AU2013203493B2 - Tamper resistant immediate release formulations - Google Patents
Tamper resistant immediate release formulations Download PDFInfo
- Publication number
- AU2013203493B2 AU2013203493B2 AU2013203493A AU2013203493A AU2013203493B2 AU 2013203493 B2 AU2013203493 B2 AU 2013203493B2 AU 2013203493 A AU2013203493 A AU 2013203493A AU 2013203493 A AU2013203493 A AU 2013203493A AU 2013203493 B2 AU2013203493 B2 AU 2013203493B2
- Authority
- AU
- Australia
- Prior art keywords
- dosage form
- immediate release
- solid oral
- active agent
- oral dosage
- 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.)
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- A61K9/5073—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
- A61K9/5078—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings with drug-free core
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
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- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
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- Biomedical Technology (AREA)
- Emergency Medicine (AREA)
- Biophysics (AREA)
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- Pain & Pain Management (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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| US61/724,141 | 2012-11-08 | ||
| PCT/IB2013/000444 WO2013128276A2 (en) | 2012-03-02 | 2013-03-01 | Tamper resistant immediate release formulations |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7776314B2 (en) | 2002-06-17 | 2010-08-17 | Grunenthal Gmbh | Abuse-proofed dosage system |
| ES2570454T3 (es) | 2003-03-26 | 2016-05-18 | Egalet Ltd | Sistema de liberación controlada de morfina |
| DE102005005446A1 (de) | 2005-02-04 | 2006-08-10 | Grünenthal GmbH | Bruchfeste Darreichungsformen mit retardierter Freisetzung |
| DE10336400A1 (de) | 2003-08-06 | 2005-03-24 | Grünenthal GmbH | Gegen Missbrauch gesicherte Darreichungsform |
| DE10361596A1 (de) | 2003-12-24 | 2005-09-29 | Grünenthal GmbH | Verfahren zur Herstellung einer gegen Missbrauch gesicherten Darreichungsform |
| US20070048228A1 (en) | 2003-08-06 | 2007-03-01 | Elisabeth Arkenau-Maric | Abuse-proofed dosage form |
| 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 |
| JP2010522135A (ja) | 2006-10-09 | 2010-07-01 | チャールストン ラボラトリーズ，インコーポレイテッド | 医薬組成物 |
| JP5714910B2 (ja) | 2008-01-09 | 2015-05-07 | チャールストン ラボラトリーズ，インコーポレイテッド | 薬学的組成物 |
| NZ586792A (en) | 2008-01-25 | 2012-09-28 | Gruenenthal Chemie | Tamper resistant controlled release pharmaceutical tablets form having convex and concave surfaces |
| AU2010211220B2 (en) | 2009-02-06 | 2013-08-01 | Egalet Ltd. | Immediate release composition resistant to abuse by intake of alcohol |
| CA2766179A1 (en) | 2009-06-24 | 2010-12-29 | Egalet Ltd. | Controlled release formulations |
| EP3311667A1 (en) | 2009-07-08 | 2018-04-25 | Charleston Laboratories, Inc. | Pharmaceutical compositions |
| EP2456427B1 (en) | 2009-07-22 | 2015-03-04 | Grünenthal GmbH | Hot-melt extruded controlled release dosage form |
| RU2555531C2 (ru) | 2009-07-22 | 2015-07-10 | Грюненталь Гмбх | Защищенная от применения не по назначению лекарственная форма для чувствительных к окислению опиоидов |
| PE20131102A1 (es) | 2010-09-02 | 2013-10-12 | Gruenenthal Chemie | Forma de dosificacion resistente a manipulacion que comprende una sal inorganica |
