Solid Pharmaceutical Dosage Formulation

Abstract

The present invention provides a pharmaceutical dosage formulation, and more particularly, a pharmaceutical dosage formulation comprising an HIV protease inhibitor.

1 . A method of treating HIV/AIDS by administering to a patient in need thereof a solid pharmaceutical dosage form comprising an undissolved form of lopinavir, wherein said dosage form is taken by said patient without food or under a fasting condition. 
     
     
         2 . The method of  claim 1 , wherein said undissolved form of lopinavir is a solid dispersion comprising lopinavir in a matrix, said matrix comprising a pharmaceutically acceptable water-soluble polymer having a Tg of at least 50° C. and a pharmaceutically acceptable surfactant having an HLB value of from 4 to 10. 
     
     
         3 . The method of  claim 2 , wherein said dosage form comprises from 50 to 85% by weight of the total dosage form of said water-soluble polymer, and from 2 to 20% by weight of the total dosage form of said surfactant. 
     
     
         4 . The method of  claim 3 , wherein said solid dispersion further comprises ritonavir. 
     
     
         5 . The method of  claim 4 , wherein said water-soluble polymer is a copolymer of N-vinyl pyrrolidone and vinyl acetate. 
     
     
         6 . The method of  claim 4 , wherein said surfactant is a sorbitan fatty acid ester. 
     
     
         7 . The method of  claim 4 , wherein said water-soluble polymer is a copolymer of N-vinyl pyrrolidone and vinyl acetate, and said surfactant is a sorbitan fatty acid ester. 
     
     
         8 . The method of  claim 4 , wherein said water-soluble polymer is copovidone, and said surfactant is sorbitan monolaurate. 
     
     
         9 . The method of  claim 1 , wherein said undissolved form of lopinavir is a solid solution comprising lopinavir in a matrix, said matrix comprising a pharmaceutically acceptable water-soluble polymer having a Tg of at least 50° C. and a pharmaceutically acceptable surfactant having an HLB value of from 4 to 10. 
     
     
         10 . The method of  claim 9 , wherein said dosage form comprises from 50 to 85% by weight of the total dosage form of said water-soluble polymer, and from 2 to 20% by weight of the total dosage form of said surfactant. 
     
     
         11 . The method of  claim 10 , wherein said solid solution further comprises ritonavir. 
     
     
         12 . The method of  claim 11 , wherein said water-soluble polymer is a copolymer of N-vinyl pyrrolidone and vinyl acetate. 
     
     
         13 . The method of  claim 11 , wherein said surfactant is a sorbitan fatty acid ester. 
     
     
         14 . The method of  claim 11 , wherein said water-soluble polymer is a copolymer of N-vinyl pyrrolidone and vinyl acetate, and said surfactant is a sorbitan fatty acid ester. 
     
     
         15 . The method of  claim 11 , wherein said water-soluble polymer is copovidone, and said surfactant is sorbitan monolaurate.