WO2010066034A1 - Methadone formulation - Google Patents
Methadone formulation Download PDFInfo
- Publication number
- WO2010066034A1 WO2010066034A1 PCT/CA2009/001778 CA2009001778W WO2010066034A1 WO 2010066034 A1 WO2010066034 A1 WO 2010066034A1 CA 2009001778 W CA2009001778 W CA 2009001778W WO 2010066034 A1 WO2010066034 A1 WO 2010066034A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- drug
- formulation
- drug formulation
- present
- methadone
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/485—Morphinan derivatives, e.g. morphine, codeine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
-
- 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
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
Definitions
- the present application relates generally to novel drug formulations.
- the present application relates to new formulations of a pharmaceutically acceptable salt of methadone (6-(Dimethylamino)-4,4- diphenylheptan-3-one, a synthetic opioid) having a decreased abuse potential.
- methadone 6-(Dimethylamino)-4,4- diphenylheptan-3-one, a synthetic opioid
- the application further includes a method for making this formulation.
- Drug abusers and/or addicts are known to take a dosage form containing an opioid analgesic, such as oxycodone, morphine or methadone, and crush, shear, grind, chew or dissolve it in water or in alcohol, and either heat it or make it cold in order to subsequently extract the opioid component from the mixture.
- an opioid analgesic such as oxycodone, morphine or methadone
- the extract having a significant amount or even an entire amount of the drug, becomes available for immediate absorption by 1 ) injection, 2) inhalation, or 3) oral consumption.
- gel-forming or viscosity increasing agents e.g. polyvinyl alcohol, HPMC, polyethylene oxide, etc.
- nasal tissue irritants such as sodium lauryl sulfate have been used to deter extraction of active drugs.
- emetic agents such as zinc sulfate
- pharmaceutical formulations containing an opioid agonist, opioid antagonist or a bittering agent have also been evaluated (Kumar et a/., 2007, Palermo et a/., 2001 , Kaiko et a/., 2001 , Oshlack et a/., 2003) to decrease the extractability of drugs such as methadone.
- United States Patent Publication 2006/0104909 provides examples of abuse-resistant, controlled-release pharmaceutical compositions in which an effective amount of an active compound is wetted with a coating material or distributed throughout a matrix that is insoluble in water and non-erodable at a pH less than about 6.
- Examples of gel forming polymers or viscosity increasing agents to prevent filtration are known: see, for example, United States Patent Publication No. 2007/0264327 (Acura Pharmaceuticals).
- these examples are used for extended-, controlled- or slow-release pharmaceutical products, where the active pharmaceutical ingredient is released slowly from the composition over an extended period of time (i.e., 8-24 hours).
- an oral pharmaceutical formulation that makes the extraction of an active ingredient more difficult, in particular in aqueous and alcohol solvents, and therefore prevents or at least significantly reduces the potential for abuse, while allowing the pharmaceutical formulation to release the active pharmaceutical ingredient in the gastrointestinal tract upon ingestion to allow for the desired pharmacological effect.
- the formulation includes a pharmaceutically acceptable salt of a narcotic drug, wherein the narcotic drug has a chemical structure that includes one or more positively charged, protonated amine, and an alkalizing agent.
- the present application describes formulations which are suitable for many active pharmaceutical ingredients, but is most relevant to narcotic drugs, including but not limited to the opioids oxycodone, morphine, hydromorphone, hydrocodone, and methadone, among others.
- a physicochemical property required by the active pharmaceutical agent to enable the present invention to confer decreased extractability of the drug is the need for the pharmaceutical agent to be an acidic drug with a chemical structure containing at least one positively charged protonated amine group.
- Alkalizing or basifying agents (meglumine, trisodium phosphate
- Na 3 PO 4 .12H 2 O calcium carbonate
- CaCO 3 calcium carbonate
- sodium sulfate Na 2 SO 4
- sodium bicarbonate NaHCO 3
- Alkalizing agents can be added to compounds having positively charged protonated amines to convert them to their uncharged, free bases, which are less soluble in water than the positively charged protonated amines.
- Meglumine and trisodium phosphate are strongly alkaline and are used in pharmaceutical formulations as pH adjusting agents.
- Sodium bicarbonate is also used as a buffer in tablet formulations.
