Sustained-release formulations of topiramate
AssigneeSupernus Pharmaceuticals, Inc.
InventorsLikan Liang, Hua Wang, Padmanabh P. Bhatt, Michael L. Vieira
Life of this patent
Estimating the term…
Abstract
Pharmaceutical compositions of topiramate for once-a-day oral administration are provided. The formulations comprise a sustained-release component and an optional immediate-release component, the compositions of which can be selectively adjusted, respectively, to release the active ingredient along a pre-determined release profile. Method of treating or preventing pathological disorders in mammalian subjects comprising the administration of the novel formulations disclosed herein is also provided.
Claims30
A sustained release formulation of topiramate for oral administration to a mammalian subject comprising an immediate release bead population (IR), a first extended release bead population (XR1), and a second extended release bead population (XR2), wherein:
- (a) the IR bead population comprises topiramate up to 10% by wt of the total amount of topiramate in the formulation and 0.1-10% by wt of a binder, wherein the topiramate and binder form a coating on inert carrier particles, wherein the coated inert carrier particles are not coated with a release controlling coating, and wherein the IR bead population releases greater than or equal to 80% of its topiramate in a continuous manner over less than or equal to 1 hour;
- (b) the XR1 bead population comprises topiramate up to 20% by wt of the total amount of topiramate in the formulation, wherein the topiramate is a coating on inert carrier particles, wherein the topiramate coated inert carrier particles are further coated with a release controlling coating material, wherein the coating material comprises 2-15% by weight of the topiramate coated inert carrier particles, and wherein the XR1 bead population releases 80% of its topiramate in a continuous manner over less than or equal to 4 hours;
- and,
- (c) the XR2 bead population comprises topiramate at least 80% by weight of the total amount of topiramate in the formulation, wherein the topiramate is a coating on inert carrier particles, wherein the topiramate coated inert carrier particles are coated with a release controlling coating material, wherein the coating material comprises 2-15% by weight of the topiramate coated inert carrier particles, and wherein the XR2 bead population releases 80% of its topiramate in a continuous manner over less than 8 hours;
- wherein the release controlling coating materials comprise methylcellulose, ethylcellulose, hydroxypropyl cellulose, hydroxypropylmethyl cellulose, cellulose acetate, cellulose acetate phthalate, polyvinyl alcohol, polyacrylates, polymethacrylates or copolymers thereof, and
- wherein the XR1 and XR2 bead populations have their own specific rates of release.
A sustained release formulation of topiramate comprising:
- (a) a first extended release bead population (XR1) comprising up to 20% by wt of the total amount of topiramate in the formulation, wherein the topiramate is a coating on inert carrier particles and further coated with a release controlling coating material, wherein the release controlling material releases 80% of the topiramate in a continuous manner over less than or equal to 4 hours;
- and,
- (b) a second extended release bead population (XR2) comprising at least 80% by weight of the total amount of topiramate in the formulation, wherein the topiramate is coated onto inert carrier particles and further coated with a release controlling coating material,
- wherein the release controlling material releases 80% of the topiramate in a continuous manner over less than 8 hours;
- wherein the release controlling coating materials comprise methylcellulose, ethylcellulose, hydroxypropyl cellulose, hydroxypropylmethyl cellulose, cellulose acetate, cellulose acetate phthalate, polyvinyl alcohol, polyacrylates, polymethacrylates or copolymers thereof;
- and
- wherein the XR1 and XR2 bead populations have their own specific rates of release.
Dependencies are inferred from the claim text.