NO20121414A1 - Farmasoytiske sammensetninger omfattende hydromorfon og nalokson - Google Patents
Farmasoytiske sammensetninger omfattende hydromorfon og nalokson Download PDFInfo
- Publication number
- NO20121414A1 NO20121414A1 NO20121414A NO20121414A NO20121414A1 NO 20121414 A1 NO20121414 A1 NO 20121414A1 NO 20121414 A NO20121414 A NO 20121414A NO 20121414 A NO20121414 A NO 20121414A NO 20121414 A1 NO20121414 A1 NO 20121414A1
- Authority
- NO
- Norway
- Prior art keywords
- approx
- derivative
- pharmaceutically acceptable
- acceptable salt
- pharmaceutical composition
- Prior art date
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
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Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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EP10162428 | 2010-05-10 | ||
PCT/EP2011/057566 WO2011141488A2 (fr) | 2010-05-10 | 2011-05-10 | Compositions pharmaceutiques comprenant de l'hydromorphone et de la naloxone |
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NO20121414A1 true NO20121414A1 (no) | 2013-02-11 |
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NO20121414A NO20121414A1 (no) | 2010-05-10 | 2012-11-26 | Farmasoytiske sammensetninger omfattende hydromorfon og nalokson |
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US (1) | US9700508B2 (fr) |
EP (1) | EP2568967B2 (fr) |
JP (1) | JP5671609B2 (fr) |
KR (2) | KR20130030260A (fr) |
CN (2) | CN102946870A (fr) |
AP (1) | AP3441A (fr) |
AR (1) | AR083150A1 (fr) |
AU (1) | AU2011252039B2 (fr) |
BR (1) | BR112012028773A2 (fr) |
CA (1) | CA2739751C (fr) |
CH (1) | CH705273B1 (fr) |
CL (1) | CL2012003012A1 (fr) |
CO (1) | CO6640216A2 (fr) |
CR (1) | CR20120549A (fr) |
DE (1) | DE112011101605T5 (fr) |
DK (1) | DK178741B1 (fr) |
EA (1) | EA201291211A1 (fr) |
EC (1) | ECSP12012236A (fr) |
ES (1) | ES2408343B2 (fr) |
GB (1) | GB2492037A (fr) |
GT (1) | GT201200304A (fr) |
IL (1) | IL222772B (fr) |
MX (1) | MX347105B (fr) |
MY (1) | MY157673A (fr) |
NI (1) | NI201200157A (fr) |
NO (1) | NO20121414A1 (fr) |
NZ (2) | NZ603497A (fr) |
PE (1) | PE20130657A1 (fr) |
SE (1) | SE1251371A1 (fr) |
SG (1) | SG184523A1 (fr) |
TN (1) | TN2012000488A1 (fr) |
TW (2) | TWI590835B (fr) |
UA (1) | UA106278C2 (fr) |
WO (1) | WO2011141488A2 (fr) |
ZA (1) | ZA201207603B (fr) |
Families Citing this family (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US9901540B2 (en) | 2010-05-10 | 2018-02-27 | Euro-Celtique S.A. | Combination of active loaded granules with additional actives |
CN102946870A (zh) | 2010-05-10 | 2013-02-27 | 欧洲凯尔特公司 | 包含氢吗啡酮和纳洛酮的药物组合物 |
EP2568968B1 (fr) | 2010-05-10 | 2017-07-12 | Euro-Celtique S.A. | Fabrication de granules libres de principes actifs et comprimés les contenant |
ES2706994T3 (es) * | 2012-09-03 | 2019-04-02 | Daiichi Sankyo Co Ltd | Composición farmacéutica de liberación prolongada de administración oral que contiene clorhidrato de hidromorfona |