- Calcium carbonate can alternatively be employed as a pharmaceutical excipient and in this situation is mainly used in solid-dosage forms as a diluent or buffer.
- alkalizing agents which may be used in formulations according to the present application may include meglumine, sodium sulfate, sodium bicarbonate, calcium carbonate, sodium hydroxide, monoethanolamine, diethanolamine, triethanolamine, potassium bicarbonate, potassium citrate, potassium hydroxide, sodium borate, sodium citrate and others with similar physicochemical characteristics generally known in the art.
- Oral dosage forms e.g. tablets, capsules or caplets
- an opioid such as methadone
- an alkalizing agent such as meglumine
- Drug formulations according to the present application can be manufactured through dry blending, through aqueous granulation or through dry granulation.
- the formulation can be in the form of a capsule, caplet, pill, or a compressed tablet.
- the formulation can be compressed or encapsulated.
- the solubility of methadone hydrochloride in water can be effected by the addition of an alkalizing agent.
- Table 1 shown below, shows the reduction in solubility of methadone hydrochloride with various alkalizing agents at different molar ratios. The percent reduction in solubility is expressed in comparison to the solubility of methadone hydrochloride without an alkalizing agent.
- an alkalizing agent is used to reduce or impede methadone solubility.
- Table 2 shows the range of compositions for standard compressible tablets that have been found to be suitable for this purpose. They include standard compressible tablet diluents and disintegrants, fillers, and lubricants, as are generally known in the art.
- Table 3 illustrates meglumine-based formulations according to an aspect of the present application. These formulations include standard compressible tablet diluents and disintegrants, fillers and lubricants, as are known generally in the art. Table 3: Abuse-Resistant Methadone-Meglumine Formulations
- Table 4 shows a particular embodiment of a tablet formulation according to the present application.
- a pharmaceutically-acceptable colorant, as well as a protective coating, may be added to the formulation.
- Tablets as per the embodiments listed in Tables 2-4 containing various amounts of meglumine along with selected standard directly compressible excipients were prepared. Tablets were then crushed using a mortar/pestle. The powder was transferred into a glass vial and diluted in the extraction solvent. The solutions were then submitted to different treatments: 1 ) heating at 100 0 C, 2) cooling under 0 0 C and 4) magnetic stirring at 1 100 rpm. The solutions were filtered using 5ml_ BD syringe filter nylon membrane (pore size 0.45 ⁇ m) and evaluated for the release of methadone into the extraction solvent. Formulations with methadone alone (Example 1 ) demonstrated that over
- Dissolution tests are used to determine how a drug is released from solid oral pharmaceutical preparations, such as tablets and capsules. This testing is done to ensure that the drug is released from the oral preparation, and should generally be dissolved in the fluid of the gastrointestinal (Gl) tract to allow desired pharmacological effect. Indeed dissolution of the drug in physiological fluids is required for absorption of the drug from the Gl tract into the blood circulation to exert its desired physiological effect.
- Gl gastrointestinal
- dissolution solutions or media can be used to simulate dissolution in the gastrointestinal tract. These include Simulated Gastric Fluid (SGF) and 0.1 N hydrochloric acid (HCL), among others.
- SGF Simulated Gastric Fluid
- HCL hydrochloric acid
- Figure 1 Comparative dissolution profiles of methadone formulations in simulated gastric media (SGF) with various combinations of methadone and meglumine; and Figure 2: Comparative dissolution profiles of methadone formulations in water with various combinations of methadone and meglumine.
