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Claims for Patent: 7,037,529

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Claims for Patent: 7,037,529

Title:Fenofibrate pharmaceutical composition having high bioavailability and method for preparing it
Abstract:The invention provides an immediate-release fenofibrate composition comprising (a) an inert hydrosoluble carrier covered with at least one layer containing fenofibrate in a micronized form having a size less than 20 .mu.m, a hydrophilic polymer and, optionally, a surfactant, the polymer making up at least 20% by weight of (a); and (b) optionally one or several outer phase(s) or layer(s).The invention also provides a method for preparing said composition.
Inventor(s): Stamm; Andre (Griesheim, FR), Seth; Pawan (Irvine, CA)
Assignee: Laboratoires Fournier (Dijon, FR)
Application Number:09/899,026
Patent Claims: 1. A fenofibrate composition comprising granulates, wherein the granulates comprise inert carrier particles coated with an admixture comprising at least one hydrophilic polymer and micronized fenofibrate; and wherein the composition has a dissolution of at least 75% in 30 minutes, as measured using the rotating blade method at 75 rpm according to the European Pharmacopoeia, in a dissolution medium constituted by water with 2% by weight polysorbate 80 in a dissolution medium which is 0.025 M sodium lauryl sulfate.

2. The composition of claim 1, wherein the weight ratio of micronized fenofibrate to hydrophilic polymer is between 1:10 and 4:1.

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

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

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

6. The composition of claim 1, wherein the inert carrier particles are hydrosoluble.

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

8. The composition of claim 1, wherein one or more of the inert carrier particles are isolated and/or agglomerated together.

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

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

11. The composition of claim 1, wherein the composition further comprises at least one pharmaceutical excipient.

12. The composition of claim 11, wherein the at least one pharmaceutical excipient is selected from the group consisting of at least one binder, at least one filler, at least one pigment, at least one disintegrating agent, at least one lubricant, at least one wetting agent, at least one buffer, and a mixture of two or more thereof.

13. The composition of claim 1, wherein the granulates further comprise at least one outer phase and/or layer.

14. The composition of claim 13, wherein the at least one outer phase and/or layer comprises at least one pharmaceutical excipient.

15. The composition of claim 14, wherein the at least one pharmaceutical excipient is selected from the group consisting of at least one binder, at least one filler, at least one pigment, at least one disintegrating agent, at least one lubricant, at least one wetting agent, at least one buffer, and a mixture of two or more thereof.

16. The composition of claim 1, wherein two or more of the granulates are agglomerated together.

17. The composition of claim 1, wherein the micronized fenofibrate has a particle size less than or equal 20 .mu.m.

18. The composition of claim 17, wherein the micronized fenofibrate has a particle size less than or equal to 10 .mu.m.

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

20. The composition of claim 1, wherein the hydrophilic polymer is polyvinylpyrrolidone, poly(vinyl alcohol), hydroxypropylcelluose, hydroxymethylcellulose, hydroxypropylmethylcelluose, gelatin, or a mixture of two or more thereof.

21. The composition of claim 1, further comprising at least one surfactant.

22. The composition of claim 21, wherein the surfactant is present in an amount of 0.1 to 10% by weight.

23. The composition of claim 21, wherein the surfactant is sodium laurylsulfate.

24. The composition of claim 21, wherein the surfactant is sodium lauryl sulfate, monooleate polyoxyethylene sorbitane, monolanrate polyoxyethylene sorbitane, monopalmitate polyoxyethylene sorbitane, monostearate polyoxyethylene sorbitane, sodium dioctylsulfosuccinate, lecithin, stearylic alcohol, cetostearylic alcohol, cholesterol, polyoxyethylene ricin oil, a polyoxyethylene fatty acid glyceride, a poloxamer, or a mixture of two or more thereof.

25. The composition of claim 1, wherein the inert carrier particles are present in an amount of 10 to 75% by weight, the micronized fenofibrate is present in an amount of 5 to 50% by weight, and the hydrophilic polymer is present in an amount of 20 to 60% by weight.

26. The composition of claim 25, wherein the inert carrier particles are present in an amount of 20 to 50% by weight, the micronized fenofibrate is present in an amount of 20 to 45% by weight, and the hydrophilic polymer is present in an amount of 25 to 45% by weight.

