SUSTAINED-RELEASE BUPROPION AND BUPROPION/MECAMYLAMINE TABLETS

• US 20080031948A1
• Filed: 07/25/2007
• Published: 02/07/2008
• Est. Priority Date: 07/25/2006
• Status: Active Grant

• Current Assignee: IntelGenx Corporation
• Original Assignee: IntelGenx Corporation
• Inventors: Paiement, Nadine, Zerbe, Horst G.
• Granted Patent: US 7,674,479 B2
• Time in Patent Office: Days
• US Class Current: 424/470
• 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 31/13 Amines A61K31/04 takes precedence
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• 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 9/2031 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2077 Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
• CPC Class Codes: A61K 9/2846 Poly(meth)acrylates
• CPC Class Codes: A61K 9/2853 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers, poly(lactide-co-glycolide)
• CPC Class Codes: A61K 9/2866 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/5084 Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs tablets containing such a mixture A61K9/2077
• CPC Class Codes: A61P 25/34 Tobacco-abuse

Abstract

Sustained-release bupropion hydrochloride pharmaceutical tablets and combination sustained-release bupropion hydrochloride/mecamylamine hydrochloride pharmaceutical tablets are obtained by granulating the bupropion hydrochloride with a hydroxyalkylcelluose, and blending the resulting granules within an extragranular phase composed of a particulate material that provides a sustained-release matrix, and compressing the blend into a tablet form, which then is coated, with a means to provide delayed release, such as with an enteric coating composition. The mecamylamine hydrochloride can be contained in a second granule comprising a hydroxyalkylcellulose.

Claims

1. A sustained release pharmaceutical tablet comprising:

sustained release granules consisting essentially of bupropion hydrochloride admixed with a hydroxyalkylcellulose; and

an extragranular phase comprising a particulate material that provides a sustained release matrix;

said particulate material is selected from the group consisting of polyvinylacetate, blends of polyvinylacetate and polyvinylpyrrolidone, a vinylpyrrolidone copolymer and polyethylene oxide,

the granules being distributed within the extragranular phase.

2. The tablet of claim 1 further comprising sustained release mecamylamine hydrochloride granules.

3. The tablet of claim 1, wherein said extragranular phase further comprises mecamylamine hydrochloride.

4. The tablet of claim 1, wherein said hydroxyalkylcellulose is hydroxypropylcellulose.

5. The tablet of claim 1, further comprising an enteric coating.

6. A sustained release pharmaceutical tablet comprising:

an uncoated sustained release granular phase comprising bupropion hydrochloride admixed with a hydroxyalkylcellulose; and

an extragranular phase comprising a particulate material that provides a sustained release matrix;

said particulate material is selected from the group consisting of polyvinylacetate, blends of polyvinylacetate and polyvinylpyrrolidone, a vinylpyrrolidone copolymer and polyethylene oxide,

the uncoated granular phase being distributed within the extragranular phase.

7. The tablet of claim 6, further comprising sustained release mecamylamine hydrochloride granules.

8. The tablet of claim 6, wherein said extragranular phase further comprises mecamylamine hydrochloride.

9. The tablet of claim 6, wherein said hydroxyalkylcellulose is hydroxypropylcellulose.

10. The tablet of claim 6, further comprising an enteric coating.