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Details for Patent: 8,329,214

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Details for Patent: 8,329,214

Title:Process for producing fenofibrate tablets
Abstract: The invention provides processes using suspensions to produce fenofibrate compositions. The resulting fenofibrate compositions can be made in the form of a tablet.
Inventor(s): Stamm; Andre (Griesheim, FR), Seth; Pawan (Irvine, CA)
Assignee: Laboratoires Fournier S.A. (Dijon, FR)
Filing Date:Mar 21, 2007
Application Number:11/723,646
Claims:1. A process for producing a tablet comprising micronized fenofibrate, wherein the process comprises: (i) preparing an aqueous suspension comprising at least one hydrophilic polymer wherein one of the hydrophilic polymers is polyvinylpyrrolidone with a molecular weight between 20,000 and 100,000; and micronized fenofibrate particles having a particle size of less than 20 .mu.m; (ii) spraying the suspension onto inert carriers to form granulates; and (iii) compressing the granulates to form the tablet.

2. The process of claim 1, wherein step (i) of preparing the suspension comprises (a) preparing a solution comprising at least one hydrophilic polymer and (b) adding the fenofibrate to the solution to produce the suspension.

3. The process of claim 1, wherein step (i) of preparing the suspension comprises (a) preparing a solution comprising at least one hydrophilic polymer by dissolving the hydrophilic polymer and (b) adding the fenofibrate to the solution to produce the suspension.

4. The process of claim 1, wherein step (i) of preparing the suspension comprises (a) adding the fenofibrate to a solution to form the suspension, and (b) dissolving at least one hydrophilic polymer in the suspension.

5. The process of claim 1, wherein the suspension further comprises at least one surfactant.

6. The process of claim 1, wherein the suspension comprises fenofibrate and hydrophilic polymer in a weight ratio of fenofibrate/hydrophilic polymer between 1/10 and 4/1.

7. The process of claim 1, wherein the suspension comprises fenofibrate and hydrophilic polymer in a weight ratio of fenofibrate/hydrophilic polymer between 1/2 and 2/1.

8. The process of claim 1, wherein the fenofibrate has a particle size less than 10 .mu.m.

9. The process of claim 1, wherein the suspension comprises fenofibrate in an amount from 1 to 40% by weight.

10. The process of claim 9, wherein the suspension comprises fenofibrate in an amount from 10 to 25% by weight.

11. The process of claim 1, wherein the suspension comprises the hydrophilic polymer in an amount from 5 to 40% by weight.

12. The process of claim 11, wherein the suspension comprises the hydrophilic polymer in an amount from 10 to 25% by weight.

13. The process of claim 1, wherein the hydrophilic polymer further comprises a poly(vinyl alcohol), a hydroxypropylcellulose, a hydroxy-methylcellulose, a hydroxypropylmethylcellulose, a gelatin, or a mixture of two or more thereof.

14. The process of claim 5, wherein the suspension comprises the surfactant in an amount of up to 10% by weight.

15. The process of claim 14, wherein the suspension comprises the surfactant in an amount of up to 5% by weight.

16. The process of claim 5, wherein the suspension comprises surfactant and hydrophilic polymer in a weight ratio of surfactant/hydrophilic polymer between 1/500 and 1/10.

17. The process of claim 5, wherein the suspension comprises surfactant and hydrophilic polymer in a weight ratio of surfactant/hydrophilic polymer between 1/100 and 5/100.

18. The process of claim 5, wherein the surfactant is sodium lauryl sulfate, monooleate, monolaurate, monopalmitate, monostearate or another ester of polyoxyethylene sorbitane, sodium dioctylsulfosuccinate, lecithin, stearylic alcohol, cetostearylic alcohol, cholesterol, polyoxyethylene ricin oil, polyoxyethylene fatty acid glycerides, poloxamer, or a mixture of two or more thereof.