27. A process for preparing the composition of claim 1, comprising the steps of: (a) preparing a micronized fenofibrate suspension in a solution comprising at least one hydrophilic polymer, and, optionally, at least one surfactant; (b) spraying the micronized fenofibrate suspension from step (a) onto inert carrier particles to form granules; and (c) optionally coating the granules from step (b) with one or more phase(s) or layer(s).

28. The method of claim 27, wherein step (b) is carried out in a fluidized-bed granulator.

29. The method of claim 27, further comprising compressing the granules of step (b) or step (c).

30. A fenofibrate composition comprising granules, wherein the granules comprise: (i) carrier particles; and (ii) one or more layers comprising an admixture of micronized fenofibrate and at least one hydrophilic polymer, wherein the one or more layers are deposited on the carrier particles; and wherein the composition has a dissolution of at least 75% in 30 minutes, as measured using the rotating blade method at 75 rpm according to the European Pharmacopoeia, in a dissolution medium constituted by water with 2% by weight polysorbate 80 or in a dissolution medium which is 0.025 M sodium lauryl sulfate.

31. The composition of claim 30, wherein the weight ratio of micronized fenofibrate to hydrophilic polymer is between 1:10 and 4:1.

32. The composition of claim 30, wherein the carrier particles comprise lactose, saccharose, hydrolyzed starch, or a mixture of two or more thereof.

33. The composition of claim 30, wherein the hydrophilic polymer is polyvinyl pyrrolidone, poly(vinylalcohol), hydroxypropylcellulos, hydroxymethylcellulose, hydroxypropylmethylcellulose; gelatin, or a mixture of two or more thereof.

34. The composition of claim 30, wherein the at least one hydrophilic polymer is a mixture of at least two hydrophilic polymers.

35. The composition of claim 30, wherein the carrier particles are lactose and the hydrophilic polymer is polyvinylpyrrolidone.

36. The composition of claim 30, wherein the carrier particles are present in an amount from 10 to 75% by weight; the micronized fenofibrate is present in an amount from 5 to 50% by weight; and the hydrophilic polymer is present in an amount from 20 to 60% by weight.

37. The composition of claim 36, wherein the carrier particles are present in an amount from 20 to 50% by weight; the micronized fenofibrate is presented in an amount from 20 to 45% by weight; and the hydrophilic polymer is present in an amount from 25 to 45% by weight.

38. The composition of claim 30, further comprising at least one surfactant.

39. The composition of claim 38, wherein the surfactant is sodium lauryl sulfate, monooleate polyoxyethylene sorbitane, monolaurate polyoxyethylene sorbitane, monopalmitate polyoxyethylene sorbitane, monostearate polyoxyethylene sorbitane, sodium dioctylsulfosuccinate, lecithin, stearylic alcohol, cetostearylic alcohol, cholesterol, polyoxyethylene ricin oil, a polyoxyethylene fatty acid glyceride, a poloxamer, or a mixture of two or more thereof.

40. The composition of claim 38, wherein the surfactant is sodium lauryl sulfate.

41. The composition of claim 38, wherein the surfactant is present in an amount from 0.1 to 3% by weight.

42. The composition of claim 30, wherein the composition further contains at least one pharmaceutical excipient.

43. The composition of claim 42, wherein the at least one pharmaceutical excipient is at least one binder, at least one filler, at least one pigment, at least one disintegrating agent, at least one lubricant, at least one wetting agent, at least one buffer, or a mixture of two or more thereof.

44. The composition of claim 30, wherein the inert carrier particles are hydrosoluble.

45. The composition of claim 38, wherein the inert carrier particles are hydrosoluble.

46. A composition comprising granulates, wherein the granulates comprise carrier particles coated with an admixture comprising at least one hydrophilic polymer and micronized fenofibrate particles; wherein the carrier particles have a particle size between 50 and 500 micron; wherein the weight ratio of micronized fenofibrate particles to hydrophilic polymer is between 1:10 and 4:1; and wherein the composition has a dissolution of at least 75% in 30 minutes, as measured using the rotating blade method at 75 rpm according to the European Pharmacopoeia, in a dissolution medium constituted by water with 2% by weight polysorbate 80 or in a dissolution medium which is 0.025 M sodium lauryl sulfate.

