US2017202825A1PendingUtilityA1

Apixaban formulations

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Assignee: BRISTOL MYERS SQUIBB COPriority: Feb 25, 2010Filed: Mar 30, 2017Published: Jul 20, 2017
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 9/20A61K 9/2095A61K 31/4412A61K 9/16A61K 31/437A61K 9/2018A61K 9/2013A61K 9/4833A61K 9/48A61K 31/4162A61K 9/2054A61K 47/00A61P 1/00A61K 9/0053
58
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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 tablet comprising about 2.5 mg to about 5 mg of apixaban and a pharmaceutically acceptable diluent or carrier, which is prepared by a process comprising:
 blending raw materials comprising apixaban; and   granulating,   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.   
     
     
         11 . The tablet as defined in  claim 10 , wherein the granulating is by dry granulation. 
     
     
         12 . The tablet as defined in  claim 10 , wherein granules produced by the granulating are blended with extragranular raw materials to produce a blend. 
     
     
         13 . The tablet as defined in  claim 12 , wherein the blend is compressed into tablets. 
     
     
         14 . The tablet as defined in  claim 10 , wherein the tablet comprises 2.5 mg of apixaban. 
     
     
         15 . The tablet as defined in  claim 10 , wherein the tablet comprises 5 mg of apixaban. 
     
     
         16 . A capsule comprising about 2.5 mg to about 5 mg of apixaban and a pharmaceutically acceptable diluent or carrier, which is prepared by a process comprising blending raw materials comprising apixaban,
 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.   
     
     
         17 . The capsule as defined in  claim 16 , wherein the capsule comprises 2.5 mg of apixaban. 
     
     
         18 . The capsule as defined in  claim 16 , wherein the capsule comprises 5 mg of apixaban. 
     
     
         19 . A process for preparing a tablet comprising about 2.5 mg to about 5 mg of apixaban and a pharmaceutically acceptable diluent or carrier, the process comprising:
 blending raw materials comprising apixaban; and   granulating,   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.   
     
     
         20 . The process as defined in  claim 19 , wherein the granulating is by dry granulation. 
     
     
         21 . The process as defined in  claim 19 , further comprising blending granules produced by the granulating with extragranular raw materials to produce a blend. 
     
     
         22 . The process as defined in  claim 21 , further comprising compressing the blend into tablets. 
     
     
         23 . The process as defined in  claim 19 , wherein the tablet comprises 2.5 mg of apixaban. 
     
     
         24 . The process as defined in  claim 19 , wherein the tablet comprises 5 mg of apixaban. 
     
     
         25 . A process for preparing a capsule comprising about 2.5 mg to about 5 mg of apixaban and a pharmaceutically acceptable diluent or carrier, the process comprising blending raw materials comprising apixaban,
 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.   
     
     
         26 . The process as defined in  claim 25 , wherein the capsule comprises 2.5 mg of apixaban. 
     
     
         27 . The process as defined in  claim 25 , wherein the capsule comprises 5 mg of apixaban. 
     
     
         28 . A tablet comprising about 2.5 mg to about 5 mg of apixaban and a pharmaceutically acceptable diluent or carrier, which is prepared by a process comprising:
 blending raw materials comprising crystalline apixaban particles; and   granulating using dry granulation,   wherein the crystalline apixaban particles have a D90 equal to or less than 89 μm.   
     
     
         29 . The tablet as defined in  claim 28 , wherein the crystalline apixaban particles comprise Form N-1 of apixaban. 
     
     
         30 . The tablet as defined in  claim 28 , wherein the D 90  is equal to or less than 85 μm. 
     
     
         31 . The tablet as defined in  claim 28 , wherein the D 90  is equal to or less than 50 μm. 
     
     
         32 . The tablet as defined in  claim 28 , wherein the D 90  is equal to or less than 30 μm. 
     
     
         33 . The tablet as defined in  claim 28 , wherein the D 90  is equal to or less than 25 μm. 
     
     
         34 . The tablet as defined in  claim 28 , wherein the tablet comprises 2.5 mg of apixaban. 
     
     
         35 . The tablet as defined in  claim 28 , wherein the tablet comprises 5 mg of apixaban. 
     
     
         36 . A capsule comprising about 2.5 mg to about 5 mg of apixaban and a pharmaceutically acceptable diluent or carrier, which is prepared by a process comprising blending raw materials comprising crystalline apixaban particles,
 wherein the crystalline apixaban particles have a D90 equal to or less than 89 μm.   
     
     
         37 . The capsule as defined in  claim 36 , wherein the crystalline apixaban particles comprise Form N-1 of apixaban. 
     
     
         38 . The capsule as defined in  claim 36 , wherein the D 90  is equal to or less than 85 μm. 
     
     
         39 . The capsule as defined in  claim 36 , wherein the D 90  is equal to or less than 50 μm. 
     
     
         40 . The capsule as defined in  claim 36 , wherein the D 90  is equal to or less than 30 μm. 
     
     
         41 . The capsule as defined in  claim 36 , wherein the D 90  is equal to or less than 25 μm. 
     
     
         42 . The capsule as defined in  claim 36 , wherein the capsule comprises 2.5 mg of apixaban. 
     
     
         43 . The capsule as defined in  claim 36 , wherein the capsule comprises 5 mg of apixaban. 
     
     
         44 . A process for preparing a tablet comprising about 2.5 mg to about 5 mg of apixaban and a pharmaceutically acceptable diluent or carrier, the process comprising:
 blending raw materials comprising crystalline apixaban particles; and   granulating using dry granulation,   wherein the crystalline apixaban particles have a D90 equal to or less than 89 μm.   
     
     
         45 . The process as defined in  claim 44 , further comprising blending granules produced by the granulating with extragranular raw materials to produce a blend. 
     
     
         46 . The process as defined in  claim 45 , further comprising compressing the blend into tablets. 
     
     
         47 . The process as defined in  claim 44 , wherein the crystalline apixaban particles comprise Form N-1 of apixaban. 
     
     
         48 . The process as defined in  claim 44 , wherein the D 90  is equal to or less than 85 μm. 
     
     
         49 . The process as defined in  claim 44 , wherein the D 90  is equal to or less than 50 μm. 
     
     
         50 . The process as defined in  claim 44 , wherein the tablet comprises 2.5 mg of apixaban. 
     
     
         51 . The process as defined in  claim 44 , wherein the tablet comprises 5 mg of apixaban. 
     
     
         52 . A process for preparing a capsule comprising about 2.5 mg to about 5 mg of apixaban and a pharmaceutically acceptable diluent or carrier, the process comprising blending raw materials comprising crystalline apixaban particles,
 wherein the crystalline apixaban particles have a D90 equal to or less than 89 μm.   
     
     
         53 . The process as defined in  claim 52 , wherein the crystalline apixaban particles comprise Form N-1 of apixaban. 
     
     
         54 . The process as defined in  claim 52 , wherein the D 90  is equal to or less than 85 μm. 
     
     
         55 . The process as defined in  claim 52 , wherein the D 90  is equal to or less than 50 μm. 
     
     
         56 . The process as defined in  claim 52 , wherein the D 90  is equal to or less than 30 μm. 
     
     
         57 . The process as defined in  claim 52 , wherein the D 90  is equal to or less than 25 μm. 
     
     
         58 . The process as defined in  claim 52 , wherein the capsule comprises 2.5 mg of apixaban. 
     
     
         59 . The process as defined in  claim 52 , wherein the capsule comprises 5 mg of apixaban.

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