- SGF simulated gastric media
Abstract
Description
Claims
Priority Applications (8)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP09831343A EP2379111B1 (en) | 2008-12-12 | 2009-12-14 | Narcotic drug formulations with decreased abuse potential |
BRPI0917608A BRPI0917608B8 (en) | 2008-12-12 | 2009-12-14 | oral drug formulation for the reduction of potential abuse, process for manufacturing a drug formulation and its use |
CA2690824A CA2690824C (en) | 2008-12-12 | 2009-12-14 | Methadone formulation |
MX2011006173A MX2011006173A (en) | 2008-12-12 | 2009-12-14 | Narcotic drug formulations with decreased abuse potential. |
US13/133,141 US8460640B2 (en) | 2008-12-12 | 2009-12-14 | Narcotic drug formulations with decreased abuse potential |
ES09831343T ES2414856T3 (en) | 2008-12-12 | 2009-12-14 | Narcotic drug formulations with decreased addiction potential |
PL09831343T PL2379111T3 (en) | 2008-12-12 | 2009-12-14 | Narcotic drug formulations with decreased abuse potential |
ZA2011/04337A ZA201104337B (en) | 2008-12-12 | 2011-06-10 | Narcotic drug formulations with decreased abuse potential |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US12211708P | 2008-12-12 | 2008-12-12 | |
US61/122,117 | 2008-12-12 |
Publications (2)
Publication Number | Publication Date |
---|---|
WO2010066034A1 true WO2010066034A1 (en) | 2010-06-17 |
WO2010066034A8 WO2010066034A8 (en) | 2010-08-19 |
Family
ID=42242269
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/CA2009/001778 WO2010066034A1 (en) | 2008-12-12 | 2009-12-14 | Methadone formulation |
Country Status (8)
Country | Link |
---|---|
US (1) | US8460640B2 (en) |
EP (1) | EP2379111B1 (en) |
BR (1) | BRPI0917608B8 (en) |
ES (1) | ES2414856T3 (en) |
MX (1) | MX2011006173A (en) |
PL (1) | PL2379111T3 (en) |
WO (1) | WO2010066034A1 (en) |
ZA (1) | ZA201104337B (en) |
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---|---|---|---|---|
US20120321716A1 (en) * | 2011-02-17 | 2012-12-20 | Michael Vachon | Technology for preventing abuse of solid dosage forms |
US20120321674A1 (en) * | 2011-02-17 | 2012-12-20 | Michael Vachon | Technology for Preventing Abuse of Solid Dosage Forms |
WO2013128276A3 (en) * | 2012-03-02 | 2013-12-27 | Rhodes Pharmaceuticals L.P. | Tamper resistant immediate release formulations |
US8808745B2 (en) | 2001-09-21 | 2014-08-19 | Egalet Ltd. | Morphine polymer release system |
US8877241B2 (en) | 2003-03-26 | 2014-11-04 | Egalet Ltd. | Morphine controlled release system |
KR20140131943A (en) * | 2012-03-02 | 2014-11-14 | 로도스 파머시티컬스 엘.피. | Tamper resistant immediate release formulations |
US9005660B2 (en) | 2009-02-06 | 2015-04-14 | Egalet Ltd. | Immediate release composition resistant to abuse by intake of alcohol |
US9023394B2 (en) | 2009-06-24 | 2015-05-05 | Egalet Ltd. | Formulations and methods for the controlled release of active drug substances |
US9044402B2 (en) | 2012-07-06 | 2015-06-02 | Egalet Ltd. | Abuse-deterrent pharmaceutical compositions for controlled release |
US9161917B2 (en) | 2008-05-09 | 2015-10-20 | Grünenthal GmbH | Process for the preparation of a solid dosage form, in particular a tablet, for pharmaceutical use and process for the preparation of a precursor for a solid dosage form, in particular a tablet |
US9629807B2 (en) | 2003-08-06 | 2017-04-25 | Grünenthal GmbH | Abuse-proofed dosage form |
US9636303B2 (en) | 2010-09-02 | 2017-05-02 | Gruenenthal Gmbh | Tamper resistant dosage form comprising an anionic polymer |
US9642809B2 (en) | 2007-06-04 | 2017-05-09 | Egalet Ltd. | Controlled release pharmaceutical compositions for prolonged effect |
