.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Claims for Patent: 5,948,436

« Back to Dashboard

Claims for Patent: 5,948,436

Title: Pharmaceutical composition
Abstract:A pharmaceutical composition is disclosed which comprises a solution of an HIV protease inhibiting compound in a pharmaceutically acceptable organic solvent comprising a pharmaceutically acceptable alcohol. The composition can optionally comprise a pharmaceutically acceptable acid or a combination of pharmaceutically acceptable acids. The solution can optionally be encapsulated in hard gelatin capsules or soft elastic gelatin capsules. The solution can optionally be granulated with a pharmaceutically acceptable granulating agent.
Inventor(s): Al-Razzak; Laman A. (Libertyville, IL), Marsh; Kennan C. (Lake Forest, IL), Kaul; Dilip (Waukegan, IL), Manning; Lourdes P. (Grayslake, IL)
Assignee: Abbott Laboratories (Abbott Park, IL)
Application Number:08/402,690
Patent Claims: 1. A pharmaceutical composition comprising a solution of a compound of the formula: ##STR6## in (i) a pharmaceutically acceptable organic solvent which is a pharmaceutically acceptable alcohol or (ii) a mixture of pharmaceutically acceptable organic solvents wherein the mixture comprises a pharmaceutically acceptable alcohol.

2. The composition of claim 1 wherein the solution is encapsulated in a hard gelatin capsule or a soft elastic gelatin capsule.

3. The composition of claim 1 further comprising a pharmaceutically acceptable acid.

4. The composition of claim 1 further comprising an additive or a mixture of additives independently selected from the group consisting of glycerin, pharmaceutically acceptable surfactants and antioxidants.

5. A pharmaceutical composition comprising a solution of (a) a compound of the formula: ##STR7## (b) a pharmaceutically acceptable acid or a combination of pharmaceutically acceptable acids in (i) a pharmaceutically acceptable organic solvent which is a pharmaceutically acceptable alcohol or (ii) a mixture of pharmaceutically acceptable organic solvents wherein the mixture comprises a pharmaceutically acceptable alcohol.

6. The composition of claim 5 wherein the solution is encapsulated in a hard gelatin capsule or a soft elastic gelatin capsule.

7. The composition of claim 5 further comprising water.

8. The composition of claim 5 further comprising an additive or a mixture of additives independently selected from the group consisting of glycerin, pharmaceutically acceptable surfactants and antioxidants.

9. The composition of claim 5 comprising a solution of (a) about 8.8% by weight of the total solution of (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; and (b) about 2 molar equivalents, based upon the amount of the compound of part (a), of hydrochloric acid in a mixture of propylene glycol in the amount of about 82% by weight of the total solution, ethanol in the amount of about 3.5% by weight of the total solution and water in the amount of about 4.4% by weight of the total solution.

10. The composition of claim 9 wherein the solution is encapsulated in a hard gelatin capsule.

11. The composition of claim 5 comprising a solution of (1) (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-diphen yl-3-hydroxyhexane in the amount of from about 2% to about 30% by weight of the total solution and (2) a total of from about 0.2 to about 2 molar equivalents (based on the compound of part (1)) of (i) a pharmaceutically acceptable acid or (ii) a mixture of pharmaceutically acceptable acids in a mixture of (a) a pharmaceutically acceptable alcohol or mixture of pharmaceutically acceptable alcohols in a total amount of from about 2% to about 50% by weight of the total solution, said alcohol or mixture of alcohols being a liquid at room temperature and (b) a pharmaceutically acceptable organic solvent or a mixture of pharmaceutically acceptable organic solvents in a total amount of from about 20% to about 60% by weight of the total solution, said solvent or mixture of solvents having a melting point between about 20.degree. C. and about 60.degree. C., said solvent or mixture of solvents being miscible with the alcohol or mixture of alcohols and providing a homogeneous mixture with the alcohol or mixture of alcohols, said homogeneous mixture being a solid or semi-solid at about 20.degree. C., wherein the solution is encapsulated in a soft elastic capsule or a hard gelatin capsule.

