Orally administrable formulations for the controlled release of a pharmacologically active agent
AssigneeVivus, Inc.
InventorsCalvin Theodore BROMAN, Eric SHEU
Life of this patent
Estimating the term…
Abstract
Drug tablets that include a controlled release layer of a moisture-sensitive active agent are prepared with a lipidic matrix forming excipient, a water-soluble, channel forming excipient and a filler, each being non-hygroscopic. The tablets are formed in a process where the components are blended in the absence of moisture and in particulate form.
Claims20
An orally administrable compressed tablet for controlled release of a moisture-sensitive pharmacologically active agent, comprising:
- a non-hygroscopic, lipidic matrix-forming excipient having a melting point greater than about 40° C.;
- a non-hygroscopic, water-soluble, channel-forming excipient;
- a non-hygroscopic filler;
- and
- a therapeutically effective amount of the pharmacologically active agent, wherein the tablet is substantially free of hygroscopic excipients.
An orally administrable bilayer tablet for controlled release of topiramate and immediate release of phentermine, comprising:
- (a) a first layer comprising
- a controlled release layer of a non-hygroscopic, lipidic matrix-forming excipient having a melting point greater than about 40° C.;
- a non-hygroscopic, water-soluble, channel-forming excipient;
- a non-hygroscopic filler;
- and
- a therapeutically effective amount of topiramate, wherein the first layer is substantially free of hygroscopic excipients;
- and,
- (b) adhered to the first layer, a second layer comprising:
- a non-hygroscopic, water-soluble, channel-forming excipient;
- a non-hygroscopic filler;
- and
- a therapeutically effective amount of phentermine, wherein the second layer is substantially free of hygroscopic excipients.
A process for manufacturing an orally administrable compressed tablet for controlled release of a moisture-sensitive pharmacologically active agent and immediate release of a second pharmacologically active agent, comprising:
- blending, in the absence of moisture and in particulate form, a non-hygroscopic, water-soluble, channel-forming excipient, a non-hygroscopic filler, and manufacturing aids, to form an initial excipient mixture;
- dividing the initial excipient mixture into a first batch and a second batch;
- incorporating a lipidic matrix-forming excipient and a moisture-sensitive active agent into the initial excipient mixture, to form a controlled release formulation;
- incorporating a second active agent into the second batch, to form an immediate release formulation;
- applying compressive force to a contained quantity of the controlled release formulation to form a controlled release layer;
- applying compressive force to a contained quantity of the immediate release formulation to form an immediate release layer;
- and
- compressing the immediate release layer to the controlled release layer in a manner that facilitates bonding of the two layers.
Dependencies are inferred from the claim text.