US9655853B2 (en) | 2012-02-28 | 2017-05-23 | Grünenthal GmbH | Tamper-resistant dosage form comprising pharmacologically active compound and anionic polymer |
US9675610B2 (en) | 2002-06-17 | 2017-06-13 | Grünenthal GmbH | Abuse-proofed dosage form |
US9694080B2 (en) | 2001-09-21 | 2017-07-04 | Egalet Ltd. | Polymer release system |
US9737490B2 (en) | 2013-05-29 | 2017-08-22 | Grünenthal GmbH | Tamper resistant dosage form with bimodal release profile |
US9750701B2 (en) | 2008-01-25 | 2017-09-05 | Grünenthal GmbH | Pharmaceutical dosage form |
US9855263B2 (en) | 2015-04-24 | 2018-01-02 | Grünenthal GmbH | Tamper-resistant dosage form with immediate release and resistance against solvent extraction |
US9872835B2 (en) | 2014-05-26 | 2018-01-23 | Grünenthal GmbH | Multiparticles safeguarded against ethanolic dose-dumping |
US9913814B2 (en) | 2014-05-12 | 2018-03-13 | Grünenthal GmbH | Tamper resistant immediate release capsule formulation comprising tapentadol |
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US10058548B2 (en) | 2003-08-06 | 2018-08-28 | Grünenthal GmbH | Abuse-proofed dosage form |
US10064945B2 (en) | 2012-05-11 | 2018-09-04 | Gruenenthal Gmbh | Thermoformed, tamper-resistant pharmaceutical dosage form containing zinc |
US10080721B2 (en) | 2009-07-22 | 2018-09-25 | Gruenenthal Gmbh | Hot-melt extruded pharmaceutical dosage form |
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Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3885027A (en) * | 1971-04-12 | 1975-05-20 | West Laboratories Inc | Orally administered drug composition for therapy in the treatment of narcotic drug addiction |
US3980766A (en) * | 1973-08-13 | 1976-09-14 | West Laboratories, Inc. | Orally administered drug composition for therapy in the treatment of narcotic drug addiction |
US6663893B2 (en) * | 2000-04-20 | 2003-12-16 | Bristol-Myers Squibb Co. | Taste masking coating composition |
US20060019872A1 (en) * | 2002-12-11 | 2006-01-26 | Chong Kun Dang Pharmaceutical Corp. | Oral formulations for poorly absorptive hydrophilic drugs |
CA2671197A1 (en) * | 2006-07-21 | 2008-01-24 | Lab International Srl | Hydrophobic abuse deterrent delivery system |
Family Cites Families (80)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB9401894D0 (en) * | 1994-02-01 | 1994-03-30 | Rhone Poulenc Rorer Ltd | New compositions of matter |
US6375957B1 (en) * | 1997-12-22 | 2002-04-23 | Euro-Celtique, S.A. | Opioid agonist/opioid antagonist/acetaminophen combinations |
CN1204890C (en) * | 1997-12-22 | 2005-06-08 | 欧罗赛铁克股份有限公司 | Method for preventing abuse of opioid dosage forms |
RU2241458C2 (en) * | 1997-12-22 | 2004-12-10 | Эро-Селтик, С.А. | Combinations of agonist/antagonist for opioid |
US20030170181A1 (en) * | 1999-04-06 | 2003-09-11 | Midha Kamal K. | Method for preventing abuse of methylphenidate |
US20030118641A1 (en) * | 2000-07-27 | 2003-06-26 | Roxane Laboratories, Inc. | Abuse-resistant sustained-release opioid formulation |
US6716449B2 (en) * | 2000-02-08 | 2004-04-06 | Euro-Celtique S.A. | Controlled-release compositions containing opioid agonist and antagonist |
JP2003522144A (en) * | 2000-02-08 | 2003-07-22 | ユーロ−セルティーク,エス.エイ. | Controlled release compositions comprising opioid agonists and antagonists |
GB0026137D0 (en) * | 2000-10-25 | 2000-12-13 | Euro Celtique Sa | Transdermal dosage form |
US20020187192A1 (en) | 2001-04-30 | 2002-12-12 | Yatindra Joshi | Pharmaceutical composition which reduces or eliminates drug abuse potential |
US20030004177A1 (en) * | 2001-05-11 | 2003-01-02 | Endo Pharmaceuticals, Inc. | Abuse-resistant opioid dosage form |
CN1525851A (en) * | 2001-05-11 | 2004-09-01 | ������ҩ������˾ | Abuse-resistant controlled-release opioid dosage form |