| NZ608865A (en) | 2010-09-02 | 2015-03-27 | Gruenenthal Chemie | Tamper resistant dosage form comprising an anionic polymer |
| CN103857386A (zh) | 2011-07-29 | 2014-06-11 | 格吕伦塔尔有限公司 | 提供药物立即释放的抗破碎片剂 |
| NO2736495T3 (cg-RX-API-DMAC7.html) | 2011-07-29 | 2018-01-20 | ||
| BR112014019988A8 (pt) | 2012-02-28 | 2017-07-11 | Gruenenthal Gmbh | Forma de dosagem resistente a socamento compreendendo um composto farmacologicamente ativo e um polímero aniônico |
| AR090695A1 (es) | 2012-04-18 | 2014-12-03 | Gruenenthal Gmbh | Forma de dosificacion farmaceutica resistente a la adulteracion y resistente a la liberacion inmediata de la dosis |
| US10064945B2 (en) | 2012-05-11 | 2018-09-04 | Gruenenthal Gmbh | Thermoformed, tamper-resistant pharmaceutical dosage form containing zinc |
| WO2014191397A1 (en) | 2013-05-29 | 2014-12-04 | Grünenthal GmbH | Tamper-resistant dosage form containing one or more particles |
| AR096439A1 (es) | 2013-05-29 | 2015-12-30 | Gruenenthal Gmbh | Forma de dosificación resistente al uso indebido que contiene una o más partículas |
| CA2917136C (en) | 2013-07-12 | 2022-05-31 | Grunenthal Gmbh | Tamper-resistant dosage form containing ethylene-vinyl acetate polymer |
| CA2919892C (en) | 2013-08-12 | 2019-06-18 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded immediate release abuse deterrent pill |
| US9770514B2 (en) | 2013-09-03 | 2017-09-26 | ExxPharma Therapeutics LLC | Tamper-resistant pharmaceutical dosage forms |
| US20150118300A1 (en) * | 2013-10-31 | 2015-04-30 | Cima Labs Inc. | Immediate Release Abuse-Deterrent Granulated Dosage Forms |
| EP3062778A4 (en) * | 2013-10-31 | 2017-07-19 | Cima Labs Inc. | Immediate release abuse-deterrent granulated dosage forms |
| JP6480936B2 (ja) | 2013-11-26 | 2019-03-13 | 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 | クライオミリングによる粉末状医薬組成物の調製 |
| WO2015095391A1 (en) | 2013-12-17 | 2015-06-25 | 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 |
| WO2015120201A1 (en) | 2014-02-05 | 2015-08-13 | Kashiv Pharma, Llc | Abuse-resistant drug formulations with built-in overdose protection |
| CA2943728C (en) * | 2014-03-26 | 2020-03-24 | Sun Pharma Advanced Research Company Ltd. | Abuse deterrent immediate release biphasic matrix solid dosage form |
| JP2017518980A (ja) | 2014-05-12 | 2017-07-13 | 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 | タペンタドールを含む、改変防止即時放出カプセル製剤 |
| US9872835B2 (en) | 2014-05-26 | 2018-01-23 | Grünenthal GmbH | Multiparticles safeguarded against ethanolic dose-dumping |
| EP3169315B1 (en) | 2014-07-17 | 2020-06-24 | Pharmaceutical Manufacturing Research Services, Inc. | Immediate release abuse deterrent liquid fill dosage form |
| US9132096B1 (en) | 2014-09-12 | 2015-09-15 | Alkermes Pharma Ireland Limited | Abuse resistant pharmaceutical compositions |
| AU2015336065A1 (en) | 2014-10-20 | 2017-05-04 | Pharmaceutical Manufacturing Research Services, Inc. | Extended release abuse deterrent liquid fill dosage form |
| WO2016094358A1 (en) * | 2014-12-08 | 2016-06-16 | Cima Labs Inc. | Immediate release abuse-deterrent granulated dosage forms |
| EP3285746A1 (en) * | 2015-04-24 | 2018-02-28 | Grünenthal GmbH | Tamper-resistant fixed dose combination providing fast release of two drugs from particles and a powder |
| AU2016251853A1 (en) * | 2015-04-24 | 2017-11-23 | Grünenthal GmbH | Tamper-resistant fixed dose combination providing fast release of two drugs from different particles |