47. The composition of claim 46, wherein the carrier particles have a particle size between 100 and 400 microns.

48. The composition of claim 46, wherein the carrier particles comprise lactose.

49. The composition of claim 46, wherein the composition is in the form of a tablet.

50. The composition of claim 46, wherein the hydrophilic polymer is polyvinylpyrrolidone.

51. The composition of claim 46, wherein the composition further comprises at least one pharmaceutical excipient.

52. The composition of claim 51, wherein the at least one pharmaceutical excipient is selected from the group consisting of at least one binder, at least one filler, at least one pigment, at least one disintegrating agent, at least one lubricant, at least one wetting agent, at least one buffer, and a mixture of two or more thereof.

53. The composition of claim 46, wherein the granulates further comprise at least one outer phase and/or layer.

54. The composition of claim 46, wherein the at least one outer phase and/or layer comprises at least one pharmaceutical excipient.

55. The composition of claim 54, wherein the at least one pharmaceutical excipient is selected from the group consisting of at least one binder, at least one filler, at least one pigment, at least one disintegrating agent, at least one lubricant, at least one wetting agent, at least one buffer, and a mixture of two or more thereof.

56. The composition of claim 46, wherein two or more of the granulates are agglomerated together.

57. The composition of claim 46, wherein the micronized fenofibrate particles have a particle size of less or equal to 20 .mu.m.

58. The composition of claim 46, wherein the carrier particles are comprised of lactose, saccharose, hydrolyzed starch, at a mixture of two or more thereof.

59. The composition of claim 46, wherein the carrier particles are hydrosoluble.

60. The composition of claim 46, wherein the hydrophilic polymer is polyvinylpyrrolidone, poly(vinyl alcohol), hydroxypropylcellulose, hydroxymethylcellulose, hydroxypropylmethylcellulose, gelatin, or a mixture of two or more thereof.

61. The composition of claim 46, further comprising at least one surfactant.

62. The composition of claim 61, wherein the surfactant is sodium laurylsulfate.

63. The composition of claim 61, wherein the surfactant is sodium lauryl sulfate, monooleate polyoxyethylene sorbitane, monolaurate polyoxyethylene sorbitane, monopalmitate polyoxyethylene sorbitane, monostearate polyoxyethylene sorbitane, sodium dioctylsulfosuccinate, lecithin, stearylic alcohol, cetostearylic alcohol, cholesterol, polyoxyethylene ricin oil, a polyoxyethylene fatty acid glyceride, a poloxamer, or a mixture of two or more thereof.

64. The composition of claim 61, wherein the surfactant is present in an amount of 0.1 to 10% by weight.

65. The composition of claim 46, wherein the carrier particles are present in an amount of 10 to 75% by weight, the micronized fenofibrate is present in an amount of 5 to 50% by weight, and the hydrophilic polymer is present in an amount of 20 to 60% by weight.

66. The composition of claim 65, wherein the carrier particles are present in an amount of 20 to 50% by weight, the micronized fenofibrate is present in an amount of 20 to 45% by weight, and the hydrophilic polymer is present in an amount of 25 to 45% by weight.

67. The composition of claim 46, wherein one or more of the carrier particles are isolated and/or agglomerated together.

68. The composition of claim 46, wherein the at least one hydrophilic polymer is a mixture of at least two hydrophilic polymers.

69. The composition of claim 46, wherein the carrier particles are lactose and the hydrophilic polymer is polyvinylpyrrolidone.

70. A method for preparing the composition of claim 46, comprising the steps of: (a) preparing a micronized fenofibrate supension in a solution comprising at least one hydrophilic polymer, and, optionally, at least one surfactant; (b) spraying the micronized fenofibrate suspension from step (a) onto inert carrier particles having a particle size between 100 and 400 microns to form granules in a fluidized-bed granulator; and (c) optionally coating the granules from (b) with one or more phase(s) or layer(s).

71. The method of claim 70, further comprising compressing the granules of step (b) or step (c).

72. The composition of claim 30, wherein the micronized fenofibrate particles have a particle size of less than equal to 20 .mu.m.

73. The composition of claim 72, wherein the micronized fenofibrate particles have a particle size of less than or equal to 10 .mu.m.

74. The composition of claim 57, wherein the micronized fenofibrate particles have a particle size of less than or equal to 10 .mu.m.

