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 (enrdf_load_stackoverflow) | 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 (enrdf_load_stackoverflow) |
| JP (1) | JP2004515455A (enrdf_load_stackoverflow) |
| AU (1) | AU5945801A (enrdf_load_stackoverflow) |
| CA (1) | CA2408106A1 (enrdf_load_stackoverflow) |
| WO (1) | WO2001085257A2 (enrdf_load_stackoverflow) |
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 |
| EP1685839B8 (en) | 1997-12-22 | 2013-06-26 | Euro-Celtique S.A. | Pharmaceutical oral dosage form comprising a combination of an opioid agonist and opioid antagonist |
| SI2277521T1 (sl) | 2000-02-08 | 2015-07-31 | Euro-Celtique S.A. | Oralne formulacije opioidnih agonistov, varne pred zlorabo |
| ATE493130T1 (de) | 2001-05-11 | 2011-01-15 | Endo Pharmaceuticals Inc | Opioid enthaltende arzneiform gegen missbrauch |
| US7968119B2 (en) | 2001-06-26 | 2011-06-28 | Farrell John J | Tamper-proof narcotic delivery system |
| JP4256259B2 (ja) | 2001-07-18 | 2009-04-22 | ユーロ−セルティーク エス．エイ． | オキシコドン及びナロキソンの医薬配合物 |
| MXPA04001210A (es) | 2001-08-06 | 2004-07-08 | Euro Celtique Sa | Formulaciones de agonista opioide con antagonista liberable y aislado. |
| US20030157168A1 (en) | 2001-08-06 | 2003-08-21 | Christopher Breder | Sequestered antagonist formulations |
| US8128957B1 (en) | 2002-02-21 | 2012-03-06 | Valeant International (Barbados) Srl | Modified release compositions of at least one form of tramadol |
| ATE510534T1 (de) * | 2002-03-14 | 2011-06-15 | Euro Celtique Sa | Naltrexonhydrochlorid-zusammensetzungen |
| SI2425821T1 (sl) | 2002-04-05 | 2017-06-30 | Mundipharma Medical Cee Gmbh | Farmacevtski pripravek, ki vsebuje oksikodon in nalokson |
| KR20050086409A (ko) * | 2002-08-15 | 2005-08-30 | 유로-셀티크 소시에떼 아노뉨 | 약학 조성물 |
| PT1551372T (pt) | 2002-09-20 | 2018-07-23 | Alpharma Pharmaceuticals Llc | Subunidade de sequestração e composições e métodos relacionados |
| HRP20150037T4 (hr) | 2003-04-08 | 2022-09-02 | Progenics Pharmaceuticals, Inc. | Farmaceutske formulacije koje sadrže metilnaltrekson |
| MY135852A (en) | 2003-04-21 | 2008-07-31 | Euro Celtique Sa | Pharmaceutical products |
| PL1617832T3 (pl) | 2003-04-29 | 2009-01-30 | Orexigen Therapeutics Inc | Kompozycje wpływające na utratę wagi |
| 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 |
| JP5241484B2 (ja) | 2005-03-07 | 2013-07-17 | ザ ユニヴァーシティー オヴ シカゴ | 内皮細胞増殖及び内皮細胞遊走を減弱するためのオピオイドアンタゴニストの使用 |
| US9662325B2 (en) | 2005-03-07 | 2017-05-30 | The University Of Chicago | Use of opioid antagonists to attenuate endothelial cell proliferation and migration |
| AR057035A1 (es) | 2005-05-25 | 2007-11-14 | Progenics Pharm Inc | SíNTESIS DE (R)-N-METILNALTREXONA, COMPOSICIONES FARMACÉUTICAS Y USOS |
| 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 |
| CA2630624C (en) | 2005-11-22 | 2013-08-06 | Orexigen Therapeutics, Inc. | Compositions and methods for increasing insulin sensitivity |
| JP5586151B2 (ja) | 2005-12-13 | 2014-09-10 | バイオデリバリー サイエンシーズ インターナショナル インコーポレイティッド | 乱用抵抗性経粘膜薬剤送達デバイス |
| US8916195B2 (en) | 2006-06-05 | 2014-12-23 | Orexigen Therapeutics, Inc. | Sustained release formulation of naltrexone |