| BR112017022856A2 (pt) * | 2015-04-24 | 2018-07-17 | Gruenenthal Gmbh | combinação de dose fixa inviolável que proporciona rápida liberação de duas drogas a partir de partículas |
| 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 |
| AU2016251302A1 (en) * | 2015-04-24 | 2017-11-23 | Grünenthal GmbH | Tamper-resistant fixed dose combination providing fast release of two drugs from particles and a matrix |
| WO2016200960A1 (en) * | 2015-06-09 | 2016-12-15 | KVK-Tech, Inc. | Abuse deterrent pharmaceutical compositions |
| US10842750B2 (en) | 2015-09-10 | 2020-11-24 | Grünenthal GmbH | Protecting oral overdose with abuse deterrent immediate release formulations |
| EP3522890A4 (en) * | 2016-10-10 | 2020-06-03 | Rhodes Pharmaceuticals L.P. | PHARMACEUTICAL RESINATE COMPOSITIONS AND METHOD FOR THE PRODUCTION AND USE THEREOF |
| WO2018119108A1 (en) * | 2016-12-21 | 2018-06-28 | Tioga Pharmaceuticals Inc. | Splid pharmaceutical formulations of asimadoline |
| EP3694555A4 (en) | 2017-10-09 | 2021-07-07 | Rhodes Pharmaceuticals L.P. | RESINATE-BASED PHARMACEUTICAL COMPOSITIONS AND THEIR MANUFACTURING AND USE PROCESSES |
| 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 |
| CN117715538A (zh) * | 2021-05-03 | 2024-03-15 | 剑桥糖质科学有限公司 | 可溶性糖和不溶性糖的组合物及相关方法 |
Citations (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6455557B1 (en) * | 2001-11-28 | 2002-09-24 | Elan Pharmaceuticals, Inc. | Method of reducing somnolence in patients treated with tizanidine |
| US20040091544A1 (en) * | 2002-11-08 | 2004-05-13 | Ruff Michael D. | Coated dibasic calcium phosphate |
| WO2004067039A1 (en) * | 2003-01-28 | 2004-08-12 | Collegium Pharmaceutical, Inc. | Multiparticulate compositions of milnacipran for oral administration |
| WO2004069135A2 (en) * | 2003-02-05 | 2004-08-19 | Ethypharm | Composition comprising a mixture of active principles, and method of preparation |
| US20050112195A1 (en) * | 2003-09-26 | 2005-05-26 | Evangeline Cruz | Drug coating providing high drug loading and methods for providing same |
| WO2005046684A1 (en) * | 2003-11-04 | 2005-05-26 | Shire Laboratories, Inc. | Once daily dosage forms of trospium |
| US20060210630A1 (en) * | 2004-09-30 | 2006-09-21 | Likan Liang | Controlled release compositions of gamma-hydroxybutyrate |
| WO2007120135A1 (en) * | 2006-04-17 | 2007-10-25 | Forest Laboratories, Inc. | Lercanidipine immediate release composition |
| WO2008012474A2 (fr) * | 2006-07-28 | 2008-01-31 | Bouchara-Recordati | Compositions pharmaceutiques de substances actives difficilement detournables de la voie d'administration a laquelle elles sont destinees |
| US20080152595A1 (en) * | 2004-11-24 | 2008-06-26 | Acura Pharmaceuticals, Inc. | Methods and compositions for deterring abuse of orally administered pharmaceutical products |
| EP1967183A1 (en) * | 2005-12-28 | 2008-09-10 | Takeda Pharmaceutical Company Limited | Controlled release solid preparation |
| US20090022798A1 (en) * | 2007-07-20 | 2009-01-22 | Abbott Gmbh & Co. Kg | Formulations of nonopioid and confined opioid analgesics |
| WO2010044842A1 (en) * | 2008-10-16 | 2010-04-22 | University Of Tennessee Research Foundation | Tamper resistant oral dosage forms containing an embolizing agent |
| WO2010066034A1 (en) * | 2008-12-12 | 2010-06-17 | Paladin Labs Inc. | Methadone formulation |