12. The composition of claim 11 comprising a solution of (1) (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-diphen yl-3-hydroxyhexane in the amount of from about 2% to about 30% by weight of the total solution and (2) a total of from about 0.2 to about 2 molar equivalents (based on the compound of part (1)) of (i) a pharmaceutically acceptable acid or (ii) a mixture of pharmaceutically acceptable acids in a mixture of (a) propylene glycol in the amount of from about 4% to about 40% by weight of the total solution, (b) ethanol in the amount of from about 2% to about 20% by weight of the total solution, and (c) polyethylene glycol 540 in the amount of from about 20% to about 60% by weight of the total solution or a total amount of from about 20% to about 60% by weight of the total solution of (i) a saturated polyglycolized glyceride or (ii) a mixture of saturated polyglycolized glycerides, wherein the solution is encapsulated in a soft elastic capsule or a hard gelatin capsule.

13. The composition of claim 12 comprising a solution of (1) (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-diphen yl-3-hydroxyhexane in the amount of from about 20% to about 25% by weight of the total solution and (2) a total of from about 1.5 to about 2 molar equivalents (based on the compound of part (1)) of hydrochloric acid in a mixture of (a) propylene glycol in the amount of from about 20% to about 22% by weight of the total solution, (b) ethanol in the amount of from about 5% to about 6% by weight of the total solution, and (c) a saturated polyglycolized glyceride in the amount of from about 30% to about 35% by weight of the total solution, wherein the solution is encapsulated in a hard gelatin capsule.

14. The composition of claim 12 comprising a solution of (1) (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 in the amount of from about 15% to about 20% by weight of the total solution and (2) a total of from about 0.3 to about 0.6 molar equivalents (based on the compound of part (1)) of hydrochloric acid in a mixture of (a) propylene glycol in the amount of about 12% by weight of the total solution, (b) ethanol in the amount of from about 5% to about 6% by weight of the total solution, and (c) a saturated polyglycolized glyceride in the amount of from about 30% to about 35% by weight of the total solution, wherein the solution is encapsulated in a hard gelatin capsule.

15. The composition of claim 12 comprising a solution of: (1) (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-diphe nyl-3-hydroxyhexane in the amount of from about 15% to about 20% by weight of the total solution in a mixture of (a) propylene glycol in the amount of about 40% by weight of the total solution, (b) ethanol in the amount of about 2% to about 3% by weight of the total solution, and (c) polyethylene glycol 540 in the amount of from about 30% to about 35% by weight of the total solution, wherein the solution is encapsulated in a hard gelatin capsule.

16. The composition of claim 12 comprising a solution of (1) (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-diphen yl-3-hydroxyhexane in the amount of from about 15% to about 20% by weight of the total solution and (2) a total of from about 0.3 to about 0.6 molar equivalents (based on the compound of part (1)) of hydrochloric acid in a mixture of (a) propylene glycol in the amount of about 12% by weight of the total solution, (b) ethanol in the amount of from about 10% to about 15% by weight of the total solution, and (c) a saturated polyglycolized glyceride in the amount of from about 30% to about 35% by weight of the total solution, wherein the solution is encapsulated in a hard gelatin capsule.

17. The composition of claim 12 comprising a solution of (1) (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 in the amount of from about 4% to about 30% by weight of the total solution and (2) a total of about two molar equivalents (based on the compound (1)) of (i) a pharmaceutically acceptable acid or (ii) a mixture of pharmaceutically acceptable acids in a mixture of (a) propylene glycol in the amount of from about 10% to about 40% by weight of the total solution, (b) ethanol in the amount of from about 2% to about 8%, and (c) polyethylene glycol 540 in the amount of from about 25% to about 60% by weight of the total solution or saturated polyglycolized glyceride in the amount of from about 25% to about 60% by weight of the total solution.

18. The composition of claim 17 wherein the solution is encapsulated in a hard gelatin capsule.

19. The composition of claim 12 comprising a solution of (1) (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-diphen yl-3-hydroxyhexane in the amount of from about 20% to about 25% by weight of the total solution and (2) a total of about two molar equivalents (based on the compound of part (1)) of hydrochloric acid in a mixture of (a) propylene glycol in the amount of from about 22% by weight of the total solution, (b) ethanol in the amount of from about 5% to about 6% by weight of the total solution, and (c) saturated polyglycolized glyceride in the amount of from about 30% to about 35% by weight of the total solution.

