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US 10,292,966 B2Granted
Sustained release pharmaceutical compositions
AssigneeWyeth
InventorsEric J. Benjamin, Wendy A. Dulin, Yanning Lin, Kai Zhuang
Life of this patent
Estimating the term…
Abstract
The present invention provides controlled release dosage formulations of compounds having the Formula: or pharmaceutically acceptable salts thereof, and in particular, aplindore. The dosage forms are useful, inter alia, for reducing side effects from administration of such compounds.
Claims21
A controlled release oral dosage formulation comprising aplindore, or a pharmaceutically acceptable salt thereof;
- and
- one or more release-rate controlling polymers or release-retarding materials;
- wherein the controlled release oral dosage formulation comprises one or more of the following:
- a wax matrix wherein the wax is present in an amount by weight of from about 10% to about 60% of the formulation;
- a polyethylene oxide matrix wherein the polyethylene oxide is present in an amount by weight of from about 5% to about 40% of the formulation;
- or a hydroxypropyl methylcellulose matrix wherein the hydroxypropyl methylcellulose is present in an amount by weight of from about 15% to about 80% of the formulation and the hydroxypropyl methylcellulose comprises one high viscosity hydroxypropyl methyl cellulose and one low viscosity hydroxypropyl methyl cellulose;
- wherein the aplindore, or the pharmaceutically acceptable salt thereof, is released at a rate effective to provide a Cmax that is about 4,000 pg/mL to about 14,000 pg/mL;
- and wherein the aplindore, or the pharmaceutically acceptable salt thereof of the controlled release oral dosage formulation, is released at a rate to provide an AUC0-12 of about 36,000 pg*h/mL to about 109,000 pg*h/mL;
- and
- wherein the controlled release oral dosage formulation comprises a tablet, an encapsulated dosage form, one or more microparticles, or powder, or a combination thereof.
7 more elements
A controlled release oral dosage formulation comprising aplindore, or a pharmaceutically acceptable salt thereof;
- wherein the aplindore, or the pharmaceutically acceptable salt thereof of the controlled release oral dosage formulation, is released at a rate effective to provide a Cmax of about 4,000 pg/mL to about 14,000 pg/mL;
- and wherein the aplindore, or the pharmaceutically acceptable salt thereof of the controlled release oral dosage formulation is released at a rate to provide an AUC0-12 of about 36,000 pg*h/mL to about 109,000 pg*h/mL;
- and
- wherein the controlled release oral dosage formulation comprises a microparticle wherein the microparticle comprises an inert core;
- a layer comprising the aplindore or the pharmaceutically acceptable salt thereof disposed on the inert core;
- and a coating comprising at least one release rate controlling polymer disposed on the layer of the compound.
3 more elements
Dependencies are inferred from the claim text.