WO2002094172A2 (en) * | 2001-05-22 | 2002-11-28 | Euro-Celtique | Compartmentalized dosage form |
US7332182B2 (en) * | 2001-08-06 | 2008-02-19 | Purdue Pharma L.P. | Pharmaceutical formulation containing opioid agonist, opioid antagonist and irritant |
US20030068375A1 (en) * | 2001-08-06 | 2003-04-10 | Curtis Wright | Pharmaceutical formulation containing gelling agent |
US7842307B2 (en) | 2001-08-06 | 2010-11-30 | Purdue Pharma L.P. | Pharmaceutical formulation containing opioid agonist, opioid antagonist and gelling agent |
US20030157168A1 (en) * | 2001-08-06 | 2003-08-21 | Christopher Breder | Sequestered antagonist formulations |
US7141250B2 (en) * | 2001-08-06 | 2006-11-28 | Euro-Celtique S.A. | Pharmaceutical formulation containing bittering agent |
US7157103B2 (en) * | 2001-08-06 | 2007-01-02 | Euro-Celtique S.A. | Pharmaceutical formulation containing irritant |
WO2003015531A2 (en) * | 2001-08-06 | 2003-02-27 | Thomas Gruber | Pharmaceutical formulation containing dye |
US7144587B2 (en) | 2001-08-06 | 2006-12-05 | Euro-Celtique S.A. | Pharmaceutical formulation containing opioid agonist, opioid antagonist and bittering 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 |
CA2459976A1 (en) * | 2001-09-26 | 2003-04-03 | Penwest Pharmaceuticals Company | Opioid formulations having reduced potential for abuse |
US20040126428A1 (en) * | 2001-11-02 | 2004-07-01 | Lyn Hughes | Pharmaceutical formulation including a resinate and an aversive agent |
CA2464528A1 (en) * | 2001-11-02 | 2003-05-15 | Elan Corporation, Plc | Pharmaceutical composition |
AU2003219863C1 (en) | 2002-02-22 | 2009-03-05 | Shire Llc | Novel sustained release pharmaceutical compounds to prevent abuse of controlled substances |
AU2003228654A1 (en) * | 2002-04-29 | 2003-11-17 | The General Hospital Corporation | Compositions and methods for preventing abuse of orally administered medications |
WO2004041154A2 (en) * | 2002-05-13 | 2004-05-21 | Endo Pharmaceuticals Inc. | Abuse-resistant opioid dosage form |
CA2486075A1 (en) * | 2002-05-13 | 2003-11-20 | Endo Pharmaceuticals Inc. | Abuse-resistant opioid solid dosage form |
WO2004004693A1 (en) * | 2002-07-05 | 2004-01-15 | Collgegium Pharmaceutical | Abuse-deterrent pharmaceutical compositions of opiods and other drugs |
DE10239651A1 (en) * | 2002-08-29 | 2004-03-11 | Minebea Co., Ltd. | Hydrodynamic bearing system and method for its assembly |
PT1551372T (en) * | 2002-09-20 | 2018-07-23 | Alpharma Pharmaceuticals Llc | Sequestering subunit and related compositions and metohds |
JP5189242B2 (en) * | 2002-09-23 | 2013-04-24 | アルケルメス ファーマ アイルランド リミテッド | Abuse-resistant pharmaceutical composition |
DE10250084A1 (en) * | 2002-10-25 | 2004-05-06 | Grünenthal GmbH | Dosage form protected against abuse |
US20050186139A1 (en) * | 2002-10-25 | 2005-08-25 | Gruenenthal Gmbh | Abuse-proofed dosage form |
US20050191244A1 (en) * | 2002-10-25 | 2005-09-01 | Gruenenthal Gmbh | Abuse-resistant pharmaceutical dosage form |
US7524515B2 (en) * | 2003-01-10 | 2009-04-28 | Mutual Pharmaceuticals, Inc. | Pharmaceutical safety dosage forms |
US8133881B2 (en) * | 2003-01-13 | 2012-03-13 | Shire Llc | Carbohydrate conjugates to prevent abuse of controlled substances |
US9579286B2 (en) * | 2003-04-21 | 2017-02-28 | Purdue Pharma L.P. | Tamper resistant dosage form comprising co-extruded, sequestered adverse agent particles and process of making same |
US8906413B2 (en) * | 2003-05-12 | 2014-12-09 | Supernus Pharmaceuticals, Inc. | Drug formulations having reduced abuse potential |
US8075872B2 (en) * | 2003-08-06 | 2011-12-13 | Gruenenthal Gmbh | Abuse-proofed dosage form |