CA2795324C (fr) * | 2012-11-09 | 2015-07-14 | Purdue Pharma | Compositions pharmaceutiques comprenant de l'hydromorphone et de la naloxone |
US9517208B2 (en) * | 2013-03-15 | 2016-12-13 | Purdue Pharma L.P. | Abuse-deterrent dosage forms |
GB201313915D0 (en) * | 2013-08-02 | 2013-09-18 | Johnson Matthey Plc | Process |
WO2015071380A1 (fr) * | 2013-11-13 | 2015-05-21 | Euro-Celtique S.A. | Hydromorphone et naloxone utilisées pour le traitement de la douleur et du syndrome de dysfonctionnement intestinal dû aux opioïdes |
CA2847781C (fr) * | 2014-03-28 | 2019-03-12 | Purdue Pharma | Reduction de l'appreciation de medicament chez un sujet |
WO2016091805A2 (fr) * | 2014-12-08 | 2016-06-16 | Develco Pharma Schweiz Ag | Monopréparation de naloxone et comprimé multicouche |
EP4103181A4 (fr) * | 2020-02-14 | 2024-03-06 | Teikoku Pharma USA, Inc. | Compositions topiques de naloxone et leurs procédés d'utilisation |
Family Cites Families (102)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
IE49324B1 (en) | 1979-12-19 | 1985-09-18 | Euro Celtique Sa | Controlled release compositions |
US4457933A (en) * | 1980-01-24 | 1984-07-03 | Bristol-Myers Company | Prevention of analgesic abuse |
HU190619B (en) | 1983-11-11 | 1986-09-29 | Bezzegh,Denes,Hu | Process for producing tablets with controlled dissolution of active ingredients |
EP0164669B1 (fr) | 1984-06-13 | 1991-01-23 | Röhm Gmbh | Procédé pour enrober des formes pharmaceutiques |
US4769372A (en) | 1986-06-18 | 1988-09-06 | The Rockefeller University | Method of treating patients suffering from chronic pain or chronic cough |
GB8626098D0 (en) † | 1986-10-31 | 1986-12-03 | Euro Celtique Sa | Controlled release hydromorphone composition |
EP0352361A1 (fr) † | 1988-07-29 | 1990-01-31 | The Rockefeller University | Procédé pour traiter des patients souffrant de douleurs chroniques ou de toux chronique |
FR2653337B1 (fr) | 1989-10-23 | 1992-02-07 | Dow Corning Sa | Element a liberation prolongee et procede pour le fabriquer. |
US5662933A (en) | 1993-09-09 | 1997-09-02 | Edward Mendell Co., Inc. | Controlled release formulation (albuterol) |
US5965161A (en) | 1994-11-04 | 1999-10-12 | Euro-Celtique, S.A. | Extruded multi-particulates |
DE4443105C2 (de) | 1994-12-03 | 1997-03-13 | Hoechst Ag | Verfahren zur Herstellung Molsidomin-haltiger Tabletten |
US6488961B1 (en) | 1996-09-20 | 2002-12-03 | Ethypharm, Inc. | Effervescent granules and methods for their preparation |
DE19651551C2 (de) * | 1996-12-11 | 2000-02-03 | Klinge Co Chem Pharm Fab | Opioidantagonisthaltige galenische Formulierung |
CA2270975C (fr) | 1997-07-02 | 2003-04-01 | Euro-Celtique, S.A. | Formulations de tramadol stabilisees a liberation prolongee |
PT1685839E (pt) | 1997-12-22 | 2013-07-08 | Euro Celtique Sa | Forma de dosagem farmacêutica por via oral compreendendo uma combinação de um agonista opióide e de um antagonista opióide |
ECSP003314A (es) | 2000-01-11 | 2000-03-22 | Formulaciones medicamentosas retardadas que contienen una combinacion de un opioide y un - agonista | |
