Pharmaceutical compositions comprising colloidal silicon dioxide

Abstract

A pharmaceutical composition comprising a macrolide solid dispersion, a disintegrant and colloidal silicon dioxide, wherein the composition comprises 1 to 5% colloidal silicon dioxide by weight.

1 . A pharmaceutical composition comprising a macrolide solid dispersion, a disintegrant and colloidal silicon dioxide, wherein the composition comprises 1 to 5% colloidal silicon dioxide by weight. 
     
     
         2 . A pharmaceutical composition according to  claim 1 , wherein 250 mg of the composition, when compressed using a force of 8 to 11 kN with a 9 mm die and standard flat punches, forms a tablet having a hardness of 35 to 80 N and a disintegration time of 3 minutes or less. 
     
     
         3 . A composition according to  claim 1 , wherein the composition is in the form of a dispersible tablet. 
     
     
         4 . A composition according to  claim 3 , wherein the tablet has a disintegration time of 90 seconds or less. 
     
     
         5 . A composition as claimed in  claim 1 , wherein the macrolide is rapamycin, ascomycin or a derivative thereof. 
     
     
         6 . A composition as claimed in  claim 1 , wherein the derivative of rapamycin is 40-o-(2-hydroxy)ethyl-rapamycin. 
     
     
         7 . (canceled) 
     
     
         8 . A method of administering a pharmaceutical composition of  claim 1  to a subject in need of such therapy which comprises (i) contacting the composition with an aqueous solution (ii) allowing the composition to disperse in the aqueous solution to form a dispersed mixture and (ii) ingesting the dispersed mixture. 
     
     
         9 . (canceled) 
     
     
         10 . A process for producing a macrolide-containing dispersible tablet, comprising preparing a macrolide solid dispersion, mixing the macrolide solid dispersion with a disintegrant and colloidal silicon dioxide to form a pharmaceutical composition and compressing the pharmaceutical composition to form the dispersible tablet.