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 |
|---|---|---|---|
| US20226800P | 2000-05-05 | 2000-05-05 | |
| US56607100A | 2000-05-05 | 2000-05-05 | |
| US20222700P | 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 |
| ES2412409T3 (es) | 1997-12-22 | 2013-07-11 | Euro-Celtique S.A. | Forma farmacéutica para dosificación oral que comprende una combinación de un agonista opiáceo y un antagonista opiáceo |
| SI1299104T1 (sl) | 2000-02-08 | 2009-10-31 | Euro Celtique Sa | Oralne formulacije opioidnih agonistov, varne pred zlorabo |
| US20030065002A1 (en) | 2001-05-11 | 2003-04-03 | Endo Pharmaceuticals, Inc. | Abuse-resistant controlled-release opioid dosage form |
| US7968119B2 (en) | 2001-06-26 | 2011-06-28 | Farrell John J | Tamper-proof narcotic delivery system |
| AU2002316738B2 (en) | 2001-07-18 | 2009-01-08 | Euro-Celtique S.A. | Pharmaceutical combinations of oxycodone and naloxone |
| WO2003013433A2 (en) | 2001-08-06 | 2003-02-20 | Euro-Celtique S.A. | Sequestered antagonist formulations |
| US7914818B2 (en) | 2001-08-06 | 2011-03-29 | Purdue Pharma L.P. | Opioid agonist formulations with releasable and sequestered antagonist |
| US8128957B1 (en) | 2002-02-21 | 2012-03-06 | Valeant International (Barbados) Srl | Modified release compositions of at least one form of tramadol |
| US20030229111A1 (en) * | 2002-03-14 | 2003-12-11 | Benjamin Oshlack | Naltrexone hydrochloride compositions |
| ES2320748T5 (es) | 2002-04-05 | 2017-02-20 | Euro-Celtique S.A. | Matriz para la liberación sostenida, invariable e independiente de compuestos activos |
| EP1894562B1 (en) * | 2002-08-15 | 2010-12-15 | Euro-Celtique S.A. | Pharmaceutical compositions comprising an opioid antagonist |
| EP2422773A3 (en) | 2002-09-20 | 2012-04-18 | Alpharma, Inc. | Sequestering subunit and related compositions and methods |
| BRPI0409133B8 (pt) | 2003-04-08 | 2021-05-25 | Progenics Pharm Inc | preparações farmacêuticas estavéis compreendendo metilnaltrexona |
| MY135852A (en) | 2003-04-21 | 2008-07-31 | Euro Celtique Sa | Pharmaceutical products |
| ES2639579T3 (es) | 2003-04-29 | 2017-10-27 | Orexigen Therapeutics, Inc. | Composiciones para afectar la pérdida de peso que comprende un antagonista opioide y bupropión |
| EP1702558A1 (en) | 2005-02-28 | 2006-09-20 | Euro-Celtique S.A. | Method and device for the assessment of bowel function |
| US8518962B2 (en) | 2005-03-07 | 2013-08-27 | The University Of Chicago | Use of opioid antagonists |
| US8524731B2 (en) | 2005-03-07 | 2013-09-03 | The University Of Chicago | Use of opioid antagonists to attenuate endothelial cell proliferation and migration |
| BRPI0608818A2 (pt) | 2005-03-07 | 2010-01-26 | Univ Chicago | uso de antagonista opióides para atenuação de proliferação e migração de células endoteliais |
| US9662325B2 (en) | 2005-03-07 | 2017-05-30 | The University Of Chicago | Use of opioid antagonists to attenuate endothelial cell proliferation and migration |
| AR057325A1 (es) | 2005-05-25 | 2007-11-28 | Progenics Pharm Inc | Sintesis de (s)-n-metilnaltrexona, composiciones farmaceuticas y usos |
| 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 |
| AR057035A1 (es) | 2005-05-25 | 2007-11-14 | Progenics Pharm Inc | SíNTESIS DE (R)-N-METILNALTREXONA, COMPOSICIONES FARMACÉUTICAS Y USOS |
| JP5180092B2 (ja) | 2005-11-22 | 2013-04-10 | オレキシジェン・セラピューティクス・インコーポレーテッド | インスリン感受性を増すための組成物および方法 |
| EP1968539A2 (en) | 2005-12-13 | 2008-09-17 | 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 |
| ES2636657T3 (es) | 2006-06-19 | 2017-10-06 | Alpharma Pharmaceuticals Llc | Composición farmacéutica |
| RS54764B1 (sr) | 2006-07-21 | 2016-10-31 | Biodelivery Sciences Int Inc | Sredstvo za transmukozalnu isporuku sa povećanim nakupljanjem |
| 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 |
| CN101573103A (zh) | 2006-11-09 | 2009-11-04 | 奥雷西根治疗公司 | 用于施用重量减轻药物的单位剂量包装和方法 |