US6716449B2 (en) | 2000-02-08 | 2004-04-06 | Euro-Celtique S.A. | Controlled-release compositions containing opioid agonist and antagonist |
AU776904B2 (en) | 2000-02-08 | 2004-09-23 | Euro-Celtique S.A. | Controlled-release compositions containing opioid agonist and antagonist |
US20040115133A1 (en) | 2000-05-10 | 2004-06-17 | Wermeling Daniel P. | Intranasal opioid compositions |
GB0102342D0 (en) | 2001-01-30 | 2001-03-14 | Smithkline Beecham Plc | Pharmaceutical formulation |
WO2002092059A1 (fr) * | 2001-05-11 | 2002-11-21 | Endo Pharmaceuticals, Inc. | Forme posologique d'opioides empechant la consommation abusive |
DE60238756D1 (de) * | 2001-05-11 | 2011-02-10 | Endo Pharmaceuticals Inc | Opioid enthaltende arzneiform gegen missbrauch |
CA2449519A1 (fr) | 2001-06-08 | 2002-12-19 | Endo Pharmaceuticals, Inc. | Formes posologiques a liberation controlee utilisant un polymere acrylique, et leur procede d'obtention |
JP2005501067A (ja) | 2001-08-06 | 2005-01-13 | ユーロ−セルティーク,エス.エイ. | オピオイドの乱用を防ぐための組成物および方法 |
JP4504013B2 (ja) * | 2001-08-06 | 2010-07-14 | ユーロ−セルティーク エス.エイ. | 放出可能な及び封鎖されたアンタゴニストを有するオピオイドアゴニスト製剤 |
US7332182B2 (en) * | 2001-08-06 | 2008-02-19 | Purdue Pharma L.P. | Pharmaceutical formulation containing opioid agonist, opioid antagonist and irritant |
ES2345327T3 (es) | 2001-08-23 | 2010-09-21 | N.V. Organon | Proceso para la preparacion de un derivado de 14-hidroxinormorfinona. |
DE10146275A1 (de) | 2001-09-18 | 2003-04-24 | Gruenenthal Gmbh | Kombination ausgewählter Opioide mit Muscarin-Antagonisten zur Therapie der Harninkontinenz |
DE20308437U1 (de) | 2002-04-05 | 2003-11-13 | Euroceltique S.A., Luxemburg/Luxembourg | Matrix zur verzögerten, gleichbleibenden und unabhängigen Freisetzung von Wirkstoffen |
DE10215131A1 (de) * | 2002-04-05 | 2003-10-16 | Euro Celtique Sa | Matrix zur verzögerten, gleichbleibenden und unabhängigen Freisetzung von Wirkstoffen |
JP2005538973A (ja) | 2002-07-04 | 2005-12-22 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | 異なる2種類のポリマーマトリックスを含んで成る固体分散体 |
SI2368553T1 (sl) | 2003-04-08 | 2015-05-29 | Progenics Pharmaceuticals, Inc. | Farmacevtske formulacije, vsebujoče metilnatrekson |
RU2373936C2 (ru) | 2003-04-08 | 2009-11-27 | Проджиникс Фармасьютикалз, Инк. | Применение метилналтрексона для лечения синдрома раздраженного кишечника |
JP2006522819A (ja) | 2003-04-08 | 2006-10-05 | プロジェニックス ファーマシューティカルズ,インコーポレーテッド | 緩下薬および末梢オピオイドアンタゴニストを組み合わせた便秘の組み合わせ療法 |
KR101159828B1 (ko) | 2003-04-30 | 2012-07-04 | 퍼듀 퍼머 엘피 | 활성제 구성요소 및 활성제 층의 원위부에 억제제 구성요소를 포함하는 내변조성 경피제형 |
US9114199B2 (en) | 2003-07-31 | 2015-08-25 | Boston Scientific Scimed, Inc. | Implantable or insertable medical devices containing acrylic copolymer for controlled delivery of therapeutic agent |
US20050079221A1 (en) | 2003-10-10 | 2005-04-14 | Groenewoud Pieter Jurjen | Ibuprofen narcotic composition and method for making same |
US20050232987A1 (en) | 2004-03-12 | 2005-10-20 | Viswanathan Srinivasan | Dosage form containing a morphine derivative and another drug |