DE10336400A1 (en) * | 2003-08-06 | 2005-03-24 | Grünenthal GmbH | Anti-abuse dosage form |
US20070048228A1 (en) * | 2003-08-06 | 2007-03-01 | Elisabeth Arkenau-Maric | Abuse-proofed dosage form |
DE502004004205D1 (en) * | 2003-08-06 | 2007-08-09 | Gruenenthal Gmbh | AGAINST MISUSE SECURED PHARMACEUTICAL FORM |
DE102004032051A1 (en) * | 2004-07-01 | 2006-01-19 | Grünenthal GmbH | Process for the preparation of a secured against misuse, solid dosage form |
DE102004020220A1 (en) * | 2004-04-22 | 2005-11-10 | Grünenthal GmbH | Process for the preparation of a secured against misuse, solid dosage form |
DE10361596A1 (en) * | 2003-12-24 | 2005-09-29 | Grünenthal GmbH | Process for producing an anti-abuse dosage form |
DE102005005446A1 (en) * | 2005-02-04 | 2006-08-10 | Grünenthal GmbH | Break-resistant dosage forms with sustained release |
CN100588391C (en) * | 2003-08-12 | 2010-02-10 | 恩德制药公司 | Single long acting slow-release tablet for deterring abuse of medicine |
US7201920B2 (en) * | 2003-11-26 | 2007-04-10 | Acura Pharmaceuticals, Inc. | Methods and compositions for deterring abuse of opioid containing dosage forms |
EP1691892B1 (en) | 2003-12-09 | 2007-02-28 | Euro-Celtique S.A. | Tamper resistant co-extruded dosage form containing an active agent and an adverse agent and process of making same |
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 |
BRPI0508769A (en) * | 2004-03-30 | 2007-08-28 | Euro Celtique Sa | tamper-resistant dosage form comprising an adsorbent and an adverse agent |
DE102004019916A1 (en) * | 2004-04-21 | 2005-11-17 | Grünenthal GmbH | Anti-abuse drug-containing patch |
US20050271594A1 (en) | 2004-06-04 | 2005-12-08 | Groenewoud Pieter J | Abuse resistent pharmaceutical composition |
ITMI20041317A1 (en) * | 2004-06-30 | 2004-09-30 | Ibsa Inst Biochimique Sa | PHARMACEUTICAL FORMULATIONS FOR THE SAFE ADMINISTRATION OF DRUGS USED IN THE TREATMENT OF DRUG ADDICTION AND PROCEDURE FOR THEIR OBTAINING |
DE102004032049A1 (en) * | 2004-07-01 | 2006-01-19 | Grünenthal GmbH | Anti-abuse, oral dosage form |
US20060051298A1 (en) * | 2004-09-03 | 2006-03-09 | Groenewoud Pieter J | Abuse resistent pharmaceutical dosage and method of making same |
US9308176B2 (en) * | 2004-10-15 | 2016-04-12 | Supernus Pharmaceuticals, Inc | Less abusable pharmaceutical preparations |
FR2878161B1 (en) * | 2004-11-23 | 2008-10-31 | Flamel Technologies Sa | ORAL MEDICINE FORM, SOLID AND DESIGNED TO AVOID MEASUREMENT |
US20080152595A1 (en) * | 2004-11-24 | 2008-06-26 | Acura Pharmaceuticals, Inc. | Methods and compositions for deterring abuse of orally administered pharmaceutical products |
US20070231268A1 (en) * | 2004-11-24 | 2007-10-04 | Acura Pharmaceuticals, Inc. | Methods and compositions for deterring abuse of orally administered pharmaceutical products |
US20060177380A1 (en) * | 2004-11-24 | 2006-08-10 | Acura Pharmaceuticals, Inc. | Methods and compositions for deterring abuse of orally administered pharmaceutical products |
US20060110327A1 (en) * | 2004-11-24 | 2006-05-25 | Acura Pharmaceuticals, Inc. | Methods and compositions for deterring abuse of orally administered pharmaceutical products |
US20060257323A1 (en) * | 2005-05-02 | 2006-11-16 | Kulli John C | Preventing insufflation and injection modes of drug abuse |
WO2006133733A1 (en) * | 2005-06-13 | 2006-12-21 | Flamel Technologies | Oral dosage form comprising an antimisuse system |
US20070020339A1 (en) * | 2005-07-20 | 2007-01-25 | Pharmorx Inc. | Compositions and methods for controlling abuse of medications |