| EP2134718A2 (en) | 2007-03-29 | 2009-12-23 | Progenics Pharmaceuticals, Inc. | Crystal forms of (r)-n-methylnaltrexone bromide and uses thereof |
| PT2139890E (pt) | 2007-03-29 | 2014-09-03 | Wyeth Llc | Antagonistas do receptor opióide periférico e respectivas utilizações |
| CA2682125C (en) | 2007-03-29 | 2015-06-16 | Progenics Pharmaceuticals, Inc. | Peripheral opioid receptor antagonists and uses thereof |
| US8623418B2 (en) | 2007-12-17 | 2014-01-07 | Alpharma Pharmaceuticals Llc | Pharmaceutical composition |
| CA2713568C (en) | 2008-02-06 | 2016-09-20 | Progenics Pharmaceuticals, Inc. | Preparation and use of (r),(r)-2,2'-bis-methylnaltrexone |
| JP2011511782A (ja) * | 2008-02-12 | 2011-04-14 | アボット・ラボラトリーズ | 長期放出性ヒドロコドンアセトアミノフェンならびにその関連方法および用途 |
| AU2009225434B2 (en) | 2008-03-21 | 2014-05-22 | The University Of Chicago | Treatment with opioid antagonists and mTOR inhibitors |
| US20110144145A1 (en) | 2008-05-30 | 2011-06-16 | Orexigen Therapeutics, Inc. | Methods for treating visceral fat conditions |
| EP2306829B1 (en) * | 2008-07-01 | 2017-01-04 | University of Chicago | Particles containing a peripheral opioid receptor antagonist |
| CA2676881C (en) | 2008-09-30 | 2017-04-25 | Wyeth | Peripheral opioid receptor antagonists and uses thereof |
| UY32487A (es) | 2009-03-10 | 2010-06-30 | Euro Celtique Sa | Composiciones farmacéuticas de liberación inmediata comprendiendo oxicodona y naloxona |
| KR20120124423A (ko) | 2010-01-11 | 2012-11-13 | 오렉시젠 세러퓨틱스 인크. | 주우울증 환자들에 있어서 체중 감량 치료를 제공하는 방법 |
| US9901539B2 (en) | 2011-12-21 | 2018-02-27 | Biodelivery Sciences International, Inc. | Transmucosal drug delivery devices for use in chronic pain relief |
| RS67076B1 (sr) | 2012-06-06 | 2025-08-29 | Nalpropion Pharmaceuticals Llc | Kompozicija za upotrebu u postupku lečenja prekomerne težine i gojaznosti kod pacijenata sa visokim kardiovaskularnim rizikom |
| UA116567C2 (uk) | 2013-07-23 | 2018-04-10 | Євро-Селтік С.А. | Комбінація оксикодону та налоксону для застосування в лікуванні болю у пацієнтів, які страждають від болю та захворювання, що призводить до дисбактеріозу кишечнику та/або підвищує ризик кишкової бактеріальної транслокації |
| CA2919892C (en) | 2013-08-12 | 2019-06-18 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded immediate release abuse deterrent pill |
| US10172797B2 (en) | 2013-12-17 | 2019-01-08 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded extended release abuse deterrent pill |
| US9492444B2 (en) | 2013-12-17 | 2016-11-15 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded extended release abuse deterrent pill |
| DK3169315T3 (da) | 2014-07-17 | 2020-08-10 | Pharmaceutical Manufacturing Res Services In | Væskefyldt doseringsform til forhindring af misbrug med øjeblikkelig frigivelse |
| EP3209282A4 (en) | 2014-10-20 | 2018-05-23 | Pharmaceutical Manufacturing Research Services, Inc. | Extended release abuse deterrent liquid fill dosage form |
| EP3939570A1 (en) * | 2016-02-18 | 2022-01-19 | Immune Therapeutics, Inc. | Naltrexone for treating or preventing autoimmune and inflammatory diseases |
| CA3145794A1 (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 |
| 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 |
| 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 |
| 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 |
| ES2412409T3 (es) * | 1997-12-22 | 2013-07-11 | Euro-Celtique S.A. | Forma farmacéutica para dosificación oral que comprende una combinación de un agonista opiáceo y un antagonista opiáceo |
| CN1204890C (zh) * | 1997-12-22 | 2005-06-08 | 欧罗赛铁克股份有限公司 | 防止阿片样物质滥用的方法 |
-
2001
- 2001-05-04 AU AU5945801A patent/AU5945801A/xx active Pending
- 2001-05-04 CA CA002408106A patent/CA2408106A1/en not_active Abandoned
- 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
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