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Claims for Patent: 6,589,552

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Claims for Patent: 6,589,552

Title: Fenofibrate pharmaceutical composition having high bioavailability and method for preparing it
Abstract:The invention provides fenofibrate compositions comprising granulates. The granulates can comprise micronized fenofibrate, inert hydrosoluble carrier particles, hydrophilic polymers, and, optionally, surfactants.
Inventor(s): Stamm; Andre (Griesheim, FR), Seth; Pawan (Irvine, CA)
Assignee: Laboratoires Fournier, S.A. (Dijon, FR)
Application Number:10/126,875
Patent Claims: 1. A fenofibrate composition comprising granulates, wherein the granulates comprise micronized fenofibrate having a particle size below 20 .mu.m, inert hydrosoluble carrier particles and at least 20% by weight of at least one hydrophilic polymer, wherein the weight ratio of fenofibrate to hydrophuic polymer is from 1/10 to 4/1.

2. The composition of claim 1, wherein the micronized fenofibrate has a particle size below 10 .mu.m.

3. The composition of claim 1, wherein the fenofibrate is present in an amount of from 5 to 50% by weight.

4. The composition of claim 1, wherein the fenofibrate is present in an amount of from 20 to 45% by weight.

5. The composition of claim 1, wherein the hydrophilic polymer is present in an amount from 20 to 60% by weight.

6. The composition of claim 1, wherein the hydrophilic polymer is present in an amount of at least 25% by weight.

7. The composition of claim 1, wherein the hydrophilic polymer is present in an amount of from 25 to 45% by weight.

8. The composition of claim 1, wherein the weight ratio of fenofibrate to hydrophilic polymer is from 1/2 to 2/1.

9. The composition of claim 1, wherein the hydrophilic polymer is polyvinyl pyrrolidone, poly(vinylalcohol), hydroxypropylcellulose, hydroxymethylcellulose, hydroxypropylmethylcellulose; gelatin, or a mixture of two or more thereof.

10. The composition of claim 1, wherein the hydrophilic polymer is polyvinylpyrrolidone.

11. The composition of claim 1, wherein the carrier particles are present in an amount of from 10 to 80% by weight.

12. The composition of claim 1, wherein the carrier particles are present in an amount of from 20 to 50% by weight.

13. The composition of claim 1, wherein the carrier particles have a particle size between 50 and 500 microns.

14. The composition of claim 1, wherein the carrier particles have a particle size between 100 and 400 microns.

15. The composition of claim 1, wherein the carrier particles comprise lactose, saccharose, hydrolyzed starch, or a mixture of two or more thereof.

16. The composition of claim 1, wherein the carrier particles comprise lactose.

17. The composition of claim 1, further comprising a surfactant.

18. The composition of claim 17, wherein the surfactant is sodium lauryl sulfate, monooleate polyoxyethylene sorbitane, monolaurate polyoxyethylene sorbitane, monopalmitate polyoxyethylene sorbitane, monosterate polyoxyethylene sorbitane, sodium dioctylsulfosuccinate, lecithin, stearylic alcohol, cetostarylic alcohol, cholesterol, polyoxyethylene ricin oil, polyoxyethylene fatty acid glyceride, poloxamer, or a mixture of two or more thereof.

19. The composition of claim 17, wherein the surfactant is sodium lauryl sulfate.

20. The composition of claim 17, wherein the surfactant is present in an amount up to 10% by weight.

21. The composition of claim 17, wherein the surfactant is present in an amount of from 0.1 to 3% by weight.

22. The composition of claim 17, wherein the weight ratio of surfactant to hydrophilic polymer is from 1/500 to 1/10.

23. The composition of claim 17, wherein the weight ratio of surfactant to hydrophilic polymer is from 1/100 to 5/100.

24. The composition of claim 1, wherein the composition has a dissolution of at least 10% in 5 minutes, 20% in 10 minutes, 50% in 20 minutes and 75% in 30 minutes, as measured using a rotating blade method at 75 rpm according to the European Pharmacopocia, in a dissolution medium comprising water with 2% by weight polysorbate 80.

25. The composition of claim 1, wherein the composition has a dissolution of at least 10% in 5 minutes, 20% in 10 minutes, 50% in 20 minutes and 75% in 30 minutes, as measured using a rotating blade method at 75 rpm according to the European Pharinacopocia, in a dissolution medium comprising water with 0.025 M sodium lauryl sulfate.

