MODIFIED RELEASE FORMULATIONS OF A BUPROPION SALT

• US 20070269516A1
• Filed: 05/22/2007
• Published: 11/22/2007
• Est. Priority Date: 06/27/2005
• Status: Active Grant

• Current Assignee: Valeant International (Barbados) Srl (Bausch Health Cos., Inc.)
• Original Assignee: Biovail Laboratories International Srl (Bausch Health Cos., Inc.)
• Inventors: Massardo, Pietro, Jackson, Graham, Maes, Paul, Oberegger, Werner, Turchetta, Stefano, Saleh, Mohammad, Zhou, Fang
• Granted Patent: US 7,563,823 B2
• Time in Patent Office: Days
• US Class Current: 424/480
• 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 controlled release matrix comprising bupropion hydrobromide dispersed within a matrix.

2. The controlled release matrix according to claim 1, wherein said matrix is an insoluble polymer matrix.

3. The controlled release matrix according to claim 1, wherein said matrix is a swellable matrix.

4. The controlled release matrix according to claim 1, wherein said matrix is a lipid matrix.

5. The controlled release matrix according to claim 1, wherein said matrix is a hydrophilic colloid matrix.

6. The controlled release matrix according to claim 1, wherein said matrix is an erodible matrix.

7. The controlled release matrix according to claim 1, wherein said matrix is a reservoir matrix.

8. The controlled release matrix according to claim 1, wherein said matrix comprises at least one pharmaceutically acceptable excipient.

9. The controlled release matrix according to claim 1, wherein said bupropion hydrobromide is present in the controlled release matrix in an amount of from 40% to 90% by weight of the matrix dry weight.

10. The controlled release matrix according to claim 1, wherein said matrix comprises at least one member selected from the group consisting of hydrophobic polymers, hydrophilic polymers, lipophilic materials and mixtures thereof.

11. The controlled release matrix according to claim 1, wherein said matrix is a doughnut-shaped matrix with a hole though the middle.

12. The controlled release matrix according to claim 1, wherein said matrix provides zero order release kinetics.

13. The controlled release matrix according to claim 1, wherein said matrix comprises (a) a polymer or a mixture of polymers, (b) said bupropion hydrobromide and, optionally, (c) one or more pharmaceutically acceptable excipients, and wherein said matrix is coated with a coating having at least one opening.

14. The controlled release matrix according to claim 12, wherein the coating comprises a first cellulose derivative which has thermoplastic properties and which is substantially insoluble, and at least one of a second cellulose derivative which is soluble or dispersible in water, a plasticizer, and a filler.

15. The controlled release matrix according to claim 3, wherein said swellable matrix achieves at least one of the following objectives:

(i) renders the matrix sufficiently large to cause retention in the stomach during the fed mode;

(ii) localizes the release of the bupropion hydrobromide to the stomach and small intestine so that the bupropion hydrobromide will have its full effect without colonic degradation, inactivation, or loss of bioavailability; and

(iii) retards the rate of diffusion of the bupropion hydrobromide long enough to provide multi-hour, controlled delivery of the bupropion hydrobromide into the stomach.