75. The composition of claim 30, wherein the composition is in the form of a tablet.

76. The composition of claim 1, wherein the hydrophilic polymer dissolves in a solution.

77. The composition of claim 1, wherein the hydrophilic polymer forms a gel in a solution.

78. The composition of claim 1, wherein the hydrophilic polymer forms a suspension in a solution.

79. The composition of claim 30, wherein the hydrophilic polymer dissolves in a solution.

80. The composition of claim 30, wherein the hydrophilic polymer forms a gel in a solution.

81. The composition of claim 30, wherein the hydrophilic polymer forms a suspension in a solution.

82. The composition of claim 46, wherein the hydrophilic polymer dissolves in a solution.

83. The composition of claim 46, wherein the hydrophilic polymer forms a gel in a solution.

84. The composition of claim 46, wherein the hydrophilic polymer forms a suspension in a solution.

85. A fenofibrate composition comprising granulates, wherein the granulates comprise inert carrier particles coated with an admixture comprising at least one hydrophilic polymer and micronized fenofibrate; and wherein the composition has a dissolution of at least 95.9% in 30 minutes, as measured using the rotating blade method at 75 rpm according to the European Pharmacopoeia, in a dissolution medium constituted by water with 2% by weight polysorbate 80 or in a dissolution medium constituted by water with 0.025 M sodium lauryl sulfate.

86. A fenofibrate composition comprising granules, wherein the granules comprise: (i) carrier particles; and (ii) one or more layers comprising an admixture of micronized fenofibrate and at least one hydrophilic polymer, wherein the one or more layers are deposited on the carrier particles; and wherein the composition has a dissolution of at least 95.5% in 30 minutes, as measured using the rotating blade method at 75 rpm according to the European Pharmacopoeia, in a dissolution medium constituted by water with 2% by weight polysorbate 80 or in a dissolution medium constituted by water with 0.025 M sodium lauryl sulfate.

87. A composition comprising granulates, wherein the granulates comprise carrier particles coated with an admixture comprising at least one hydrophilic polymer and micronized fenofibrate particles; wherein the carrier particles have a particle size between 50 and 500 microns; wherein the weight ratio of micronized fenofibrate particles to hydrophilic polymer is between 1:10 and 4:1; and wherein the composition has a dissolution of at least 95.9% in 30 minutes, as measured using the rotating blade method at 75 rpm according to the European Pharmacopoeia, in a dissolution medium constituted by water with 2% by weight polysorbate 80 or in a dissolution medium constituted by water with 0.025 M sodium lauryl sulfate.

88. A fenofibrate composition comprising granulates, wherein the granulates comprise inert carrier particles coated with an admixture comprising at least one hydrophilic polymer and micronized fenofibrate; and wherein the composition has a dissolution of at least 95.9% .+-.2.1% in 30 minutes, as measured using the rotating blade method at 75 rpm according to the European Pharmacopoeia, in a dissolution medium constituted by water with 2% by weight polysorbate 80 or in a dissolution medium constituted by water with 0.025 M sodium lauryl sulfate.

89. A fenofibrate composition comprising granules, wherein the granules comprise: (i) carrier particles; and (ii) one or more layers comprising and admixture of micronized fenofibrate and at least on hydrophilic polymer, wherein the one or more layers are deposited on the carrier particles; and wherein the composition has a dissolution of at least 95.9% .+-.2.1% in 30 minutes, as measured using the rotating blade method at 75 rpm according to the European Pharmacopoeia, in a dissolution medium constituted by water with 2% by weight polysorbate 80 or in a dissolution medium constituted by water with 0.025 M sodium lauryl sulfate.

90. A composition comprising granulates, wherein the granulates comprise carrier particles coated with an admixture comprising at least one hydrophilic polymer and micronized fenofibrate particles; wherein the carrier particles have a particle size between 50 and 500 microns; wherein the weight ratio of micronized fenofibrate polymer is between 1:10and 4:1; and wherein the composition has a dissolution of at least 95.9% .+-.2.1% in 30 minutes, as measured using the rotating blade method at 75 rpm according to the European Pharmacopoeia, in a dissolution method constituted by water with 2% by weight polysorbate 80 or in a dissolution medium constituted by water with 0.025 M sodium lauryl sulfate.
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