| SI2526932T1 (sl) | 2006-06-19 | 2017-07-31 | Alpharma Pharmaceuticals Llc | Farmacevtski sestavek |
| WO2008011194A2 (en) | 2006-07-21 | 2008-01-24 | Biodelivery Sciences International, Inc. | Transmucosal delivery devices with enhanced uptake |
| 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 |
| US20080110792A1 (en) | 2006-11-09 | 2008-05-15 | Orexigen Therapeutics, Inc. | Methods for administering weight loss medications |
| WO2008121860A1 (en) | 2007-03-29 | 2008-10-09 | Wyeth | Peripheral opioid receptor and antagonists and uses thereof |
| PE20130480A1 (es) | 2007-03-29 | 2013-05-08 | Progenics Pharm Inc | Compuestos heterociclicos como antagonistas del receptor opioide periferico |
| MX2009010550A (es) | 2007-03-29 | 2009-12-14 | Progenics Pharm Inc | Formas de cristal de bromuro de (r)-n-metilnaltrexona y uso de las mismas. |
| 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 |
| JP5358587B2 (ja) | 2008-02-06 | 2013-12-04 | プロジェニックス・ファーマシューティカルス・インコーポレイテッド | （ｒ），（ｒ）−２，２’−ビス−メチルナルトレキソンの製造及び用途 |
| JP5647098B2 (ja) | 2008-03-21 | 2014-12-24 | ザ ユニヴァーシティー オヴ シカゴ | オピオイド拮抗薬とｍＴＯＲ阻害薬を用いた治療 |
| WO2009158114A1 (en) | 2008-05-30 | 2009-12-30 | Orexigen Therapeutics, Inc. | Methods for treating visceral fat conditions |
| ES2620373T3 (es) | 2008-07-01 | 2017-06-28 | University Of Chicago | Partículas que contienen un antagonista del receptor de opioides periférico |
| CA2676881C (en) | 2008-09-30 | 2017-04-25 | Wyeth | Peripheral opioid receptor antagonists and uses thereof |
| MX347106B (es) | 2009-03-10 | 2017-04-12 | Euro-Celtique S A * | Coposiciones farmacéuticas de liberación inmediata que comprenden oxicodona y naloxona. |
| 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 |
| KR20150016405A (ko) | 2012-06-06 | 2015-02-11 | 오렉시젠 세러퓨틱스 인크. | 과체중 및 비만의 치료 방법 |
| JP2016525138A (ja) | 2013-07-23 | 2016-08-22 | ユーロ−セルティーク エス．エイ． | 疼痛および腸内ディスバイオシスをもたらす疾患および／または腸内細菌移行に対するリスクを高める疾患に罹患している患者における痛みの治療への使用のためのオキシコドンおよびナロキソンの組み合わせ |
| AU2014306759B2 (en) | 2013-08-12 | 2018-04-26 | 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 |
| US9707184B2 (en) | 2014-07-17 | 2017-07-18 | Pharmaceutical Manufacturing Research Services, Inc. | Immediate release abuse deterrent liquid fill dosage form |
| JP2017531026A (ja) | 2014-10-20 | 2017-10-19 | ファーマシューティカル マニュファクチュアリング リサーチ サービシズ，インコーポレーテッド | 徐放性乱用抑止性液体充填剤形 |
| EP3416619A2 (en) * | 2016-02-18 | 2018-12-26 | Immune Therapeutics, Inc. | Method for inducing a sustained immune response |
| US20220273645A1 (en) | 2019-07-10 | 2022-09-01 | 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 |
| EP1041988A4 (en) * | 1997-12-22 | 2002-03-13 | Euro Celtique Sa | METHOD FOR PREVENTING ABUSE OF OPIOID DOSES FORMS |
| EP1685839B8 (en) * | 1997-12-22 | 2013-06-26 | Euro-Celtique S.A. | Pharmaceutical oral dosage form comprising a combination of an opioid agonist and opioid antagonist |
-
2001
- 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
- 2001-05-04 WO PCT/US2001/014377 patent/WO2001085257A2/en active Application Filing
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