US20050165038A1 (en) | 2004-01-22 | 2005-07-28 | Maxwell Gordon | Analgetic dosage forms that are resistant to parenteral and inhalation dosing and have reduced side effects |
GEP20084454B (en) | 2004-02-06 | 2008-08-10 | Euro Celtique Sa | Methods for making 3-o-protected morphinones and 3-o-protected morphinone dienol carboxylates |
TWI350762B (en) | 2004-02-12 | 2011-10-21 | Euro Celtique Sa | Particulates |
US9016221B2 (en) | 2004-02-17 | 2015-04-28 | University Of Florida Research Foundation, Inc. | Surface topographies for non-toxic bioadhesion control |
TWI483944B (zh) | 2004-03-30 | 2015-05-11 | Euro Celtique Sa | 含有小於25ppm14-羥可待因酮之羥可酮鹽酸鹽組成物、醫藥劑型、延遲釋出口服劑型及醫藥上可以接受的包裝 |
US7700626B2 (en) | 2004-06-04 | 2010-04-20 | Adolor Corporation | Compositions containing opioid antagonists |
EP1604666A1 (fr) | 2004-06-08 | 2005-12-14 | Euro-Celtique S.A. | Opioides pour le traitement de la bronchopneumopathie chronique obstructive |
EP1604667A1 (fr) | 2004-06-08 | 2005-12-14 | Euro-Celtique S.A. | Opioides pour le traitement des impatiences des membres inférieurs |
GB2418854B (en) | 2004-08-31 | 2009-12-23 | Euro Celtique Sa | Multiparticulates |
EP1814528A2 (fr) | 2004-10-08 | 2007-08-08 | Rubicon Research Private Limited | Procede pour fabriquer des compositions fortement compressible a delivrance controllee de metformine |
GB0423103D0 (en) | 2004-10-19 | 2004-11-17 | Boots Healthcare Int Ltd | Therapeutic agents |
WO2006078842A1 (fr) | 2005-01-20 | 2006-07-27 | Progenics Pharmaceuticals, Inc. | Utilisation de methylnaltrexone et de composes apparentes pour traiter un dysfonctionnement gastrointestinal post-operatoire |
EP1771160A2 (fr) | 2005-01-28 | 2007-04-11 | Euroceltique S.A. | Formes posologiques resistant a l'extraction alcoolique |
EP1695700A1 (fr) | 2005-02-28 | 2006-08-30 | Euro-Celtique S.A. | Forme posologique contenant de l'oxycodone et de la naloxone |
NL1028460C2 (nl) * | 2005-03-04 | 2006-09-06 | Sara Lee De Nv | Inrichting voor het bereiden en afgeven van al dan niet althans gedeeltelijk opgeschuimde dranken. |
JP4741865B2 (ja) | 2005-03-24 | 2011-08-10 | 共和薬品工業株式会社 | ペルゴリド錠剤の製造方法 |
US20070026025A1 (en) | 2005-04-12 | 2007-02-01 | Aquegel Cosmetics, Llc | Topical ointment and method for making and using same |
TWI366460B (en) | 2005-06-16 | 2012-06-21 | Euro Celtique Sa | Cannabinoid active pharmaceutical ingredient for improved dosage forms |
WO2007013047A2 (fr) | 2005-07-29 | 2007-02-01 | Ranbaxy Laboratories Limited | Compositions pharmaceutiques anti-retrovirales dispersibles dans l'eau |
US20070048364A1 (en) | 2005-08-04 | 2007-03-01 | Yingxu Peng | Free flowing granules containing carbomer |
DE102005047561A1 (de) | 2005-10-04 | 2007-04-05 | Bayer Healthcare Ag | Feste, oral applizierbare pharmazeutische Darreichungsformen mit schneller Wirkstofffreisetzung |
PL1962808T3 (pl) | 2005-12-14 | 2011-03-31 | Hoffmann La Roche | Preparat proleku przeciw HCV |
