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)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Emergency Medicine (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- 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)
Priority Applications (1)
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| AU2016202846A AU2016202846B2 (en) | 2012-03-02 | 2016-05-04 | Tamper resistant immediate release formulations |
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| US201261606156P | 2012-03-02 | 2012-03-02 | |
| US61/606,156 | 2012-03-02 | ||
| US201261724141P | 2012-11-08 | 2012-11-08 | |
| 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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| AU2013203493A1 AU2013203493A1 (en) | 2013-09-19 |
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| AU2016202846A Active AU2016202846B2 (en) | 2012-03-02 | 2016-05-04 | Tamper resistant immediate release formulations |
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| AU2016202846A Active AU2016202846B2 (en) | 2012-03-02 | 2016-05-04 | Tamper resistant immediate release formulations |
Country Status (21)
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| EP (2) | EP2819653B1 (OSRAM) |
| JP (2) | JP6199321B2 (OSRAM) |
| CN (2) | CN104144681A (OSRAM) |
| AR (1) | AR090218A1 (OSRAM) |
| AU (2) | AU2013203493B2 (OSRAM) |
| CA (1) | CA2852042C (OSRAM) |
| CL (1) | CL2014002283A1 (OSRAM) |
| EA (1) | EA028224B1 (OSRAM) |
| ES (2) | ES2619574T3 (OSRAM) |
| IL (1) | IL234256B (OSRAM) |
| IN (1) | IN2014MN01901A (OSRAM) |
| MX (1) | MX354677B (OSRAM) |
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| PH (1) | PH12014501910A1 (OSRAM) |
| SG (1) | SG11201405011PA (OSRAM) |
| TW (2) | TW201722406A (OSRAM) |
| UY (1) | UY34651A (OSRAM) |
| WO (1) | WO2013128276A2 (OSRAM) |
| ZA (1) | ZA201405960B (OSRAM) |
Families Citing this family (54)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7776314B2 (en) | 2002-06-17 | 2010-08-17 | Grunenthal Gmbh | Abuse-proofed dosage system |
| ATE495732T1 (de) | 2003-03-26 | 2011-02-15 | Egalet As | Morphin-system mit kontrollierter freisetzung |
| DE10336400A1 (de) | 2003-08-06 | 2005-03-24 | Grünenthal GmbH | Gegen Missbrauch gesicherte Darreichungsform |
| US20070048228A1 (en) | 2003-08-06 | 2007-03-01 | Elisabeth Arkenau-Maric | Abuse-proofed dosage form |
| DE102005005446A1 (de) | 2005-02-04 | 2006-08-10 | Grünenthal GmbH | Bruchfeste Darreichungsformen mit retardierter Freisetzung |
| DE10361596A1 (de) | 2003-12-24 | 2005-09-29 | Grünenthal GmbH | Verfahren zur Herstellung einer gegen Missbrauch gesicherten Darreichungsform |
| 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 |
| EP2124556B1 (en) | 2006-10-09 | 2014-09-03 | Charleston Laboratories, Inc. | Pharmaceutical compositions |
| CA2905541C (en) | 2008-01-09 | 2020-02-11 | Charleston Laboratories, Inc. | Pharmaceutical compositions comprising an antiemetic and an opioid analgesic |
| NZ586792A (en) | 2008-01-25 | 2012-09-28 | Gruenenthal Chemie | Tamper resistant controlled release pharmaceutical tablets form having convex and concave surfaces |
| EP2393484A1 (en) | 2009-02-06 | 2011-12-14 | Egalet Ltd. | Immediate release composition resistant to abuse by intake of alcohol |
| EP2445487A2 (en) | 2009-06-24 | 2012-05-02 | Egalet Ltd. | Controlled release formulations |
| EP3311667A1 (en) | 2009-07-08 | 2018-04-25 | Charleston Laboratories, Inc. | Pharmaceutical compositions |
| ES2534908T3 (es) | 2009-07-22 | 2015-04-30 | Grünenthal GmbH | Forma de dosificación de liberación controlada extruida por fusión en caliente |
| PL2456424T3 (pl) | 2009-07-22 | 2013-12-31 | Gruenenthal Gmbh | Stabilizowana przed utlenianiem odporna na naruszenie postać dawkowania |
