Pharmaceutical compositions comprising azd9291

Abstract

The present invention relates to pharmaceutical compositions suitable for oral administration, and more particularly to pharmaceutical compositions, including pharmaceutical tablet compositions, containing N-(2-{2-dimethylaminoethyl-methylamino}-4-methoxy-5-{[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide (“AZD9291”) or a pharmaceutically acceptable salt thereof, wherein such compositions comprise a certain amount of microcrystalline cellulose and at least one other pharmaceutical diluent.

1 . A pharmaceutical composition comprising:
 (a) from 2 to 70 parts of the Agent;   (b) from 5 to 96 parts of two or more pharmaceutical diluents;   (c) from 0 to 15 parts of one or more pharmaceutical disintegrants;   (d) from 0 to 1.5 parts of one or more pharmaceutical solubilising agents; and   (c) from 0 to 3 parts of one or more pharmaceutical lubricants;   
       wherein all parts are by weight and the sum of the parts (a)+(b)+(c)+(d)+(e)=100; 
       wherein one of the two or more pharmaceutical diluents is microcrystalline cellulose wherein the microcrystalline cellulose makes up from 7 to 30 wt % of the two or more pharmaceutical diluents (b); and wherein the Agent is N-(2-{2-dimethylaminoethyl-methylamino}-4-methoxy-5-{[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide or a pharmaceutically acceptable salt thereof. 
     
     
         2 . The pharmaceutical composition according to  claim 1  wherein the pharmaceutical composition comprises from 0.5 to 3 parts of the one or more pharmaceutical lubricants (e). 
     
     
         3 . The pharmaceutical composition according to  claim 2  wherein the one or more pharmaceutical lubricants (e) comprises sodium stearyl fumarate and/or one or more behenate esters of glycerine. 
     
     
         4 . The pharmaceutical composition according to any one of  claims 1  to  3 , wherein the pharmaceutical composition comprises from 2 to 15 parts of the one or more pharmaceutical disintegrants (c). 
     
     
         5 . The pharmaceutical composition according to  claim 4  wherein the one or more pharmaceutical disintegrants (c) comprises low-substituted hydroxypropyl cellulose. 
     
     
         6 . The pharmaceutical composition according to any one of  claims 1  to  5 , wherein the pharmaceutical composition comprises from 0 to 0.75 parts of one or more pharmaceutical solubilising agents (d). 
     
     
         7 . The pharmaceutical composition according to any one of  claims 1  to  6 , wherein the pharmaceutical composition comprises from 5 to 50 parts of the Agent (a). 
     
     
         8 . The pharmaceutical composition according to any one of  claims 1  to  7  wherein the Agent is the mesylate salt of N-(2-{2-dimethylaminoethyl-methylamino}-4-methoxy-5-{[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide. 
     
     
         9 . Use of the pharmaceutical composition, as claimed in any one of  claims 1  to  8 , for the manufacture of a medicament. 
     
     
         10 . A pharmaceutical composition, as claimed in any one of  claims 1  to  8 , for use as a medicament. 
     
     
         11 . A method of treating cancer in a patient in need thereof, which method comprises the oral administration to the patient of an effective amount of the pharmaceutical composition as claimed in any one of  claims 1  to  8 . 
     
     
         12 . A pharmaceutical tablet comprising the pharmaceutical composition as claimed in any one of  claims 1  to  8 . 
     
     
         13 . A pharmaceutical tablet comprising a tablet core wherein the tablet core comprises the pharmaceutical composition as claimed in any one of  claims 1  to  8 , wherein the tablet core has a coating. 
     
     
         14 . A method of treating cancer in a patient in need thereof, which method comprises the oral administration of an effective number of the pharmaceutical tablet(s), as claimed in  claim 12  or  claim 13 , to the patient.