BUPROPION HYDROBROMIDE AND THERAPEUTIC APPLICATIONS

• US 20100203128A1
• Filed: 08/06/2008
• Published: 08/12/2010
• Est. Priority Date: 08/07/2007
• Status: Abandoned Application

• Current Assignee: Valeant International (Barbados) Srl (Bausch Health Cos., Inc.)
• Original Assignee: Biovail Laboratories International Srl (Bausch Health Cos., Inc.)
• Inventors: Williams, Robert Parry, Silverstone, Peter Harris
• Application Number:
  US12/672,137
• Publication Number:
  US 20100203128A1
• Time in Patent Office: Days
• US Class Current: 424/474
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/135 having aromatic rings , e.g. ketamine, nortriptyline methadone A61K31/137
• CPC Class Codes: A61K 33/00 Medicinal preparations containing inorganic active ingredients
• 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

Abstract

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

Claims

1. A composition comprising bupropion hydrobromide and at least one pharmaceutically acceptable excipient;

wherein administration of an amount of a bupropion hydrobromide to a first rat results in less incidences of and/or less severe bupropion-induced seizures when compared to incidences of and/or severity of bupropion-induced seizures resulting from administration of an equivalent molar amount of bupropion hydrochloride to a second rat; and

wherein the incidences of and/or severity of bupropion-induced seizures are measured by an electroencephalogram analysis using a hippocampally implanted depth electrode.

2. The composition of claim 1, which is in tablet form.

3. The composition of claim 1, which is a modified release formulation.

4. The composition of claim 1, which is in tablet form and wherein the bupropion hydrobromide is contained within a core of the tablet further comprising a coating over the core.

5. The composition of claim 4, wherein the coating is a controlled release coating.

6. A composition comprising bupropion hydrobromide and at least one pharmaceutically acceptable excipient;

wherein administration of about 100 mg/kg of a bupropion hydrobromide to a first rat results in less incidences of and/or severity of bupropion-induced seizures when compared to incidences of and/or severity of bupropion-induced seizures resulting from administration of an equivalent molar amount of bupropion hydrochloride to a second rat; and

wherein the incidences of and/or severity of bupropion-induced seizures are measured by an electroencephalogram analysis using a hippocampally implanted depth electrode.

7. A method of treating a subject at risk of bupropion-induced seizures in need of bupropion treatment, the method comprising:

administering a composition comprising bupropion hydrobromide to said subject in an amount sufficient to treat said subject.

8. The method of claim 7, wherein the composition comprises an amount of bupropion hydrobromide chosen from 174 mg, 348 mg and 522 mg.

9. The method of claim 7, wherein the composition is in tablet form and the administering comprises oral administration.

10. The method of claim 7, wherein the composition is a modified release formulation.

11. The method of claim 7, wherein the composition is in tablet form and wherein the bupropion hydrobromide is contained within a core of the tablet further comprising a coating over the core.

12. The method of claim 7, wherein the coating is a controlled release coating.

13. A method of reducing incidences of bupropion-induced seizures comprising:

administering a pharmaceutically effective amount of bupropion hydrobromide to a subject in need of bupropion administration;

wherein incidences of bupropion-induced seizures resulting from the administration of bupropion hydrobromide is less than incidences of bupropion-induced seizures resulting from administration of an equivalent molar amount of bupropion hydrochloride.

14. The method of claim 13 wherein bupropion-induced seizures resulting from the administration of bupropion hydrobromide is less severe than bupropion-induced seizures resulting from administration of an equivalent molar amount of bupropion hydrochloride.

15. A method of reducing incidences of bupropion-induced seizures comprising:

administering a pharmaceutically effective amount of bupropion hydrobromide to a subject in need of bupropion administration;

wherein administration of about 100 mg/kg of the bupropion hydrobromide to a first rat results in less incidences of bupropion-induced seizures when compared to incidences of bupropion-induced seizures resulting from administration of an equivalent molar amount of bupropion hydrochloride to a second rat; and

wherein the incidences of bupropion-induced seizures in the first and second rats are measured by an electroencephalogram analysis using a hippocampally implanted depth electrode.

16. A method of reducing the incidences of bupropion induced seizures comprising coadministration of a bromide salt with a bupropion salt, wherein the bromide salt is administered in an amount of less than about 3.5 mg/kg.

17. The method of claim 16 wherein the bromide salt is sodium bromide.

18. The method of claim 16 wherein the bupropion salt is bupropion hydrochloride.

19. A composition comprising bupropion hydrobromide and at least one pharmaceutically acceptable excipient;

wherein administration of about 100 mg/kg of a bupropion hydrobromide used to manufacture the composition to a first rat results in less incidences of and/or severity of bupropion-induced seizures when compared to incidences of and/or severity of bupropion-induced seizures resulting from administration of an equivalent molar amount of bupropion hydrochloride to a second rat; and

wherein the incidences of and/or severity of bupropion-induced seizures are measured by an electroencephalogram analysis using a hippocampally implanted depth electrode.