US20070141147A1 (en) | 2005-12-21 | 2007-06-21 | Auriga Laboratories, Inc. | Sequential release pharmaceutical formulations |
EP1813276A1 (fr) | 2006-01-27 | 2007-08-01 | Euro-Celtique S.A. | Formes de dosage inviolables |
US7799790B2 (en) | 2006-07-20 | 2010-09-21 | Helm Ag | Amorphous aripiprazole and process for the preparation thereof |
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 |
DE102006051020A1 (de) | 2006-10-26 | 2008-04-30 | Evonik Röhm Gmbh | Verwendung von (Meth)acrylat-Copolymeren in Retard-Arzneiformen zur Verringerung des Einflusses von Ethanol auf die Wirkstofffreisetzung |
GB2447898B (en) | 2007-03-24 | 2011-08-17 | Reckitt Benckiser Healthcare | A tablet having improved stability with at least two actives |
ES2475199T3 (es) | 2008-09-16 | 2014-07-10 | Imuneks Farma Ila� Sanayi Ve Ticaret A.S. | Uso de antagonistas opioides para la preparación de un medicamento en el tratamiento de enfermedades degenerativas de la retina |
CA2737257C (fr) | 2008-09-18 | 2016-11-15 | Purdue Pharma L.P. | Formes galeniques comprenant de la poly(.epsilon.-caprolactone) |
PL2326313T3 (pl) | 2008-09-24 | 2015-08-31 | Evonik Roehm Gmbh | Kompozycja farmaceutyczna o zależnym od pH kontrolowanym uwalnianiu dla nieopioidów z odpornością przed wpływem etanolu |
BRPI0823096B8 (pt) | 2008-09-24 | 2022-07-05 | Evonik Roehm Gmbh | composição farmacêutica de opióide de liberação controlada, dependente do ph, com resistência contra a influência do etanol, processo para sua preparação, e seu uso |
CN102281876A (zh) | 2008-10-30 | 2011-12-14 | 格吕伦塔尔有限公司 | 新型有效的他喷他多剂型 |
US20100143486A1 (en) | 2008-12-10 | 2010-06-10 | Nipun Davar | Polyethylene glycol-coated sodium carbonate as a pharmaceutical excipient and compositions produced from the same |
US8362029B2 (en) | 2008-12-31 | 2013-01-29 | Upsher-Smith Laboratories, Inc. | Opioid-containing oral pharmaceutical compositions and methods |
EP2385943A4 (fr) | 2009-01-09 | 2012-05-30 | Harvard College | Composés fluorés et leurs procédés d'utilisation |
EP2389159A1 (fr) | 2009-01-22 | 2011-11-30 | Noramco, Inc. | Procédé de préparation de particules d'opioïdes et compositions ainsi obtenues |
EP2393487B1 (fr) | 2009-02-06 | 2016-11-02 | Egalet Ltd. | Compositions pharmaceutiques résistant à une maltraitance |
EP2398808B1 (fr) | 2009-02-17 | 2013-11-20 | Mallinckrodt LLC | Procédé d'alkylation réductrice des normorphinanes |
EP2398805A1 (fr) | 2009-02-23 | 2011-12-28 | Mallinckrodt LLC | Sels quaternaires de (+)-morphinane et procédés de préparation |
US8563727B2 (en) | 2009-02-23 | 2013-10-22 | Mallinckrodt Llc | (+)-morphinanium N-oxides and processes for their production |
US20100227876A1 (en) | 2009-03-06 | 2010-09-09 | Rechfensen Llp | Methods of Reducing Side Effects of Analgesics |
PT2405915T (pt) | 2009-03-10 | 2019-01-29 | Euro Celtique Sa | Composições farmacêuticas de libertação imediata compreendendo oxicodona e naloxona |
