US2016243101A1PendingUtilityA1

Apixaban formulations

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Assignee: BRISTOL MYERS SQUIBB COPriority: Feb 25, 2010Filed: Mar 31, 2016Published: Aug 25, 2016
Est. expiryFeb 25, 2030(~3.6 yrs left)· nominal 20-yr term from priority
Inventors:Jatin M. PatelCharles FrostJingpin JiaChandra Vemavarapu
A61K 31/4545A61K 9/14A61P 7/02A61K 31/437A61K 9/2054A61K 9/16A61K 9/2018A61K 31/4412A61K 31/4162A61K 9/4833A61K 9/48A61K 9/20A61K 9/2095A61K 9/2013A61K 47/00A61P 1/00A61K 9/0053
56
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Claims

Abstract

Compositions comprising crystalline apixaban particles having a D 90 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.

Claims

exact text as granted — not AI-modified
1 - 9 . (canceled) 
     
     
         10 . 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 D 90  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.   
     
     
         11 . The composition as defined in  claim 10 , wherein the crystalline apixaban particles comprise Form N-1 of apixaban. 
     
     
         12 . The composition as defined in  claim 10 , wherein the raw materials are granulated during preparation of the solid pharmaceutical composition. 
     
     
         13 . The composition as defined in  claim 12 , wherein the raw materials are granulated by dry granulation. 
     
     
         14 . The composition as defined in  claim 10 , wherein the D 90  is equal to or less than 85 μm. 
     
     
         15 . The composition as defined in  claim 10 , wherein the D 90  is equal to or less than 50 μm. 
     
     
         16 . The composition as defined in  claim 10 , wherein the D 90  is equal to or less than 30 μm. 
     
     
         17 . The composition as defined in  claim 10 , wherein the D 90  is equal to or less than 25 μm. 
     
     
         18 . The composition as defined in  claim 10 , wherein the pharmaceutical composition comprises from about 2.5 mg to about 5 mg of apixaban. 
     
     
         19 . The composition as defined in  claim 10 , wherein the pharmaceutical composition comprises 2.5 mg of apixaban. 
     
     
         20 . The composition as defined in  claim 10 , wherein the pharmaceutical composition comprises 5 mg of apixaban. 
     
     
         21 . The composition as defined in  claim 10 , which is a tablet. 
     
     
         22 . The composition as defined in  claim 10 , which is a capsule. 
     
     
         23 . The composition as defined in  claim 18 , which is a tablet. 
     
     
         24 . The composition as defined in  claim 18 , which is a capsule. 
     
     
         25 . The composition as defined in  claim 19 , which is a tablet. 
     
     
         26 . The composition as defined in  claim 19 , which is a capsule. 
     
     
         27 . The composition as defined in  claim 20 , which is a tablet. 
     
     
         28 . The composition as defined in  claim 20 , which is a capsule. 
     
     
         29 . 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 D 90  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.   
     
     
         30 . The tablet as defined in  claim 29 , comprising 2.5 mg of apixaban. 
     
     
         31 . The tablet as defined in  claim 29 , comprising 5 mg of apixaban. 
     
     
         32 . 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 D 90  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. 
     
     
         33 . The capsule as defined in  claim 32 , comprising 2.5 mg of apixaban. 
     
     
         34 . The capsule as defined in  claim 32 , comprising 5 mg of apixaban.

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