MODIFIED RELEASE FORMULATIONS OF A BUPROPION SALT

• US 20070281012A1
• Filed: 06/13/2007
• Published: 12/06/2007
• Est. Priority Date: 06/27/2005
• Status: Abandoned Application

• Current Assignee: Biovail Laboratories International Srl (Bausch Health Cos., Inc.)
• Original Assignee: Biovail Laboratories International Srl (Bausch Health Cos., Inc.)
• Inventors: Massardo, Pietro, Jackson, Graham, Zhou, Fang, Maes, Paul, Oberegger, Werner, Turchetta, Stefano, Saleh, Mohammad
• Application Number:
  US11/762,368
• Publication Number:
  US 20070281012A1
• Time in Patent Office: Days
• US Class Current: 424/465
• CPC Class Codes: A61K 31/135 having aromatic rings , e.g. ketamine, nortriptyline methadone A61K31/137
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• CPC Class Codes: A61K 9/0004 Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas
• CPC Class Codes: A61K 9/2027 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/28 Dragees; Coated pills or tablets , e.g. with film or compression coating A61K9/2072 takes precedence, e.g. partially coated tablets A61K9/2072, coated multilayer tablets A61K9/2086, tablets with drug-coated core A61K9/209
• CPC Class Codes: A61K 9/2846 Poly(meth)acrylates
• CPC Class Codes: A61K 9/2866 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2886 having two or more different drug-free coatings; Tablets of the type inert core-drug layer-inactive layer of the type active core-drug layer-inactive layer A61K9/209
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/06 Antimigraine agents
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• CPC Class Codes: A61P 25/24 Antidepressants
• CPC Class Codes: A61P 25/30 for treating abuse or dependence
• CPC Class Codes: A61P 25/34 Tobacco-abuse
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 3/00 Drugs for disorders of the metabolism of the blood or the extracellular fluid A61P7/00
• CPC Class Codes: A61P 3/02 Nutrients, e.g. vitamins, minerals
• CPC Class Codes: A61P 3/04 Anorexiants; Antiobesity agents
• CPC Class Codes: A61P 31/12 Antivirals
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 9/10 : for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• CPC Class Codes: C07B 2200/13 : Crystalline forms, e.g. polymorphs
• CPC Class Codes: C07C 225/16 : and containing six-membered aromatic rings

Abstract

The present invention relates to pharmaceutical compositions, formulations and medicaments comprising a bupropion salt, in particular, modified-release tablets comprising an effective amount of bupropion hydrobromide, and the use of the bupropion salt to prepare a medicament to treat a condition.

Claims

1. A microparticle comprising a solid core, said core comprising bupropion hydrobromide and at least one pharmaceutically acceptable excipient, said core of said microparticle being at least partially surrounded by a controlled release coat which permits entry of an aqueous liquid into the core and delivery of the bupropion hydrobromide from the core to the exterior of the microparticle through the controlled release coat.

2. The microparticle of claim 1, wherein said bupropion hydrobromide is in admixture with said at least one pharmaceutically acceptable excipient.

3. The microparticle of claim 1, wherein said microparticle exhibits an in-vitro release rate such that after 2 hours from 0 to 20% by weight of the bupropion hydrobromide is released, after 4 hours from 15% to 45% by weight of the bupropion hydrobromide is released, after 8 hours, from 40% to 90% by weight of the bupropion hydrobromide is released, and after 16 hours, more than 80% by weight of the bupropion hydrobromide is released.

4. The microparticle of claim 1, wherein said microparticle exhibits an in-vitro release rate such that after 2 hours no more than 40% is released, after 4 hours from 40-75% is released, after 8 hours at least 75% is released and after 16 hours at least 85% is released.

5. The microparticle of claim 1, comprising a sugar sphere or nonpareil bead coated with at least one layer comprising bupropion hydrobromide and at least one pharmaceutically acceptable excipient and/or osmagent, said at least one layer surrounded by a semipermeable membrane, said microparticle exhibiting an in-vitro release rate such that after 2 hours from 0 to 20% by weight of the bupropion hydrobromide is released, after 4 hours from 15% to 45% by weight of the bupropion hydrobromide is released, after 8 hours, from 40% to 90% by weight of the bupropion hydrobromide is released, and after 16 hours, more than 80% by weight of the bupropion hydrobromide is released.

7. The microparticle of claim 1, wherein said core comprises an osmopolymer.

8. The microparticle of claim 5, wherein said core comprises an osmopolymer.

6. A microparticle comprising a homogenous solid core, said core comprising bupropion hydrobromide and at least one pharmaceutically acceptable excipient, osmagent, and/or absorption enhancer, said microparticles compressed into a tablet, said tablet surrounded by a semipermeable membrane which permits entry of an aqueous liquid into the core and delivery of the bupropion hydrobromide from the tablet interior to the exterior thereof through at least one passageway in the semipermeable membrane and/or by diffusion through the semipermeable membrane.

9. The microparticle of claim 6, wherein said core comprises an osmopolymer.