| WO2010069050A1 (en) * | 2008-12-16 | 2010-06-24 | Labopharm Inc. | Misuse preventative, controlled release formulation |
| WO2013038267A1 (en) * | 2011-09-16 | 2013-03-21 | Purdue Pharma L.P. | Tamper resistant pharmaceutical formulations |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2530563C2 (de) | 1975-07-09 | 1986-07-24 | Bayer Ag, 5090 Leverkusen | Analgetische Arzneimittel mit vermindertem Mißbrauchspotential |
| US5965161A (en) * | 1994-11-04 | 1999-10-12 | Euro-Celtique, S.A. | Extruded multi-particulates |
| US6740341B1 (en) | 1998-11-25 | 2004-05-25 | Cima Labs Inc. | Taste masking rapid release coating system |
| TWI256309B (en) * | 1999-10-13 | 2006-06-11 | Akzo Nobel Nv | New formulation of mirtazapine |
| US20030068375A1 (en) | 2001-08-06 | 2003-04-10 | Curtis Wright | Pharmaceutical formulation containing gelling agent |
| US20030044458A1 (en) * | 2001-08-06 | 2003-03-06 | Curtis Wright | Oral dosage form comprising a therapeutic agent and an adverse-effect agent |
| EP1414413A1 (en) * | 2001-08-06 | 2004-05-06 | Euro-Celtique S.A. | Compositions and methods to prevent abuse of opioids |
| US20030068276A1 (en) * | 2001-09-17 | 2003-04-10 | Lyn Hughes | Dosage forms |
| US8906413B2 (en) * | 2003-05-12 | 2014-12-09 | Supernus Pharmaceuticals, Inc. | Drug formulations having reduced abuse potential |
| US7201920B2 (en) * | 2003-11-26 | 2007-04-10 | Acura Pharmaceuticals, Inc. | Methods and compositions for deterring abuse of opioid containing dosage forms |
| TW201509943A (zh) | 2004-03-30 | 2015-03-16 | Euro Celtique Sa | 含有小於２５ｐｐｍ１４-羥可待因酮之羥可酮鹽酸鹽之組成物、醫藥劑型、延遲釋出口服劑型及醫藥上可以接受的包裝 |
| CA2608361A1 (en) * | 2005-05-13 | 2006-11-23 | Alpharma, Inc. | Morphine sulphate formulations |
| WO2007126136A2 (en) * | 2006-04-27 | 2007-11-08 | Takeda Pharmaceutical Company Limited | Mask- tasting solid preparation of pioglitazone |
| US9023400B2 (en) | 2006-05-24 | 2015-05-05 | Flamel Technologies | Prolonged-release multimicroparticulate oral pharmaceutical form |
| US20080057122A1 (en) * | 2006-08-31 | 2008-03-06 | Aaipharma Inc. | Acetaminophen pharmaceutical compositions |
| JP4707073B2 (ja) * | 2008-09-30 | 2011-06-22 | アステラス製薬株式会社 | アトルバスタチン経口投与用粒子状医薬組成物 |
| ES2569925T3 (es) | 2009-09-30 | 2016-05-13 | Acura Pharmaceuticals, Inc. | Métodos y composiciones de disuasión del abuso |
| BR112012010102B8 (pt) | 2009-10-28 | 2021-05-25 | Basf Se | material de revestimento, uso de materiais de revestimento, e, revestimentos de película para formas de dosagem farmacêuticas |
| RU2014102492A (ru) | 2011-06-29 | 2015-08-10 | Аллерган, Инк. | Композиции макрогол 15 гидроксистеарата |
-
2013
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- 2013-03-01 JP JP2014559310A patent/JP6199321B2/ja active Active
- 2013-03-01 PE PE2014001346A patent/PE20142320A1/es not_active Application Discontinuation
- 2013-03-01 MX MX2014010534A patent/MX354677B/es active IP Right Grant
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- 2013-03-01 EP EP13713496.1A patent/EP2819653B1/en active Active
- 2013-03-01 US US14/377,900 patent/US11173155B2/en active Active
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- 2014-08-21 IL IL234256A patent/IL234256B/en active IP Right Grant
- 2014-08-22 PH PH12014501910A patent/PH12014501910A1/en unknown
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2016