19. The process of claim 18, wherein the surfactant is sodium lauryl sulfate.

20. The process of claim 1, wherein the inert carriers are inert hydrosoluble carriers.

21. The process of claim 1, which further comprises, between steps (ii) and (iii), mixing the granulates with at least one pharmaceutical excipient.

22. The process of claim 21, wherein said 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.

23. The process of claim 21, wherein said pharmaceutical excipient is selected from the group consisting of microcrystalline cellulose, lactose, starch, colloidal silica, talc, glycerol esters, sodium stearyl fumarate, titanium dioxide, magnesium stearate, stearic acid, cross-linked polyvinyl pyrrolidone, carboxymethyl starch, hydroxypropylcellulose, hydroxymethylcellulose, hydroxypropylmethylcellulose, gelatin, and a mixture of two or more thereof.

24. A process for producing a tablet comprising micronized fenofibrate, wherein the process comprises: (i) preparing an aqueous suspension comprising at least one surfactant, at least one hydrophilic polymer wherein one of the hydrophilic polymers is polyvinylpyrrolidone with a molecular weight between 20,000 and 100,000; and micronized fenofibrate particles having a particle size of less than 20 .mu.m; (ii) spraying the aqueous suspension onto inert carriers to form granulates; and (iii) compressing the granulates to form the tablet.

25. The process of claim 24, wherein step (i) of preparing the aqueous suspension comprises (a) preparing an aqueous solution comprising at least one surfactant and at least one hydrophilic polymer and (b) adding the fenofibrate to the aqueous solution to produce the aqueous suspension.

26. The process of claim 24, wherein step (i) of preparing the aqueous suspension comprises (a) preparing an aqueous solution comprising at least one surfactant and at least one hydrophilic polymer by dissolving the surfactant and hydrophilic polymer and (b) adding the fenofibrate to the aqueous solution to produce the aqueous suspension.

27. The process of claim 24, wherein step (i) of preparing the aqueous suspension comprises (a) dissolving at least one surfactant in an aqueous solution, (b) dissolving at least one hydrophilic polymer in the aqueous solution, and (c) adding the micronized fenofibrate to the aqueous solution to produce the aqueous suspension.

28. The process of claim 24, wherein step (i) of preparing the aqueous suspension comprises (a) dissolving at least one hydrophilic polymer in an aqueous solution, (b) dissolving at least one surfactant in an aqueous solution, and (c) adding the fenofibrate to the aqueous solution to form the aqueous suspension.

29. The process of claim 24, wherein step (i) of preparing the aqueous suspension comprises (a) dissolving at least one surfactant in an aqueous solution, (b) adding the fenofibrate to the aqueous solution to form the aqueous suspension, and (c) dissolving at least one hydrophilic polymer in the aqueous suspension.

30. The process of claim 24, wherein step (i) of preparing the aqueous suspension comprises (a) dissolving at least one hydrophilic polymer in an aqueous solution, (b) adding the fenofibrate to the aqueous solution to form the aqueous suspension, and (c) dissolving at least one surfactant in the aqueous suspension.

31. The process of claim 24, wherein the suspension comprises fenofibrate and hydrophilic polymer in a weight ratio of fenofibrate/hydrophilic polymer between 1/10 and 4/1.

32. The process of claim 24, wherein the suspension comprises fenofibrate and hydrophilic polymer in a weight ratio of fenofibrate/hydrophilic polymer between 1/2 and 2/1.

33. The process of claim 24, wherein the fenofibrate has a particle size less than 10 .mu.m.

34. The process of claim 24, wherein the suspension comprises fenofibrate in an amount from 1 to 40% by weight.

35. The process of claim 24, wherein the suspension comprises fenofibrate in an amount from 10 to 25% by weight.

36. The process of claim 24, wherein the suspension comprises the hydrophilic polymer in an amount from 5 to 40% by weight.

