US2013131087A1PendingUtilityA1

Pharmaceutical Compositions

Assignee: BANKS SIMONPriority: Aug 21, 2006Filed: Dec 21, 2012Published: May 23, 2013
Est. expiryAug 21, 2026(~0.1 yrs left)· nominal 20-yr term from priority
Inventors:Simon Banks
A61P 37/02A61P 7/00A61P 9/00A61P 43/00A61P 9/10A61P 7/02A61K 47/36A61K 31/519A61K 47/02A61K 47/10A61K 9/2018A61K 47/38A61K 9/2009A61K 9/16
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Claims

Abstract

The present invention relates to pharmaceutical compositions and, more particularly, to a pharmaceutical composition containing the compound {1S-[1α, 2α, 3β(1S*,2R*),5β]}-3-(7-{[2-(3,4-difluorophenyl)cyclopropyl]amino}-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol.

Claims

exact text as granted — not AI-modified
1 - 16 . (canceled) 
     
     
         17 . An oral pharmaceutical composition comprising:
 {1S-[1α, 2α, 3β(1S*,2R*),5β]}-3-(7-{[2-(3,4-difluorophenyl)cyclopropyl]amino}-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol substantially present in the form of Polymorph II in an amount of 20 to 45% by weight of the pharmaceutical composition as a whole;   mannitol in an amount of 20 to 45% by weight of the pharmaceutical composition as a whole;   dibasic calcium phosphate dihydrate in an amount of 10 to 30% by weight of the pharmaceutical composition as a whole;   hydroxypropyl cellulose in an amount of 3 to 6% by weight of the pharmaceutical composition as a whole;   sodium starch glycolate in an amount of 2 to 6% by weight of the pharmaceutical composition as a whole; and   one or more lubricants in an amount of 0.5 to 3% by weight of the pharmaceutical composition as a whole.   
     
     
         18 . An oral solid pharmaceutical composition comprising: 
       a solid core comprising
 (1) {1S-[1α, 2α, 3β(1S*,2R*),5β]}-3-(7-{[2-(3,4-difluorophenyl)cyclopropyl]amino}-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol in an amount of 90 mg; and 
 (2) means for releasing substantially all 90 mg of said 1,2-diol from the solid pharmaceutical composition after oral administration. 
 
     
     
         19 . The solid pharmaceutical composition of  claim 18 , wherein the 1,2-diol is substantially as Polymorph II. 
     
     
         20 . The solid pharmaceutical composition of  claim 18 , wherein at least 90% of the 1,2-diol is Polymorph II. 
     
     
         21 . The solid pharmaceutical composition of  claim 19 , wherein the 1,2-diol is at least 95% Polymorph II. 
     
     
         22 . The solid pharmaceutical composition of  claim 18 , wherein at least 90% of the 90 mg of the 1,2-diol is released from the solid pharmaceutical composition. 
     
     
         23 . The solid pharmaceutical composition of  claim 21 , wherein at least 90% of the 90 mg of the 1,2-diol is released from the solid pharmaceutical composition.

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