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Claims for Patent: 8,399,015

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Claims for Patent: 8,399,015

Title:Solid pharmaceutical dosage form
Abstract: A solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant, said pharmaceutically acceptable water-soluble polymer having a Tg of at least about 50.degree. C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10.
Inventor(s): Rosenberg; Joerg (Ellerstadt, DE), Reinhold; Ulrich (Heidelberg, DE), Liepold; Bernd (Dossenheim, DE), Berndl; Gunther (Herxheim, DE), Breitenbach; Joerg (Mannheim, DE), Alani; Laman (Foster City, CA), Ghosh; Soumojeet (Gurnee, IL)
Assignee: AbbVie Inc. (Waukegan, IL)
Application Number:13/240,119
Patent Claims: 1. A solid pharmaceutical dosage form comprising a solid dispersion which includes: lopinavir and ritonavir; a pharmaceutically acceptable water-soluble polymer having a Tg of at least 50.degree. C., and a pharmaceutically acceptable surfactant having an HLB value of from 4 to 10.

2. The dosage form of claim 1, wherein said surfactant is a sorbitan fatty acid ester.

3. The dosage form of claim 1, wherein said water-soluble polymer is a copolymer of N-vinyl pyrrolidone and vinyl acetate.

4. The dosage form of claim 1, wherein said water-soluble polymer is copovidone.

5. The dosage form of claim 1, wherein said water-soluble polymer is a copolymer of N-vinyl pyrrolidone and vinyl acetate, and said surfactant is a sorbitan fatty acid ester.

6. The dosage form of claim 1, wherein said solid dispersion is a solid solution or a glassy solution.

7. The dosage form of claim 5, wherein said solid dispersion is a solid solution or a glassy solution.

8. The dosage form of claim 1, wherein said water-soluble polymer has a Tg of from 80 to 180.degree. C.

9. The dosage form of claim 1, wherein said dosage form has a dose-adjusted AUC, in dogs under non-fasting conditions, of ritonavir plasma concentration of at least 9 .mu.g h/ml/100 mg, and a dose-adjusted AUC, in dogs under non-fasting conditions, of lopinavir plasma concentration of at least 20 .mu.g h/ml/100 mg.

10. The dosage form of claim 1 which contains, upon storage for 6 weeks at 40.degree. C. and 75% humidity, at least 98% of the initial content of ritonavir.

11. The dosage form of claim 1, 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.

12. A solid pharmaceutical dosage form comprising lopinavir and ritonavir formulated in solid dispersion, wherein said solid dispersion comprise (1) a pharmaceutically acceptable water-soluble polymer having a Tg of at least 50.degree. C., or a combination of pharmaceutically acceptable water-soluble polymers having a Tg of at least 50.degree. C.; and (2) a pharmaceutically acceptable surfactant having an HLB value of from 4 to 10, or a combination of pharmaceutically acceptable surfactants having an HLB value of from 4 to 10.

13. The dosage form of claim 12, wherein said solid dispersion comprises a combination of pharmaceutically acceptable water-soluble polymers having a Tg of at least 50.degree. C.

14. The dosage form of claim 12, wherein said solid dispersion comprises a combination of pharmaceutically acceptable surfactants which has an HLB value of from 4 to 10.

15. The dosage form of claim 12, wherein said solid dispersion is solid solution or glassy solution.

16. The dosage form of claim 12, wherein said dosage form has a dose-adjusted AUC, in dogs under non-fasting conditions, of ritonavir plasma concentration of at least 9 .mu.g h/ml/100 mg, and a dose-adjusted AUC, in dogs under non-fasting conditions, of lopinavir plasma concentration of at least 20 .mu.g h/ml/100 mg.

17. The dosage form of claim 12 which contains, upon storage for 6 weeks at 40.degree. C. and 75% humidity, at least 98% of the initial content of ritonavir.

18. A solid pharmaceutical dosage form comprising a solid dispersion which includes (i) ritonavir, (ii) a pharmaceutically acceptable water-soluble polymer having a Tg of at least 50.degree. C., and (iii) a pharmaceutically acceptable surfactant having an HLb value of from 4 to 10.

19. The dosage form of claim 18, wherein said solid dispersion is a solid solution or a glassy solution.

20. The dosage form of claim 19, wherein said surfactant is a sorbitan fatty acid ester.

21. The dosage form of claim 19, wherein said water-soluble polymer is a copolymer of N-vinyl pyrrolidone and vinyl acetate, and said surfactant is a sorbitan fatty acid ester.

22. The dosage form of claim 19, wherein said water-soluble polymer is copovidone, and said surfactant is sorbitan monolaurate.

23. The dosage form of claim 18, wherein said dosage form has a dose-adjusted AUC, in dogs under non-fasting conditions, of ritonavir plasma concentration of at least 9 .mu.g h/ml/100 mg.

24. The dosage form of claim 18 which contains, upon storage for 6 weeks at 40.degree. C. and 75% humidity, at least 98% of the initial content of ritonavir.

25. The dosage form of claim 19, 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.

26. The dosage form of claim 25, wherein said water-soluble polymer is a copolymer of N-vinyl pyrrolidone and vinyl acetate, and said surfactant is a sorbitan fatty acid ester.

27. The dosage form of claim 25, wherein said water-soluble polymer is copovidone, and said surfactant is sorbitan monolaurate.

28. A solid pharmaceutical dosage form comprising ritonavir formulated in solid dispersion, wherein said solid dispersion comprise (1) a pharmaceutically acceptable water soluble polymer having a Tg of at least 50.degree. C. or a combination of pharmaceutically acceptable water-soluble polymers having a Tg of at least 50.degree. C.; and (2) a pharmaceutically acceptable surfactant having an HLB value of from 4 to 10, or a combination of pharmaceutically acceptable surfactants which has an HLB value of from 4 to 10.

29. The dosage form of claim 28, wherein said solid dispersion is solid solution or glassy solution.

30. The dosage form of claim 29, wherein said solid dispersion comprises a combination of pharmaceutically acceptable surfactants which has an HLB value of from 4 to 10.

31. The dosage form of claim 29, wherein said dosage form comprises from 50 to 85% by weight of the total dosage form of said water-soluble polymer or said combination of said polymers, and from 2 to 20% by weight of the total dosage form of said surfactant or said combination of surfactants.
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