Immediate release pharmaceutical formulation of 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2h-phthalazin-1-one

Abstract

The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one for increasing the bioavailability of the drug.

1 - 14 . (canceled) 
     
     
         15 . An immediate-release pharmaceutical composition in the form of a solid dispersion, the composition comprising:
 an active agent phase comprising 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one (Compound 1) or a salt thereof; and   a carrier phase comprising copovidone; and   wherein the active agent phase is dispersed in the carrier phase:   wherein the total concentration of Compound 1 in the composition is in the range of from 10% by weight to 40% by weight;   wherein the total amount of Compound 1 in the composition is in the range of from 25 mg to 400 mg; and   wherein the weight ratio of Compound 1 to copovidone is in the range of from 1:1.5 to 1:9.   
     
     
         16 . The composition of  claim 15 , wherein Compound 1 is in an amorphous form. 
     
     
         17 . The composition of  claim 15 , wherein at least 90% of Compound 1 is in an amorphous form. 
     
     
         18 . The composition of  claim 15 , wherein the composition is made by solvent evaporation or melt extrusion. 
     
     
         19 . The composition of  claim 18 , wherein the composition is made by melt extrusion. 
     
     
         20 . An immediate-release pharmaceutical composition in the form of a solid dispersion, the composition comprising:
 an active agent phase comprising 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one (Compound 1) or a salt thereof;   and a carrier phase comprising copovidone; and   wherein the active agent phase is dispersed in the carrier phase;   wherein the total concentration of Compound 1 in the composition is in the range of from 10% by weight to 40% by weight;   wherein the total amount of Compound 1 in the composition is in the range of from 10 mg to 1,000 mg; and   wherein the weight ratio of Compound 1 to copovidone is in the range of from 1:1.5 to 1:9.