Controlled Release Muscarinic Receptor Antagonist Formulation
OwnerFelix S. Lai, Richard Ting +3inventors
InventorsFelix S. Lai, Richard Ting, Lee Foong Siew, King Yu-Kuang Chuang, Sibel Ucpinar
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Abstract
An oral controlled release pharmaceutical composition for muscarinic receptor antagonist, preferably tolterodine, that employs a drug core, a rapidly disintegrating or rapidly dissolving coating applied to the drug core and a controlled release coating.
Claims18
A stable controlled release oral pharmaceutical composition comprising:
- (a) a core comprising a therapeutically effective amount of tolterodine and at least one pharmaceutically acceptable excipient;
- (b) a rapidly disintegrating or rapidly dissolving coating applied directly to the core;
- and
- (c) a controlled release coating applied to the rapidly disintegrating or rapidly dissolving coating wherein the controlled release coating comprises a water insoluble film forming polymer and a pore forming agent.
A stable controlled release oral pharmaceutical composition comprising a plurality of particles wherein at least one of the particles consists essentially of:
- (a) a core comprising a therapeutically effective amount of tolterodine tartrate and at least one pharmaceutically acceptable excipient;
- (b) a rapidly disintegrating or rapidly dissolving coating applied directly to the core that exhibits a low water vapor transmission rate as determined by a water permeability analyzer wherein a test sample of the rapidly disintegrating or rapidly dissolving coating is tested for under 25° C./60% relative humidity, 25° C./80% relative humidity and 40° C./75% relative humidity and the slope of the water vapor transmission versus time plot exhibits a slope that is less than 60 under all three test conditions;
- and
- (c) a controlled release coating applied to the rapidly disintegrating or rapidly dissolving coating wherein the controlled release coating comprises a water insoluble film forming polymer and a pore forming agent.
A stable controlled release oral pharmaceutical pellet consisting essentially of:
- (a) an extruded spheronized core comprising a therapeutically effective amount of tolterodine tartrate, lactose and microcrystalline cellulose;
- (b) a rapidly disintegrating or rapidly dissolving coating applied directly to the core that exhibits a low water vapor transmission rate as determined by a water permeability analyzer wherein a test sample of the rapidly disintegrating or rapidly dissolving coating is tested for under 25° C./60% relative humidity, 25° C./80% relative humidity and 40° C./75% relative humidity and the slope of the water vapor transmission versus time plot exhibits a slope that is less than 40 under all three test conditions;
- (c) a controlled release coating comprising a water insoluble polymer and a pore forming agent;
- and
- (d) a delayed release coating comprising a pH dependent polymer.
Dependencies are inferred from the claim text.