Muco-adhesive, controlled release formulations of levodopa and/or esters of levodopa and uses thereof
AssigneeImpax Laboratories, LLC
InventorsAnn Hsu, Liang Dong, Amy Ding, Suneel Gupta
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Abstract
The invention provides an oral solid formulation comprising (a) a controlled release component comprising a core comprising levodopa, wherein the core is coated with a muco-adhesive coating and the muco-adhesive coating is externally coated with an enteric coating; and (b) an immediate release component comprising levodopa. The invention further provides a method for making and using the oral solid formulation.
Claims21
A multiparticulate controlled release levodopa solid oral dosage form comprising:
- (i) one or more immediate release levodopa granules;
- and
- (ii) one or more controlled release levodopa particles comprising:
- (a) a spheronized core comprising levodopa and at least one pharmaceutically acceptable excipient selected from the group consisting of a binder, a filler, a wetting agent, and mixtures thereof;
- (b) a rate controlling coating surrounding the spheronized core wherein the rate controlling coating comprises a rate controlling material;
- (c) a muco-adhesive coating surrounding the rate controlling coating wherein the muco-adhesive coating comprises a muco-adhesive material capable of forming a positive ionic charge at pHs present in a human gastro-intestinal tract;
- and
- (d) an enteric coating surrounding the muco-adhesive coating wherein the enteric coating comprises an enteric material.
A multiparticulate controlled release levodopa solid oral dosage form comprising:
- one or more controlled release levodopa particles comprising:
- (a) a core comprising levodopa and at least one pharmaceutically acceptable excipient selected from the group consisting of a binder, a filler, a wetting agent, and mixtures thereof;
- (b) a rate controlling coating surrounding the core wherein the rate controlling coating comprises a rate controlling material;
- (c) a muco-adhesive coating surrounding the rate controlling coating wherein the muco-adhesive coating comprises a muco-adhesive material capable of forming a positive ionic charge at pHs present in a human gastro-intestinal tract;
- and
- (d) an enteric coating surrounding the muco-adhesive coating wherein the enteric coating comprises an enteric material.
A multiparticulate controlled release levodopa solid oral dosage form comprising:
- (i) an immediate release component comprising one or more immediate release levodopa granules;
- and
- (ii) a controlled release component comprising one or more controlled release levodopa particles comprising:
- (a) a spheronized core comprising levodopa and (b) a muco-adhesive coating surrounding the spheronized core wherein the muco-adhesive coating comprises a muco-adhesive material capable of forming a positive ionic charge at pHs present in a human gastro-intestinal tract, and wherein ratio of levodopa in the controlled release component:levodopa in the immediate release component is about 3:1.
Dependencies are inferred from the claim text.