Claims
- 1. A pharmaceutical composition for oral administration which is a solution comprising:(a) an HIV protease inhibiting compound which is (2S,3S,5S)-5-(N-(N-((N-Methyl-N-((2-isopropyl-4-thiazolyl)methyl)-amino)carbonyl)valinyl)amino)-2-(N-((5-thiazolyl)methoxycarbonyl)amino)-1,6-diphenyl-3-hydroxyhexane (ritonavir), (b) a pharmaceutically acceptable organic solvent which comprises a pharmaceutically acceptable long chain fatty acid or a mixture of a pharmaceutically acceptable long chain fatty acid selected from the group consisting of saturated, mono-unsaturated and di-unsaturated C12 to C18 carboxylic acids which are liquids at room temperature and a pharmaceutically acceptable alcohol, and, optionally, (c) a pharmaceutically acceptable surfactant.
- 2. The composition of claim 1 comprising:(a) an HIV protease inhibiting compound which is (2S,3S,5S)-5-(N-(N-((N-Methyl-N-((2-isopropyl-4-thiazolyl)methyl)-amino)carbonyl)valinyl)amino)-2-(N-((5-thiazolyl)methoxycarbonyl)amino)-1,6-diphenyl-3-hydroxyhexane (ritonavir), in the amount of from about 1% to about 50% by weight of the total solution, (b) a pharmaceutically acceptable organic solvent which comprises (i) a pharmaceutically acceptable long chain fatty acid selected from the group consisting of saturated, mono-unsaturated and di-unsaturated C12 to C18 carboxylic acids which are liquids at room temperature in the amount of from about 20% to about 99% by weight of the total solution or (ii) a mixture of (1) a pharmaceutically acceptable long chain fatty acid selected from the group consisting of saturated, mono-unsaturated and di-unsaturated C12 to C18 carboxylic acids which are liquids at room temperature in the amount of from about 20% to about 99% by weight of the total solution and (2) a pharmaceutically acceptable alcohol in the amount of from about 0% to about 15% by weight of the total solution and (c) a pharmaceutically acceptable surfactant in the amount of from about 0% to about 40% by weight of the total solution.
- 3. The composition of claim 1 wherein the solution is encapsulated in a hard gelatin capsule or a soft elastic gelatin capsule.
- 4. The composition of claim 1 wherein the solvent comprises:(1) a pharmaceutically acceptable long chain fatty acid selected from the group consisting of saturated, mono-unsaturated and di-unsaturated C12 to C18 carboxylic acids which are liquids at room temperature in the amount of from about 40% to about 70% by weight of the total solution and (2) ethanol or propylene glycol in the amount of from about 1% to about 15% by weight of the total solution or a mixture of ethanol and propylene glycol in the amount of from about 1% to about 15% by weight of the total solution.
- 5. The composition of claim 1 wherein the solvent comprises:(1) a pharmaceutically acceptable long chain fatty acid selected from the group consisting of saturated, mono-unsaturated and di-unsaturated C12 to C18 carboxylic acids which are liquids at room temperature in the amount of from about 40% to about 70% by weight of the total solution and (2) ethanol in the amount of from about 10% to about 12% by weight of the total solution or propylene glycol in the amount of from about 5% to about 10% by weight of the total solution or a mixture of ethanol and propylene glycol in the amount of from about 5% to about 15% by weight of the total solution.
- 6. The composition of claim 1 wherein the solvent comprises (1) oleic acid in the amount of from about 40% to about 70% by weight of the total solution and (2) ethanol in the amount of from about 10% to about 12% by weight of the total solution or propylene glycol in the amount of from about 5% to about 10% by weight of the total solution or a mixture of ethanol and propylene glycol in the amount of from about 10% to about 15% by weight of the total solution.
- 7. The composition of claim 1 comprising:(a) ritonavir in the amount of from about 1% to about 30% by weight of the total solution, (b) a pharmaceutically acceptable organic solvent which comprises (i) a pharmaceutically acceptable long chain fatty acid selected from the group consisting of saturated, mono-unsaturated and di-unsaturated C12 to C18 carboxylic acids which are liquids at room temperature in the amount of from about 40% to about 99% by weight of the total solution or (ii) a mixture of (1) a pharmaceutically acceptable long chain fatty acid selected from the group consisting of saturated, mono-unsaturated and di-unsaturated C12 to C18 carboxylic acids which are liquids at room temperature in the amount of from about 40% to about 99% by weight of the total solution and (2) a pharmaceutically acceptable alcohol in the amount of from about 0% to about 15% by weight of the total solution and (c) a pharmaceutically acceptable surfactant in the amount of from about 0% to about 20% by weight of the total solution.
- 8. The composition of claim 7 wherein the solution is encapsulated in a soft elastic gelatin capsule (SEC).
- 9. The composition of claim 7 comprising:(a) ritonavir in the amount of from about 5% to about 25% by weight of the total solution, (b) a pharmaceutically acceptable organic solvent which comprises (i) a pharmaceutically acceptable long chain fatty acid selected from the group consisting of saturated, mono-unsaturated and di-unsaturated C12 to C18 carboxylic acids which are liquids at room temperature in the amount of from about 30% to about 70% by weight of the total solution or (ii) a mixture of (1) a pharmaceutically acceptable long chain fatty acid selected from the group consisting of saturated, mono-unsaturated and di-unsaturated C12 to C18 carboxylic acids which are liquids at room temperature in the amount of from about 30% to about 70% by weight of the total solution and (2) a pharmaceutically acceptable alcohol in the amount of from about 6% to about 12% by weight of the total solution and (c) a pharmaceutically acceptable surfactant in the amount of from about 5% to about 10% by weight of the total solution.