WO2007087452A2 (en) | 2006-01-27 | 2007-08-02 | Theraquest Biosciences, Llc | Abuse resistant and extended release formulations and method of use thereof |
US8652529B2 (en) * | 2005-11-10 | 2014-02-18 | Flamel Technologies | Anti-misuse microparticulate oral pharmaceutical form |
BRPI0619806A2 (en) * | 2005-12-13 | 2011-10-18 | Biodelivery Sciences Int Inc | abuse resistant transmucosal drug delivery device |
JP2009523833A (en) * | 2006-01-21 | 2009-06-25 | アボット ゲーエムベーハー ウント カンパニー カーゲー | Formulations and methods for drug delivery |
US9238073B2 (en) * | 2006-04-12 | 2016-01-19 | Wyeth Llc | Pharmaceutical composition containing sympathomimetic amine salt and co-distillable additive |
US9023400B2 (en) * | 2006-05-24 | 2015-05-05 | Flamel Technologies | Prolonged-release multimicroparticulate oral pharmaceutical form |
US20080069891A1 (en) * | 2006-09-15 | 2008-03-20 | Cima Labs, Inc. | Abuse resistant drug formulation |
WO2008024490A2 (en) | 2006-08-24 | 2008-02-28 | Theraquest Biosciences, Inc. | Oral pharmaceutical formulations of abuse deterrent cannabinoids and method of use |
SA07280459B1 (en) | 2006-08-25 | 2011-07-20 | بيورديو فارما إل. بي. | Tamper Resistant Oral Pharmaceutical Dosage Forms Comprising an Opioid Analgesic |
WO2008027442A2 (en) | 2006-08-30 | 2008-03-06 | Theraquest Biosciences, Llc | Abuse deterrent oral pharmaceutical formulations of opioid agonists and method of use |
US8187636B2 (en) * | 2006-09-25 | 2012-05-29 | Atlantic Pharmaceuticals, Inc. | Dosage forms for tamper prone therapeutic agents |
PT2101740E (en) | 2006-12-04 | 2013-12-23 | Orexo Ab | New non-abusable pharmaceutical composition comprising opioids |
-
2009
- 2009-12-14 PL PL09831343T patent/PL2379111T3/en unknown
- 2009-12-14 WO PCT/CA2009/001778 patent/WO2010066034A1/en active Application Filing
- 2009-12-14 EP EP09831343A patent/EP2379111B1/en active Active
- 2009-12-14 MX MX2011006173A patent/MX2011006173A/en active IP Right Grant
- 2009-12-14 BR BRPI0917608A patent/BRPI0917608B8/en active IP Right Grant
- 2009-12-14 US US13/133,141 patent/US8460640B2/en active Active
- 2009-12-14 ES ES09831343T patent/ES2414856T3/en active Active
-
2011
- 2011-06-10 ZA ZA2011/04337A patent/ZA201104337B/en unknown
Patent Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3885027A (en) * | 1971-04-12 | 1975-05-20 | West Laboratories Inc | Orally administered drug composition for therapy in the treatment of narcotic drug addiction |
US3980766A (en) * | 1973-08-13 | 1976-09-14 | West Laboratories, Inc. | Orally administered drug composition for therapy in the treatment of narcotic drug addiction |
US6663893B2 (en) * | 2000-04-20 | 2003-12-16 | Bristol-Myers Squibb Co. | Taste masking coating composition |
US20060019872A1 (en) * | 2002-12-11 | 2006-01-26 | Chong Kun Dang Pharmaceutical Corp. | Oral formulations for poorly absorptive hydrophilic drugs |
CA2671197A1 (en) * | 2006-07-21 | 2008-01-24 | Lab International Srl | Hydrophobic abuse deterrent delivery system |
Cited By (61)
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US9694080B2 (en) | 2001-09-21 | 2017-07-04 | Egalet Ltd. | Polymer release system |
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Also Published As
Publication number | Publication date |
---|---|
ZA201104337B (en) | 2012-03-28 |
BRPI0917608B1 (en) | 2021-04-13 |
PL2379111T3 (en) | 2013-08-30 |
US20110237615A1 (en) | 2011-09-29 |
WO2010066034A8 (en) | 2010-08-19 |
EP2379111A1 (en) | 2011-10-26 |
EP2379111A4 (en) | 2011-11-16 |
ES2414856T3 (en) | 2013-07-23 |
US8460640B2 (en) | 2013-06-11 |
BRPI0917608B8 (en) | 2021-05-25 |
MX2011006173A (en) | 2011-09-01 |
EP2379111B1 (en) | 2013-03-20 |
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