Pharmaceutical compositions of lurasidone
AssigneeCadila Healthcare Limited
InventorsBrij Khera, Aman Trehan, Pankaj Ramanbhai Patel
Life of this patent
Estimating the term…
Abstract
The present invention relates to pharmaceutical compositions of lurasidone or salts thereof. In particular, the invention relates to pharmaceutical compositions of lurasidone or salts thereof with one or more water-insoluble pharmaceutical excipients. The invention also relates to processes for the preparation of such compositions and use thereof for treatment of schizophrenia, bipolar disorders or senile dementia.
Claims20
A solid pharmaceutical composition in the form of a tablet comprising lurasidone or salts thereof and one or more water-insoluble pharmaceutical excipients, wherein the composition comprises:
- (a) granules comprising lurasidone or salt thereof, a first portion of a water-insoluble disintegrating agent, a water-insoluble polymer binder, and one or more water-insoluble excipients;
- and
- (b) a second portion of a water-insoluble disintegrating agent,
- wherein said granules are mixed in said second portion of water-insoluble disintegrating agent,
- wherein the composition is free of water-soluble excipients, and wherein the dissolution of the tablet in a Mcllvaine buffer, pH 4.0 at a paddle rotation of 50 rpm and a test solution volume of 900 ml results in between 37.4% and 62.6% dissolution of the tablet after five minutes for a tablet containing 10 mg, 20 mg, 40 mg or 80 mg of lurasidone.
A solid dosage form of a pharmaceutical composition in the form of a tablet comprising lurasidone or salts thereof and one or more pharmaceutical excipients, wherein the composition comprises:
- (a) granules comprising lurasidone or salt thereof, a first portion of a water-insoluble disintegrating agent, a water-insoluble polymer binder, and one or more water-insoluble excipients;
- and
- (b) a second portion of a water-insoluble disintegrating agent;
- wherein said granules are mixed in said second portion of water-insoluble disintegrating agent and the composition comprises (a) about 20% to about 45% by weight of lurasidone or salts thereof, (b) about 10% to about 80% by weight of microcrystalline cellulose, (c) about 1% to about 55% by weight of ethyl cellulose, and (d) about 1% to about 10% by weight of crospovidone, or mixture thereof,
- wherein the composition is free of pregelatinized starch, and exhibits a dissolution profile in a Mcllvaine buffer, pH 4.0 at a paddle rotation of 50 rpm and a test solution volume of 900 ml, such that the dissolution percentages for a tablet containing 10 mg, 20 mg, 40 mg or 80 mg of lurasidone at 15 minutes are within +/− 10% of each other.
A solid pharmaceutical composition free of water-soluble excipients and in the form of tablets comprising:
- (a) granules comprising lurasidone or salt thereof, a first portion of a water-insoluble disintegrating agent, a water-insoluble polymer binder, and one or more water-insoluble excipients;
- and
- (b) a second portion of a water-insoluble disintegrating agent;
- wherein said granules are mixed in said second portion of water-insoluble disintegrating agent,
- and the tablet exhibits a dissolution profile in a Mcllvaine buffer, pH 4.0 at a paddle rotation of 50 rpm and a test solution volume of 900 ml, such that the dissolution percentages for a solid dosage form containing 10 mg, 20 mg, 40 mg or 80 mg of lurasidone at 15 minutes are within +/− 10% of each other.
A pharmaceutical composition in the form of a tablet comprising:
- (i) granules comprising lurasidone or salt thereof, a first portion of a water-insoluble disintegrating agent, a water-insoluble polymer binder, and one or more water-insoluble excipients;
- and
- (ii) a second portion of a water-insoluble disintegrating agent;
- wherein said granules are mixed in the second portion of water-insoluble disintegrating agent,
- (a) about 20% to about 45% by weight of lurasidone or salts thereof;
- (b) about 10% to about 80% by weight of one or more water-insoluble diluents;
- (c) about 1% to about 55% by weight of one or more water-insoluble binders;
- and
- (d) about 1% to about 10% by weight of one or more water-insoluble disintegrating agents,
- wherein the composition is free of a pregelatinized starch and water-soluble excipients, and the dissolution of the tablet in a Mcllvaine buffer, pH 4.0 at a paddle rotation of 50 rpm and a test solution volume of 900 ml results in between 37.4% and 62.6% dissolution of the tablet after five minutes for a tablet containing 10 mg, 20 mg, 40 mg or 80 mg of lurasidone and a dissolution profile such that the dissolution percentages for a tablet containing 10 mg, 20 mg, 40 mg or 80 mg of lurasidone at 15 minutes are within +/− 10% of each other.
Dependencies are inferred from the claim text.