- 2016-05-04 AU AU2016202846A patent/AU2016202846B2/en active Active
-
2017
- 2017-08-23 JP JP2017159995A patent/JP6509287B2/ja active Active
-
2021
- 2021-10-14 US US17/501,641 patent/US12128042B2/en active Active
-
2024
- 2024-08-27 US US18/816,179 patent/US20240423974A1/en active Pending
Patent Citations (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6455557B1 (en) * | 2001-11-28 | 2002-09-24 | Elan Pharmaceuticals, Inc. | Method of reducing somnolence in patients treated with tizanidine |
| US20040091544A1 (en) * | 2002-11-08 | 2004-05-13 | Ruff Michael D. | Coated dibasic calcium phosphate |
| WO2004067039A1 (en) * | 2003-01-28 | 2004-08-12 | Collegium Pharmaceutical, Inc. | Multiparticulate compositions of milnacipran for oral administration |
| WO2004069135A2 (en) * | 2003-02-05 | 2004-08-19 | Ethypharm | Composition comprising a mixture of active principles, and method of preparation |
| US20050112195A1 (en) * | 2003-09-26 | 2005-05-26 | Evangeline Cruz | Drug coating providing high drug loading and methods for providing same |
| WO2005046684A1 (en) * | 2003-11-04 | 2005-05-26 | Shire Laboratories, Inc. | Once daily dosage forms of trospium |
| US20060210630A1 (en) * | 2004-09-30 | 2006-09-21 | Likan Liang | Controlled release compositions of gamma-hydroxybutyrate |
| US20080152595A1 (en) * | 2004-11-24 | 2008-06-26 | Acura Pharmaceuticals, Inc. | Methods and compositions for deterring abuse of orally administered pharmaceutical products |
| EP1967183A1 (en) * | 2005-12-28 | 2008-09-10 | Takeda Pharmaceutical Company Limited | Controlled release solid preparation |
| WO2007120135A1 (en) * | 2006-04-17 | 2007-10-25 | Forest Laboratories, Inc. | Lercanidipine immediate release composition |
| WO2008012474A2 (fr) * | 2006-07-28 | 2008-01-31 | Bouchara-Recordati | Compositions pharmaceutiques de substances actives difficilement detournables de la voie d'administration a laquelle elles sont destinees |
| US20090022798A1 (en) * | 2007-07-20 | 2009-01-22 | Abbott Gmbh & Co. Kg | Formulations of nonopioid and confined opioid analgesics |
| WO2010044842A1 (en) * | 2008-10-16 | 2010-04-22 | University Of Tennessee Research Foundation | Tamper resistant oral dosage forms containing an embolizing agent |
| WO2010066034A1 (en) * | 2008-12-12 | 2010-06-17 | Paladin Labs Inc. | Methadone formulation |
| WO2010069050A1 (en) * | 2008-12-16 | 2010-06-24 | Labopharm Inc. | Misuse preventative, controlled release formulation |
| WO2013038267A1 (en) * | 2011-09-16 | 2013-03-21 | Purdue Pharma L.P. | Tamper resistant pharmaceutical formulations |
Non-Patent Citations (4)
| Title |
|---|
| AL-TAANI BASHAR, M. et al., 'Effect of microenvironment pH of swellable and erodable buffered matrices on the release characteristics of diclofenac sodium.' AAPS PHARMSCITECH, 2003, vol. 4, no. 3, Article 43 * |
| ASLANI, P. et al, 'EFFECT OF GELATION CONDITIONS AND DISSOLUTION MEDIA ON THE RELEASE OF PARACETAMOL FROM ALGINATE GEL BEADS' JOURNAL OF MICROENCAPSULATION, 1996, Vol .13, No. 5, pages 601-614 * |
| HEINZE. T. et al., 'Carboxymethyl Ethers of Cellulose and Starch - A Review', MACROMOLECULAR SYMPOSIA, 2005, Vol. 223, pages 13-39 * |
| KOHANE, D. S. et al., 'pH-triggered release of macromolecules from spray-dried polymethacrylate microparticles', PHARMACEUTICAL RESEARCH, 2003, Vol . 20, No. 10 pages 1533-1538 * |
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