20. The composition of claim 19 wherein the solution is encapsulated in a hard gelatin capsule.

21. The composition of claim 12 comprising a solution of: (1) (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-diphen yl-3-hydroxyhexane in the amount of from about 15% to about 20% by weight of the total solution and (2) a total of about two molar equivalents (based on the compound (1)) of a mixture of citric acid and hydrochloric acid in a mixture of (a) propylene glycol in the amount of about 12% by weight of the total solution, (b) ethanol in the amount of from about 5% to about 6% by weight of the total solution, and (c) a saturated polyglycolized glyceride in the amount of from about 30% to about 35% by weight of the total solution.

22. The composition of claim 21 wherein the solution is encapsulated in a hard gelatin capsule.

23. The composition of claim 12 comprising a solution of (1) (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-diphen yl-3-hydroxyhexane in the amount of from about 15% to about 20% by weight of the total solution and (2) a total of about two molar equivalents (based on the compound (1)) of p-toluene-sulfonic acid in a mixture of (a) propylene glycol in the amount of about 40% by weight of the total solution, (b) ethanol in the amount of from about 2% to about 3% by weight of the total solution, and (c) polyethylene glycol 540 in the amount of from about 30% to about 35% by weight of the total solution.

24. The composition of claim 23 wherein the solution is encapsulated in a hard gelatin capsule.

25. The composition of claim 12 comprising a solution of: (1) (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-diphen yl-3-hydroxyhexane in the amount of about 22% by weight of the total solution and (2) a total of about 1.6 molar equivalents (based on the compound (1)) of hydrochloric acid in a mixture of (a) propylene glycol in the amount of about 20% by weight of the total solution, (b) ethanol in the amount of from about 5% to about 6% by weight of the total solution, and (c) a saturated polyglycolized glyceride in the amount of from about 30% to about 35% by weight of the total solution.

26. The composition of claim 25 wherein the solution is encapsulated in a hard gelatin capsule.

27. The composition of claim 12 comprising a solution of: (1) (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-diphen yl-3-hydroxyhexane in the amount of about 18% by weight of the total solution and (2) a total of about 0.5 molar equivalents (based on the compound (1)) of hydrochloric acid in a mixture of (a) propylene glycol in the amount of about 12% by weight of the total solution, (b) ethanol in the amount of from about 5% to about 6% by weight of the total solution, and (c) a saturated polyglycolized glyceride in the amount of from about 30% to about 35% by weight of the total solution.

28. The composition of claim 27 wherein the solution is encapsulated in a hard gelatin capsule.

29. The composition of claim 12 comprising a solution of: (1) (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-diphen yl-3-hydroxyhexane in the amount of about 22% by weight of the total solution and (2) a total of about 1.8 molar equivalents (based on the compound (1)) of hydrochloric acid in a mixture of (a) propylene glycol in the amount of about 20% by weight of the total solution, (b) ethanol in the amount of from about 5% to about 6% by weight of the total solution, and (c) a saturated polyglycolized glyceride in the amount of from about 30% to about 35% by weight of the total solution.

30. The composition of claim 29 wherein the solution is encapsulated in a hard gelatin capsule.

31. The composition of claim 12 comprising a solution of: (1) (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-diphen yl-3-hydroxyhexane in the amount of about 17% by weight of the total solution and (2) a total of about 0.4 molar equivalents (based on the compound (1)) of hydrochloric acid in a mixture of (a) propylene glycol in the amount of about 14% by weight of the total solution, (b) ethanol in the amount of about 12% by weight of the total solution, and (c) a saturated polyglycolized glyceride in the amount of from about 30% to about 35% by weight of the total solution.