37. The process of claim 24, wherein the suspension comprises the hydrophilic polymer in an amount from 10 to 25% by weight.

38. The process of claim 24, wherein the hydrophilic polymer further comprises a poly(vinyl alcohol), a hydroxypropylcellulose, a hydroxy-methylcellulose, a hydroxypropylmethylcellulose, a gelatin, or a mixture of two or more thereof.

39. The process of claim 24, wherein the suspension comprises the surfactant in an amount of up to 10% by weight.

40. The process of claim 39, wherein the suspension comprises the surfactant in an amount of up to 5% by weight.

41. The process of claim 24, wherein the suspension comprises surfactant and hydrophilic polymer in a weight ratio of surfactant/hydrophilic polymer between 1/500 and 1/10.

42. The process of claim 24, wherein the suspension comprises surfactant and hydrophilic polymer in a weight ratio of surfactant/hydrophilic polymer between 1/100 and 5/100.

43. The process of claim 24, wherein the surfactant is sodium lauryl sulfate, monooleate, monolaurate, monopalmitate, monostearate or another ester of polyoxyethylene sorbitane, sodium dioctylsulfosuccinate, lecithin, stearylic alcohol, cetostearylic alcohol, cholesterol, polyoxyethylene ricin oil, polyoxyethylene fatty acid glycerides, poloxamer, or a mixture of two or more thereof.

44. The process of claim 43, wherein the surfactant is sodium lauryl sulfate.

45. The process of claim 24, wherein the inert carriers are inert hydrosoluble carriers.

46. The process of claim 24, which further comprises, between steps (ii) and (iii), mixing the granulates with at least one pharmaceutical excipient.

47. The process of claim 46, wherein said 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.

48. The process of claim 46, wherein said pharmaceutical excipient is selected from the group consisting of microcrystalline cellulose, lactose, starch, colloidal silica, talc, glycerol esters, sodium stearyl fumarate, titanium dioxide, magnesium stearate, stearic acid, cross-linked polyvinyl pyrrolidone, carboxymethyl starch, hydroxypropylcellulose, hydroxymethylcellulose, hydroxypropylmethylcellulose, gelatin, and a mixture of two or more thereof.

49. A process for producing a tablet comprising micronized fenofibrate, wherein the process comprises: (i) preparing an aqueous suspension comprising at least one surfactant, at least one hydrophilic polymer wherein one of the hydrophilic polymers is polyvinylpyrrolidone with a molecular weight between 20,000 and 100,000; and micronized fenofibrate particles having a particle size of less than 20 .mu.m; by (a) preparing an aqueous solution comprising at least one surfactant and at least one hydrophilic polymer by dissolving said surfactant and hydrophilic polymer and (b) adding the fenofibrate particles to the solution to produce the aqueous suspension; (ii) spraying the aqueous suspension onto inert carriers to form granulates; and (iii) compressing the granulates to form the tablet.

50. The process of claim 49, wherein the suspension comprises fenofibrate and hydrophilic polymer in a weight ratio of fenofibrate/hydrophilic polymer between 1/10 and 4/1.

51. The process of claim 49, wherein the suspension comprises fenofibrate and hydrophilic polymer in a weight ratio of fenofibrate/hydrophilic polymer between 1/2 and 2/1.

52. The process of claim 49, wherein the fenofibrate has a particle size less than 10 .mu.m.

53. The process of claim 49, wherein the suspension comprises fenofibrate in an amount from 1 to 40% by weight.

54. The process of claim 53, wherein the suspension comprises fenofibrate in an amount from 10 to 25% by weight.

55. The process of claim 49, wherein the suspension comprises the hydrophilic polymer in an amount from 5 to 40% by weight.

56. The process of claim 55, wherein the suspension comprises the hydrophilic polymer in an amount from 10 to 25% by weight.

