Stabilized, acid-free formulation for sustained release of bupropion hydrochloride
AssigneeTeva Pharmaceuticals USA, Inc.
InventorsShubha Chungi, Kangwen Lin
Life of this patent
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Abstract
Stabilized bupropion hydrochloride pharmaceutical compositions are disclosed that are free of acid additives and provide for a sustained release of the bupropion hydrochloride. The particulate bupropion hydrochloride may be coated with a membrane coating and large-size particles may also be used. Methods for treating individuals using the stabilized bupropion hydrochloride pharmaceutical compositions are also provided.
Claims36
A pharmaceutical composition for oral administration, comprising a solid dosage form that is free of added acid and contains a therapeutically effective amount of particulate, crystalline bupropion hydrochloride as an active agent and a pharmaceutically acceptable carrier that provides for sustained release of the active agent from the dosage form, wherein the composition contains at least about 80 wt. % of undegraded bupropion hydrochloride after storage for three months at about 40° C. and 75% relative humidity.
A pharmaceutical composition for oral administration, comprising a solid dosage form that is free of added acid and contains a therapeutically effective amount of particulate, crystalline bupropion hydrochloride as an active agent and a pharmaceutically acceptable carrier that provides for sustained release of the active agent from the dosage form, wherein the composition contains at least about 80 wt. % of undegraded bupropion hydrochloride after storage for three months at about 40° C. and 75% relative humidity and the carrier is comprised of hydrogenated soybean oil.
A pharmaceutical composition for oral administration, comprising a solid dosage form that is free of added acid and contains a therapeutically effective amount of particulate, crystalline bupropion hydrochloride as an active agent and a pharmaceutically acceptable carrier that provides for sustained release of the active agent from the dosage form, wherein the composition contains at least about 80 wt. % of undegraded bupropion hydrochloride after storage for three months at about 40° C. and 75% relative humidity and the carrier is comprised of a carbomer.
A sustained release bupropion hydrochloride composition, comprising a compressed tablet that is free of added acid and contains:
- approximately 100 mg to 150 mg bupropion hydrochloride crystals having a particle size in the range of approximately 150μ to 800μ, said crystals coated with a cellulosic polymer selected from the group consisting of hydroxypropyl cellulose, hydroxypropyl methylcellulose, methyl cellulose, ethyl cellulose, hydroxyethyl cellulose and mixtures thereof, wherein the weight ratio of bupropion hydrochloride to cellulosic polymer is in the range of approximately 8:1 to 18:1;
- and
- a pharmaceutically acceptable carrier effective to provide sustained release of the bupropion hydrochloride such that approximately 70% to 90% of the bupropion hydrochloride is released from the tablet within four hours of oral administration, wherein the carrier is selected from the group consisting of (a) a mixture of polyvinyl acetate and polyvinyl pyrrolidone, (b) a hydrogenated oil, (c) a carbomer, (d) hydroxypropyl cellulose, (e) methyl cellulose, (f) ethyl cellulose, (g) acrylic acid polymers and copolymers, and mixtures thereof,
- wherein the composition contains at least about 90 wt. % of undegraded bupropion hydrochloride after storage for three months at about 40° C. and 75% relative humidity.
A method for preparing a stabilized bupropion hydrochloride composition for oral administration without addition of acid, comprising admixing particulate, crystalline bupropion hydrochloride with a pharmaceutically acceptable carrier selected from the group consisting of (a) a mixture of polyvinyl acetate and polyvinyl pyrrolidone, (b) a hydrogenated oil, (c) a carbomer, (d) hydroxypropyl cellulose, (e) methyl cellulose, (f) ethyl cellulose, (g) acrylic acid polymers and copolymers, and mixtures thereof, and compressing the admixture so formed into a tablet, wherein the composition contains at least about 80 wt. % of undegraded bupropion hydrochloride after storage for three months at about 40° C. and 75% relative humidity.
A method for preparing a stabilized bupropion hydrochloride composition for oral administration without addition of acid, comprising:
- (a) coating particulate, crystalline bupropion hydrochloride with an amount of a cellulosic polymer effective to provide a weight ratio of bupropion hydrochloride to cellulosic polymer in the range of approximately 8:1 to 18:1, and wherein the cellulosic polymer is selected from the group consisting of hydroxypropyl cellulose, hydroxypropyl methylcellulose, methyl cellulose, ethyl cellulose, hydroxyethyl cellulose and mixtures thereof;
- (b) admixing the coated bupropion hydrochloride with a pharmaceutically acceptable carrier selected from the group consisting of a mixture of polyvinyl acetate and polyvinyl pyrrolidone, a hydrogenated oil, a carbomer, hydroxypropyl cellulose, methylcellulose, ethylcellulose, acrylic acid polymers and copolymers, and mixtures thereof;
- and
- (c) compressing the admixture so formed into a tablet,
- wherein the composition contains at least about 80 wt. % of undegraded bupropion hydrochloride after storage for three months at about 40° C. and 75% relative humidity.
Dependencies are inferred from the claim text.