Modified release formulations of a bupropion salt

• US 8,932,628 B2
• Filed: 06/13/2007
• Issued: 01/13/2015
• Est. Priority Date: 06/27/2005
• Status: Active Grant

• Current Assignee: Valeant International (Barbados) Srl (Bausch Health Cos., Inc.)
• Original Assignee: Valeant International Bermuda (Bausch Health Cos., Inc.)
• Inventors: Oberegger, Werner, Zhou, Fang, Maes, Paul, Saleh, Mohammad Ashty, Jackson, Graham
• Primary Examiner(s): Zucker, Paul A
• Application Number:
  US11/762,343
• Publication Number:
  US 20080038348A1
• Time in Patent Office: 2,771 Days
• US Class Current: 424/463
• 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 modified release osmotic dosage form comprising

a core comprising bupropion hydrobromide;

and

a semipermeable membrane surrounding the core;

wherein the bupropion hydrobromide is present in a therapeutically effective amount, and wherein said dosage form releases the bupropion hydrobromide by dispensing the bupropion hydrobromide from the core via at least one passageway in the membrane by pressure created in the core by osmosis and/or by the expansion of a swellable material which forces the bupropion hydrobromide to be dispensed from core of the dosage form.

2. The modified release osmotic dosage form according to claim 1, wherein said dosage form exhibits an in-vitro release rate such that after 2 hours 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.

3. The modified release osmotic dosage form according to claim 1, wherein the core further comprises at least one osmagent.

4. The modified release osmotic dosage form according to claim 3, wherein said at least one osmagent is selected from the group consisting of sodium chloride, calcium chloride, calcium lactate, sodium sulfate, lactose, glucose, sucrose, mannitol, urea, and mixtures thereof.

5. The modified release osmotic dosage form according to claim 3, wherein said at least one osmagent is present in admixture with said bupropion hydrobromide.

6. The modified release osmotic dosage form of claim 1, wherein the dosage form exhibits an in-vitro release rate such that after 2 hours no more than 40% is released, after 4 hours 40-75% is released, after 8 hours at least 75% is released and after 16 hours at least 85% is released.

7. The modified release osmotic dosage form according to claim 1, wherein said core comprises bupropion hydrobromide arranged in a layered, contacting arrangement, with a swellable material to provide a core with two or more layers.

8. The modified release osmotic dosage form of claim 1, wherein the semipermeable membrane comprises at least one polymer, at least one wax, or a combination thereof.

9. The modified release osmotic dosage form of claim 1, further comprising a control-releasing coat.

10. The modified release osmotic dosage form of claim 9, wherein the control releasing-coat comprises at least one water-insoluble water-permeable film-forming polymer, at least one water-soluble polymer, and, optionally, at least one plasticizer.