26. The composition of claim 17, wherein the fenofibrate and surfactant are co-micronized.

27. The composition of claim 1, wherein the composition is in the form of a tablet.

28. The composition of claim 1, wherein the composition is in the form of granules inside a capsule.

29. The composition of claim 1, wherein the granulates are produced by a process comprising spraying a suspension containing the fenofibrate and the hydrophilic polymer onto the inert hydrosoluble carrier particles.

30. The composition of claim 29, wherein the granulates are produced by a fluidized-bed granulation technique.

31. A fenofibrate composition comprising granulates, wherein the granulates comprise micronized fenofibrate having a particle size below 20 .mu.m, inert hydrosoluble carrier particles, at least 20% by weight polyvinylpyrrolidone, and a surfactant in an amount of up to 10% by weight; and wherein the weight ratio of fenofibrate to polyvinylpyrrolidone is from 1/10 to 4/1.

32. The composition of claim 31, wherein the fenofibrate is present in an amount of from 5 to 50% by weight.

33. The composition of claim 31, wherein the fenofibrate is present in an amount of from 20 to 45% by weight.

34. The composition of claim 31, wherein the polyvinylpyrrolidone is present in an amount of from 20 to 60% by weight.

35. The composition of claim 31, wherein the polyvinylpyrrolidone is present in an amount of at least 25% by weight.

36. The composition of claim 31, wherein the polyvinylpyrrolidone is present in an amount of from 25 to 45% by weight.

37. The composition of claim 31, wherein the weight ratio of fenofibrate to polyvinylpyrrolidone is from 1/2 to 2/1.

38. The composition of claim 31, wherein the carrier particles are present in an amount of from 10 to 80% by weight.

39. The composition of claim 31, wherein the carrier particles are present in an amount of from 20 to 50% by weight.

40. The composition of claim 31, wherein the carrier particles have a particle size between 50 and 500 microns.

41. The composition of claim 31, wherein the carrier particles have a particle size between 100 and 400 microns.

42. The composition of claim 31, wherein the carrier particles comprise lactose, saccharose, hydrolyzed starch, or a mixture of two or more thereof.

43. The composition of claim 31, wherein the carrier particles comprise lactose.

44. The composition of claim 31, wherein the surfactant is sodium lauryl sulfate, monooleate polyoxyethylene sorbitane, monolaurate polyoxyethylene sorbitane, monopalmitate polyoxyethylene sorbitane, monosterate polyoxyethylene sorbitane, sodium dioctylsulfosuccinate, lecithin, stearylic alcohol, cetostarylic alcohol, cholesterol, polyoxyethylene ricin oil, polyoxyethylene fatty acid glyceride, poloxamer, or a mixture of two or more thereof.

45. The composition of claim 31, wherein the surfactant is sodium lauryl sulfate.

46. The composition of claim 31, wherein the surfactant is present in an amount of from 0.1 to 3% by weight.

47. The composition of claim 31, wherein the weight ratio of surfactant to polyvinylpyrrolidone is from 1/500 to 1/10.

48. The composition of claim 31, wherein the weight ratio of surfactant to polyvinylpyrrolidone is from 1/100 to 5/100.

49. The composition of claim 31, wherein the composition has a dissolution of at least 10% in 5 minutes, 20% in 10 minutes, 50% in 20 minutes and 75% in 30 minutes, as measured using a rotating blade method at 75 rpm according to the European Pharmacopocia, in a dissolution medium comprising water with 2% by weight polysorbate 80.

50. The composition of claim 31, wherein the composition has a dissolution of at least 10% in 5 minutes, 20% in 10 minutes, 50% in 20 minutes and 75% in 30 minutes, as measured using a rotating blade method at 75 rpm according to the European Pharmacopocia, in a dissolution medium comprising water with 0.025 M sodium lauryl sulfate.

51. The composition of claim 31, wherein the fenofibrate and surfactant are co-micronized.

52. The composition of claim 31, wherein the composition is in the form of a tablet.

53. The composition of claim 31, wherein the composition is in the form of granules inside a capsule.

54. The composition of claim 31, wherein the granulates are produced by a process comprising spraying a suspension containing the fenofibrate, the polyvinylpyrrolidone and the surfactant onto the inert hydrosoluble carrier particles.

55. The composition of claim 31, wherein the granulates are produced by a fluidized-bed granulation technique.

56. The composition of claim 1, wherein the at least one hydrophilic polymer is a mixture of hydrophilic polymers.

57. A fenofibrate composition comprising granulates, wherein the granulates comprise micronized fenofibrate having a particle size below 20 .mu.m, inert hydrosoluble carrier particles, at least 20% by weight of at least one hydrophilic polymer, and at least one surfactant; wherein the weight ratio of surfactant to hydrophilic polymer is from 1/500 to 1/10.
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