Pharmaceutical formulation

Abstract

A pharmaceutical formulation has (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-yl-quinazolin-4-yl)phenyl]-(6-methoxy-pyridazin-3-yl)methanol or pharmaceutically acceptable salt thereof.

1 . A spray-dried solid dispersion of (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-yl-quinazolin-4-yl)phenyl]-(6-methoxy-pyridazin-3-yl)methanol in a polymeric matrix comprising hypromellose acetate succinate. 
     
     
         2 - 7 . (canceled) 
     
     
         8 . The solid dispersion according to  claim 1 , wherein the solid dispersion is a solid solution. 
     
     
         9 . (canceled) 
     
     
         10 . The solid dispersion according to  claim 1 , wherein the concentration of (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-yl-quinazolin-4-yl)phenyl]-(6-methoxy-pyridazin-3-yl)methanol in the polymeric matrix is in a range of between 4 and 50 weight percent, based upon the total weight of the solid dispersion. 
     
     
         11 . (canceled) 
     
     
         12 . A pharmaceutical composition, comprising:
 the solid dispersion according to  claim 1 .   
     
     
         13 . The pharmaceutical composition according to  claim 12 , which is for oral administration. 
     
     
         14 . The pharmaceutical composition according to  claim 13 , which is an immediate release composition. 
     
     
         15 . The pharmaceutical composition according to  claim 14 , wherein the pharmaceutical composition has a disintegration time of 15 minutes or less. 
     
     
         16 - 18 . (canceled) 
     
     
         19 . The pharmaceutical composition according to  claim 12 , which is a tablet, comprising:
 at least one pharmaceutically acceptable excipient selected from the group consisting of a filler, a disintegrant, a lubricant, a pore builder, and an inorganic alkaline metal salt.   
     
     
         20 . The pharmaceutical composition according to  claim 12 , which is the tablet, comprising:
 25 to 95 wt. % of the solid dispersion ;   15 to 72.5 wt.% of a filler;   2.5 to 40 wt.% of a disintegrant;   0 to 5 wt.% of a lubricant;   0 to 20 wt.% of an inorganic alkaline metal salt; and   a total of 0 to 20 wt.% of one or more additional pharmaceutically acceptable excipients,   based upon the total weight of the tablet.   
     
     
         21 . The pharmaceutical composition according to  claim 12  which is a tablet, comprising: 
 40 to 60 wt. % of the solid dispersion ; 
 25 to 55 wt.% of a filler; 
 5 to 30 wt.% of a disintegrant; 
 0 to 5 wt.% of a lubricant; 
 0 to 15 wt.% of an inorganic alkaline metal salt: and 
 a total of 0 to 10 wt.% of one or more additional pharmaceutically acceptable excipients, 
 based upon the total weight of the tablet. 
     
     
         22 . The pharmaceutical composition according to  claim 12  which is a tablet, comprising:
 ;35 to 55 wt. % of the solid dispersion ; 
 30 to 55 wt.% of a filler; 
 5 to 20 wt.% of a disintegrant; 
 0.25 to 2.5 wt.% of a lubricant; 
 2.5 to 15 wt. % of an inorganic alkaline metal salt; and 
 a total of 0 to 10 wt.% of one or more additional pharmaceutically acceptable excipients, 
 based upon the total weight of the tablet. 
 
     
     
         23 . The pharmaceutical composition according to  claim 20  wherein said pharmaceutical composition comprises at least one of a filler, a disintegrant, and an inorganic alkaline metal salt, and wherein
 the filler is microcrystalline cellulose, 
 the disintegrant is selected from the group consisting of crospovidone, carboxymethylcellulose, and salts and derivatives thereof, and/or 
 the inorganic alkaline metal salt is an inorganic sodium salt. 
 
     
     
         24 - 32 . (canceled) 
     
     
         33 . The solid dispersion according to  claim 1 , wherein the concentration of (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-yl-quinazolin-4-yl)phenyl]-(6-methoxy-pyridazin-3-yl)methanol in the polymeric matrix is in a range of between 10 to 30 weight percent, based upon the total weight of the solid dispersion.