Apixaban formulations
AssigneesBristol-Myers Squibb Company, Pfizer Inc.
InventorsJatin Patel, Charles Frost, Jingpin Jia, Chandra Vemavarapu
Life of this patent
Estimating the term…
Abstract
Compositions comprising crystalline apixaban particles having a D90 equal to or less than 89 μm, and a pharmaceutically acceptable carrier, are substantially bioequivalent and can be used to for the treatment and/or prophylaxis of thromboembolic disorders.
Claims26
1-9. (canceled)
A solid pharmaceutical composition comprising a therapeutically effective amount of apixaban and a pharmaceutically acceptable diluent or carrier,
- wherein raw materials from which the solid pharmaceutical composition is prepared comprise crystalline apixaban particles having a D90 equal to or less than about 89 μm, and
- wherein, as measured using a USP Apparatus 2 at a paddle rotation speed of 75 rpm in 900 mL of a dissolution medium at 37° C., at least 77 wt % of apixaban in the solid pharmaceutical composition dissolves within 30 minutes in the dissolution medium, and the dissolution medium is 0.05 M sodium phosphate at a pH 6.8 containing 0.05% sodium lauryl sulfate.
A tablet comprising from about 2.5 mg to about 5 mg of apixaban and a pharmaceutically acceptable diluent or carrier,
- wherein the tablet is prepared using crystalline apixaban particles having a D90 equal to or less than about 89 μm as a raw material, and
- wherein, as measured using a USP Apparatus 2 at a paddle rotation speed of 75 rpm in 900 mL of a dissolution medium at 37° C., at least 77 wt % of apixaban in the tablet dissolves within 30 minutes in the dissolution medium, and the dissolution medium is 0.05 M sodium phosphate at a pH 6.8 containing 0.05% sodium lauryl sulfate.
A capsule comprising from about 2.5 mg to about 5 mg of apixaban and a pharmaceutically acceptable diluent or carrier, wherein the capsule is prepared using crystalline apixaban particles having a D90 equal to or less than about 89 μm as a raw material, and wherein, as measured using a USP Apparatus 2 at a paddle rotation speed of 75 rpm in 900 mL of a dissolution medium at 37° C., at least 77 wt % of apixaban in the capsule dissolves within 30 minutes in the dissolution medium, and the dissolution medium is 0.05 M sodium phosphate at a pH 6.8 containing 0.05% sodium lauryl sulfate.
Dependencies are inferred from the claim text.