| PL2611425T3 (pl) | 2010-09-02 | 2014-09-30 | Gruenenthal Gmbh | Odporna na ingerencję postać dawki zawierająca polimer anionowy |
| PE20131102A1 (es) | 2010-09-02 | 2013-10-12 | Gruenenthal Chemie | Forma de dosificacion resistente a manipulacion que comprende una sal inorganica |
| NO2736497T3 (OSRAM) | 2011-07-29 | 2018-01-20 | ||
| CA2839123A1 (en) | 2011-07-29 | 2013-02-07 | Grunenthal Gmbh | Tamper-resistant tablet providing immediate drug release |
| WO2013127831A1 (en) | 2012-02-28 | 2013-09-06 | Grünenthal GmbH | Tamper-resistant dosage form comprising pharmacologically active compound and anionic polymer |
| DK2838512T3 (en) | 2012-04-18 | 2018-11-19 | Gruenenthal Gmbh | MANIPULATED AND DOSAGE DUMPED PHARMACEUTICAL DOSAGE FORM |
| US10064945B2 (en) | 2012-05-11 | 2018-09-04 | Gruenenthal Gmbh | Thermoformed, tamper-resistant pharmaceutical dosage form containing zinc |
| AU2014273227B2 (en) | 2013-05-29 | 2019-08-15 | Grunenthal Gmbh | Tamper-resistant dosage form containing one or more particles |
| JP6466417B2 (ja) | 2013-05-29 | 2019-02-06 | 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 | 二峰性放出プロファイルを有する改変防止（ｔａｍｐｅｒ−ｒｅｓｉｓｔａｎｔ）剤形 |
| BR112016000194A8 (pt) | 2013-07-12 | 2019-12-31 | Gruenenthal Gmbh | forma de dosagem resistente à violação contendo o polímero de acetato de etileno-vinila |
| AU2014306759B2 (en) | 2013-08-12 | 2018-04-26 | 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 |
| EA032013B1 (ru) * | 2013-10-31 | 2019-03-29 | Сайма Лэбс Инк. | Препятствующие злоупотреблению гранулированные лекарственные формы с немедленным высвобождением |
| US20150118300A1 (en) | 2013-10-31 | 2015-04-30 | Cima Labs Inc. | Immediate Release Abuse-Deterrent Granulated Dosage Forms |
| WO2015078891A1 (en) | 2013-11-26 | 2015-06-04 | Farmaceutici Formenti S.P.A. | Preparation of a powdery pharmaceutical composition by means of cryo-milling |
| US9492444B2 (en) | 2013-12-17 | 2016-11-15 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded extended release abuse deterrent pill |
| WO2015095391A1 (en) | 2013-12-17 | 2015-06-25 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded extended release abuse deterrent pill |
| CA2938699A1 (en) | 2014-02-05 | 2015-08-13 | Kashiv Pharma Llc | Abuse-resistant drug formulations with built-in overdose protection |
| US9616029B2 (en) * | 2014-03-26 | 2017-04-11 | Sun Pharma Advanced Research Company Ltd. | Abuse deterrent immediate release coated reservoir solid dosage form |
| CN106572980A (zh) | 2014-05-12 | 2017-04-19 | 格吕伦塔尔有限公司 | 包含他喷他多的防篡改即释胶囊制剂 |
| EA201692388A1 (ru) | 2014-05-26 | 2017-05-31 | Грюненталь Гмбх | Лекарственная форма в виде множества частиц, защищенная от вызываемого этанолом сброса дозы |
| WO2016010771A1 (en) | 2014-07-17 | 2016-01-21 | 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 |
| CA2964628A1 (en) | 2014-10-20 | 2016-04-28 | 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 |
| CA2983638A1 (en) * | 2015-04-24 | 2016-10-27 | Grunenthal Gmbh | Tamper-resistant fixed dose combination providing fast release of two drugs from particles and a powder |
| MX2017013633A (es) * | 2015-04-24 | 2018-03-08 | Gruenenthal Gmbh | Combinacion de dosis fija resistente a la manipulacion que proporciona una liberacion rapida de dos farmacos desde particulas. |
| MX2017013637A (es) | 2015-04-24 | 2018-03-08 | Gruenenthal Gmbh | Forma de dosificacion resistente a alteraciones con liberacion inmediata y resistencia contra la extraccion por solventes. |
| MX2017013643A (es) * | 2015-04-24 | 2018-03-08 | Gruenenthal Gmbh | Combinacion de dosis fija resistente a la manipulacion que proporciona una liberacion rapida de dos farmacos desde particulas y una matriz. |
