BUPROPION HYDROBROMIDE AND THERAPEUTIC APPLICATIONS

• US 20080274181A1
• Filed: 10/31/2007
• Published: 11/06/2008
• 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: Saleh, Mohammad Ashty, Maes, Paul, Oberegger, Werner
• Granted Patent: US 7,645,802 B2
• Time in Patent Office: Days
• US Class Current: 424/472
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/284 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
• 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 15/10 for impotence
• CPC Class Codes: A61P 25/22 Anxiolytics
• CPC Class Codes: A61P 25/24 Antidepressants
• CPC Class Codes: A61P 25/26 Psychostimulants, e.g. nicotine, cocaine
• CPC Class Codes: A61P 25/30 for treating abuse or dependence
• CPC Class Codes: A61P 25/34 Tobacco-abuse
• CPC Class Codes: A61P 3/04 Anorexiants; Antiobesity agents

Abstract

Bupropion hydrobromide formulations as well as their use for the treatment of conditions is described.

Claims

1. A modified release bupropion hydrobromide composition comprising:

a core comprising a therapeutically effective amount of bupropion hydrobromide; and

a controlled release polymeric coat comprising a water-insoluble polymer and a water-soluble polymer;

wherein said coat at least partially surrounds said core; and

wherein said composition releases bupropion hydrobromide in a first dissolution medium consisting of 0.1 N HCl and 5%-40% v/v ethanol at a rate that is less than or equal to about 1.1 times the rate of release of bupropion hydrobromide from an identical modified release pharmaceutical composition in a second dissolution medium consisting of 0.1 N HCl, measured over a time period of at least from 0 to 2 hours measured using a USP Apparatus I at 75 rpm and at 37±

0.5°

C.

2. The modified release composition according to claim 1 wherein said composition releases bupropion hydrobromide in a first dissolution medium consisting of 0.1 N HCl and 5%-40% v/v ethanol at a rate that is less than or equal to the rate of release of bupropion hydrobromide from the identical modified release composition in a second dissolution medium consisting of 0.1 N HCl.

3. The modified release composition according to claim 2 wherein the first dissolution medium consists of 0.1 N HCl and 5% v/v ethanol.

4. The modified release composition according to claim 2 wherein the first dissolution medium consists of 0.1 N HCl and 40% v/v ethanol.

5. The modified release composition according to claim 1 wherein the time period is from 0 to 16 hours.

6. The modified release composition according to claim 1 wherein the composition is a tablet comprising 174 mg, 348 mg or 522 mg of bupropion hydrobromide.

7. The modified release bupropion hydrobromide composition according to claim 1 wherein said composition releases bupropion hydrobromide in a dissolution medium consisting of 0.1 N HCl and 40% v/v ethanol at a rate that is less than the rate of release of bupropion hydrochloride from a modified release bupropion hydrochloride composition, in the identical dissolution medium consisting of 0.1 N HCl and 40% v/v ethanol, measured over a time period of at least from 0 to 2 hours measured using a USP Apparatus I at 75 rpm and at 37±

0.5°

C.;

wherein the modified release bupropion hydrochloride composition comprises;

a core comprising bupropion hydrochloride, in an amount equimolar to the amount of bupropion hydrobromide in the modified release bupropion hydrobromide composition; and

the identical controlled release polymeric coat comprising a water-insoluble polymer and a water-soluble polymer, used in the bupropion hydrobromide composition; and

wherein the coat at least partially surrounds the core of the modified release bupropion hydrochloride composition.

8. A method of reducing alcohol-induced dose dumping of bupropion hydrobromide in a patient comprising administering to a patient the modified release pharmaceutical composition of claim 1.

9. The method of claim 8 wherein the composition is a tablet comprising 174 mg, 348 mg or 522 mg of bupropion hydrobromide.