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Claims for Patent: 6,232,333

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Claims for Patent: 6,232,333

Title: Pharmaceutical composition
Abstract:A liquid pharmaceutical composition providing improved oral bioavailability is disclosed for compounds which are inhibitors of HIV protease. In particular, the composition comprises a solution in a pharmaceutically acceptable organic solvent of (a) the HIV protease inhibitor and, optionally, (b) a surfactant. The composition can optionally be encapsulated in either hard gelatin capsules or soft elastic capsules (SEC).
Inventor(s): Lipari; John (Racine, WI), Al-Razzak; Laman A. (Lake Forest, IL), Ghosh; Soumojeet (Lindenhurst, IL), Gao; Rong (Park City, IL), Kaul; Dilip (Gurnee, IL)
Assignee: Abbott Laboratories (Abbott Park, IL)
Application Number:08/966,495
Patent 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)ca rbonyl)valinyl)amino)-2-(N-((5-thiazolyl)methoxycarbonyl)amino)-1,6-dipheny l-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 C.sub.12 to C.sub.18 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)ca rbonyl)valinyl)amino)-2-(N-((5-thiazolyl)methoxycarbonyl)amino)-1,6-dipheny l-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 C.sub.12 to C.sub.18 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 C.sub.12 to C.sub.18 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 C.sub.12 to C.sub.18 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 C.sub.12 to C.sub.18 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 C.sub.12 to C.sub.18 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 C.sub.12 to C.sub.18 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 C.sub.12 to C.sub.18 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 C.sub.12 to C.sub.18 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.
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