- 10. The composition of claim 9 wherein the solution is encapsulated in a soft elastic gelatin capsule (SEC).
- 11. The composition of claim 1 comprising(a) ritonavir in the amount of from about 1% to about 30% by weight of the total solution, (b) a pharmaceutically acceptable organic solvent which comprises (i) oleic acid in the amount of from about 15% to about 99% by weight of the total solution or (ii) a mixture of (1) oleic acid in the amount of from about 15% to about 99% by weight of the total solution and (2) ethanol in the amount of from about 0% to about 12% by weight of the total solution or propylene glycol in the amount of from about 0% to about 10% by weight of the total solution or a mixture thereof in the amount of from about 0% to about 15% by weight of the total solution and (c) polyoxyl 35 castor oil in the amount of from about 0% to about 20% by weight of the total solution.
- 12. The composition of claim 11 comprising(a) ritonavir in the amount of from about 5% to about 25% by weight of the total solution, (b) a pharmaceutically acceptable organic solvent which comprises (i) oleic acid in the amount of from about 30% to about 70% by weight of the total solution or (ii) a mixture of (1) oleic acid in the amount of from about 30% to about 70% by weight of the total solution and (2) ethanol in the amount of from about 10% to about 12% by weight of the total solution or propylene glycol in the amount of from about 5% to about 10% by weight of the total solution or a mixture thereof in the amount of from about 10% to about 15% by weight of the total solution and (c) polyoxyl 35 castor oil in the amount of from about 5% to about 10% by weight of the total solution.
- 13. The composition of claim 11 wherein the solution is encapsulated in a soft elastic gelatin capsule (SEC).
- 14. The composition of claim 11 comprising(a) ritonavir in the amount of about 20% by weight of the total solution, (b) a pharmaceutically acceptable organic solvent which comprises a mixture of (1) oleic acid in the amount of from about 62% to about 64% by weight of the total solution and (2) ethanol in the amount of from about 10% to about 12% by weight of the total solution and (c) polyoxyl 35 castor oil in the amount of about 6% by weight of the total solution.
- 15. The composition of claim 11 comprising(a) ritonavir in the amount of about 20% by weight of the total solution, (b) a pharmaceutically acceptable organic solvent which comprises a mixture of (1) oleic acid in the amount of about 65% by weight of the total solution and (2) ethanol in the amount of about 10% by weight of the total solution and (c) polyoxyl 35 castor oil in the amount of about 5% by weight of the total solution.
- 16. The composition of claim 11 comprising(a) ritonavir in the amount of about 20% by weight of the total solution, (b) a pharmaceutically acceptable organic solvent which comprises a mixture of (1) oleic acid in the amount of about 60% by weight of the total solution and (2) ethanol in the amount of about 10% by weight of the total solution and (c) polyoxyl 35 castor oil in the amount of about 10% by weight of the total solution.
Parent Case Info
This application claims the benefit of U.S. Provisional Application for Patent No. 60/031,463, filed Nov. 21, 1996 now abandoned.
US Referenced Citations (10)
Foreign Referenced Citations (27)
Number |
Date |
Country |
0490667 |
Jun 1992 |
EP |
490667 |
Jun 1992 |
EP |
0580402 |
Jan 1993 |
EP |
0532466 |
Mar 1993 |
EP |
532466 |
Mar 1993 |
EP |
0541168 |
May 1993 |
EP |
0560268 |
Sep 1993 |
EP |
560268 |
Sep 1993 |
EP |
580402 |
Jan 1994 |
EP |
WO 9208701 |
May 1992 |
WO |
9208701 |
May 1992 |
WO |
9307128 |
Oct 1992 |
WO |
WO 9307128 |
Apr 1993 |
WO |
9323368 |
Nov 1993 |
WO |
WO 9323368 |
Nov 1993 |
WO |
WO 9405639 |
Mar 1994 |
WO |
9405639 |
Mar 1994 |
WO |
9506061 |
Mar 1995 |
WO |
9509614 |
Apr 1995 |
WO |
9509843 |
Apr 1995 |
WO |
9520384 |
Aug 1995 |
WO |
9530670 |
Nov 1995 |
WO |
WO 9530670 |
Nov 1995 |
WO |
WO 9603113 |
Feb 1996 |
WO |
9701349 |
Jan 1997 |
WO |
WO 9721685 |
Jun 1997 |
WO |
9720554 |
Jun 1997 |
WO |
Non-Patent Literature Citations (3)
Entry |
Mimoto, et al., Chem Pharm Bull. 40 (8) 2251-2253 (1992). |
Kempf, et al., Proc. Natl. Acad Sci. USA 92 2484 (1995). |
Mazur, et al., Chem Abstr. 83: 1409r (1975). |
Provisional Applications (1)
|
Number |
Date |
Country |
|
60/031463 |
Nov 1996 |
US |