| MX2017013636A (es) * | 2015-04-24 | 2018-03-08 | Gruenenthal Gmbh | Combinacion de dosis fija resistente a la manipulacion que proporciona una liberacion rapida de dos farmacos desde diferentes particulas. |
| WO2016200960A1 (en) * | 2015-06-09 | 2016-12-15 | KVK-Tech, Inc. | Abuse deterrent pharmaceutical compositions |
| CA2998259A1 (en) | 2015-09-10 | 2017-03-16 | Grunenthal 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 |
| CA3047325A1 (en) * | 2016-12-21 | 2018-06-28 | Tioga Pharmaceuticals Inc. | Solid pharmaceutical formulations of asimadoline |
| JP2020536892A (ja) | 2017-10-09 | 2020-12-17 | ローズ ファーマシューティカルズ エル．ピー． | 医薬レジネート組成物、それを作製する方法、およびその使用 |
| US20220062200A1 (en) | 2019-05-07 | 2022-03-03 | Clexio Biosciences Ltd. | Abuse-deterrent dosage forms containing esketamine |
| WO2020225773A1 (en) | 2019-05-07 | 2020-11-12 | Clexio Biosciences Ltd. | Abuse-deterrent dosage forms containing esketamine |
| EP4333646A2 (en) * | 2021-05-03 | 2024-03-13 | Cambridge Glycoscience Ltd | Soluble and insoluble saccharide compositions and related methods |
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 |
| WO2003013476A1 (en) * | 2001-08-06 | 2003-02-20 | Euro-Celtique S.A. | Compositions and methods to prevent abuse of opioids |
| 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 |
| 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 |
| US20100151034A1 (en) * | 2008-09-30 | 2010-06-17 | Astellas Pharma Inc. | Granular pharmaceutical composition of atorvastatin for oral administration |
| ES2569925T3 (es) | 2009-09-30 | 2016-05-13 | Acura Pharmaceuticals, Inc. | Métodos y composiciones de disuasión del abuso |
| WO2011051155A2 (en) * | 2009-10-28 | 2011-05-05 | Basf Se | Stable protective coatings for pharmaceutical dosage forms |
| AU2012275115A1 (en) | 2011-06-29 | 2014-01-30 | Allergan, Inc. | Macrogol 15 hydroxystearate formulations |
-
2013
- 2013-03-01 CA CA2852042A patent/CA2852042C/en active Active
- 2013-03-01 EP EP13713496.1A patent/EP2819653B1/en active Active
- 2013-03-01 AU AU2013203493A patent/AU2013203493B2/en active Active
- 2013-03-01 JP JP2014559310A patent/JP6199321B2/ja active Active
- 2013-03-01 WO PCT/IB2013/000444 patent/WO2013128276A2/en not_active Ceased
- 2013-03-01 PE PE2014001346A patent/PE20142320A1/es not_active Application Discontinuation
- 2013-03-01 EA EA201400972A patent/EA028224B1/ru not_active IP Right Cessation
- 2013-03-01 ES ES13713496.1T patent/ES2619574T3/es active Active
- 2013-03-01 CN CN201380012104.8A patent/CN104144681A/zh active Pending
- 2013-03-01 CN CN201910170603.9A patent/CN109820830A/zh active Pending
- 2013-03-01 ES ES17150886T patent/ES2821773T3/es active Active
- 2013-03-01 AR ARP130100669A patent/AR090218A1/es unknown
- 2013-03-01 TW TW105127500A patent/TW201722406A/zh unknown
- 2013-03-01 TW TW102107275A patent/TWI614037B/zh not_active IP Right Cessation
- 2013-03-01 MX MX2014010534A patent/MX354677B/es active IP Right Grant
- 2013-03-01 EP EP17150886.4A patent/EP3170492B1/en active Active
- 2013-03-01 UY UY0001034651A patent/UY34651A/es not_active Application Discontinuation
- 2013-03-01 NZ NZ629468A patent/NZ629468A/en not_active IP Right Cessation
- 2013-03-01 SG SG11201405011PA patent/SG11201405011PA/en unknown
- 2013-03-01 US US14/377,900 patent/US11173155B2/en active Active
- 2013-03-01 IN IN1901MUN2014 patent/IN2014MN01901A/en unknown
-
2014
- 2014-08-14 ZA ZA2014/05960A patent/ZA201405960B/en unknown
- 2014-08-21 IL IL234256A patent/IL234256B/en active IP Right Grant
- 2014-08-22 PH PH12014501910A patent/PH12014501910A1/en unknown
- 2014-08-28 CL CL2014002283A patent/CL2014002283A1/es unknown
-
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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