32. The composition of claim 31 wherein the solution is encapsulated in a hard gelatin capsule.

33. The composition of claim 12 comprising a solution of: (1) (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-diphen yl-3-hydroxyhexane in the amount of from about 15% to about 20% by weight of the total solution and (2) a total of from about 0.2 to about 0.8 molar equivalents (based on the compound (1)) of hydrochloric acid in a mixture of (a) propylene glycol in the amount of from about 13% to about 14% by weight of the total solution, (b) ethanol in the amount of about 14% by weight of the total solution, and (c) a saturated polyglycolized glyceride in the amount of from about 30% to about 35% by weight of the total solution.

34. The composition of claim 33 wherein the solution is encapsulated in a hard gelatin capsule.

35. The composition of claim 12 comprising a solution of: (1) (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-diphen yl-3-hydroxyhexane in the amount of from about 10% to about 15% by weight of the total solution and (2) a total of from about 1.10 to about 1.30 molar equivalents (based on the compound (1)) of citric acid in a mixture of (a) propylene glycol in the amount of from about 5% to about 7% by weight of the total solution, (b) ethanol in the amount of from about 15% to about 20% by weight of the total solution, and (c) a saturated polyglycolized glyceride in the amount of from about 30% to about 35% by weight of the total solution.

36. The composition of claim 35 wherein the solution is encapsulated in a hard gelatin capsule.

37. The composition of claim 12 comprising a solution of: (1) (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-diphen yl-3-hydroxyhexane in the amount of from about 10% to about 15% by weight of the total solution and (2) a total of from about 0.8 to about 0.9 molar equivalents (based on the compound (1)) of citric acid in a mixture of (a) propylene glycol in the amount of from about 5% to about 7% by weight of the total solution, (b) ethanol in the amount of from about 10% to about 15% by weight of the total solution, (c) benzyl alcohol in the amount of from about 3% to about 4% by weight of the total solution, and (d) a saturated polyglycolized glyceride in the amount of from about 35% to about 40% by weight of the total solution.

38. The composition of claim 37 wherein the solution is encapsulated in a hard gelatin capsule.

39. The composition of claim 12 comprising a solution of: (1) (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-diphen yl-3-hydroxyhexane in the amount of about 20% by weight of the total solution and (2) a total of from about 0.7 to about 0.8 molar equivalents (based on the compound (1)) of citric acid in a mixture of (a) propylene glycol in the amount of from about 4% to about 6% by weight of the total solution, (b) ethanol in the amount of from about 10% to about 15% by weight of the total solution, (c) benzyl alcohol in the amount of from about 4% to about 6% by weight of the total solution, and (d) a saturated polyglycolized glyceride in the amount of from about 30% to about 35% by weight of the total solution.

40. The composition of claim 39 wherein the solution is encapsulated in a hard gelatin capsule.

41. The composition of claim 12 comprising a solution of: (1) (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-diphen yl-3-hydroxyhexane in the amount of about 25% by weight of the total solution and (2) a mixture of a total of from about 0.4 to about 0.5 molar equivalents (based on the compound (1)) of citric acid and from about 0.10 to about 0.25 molar equivalents (based on the compound (1)) of sulfuric acid in a mixture of (a) propylene glycol in the amount of from about 5% to about 7% by weight of the total solution, (b) ethanol in the amount of from about 10% to about 15% by weight of the total solution, (c) benzyl alcohol in the amount of from about 4% to about 6% by weight of the total solution, and (d) a saturated polyglycolized glyceride in the amount of from about 25% to about 30% by weight of the total solution.

42. The composition of claim 41 wherein the solution is encapsulated in a hard gelatin capsule.

43. The composition of claim 12 comprising a solution of: (1) (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-diphen yl-3-hydroxyhexane in the amount of about 25% by weight of the total solution and (2) a total of from about 0.7 to about 0.8 molar equivalents (based on the compound (1)) of citric acid in a mixture of (a) propylene glycol in the amount of from about 4% to about 6% by weight of the total solution, (b) ethanol in the amount of from about 15% to about 20% by weight of the total solution, (c) benzyl alcohol in the amount of from about 5% to about 10% by weight of the total solution, and (d) a saturated polyglycolized glyceride in the amount of from about 25% to about 30% by weight of the total solution.

44. The composition of claim 43 wherein the solution is encapsulated in a hard gelatin capsule.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

How are People Using DrugPatentWatch?

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc