-13 | Progenics Pharm Inc | Compuestos heterociclicos como antagonistas del receptor opioide periferico |
| BRPI0809579B8 (pt) | 2007-03-29 | 2021-05-25 | Progenics Pharm Inc | formas cristalinas e seus usos |
| PL2139890T3 (pl) | 2007-03-29 | 2014-11-28 | Wyeth Llc | Antagoniści obwodowych receptorów opioidowych i ich zastosowania |
| US8623418B2 (en) | 2007-12-17 | 2014-01-07 | Alpharma Pharmaceuticals Llc | Pharmaceutical composition |
| US9226907B2 (en) * | 2008-02-01 | 2016-01-05 | Abbvie Inc. | Extended release hydrocodone acetaminophen and related methods and uses thereof |
| WO2009099411A1 (en) | 2008-02-06 | 2009-08-13 | Progenics Pharmaceuticals, Inc. | Preparation and use of (r),(r)-2,2'-bis-methylnaltrexone |
| AU2009225434B2 (en) | 2008-03-21 | 2014-05-22 | The University Of Chicago | Treatment with opioid antagonists and mTOR inhibitors |
| EP2303025A4 (en) | 2008-05-30 | 2012-07-04 | Orexigen Therapeutics Inc | METHOD FOR TREATING DIGITAL FAT SWITCHES |
| AU2009265034B2 (en) * | 2008-07-01 | 2015-09-03 | University Of Chicago | Particles containing an opioid receptor antagonist and methods of use |
| CA2676881C (en) | 2008-09-30 | 2017-04-25 | Wyeth | Peripheral opioid receptor antagonists and uses thereof |
| HUE042105T2 (hu) | 2009-03-10 | 2019-06-28 | Euro Celtique Sa | Oxikodont és naloxont tartalmazó azonnali hatóanyagleadású orális gyógyászati készítmények |
| EP3659604A1 (en) | 2010-01-11 | 2020-06-03 | Nalpropion Pharmaceuticals, Inc. | Methods of providing weight loss therapy in patients with major depression |
| US9901539B2 (en) | 2011-12-21 | 2018-02-27 | Biodelivery Sciences International, Inc. | Transmucosal drug delivery devices for use in chronic pain relief |
| PT3730132T (pt) | 2012-06-06 | 2022-08-16 | Nalpropion Pharmaceuticals Llc | Composição para utilização num método de tratamento de excesso de peso e obesidade em doentes com alto risco cardiovascular |
| EP3024461B1 (en) | 2013-07-23 | 2020-05-13 | Euro-Celtique S.A. | A combination of oxycodone and naloxone for use in treating pain in patients suffering from pain and a disease resulting in intestinal dysbiosis and/or increasing the risk for intestinal bacterial translocation |
| CA3042642A1 (en) | 2013-08-12 | 2015-02-19 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded immediate release abuse deterrent pill |
| US9492444B2 (en) | 2013-12-17 | 2016-11-15 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded extended release abuse deterrent pill |
| US10172797B2 (en) | 2013-12-17 | 2019-01-08 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded extended release abuse deterrent pill |
| AU2015290098B2 (en) | 2014-07-17 | 2018-11-01 | Pharmaceutical Manufacturing Research Services, Inc. | Immediate release abuse deterrent liquid fill dosage form |
| US20160106737A1 (en) | 2014-10-20 | 2016-04-21 | Pharmaceutical Manufacturing Research Services, Inc. | Extended Release Abuse Deterrent Liquid Fill Dosage Form |
| WO2017141104A2 (en) * | 2016-02-18 | 2017-08-24 | Immune Therapeutics, Inc. | Method for inducing a sustained immune response |
| WO2021005501A1 (en) | 2019-07-10 | 2021-01-14 | Intas Pharmaceuticals Ltd. | Naltrexone formulation |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4889860A (en) * | 1985-09-23 | 1989-12-26 | Nova Pharmaceutical Corporation | Oximes of oxymorphone, naltrexone and naloxone as potent, selective opioid receptor agonists and antagonists |
| US5580876A (en) * | 1992-09-21 | 1996-12-03 | Albert Einstein College Of Medicine Of Yeshiva University, A Division Of Yeshiva University | Method of simultaneously enhancing analgesic potency and attenuating dependence liability caused by morphine and other bimodally-acting opioid agonists |
| US5512578A (en) * | 1992-09-21 | 1996-04-30 | Albert Einstein College Of Medicine Of Yeshiva University, A Division Of Yeshiva University | Method of simultaneously enhancing analgesic potency and attenuating dependence liability caused by exogenous and endogenous opiod agonists |
| US6103258A (en) * | 1996-04-12 | 2000-08-15 | Simon; David Lew | Salts and bases of the 17-(Cyclopropylmethyl)-4,5 alpha-epoxy-6-Methylenemorphinan-3,14 diol molecule for optimizing dopamine homeostasis during administration of opioid analgesics |
| BR9813826A (pt) * | 1997-12-22 | 2000-10-10 | Euro Celtique Sa | Potencial de uso abusivo de administração oral de opióide analgésico |
| 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 |
-
2001
- 2001-05-04 WO PCT/US2001/014377 patent/WO2001085257A2/en not_active Ceased
- 2001-05-04 JP JP2001581910A patent/JP2004515455A/ja active Pending
- 2001-05-04 EP EP01932983A patent/EP1284736A2/en not_active Withdrawn
- 2001-05-04 AU AU5945801A patent/AU5945801A/xx active Pending
- 2001-05-04 CA CA002408106A patent/CA2408106A1/en not_active Abandoned
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