Pharmaceutical dosage form comprising polymeric carrier composition

Abstract

A pharmaceutical dosage form comprises a solid dispersion product of at least one active ingredient dispersed in a polymeric binder composition, the polymeric carrier composition comprising a) a vinylpyrrolidone homopolymer, wherein at least 95% by weight of the vinylpyrrolidone homopolymer has a molecular weight distribution within the range of from 1000 to 13 000; and b) a vinylpyrrolidone copolymer having a weight-average molecular weight of from 5000 to 1 500 000. The dosage form is preferably prepared by a melt extrusion process. The polymeric carrier composition exhibits a high drug dissolution power and allows a reduction of the viscosity of the melt without deteriorating the mechanical properties and storage stability of the dosage form.

1 . A pharmaceutical dosage form which comprises a solid dispersion product of at least one active ingredient dispersed in a polymeric carrier composition, the polymeric carrier composition comprising
 a) a vinylpyrrolidone homopolymer having a molecular weight distribution such that at least 95% by weight of the homopolymer has a molecular weight within the range of from 1000 to 13 000; and   b) a vinylpyrrolidone copolymer having a weight-average molecular weight of from 5000 to 1 500 000.   
     
     
         2 . The dosage form of  claim 1 , wherein the vinylpyrrolidone copolymer has a ratio Mw/Mn in the range of from 1.5 to 5.0. 
     
     
         3 . The dosage form of  claim 1 ,  2  or  3 , wherein the vinylpyrrolidone copolymer comprises from 20 to 80% by weight of vinylpyrrolidone units, relative to the total weight of the copolymer. 
     
     
         4 . The dosage form of  claim 1  or  2 , wherein the vinylpyrrolidone copolymer is a copolymer of vinylpyrrolidone and at least one vinylester. 
     
     
         5 . The dosage form of  claim 4 , wherein the vinylester is vinylacetate. 
     
     
         6 . The dosage form of  claim 1 , wherein the vinylpyrrolidone homopolymer consists of PVP K12 or PVP K17 or a mixture of both. 
     
     
         7 . The dosage form of  claim 1 , wherein the polymeric carrier composition exhibits a single Tg. 
     
     
         8 . The dosage form of  claim 1 , wherein the weight ratio of a) to b) is in the range of from 5:95 to 50:50. 
     
     
         9 . The dosage form of  claim 1 , wherein the active ingredient is molecularly dispersed in the polymeric carrier composition. 
     
     
         10 . The dosage form of  1 , wherein the solid dispersion product additionally comprises at least one additive selected from solubilizers, flow regulators, disintegrants, bulking agents and lubricants. 
     
     
         11 . A method of preparing a solid dosage form of  claim 1  which comprises:
 a) preparing a liquid mixture containing the at least one active agent, the polymeric carrier composition and at least one solvent, and 
 b) removing the solvent(s) from the liquid mixture to obtain a solid dispersion product. 
 
     
     
         12 . A method of preparing a solid dosage form of  claim 1  which comprises:
 a) preparing a homogeneous melt of said at least one active ingredient and the polymeric carrier composition, and 
 b) allowing the melt to solidify to obtain a solid dispersion product. 
 
     
     
         13 . The method of  claim 12 , additionally comprising grinding said solid dispersion product and compressing said solid dispersion product into a tablet.