57. The process of claim 49, wherein the hydrophilic polymer further comprises a poly(vinyl alcohol), a hydroxypropylcellulose, a hydroxy-methylcellulose, a hydroxypropylmethylcellulose, a gelatin, or a mixture of two or more thereof.

58. The process of claim 49, wherein the suspension comprises the surfactant in an amount of up to 10% by weight.

59. The process of claim 58, wherein the suspension comprises the surfactant in an amount of up to 5% by weight.

60. The process of claim 49, wherein the suspension comprises surfactant and hydrophilic polymer in a weight ratio of surfactant/hydrophilic polymer between 1/500 and 1/10.

61. The process of claim 49, wherein the suspension comprises surfactant and hydrophilic polymer in a weight ratio of surfactant/hydrophilic polymer between 1/100 and 5/100.

62. The process of claim 49, wherein the surfactant is sodium lauryl sulfate, monooleate, monolaurate, monopalmitate, monostearate or another ester of polyoxyethylene sorbitane, sodium dioctylsulfosuccinate, lecithin, stearylic alcohol, cetostearylic alcohol, cholesterol, polyoxyethylene ricin oil, polyoxyethylene fatty acid glycerides, poloxamer, or a mixture of two or more thereof.

63. The process of claim 62, wherein the surfactant is sodium lauryl sulfate.

64. The process of claim 49, wherein the inert carriers are inert hydrosoluble carriers.

65. The process of claim 49, which further comprises, between steps (ii) and (iii), mixing the granulates with at least one pharmaceutical excipient.

66. The process of claim 65, wherein said 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.

67. The process of claim 65, wherein said pharmaceutical excipient is selected from the group consisting of microcrystalline cellulose, lactose, starch, colloidal silica, talc, glycerol esters, sodium stearyl fumarate, titanium dioxide, magnesium stearate, stearic acid, cross-linked polyvinyl pyrrolidone, carboxymethyl starch, hydroxypropylcellulose, hydroxymethylcellulose, hydroxypropylmethylcellulose, gelatin, and a mixture of two or more thereof.

68. The process of claim 1, wherein the tablet comprises from 5 to 50% by weight of fenofibrate, from 10 to 75% by weight of carrier, and from 20 to 60% by weight of hydrophilic polymer.

69. The process of claim 68, wherein the tablet comprises from 20 to 45% by weight fenofibrate, from 20 to 50% by weight carrier, and from 25 to 45% by weight hydrophilic polymer.

70. The process of claim 68, wherein the tablet further comprises up to 10% by weight surfactant.

71. The process of claim 70, wherein the tablet further comprises from 0.1 to 3% by weight surfactant.

72. The process of claim 24, wherein the tablet comprises from 5 to 50% by weight fenofibrate, from 10 to 75% by weight carrier, from 20 to 60% by weight hydrophilic polymer, and up to 10% by weight surfactant.

73. The process of claim 72, wherein the tablet comprises from 20 to 45% by weight fenofibrate, from 20 to 50% by weight carrier, from 25 to 45% by weight hydrophilic polymer, and from 0.1 to 3% by weight surfactant.

74. The process of claim 49, wherein the tablet comprises from 5 to 50% by weight fenofibrate, from 10 to 75% by weight carrier, from 20 to 60% by weight hydrophilic polymer, and up to 10% by weight surfactant.

75. The process of claim 74, wherein the tablet comprises from 20 to 45% by weight fenofibrate, from 20 to 50% by weight carrier, from 25 to 45% by weight hydrophilic polymer, and from 0.1 to 3% by weight surfactant.

76. The process of claim 1, wherein step (ii) is fluidized bed granulation.

77. The process of claim 24, wherein step (ii) is fluidized bed granulation.

78. The process of claim 49, wherein step (ii) is fluidized bed granulation.

79. The process of claim 1, wherein said tablet is an immediate release tablet.

80. The process of claim 24, wherein said tablet is an immediate release tablet.

81. The process of claim 49, wherein said tablet is an immediate release tablet.
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