EP2408436B1 (fr) | 2009-03-18 | 2017-02-22 | Evonik Röhm GmbH | Composition pharmaceutique à libération controlée avec résistance contre l'influence de l'éthanol au moyen d'un enrobage comportant des polymères vinyliques et excipients neutres |
JP5619131B2 (ja) | 2009-03-18 | 2014-11-05 | エボニック レーム ゲゼルシャフト ミット ベシュレンクテル ハフツングEvonik RoehmGmbH | ポリマー混合物と賦形剤とを含むコーティングを使用するエタノールの影響に対する耐性を有する制御放出性医薬組成物 |
EP2413937A1 (fr) | 2009-04-02 | 2012-02-08 | Shire LLC | Nouveaux promédicaments d'opioïdes à base d'acide aminé et de peptide liés à l'acide dicarboxylique et leurs utilisations |
EP2419398A4 (fr) | 2009-04-14 | 2012-11-28 | Infiniton Ab | Promédicament comprenant un acide bêta-céto carboxylique, un sel d'acide bêta-céto carboxylique ou un ester d'acide bêta-céto carboxylique pour l'administration de médicament |
US20100291151A1 (en) | 2009-04-21 | 2010-11-18 | Auspex Pharmaceuticals, Inc. | 1-methylpyrazole modulators of substance p, calcitonin gene-related peptide, adrenergic receptor, and/or 5-ht receptor |
EP2421507B1 (fr) | 2009-04-24 | 2019-01-23 | Fertin Pharma A/S | Gomme à mâcher et matière particulaire pour la libération contrôlée de principes actifs |
WO2010141505A1 (fr) | 2009-06-01 | 2010-12-09 | Protect Pharmaceutical Corporation | Systèmes d'administration résistants aux abus |
GB0909680D0 (en) | 2009-06-05 | 2009-07-22 | Euro Celtique Sa | Dosage form |
WO2010144641A1 (fr) | 2009-06-11 | 2010-12-16 | Mallinckrodt Inc. | Préparation de morphinanes 6-alpha-amino n-substitués par transfert catalytique d'hydrogène |
FR2946533A1 (fr) | 2009-06-12 | 2010-12-17 | Ethypharm Sa | Reduction des fluctuations plasmatiques d'opioides. |
WO2011009020A2 (fr) | 2009-07-16 | 2011-01-20 | Mallinckrodt Inc. | Composés et compositions pour une utilisation en photothérapie et dans le traitement d'une maladie néovasculaire oculaire et de cancers |
ES2560210T3 (es) | 2009-07-22 | 2016-02-17 | Grünenthal GmbH | Forma de dosificación resistente a la manipulación para opiádes sensibles a la oxidación |
CN102573805A (zh) | 2009-07-22 | 2012-07-11 | 格吕伦塔尔有限公司 | 热熔挤出的控制释放剂型 |
GB0914338D0 (en) | 2009-08-17 | 2009-09-30 | Johnson Matthey Plc | Improved process |
CN102695545B (zh) | 2009-09-08 | 2016-08-17 | 特色疗法股份有限公司 | 包括酶可剪切的酮改性的阿片样物质药物前体以及其可任选的抑制剂的组合物 |
CA2775890C (fr) | 2009-09-30 | 2016-06-21 | Acura Pharmaceuticals, Inc. | Procedes et compositions de dissuasion d'abus |
WO2011041470A2 (fr) | 2009-09-30 | 2011-04-07 | Mallinckrodt Inc. | Compositions à libération prolongée d'opiacé et de dérivés d'opiacé |
EP2568968B1 (fr) | 2010-05-10 | 2017-07-12 | Euro-Celtique S.A. | Fabrication de granules libres de principes actifs et comprimés les contenant |
US9901540B2 (en) | 2010-05-10 | 2018-02-27 | Euro-Celtique S.A. | Combination of active loaded granules with additional actives |
CN102946870A (zh) | 2010-05-10 | 2013-02-27 | 欧洲凯尔特公司 | 包含氢吗啡酮和纳洛酮的药物组合物 |
GB201020895D0 (en) | 2010-12-09 | 2011-01-26 | Euro Celtique Sa | Dosage form |
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