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Claims for Patent: 8,933,097

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Claims for Patent: 8,933,097

Title:Fexofenadine suspension formulation
Abstract: The present invention is directed to an aqueous pharmaceutical suspension of fexofenadine zwitterionic dihydrate Form I.
Inventor(s): Chrzan; Kazimierz (New Hope, PA), Haribhakti; Rajiv (Churchville, PA), Mermey; Matthew (Leawood, KS), Porcello; Curtis J. (Ewing, NJ), Silvey; Gary Lee (Overland Park, KS), Tran; Vinh (Leawood, KS), Agrawala; Prafulla (Kendall Park, NJ)
Assignee: Sanofi-Aventis U.S. LLC (Bridgewater, NJ)
Application Number:12/138,468
Patent Claims: 1. An aqueous pharmaceutical suspension, having a pH 5.8 to 7.0 adjusted by a buffer system, comprising, by weight/volume (g/100 mL), 0.03% to 4.80% of fexofenadine zwitterionic dihydrate Form I of formula (I) having a particle size of less than 280 .mu.m for at least 90% of the fexofenadine zwitterionic dihydrate Form I; ##STR00002## 0.01% to 0.20% of a wetting agent; a suspending agent selected from 0.10% to 0.50% of a hydrocolloid gum, or 0.1% to 1.0% of hydroxyethylcellulose; a sweetener system comprising 5% to 40% of sucrose or invert sucrose; and 5% to 40% of xylitol, sorbitol or sorbitol solution, or maltitol solution; provided that the ratio of the amount of (sucrose or invert sucrose) : (xylitol, sorbitol or sorbitol solution, or maltitol solution) is 1:1 to 2:1; and a preservative system comprising 0.010% to 0.058% of propylparaben, sodium propylparaben or potassium propylparaben; 0.0005% to 0.0350% of butylparaben or sodium butylparaben; and 0.06% to 0.26% of edetate disodium, 0.01% to 0.27% of benzoic acid or sodium benzoate, 0.01% to 0.30% of sorbic acid or potassium sorbate or 0.10% to 1.50% of benzyl alcohol.

2. The aqueous pharmaceutical suspension according to claim 1, wherein the particle size is less than 50 .mu.m for at least 90% of the fexofenadine zwitterionic dihydrate Form I.

3. The aqueous pharmaceutical suspension according to claim 1, wherein the particle size is less than 40 .mu.m for at least 90% of the fexofenadine zwitterionic dihydrate Form I.

4. The aqueous pharmaceutical suspension according to claim 3, wherein the fexofenadine zwitterionic dihydrate Form I is, by weight/volume (g/100 mL), 0.6% to 1.2%.

5. The aqueous pharmaceutical suspension according to claim 3, wherein the fexofenadine zwitterionic dihydrate Form I is, by weight/volume (g/100 mL), 0.6%.

6. The aqueous pharmaceutical suspension according to claim 3, wherein the wetting agent is, by weight/volume (g/100 mL), 0.01% to 0.05%.

7. The aqueous pharmaceutical suspension according to claim 3, wherein the wetting agent is, by weight/volume (g/100 mL), 0.02% to 0.05%.

8. The aqueous pharmaceutical suspension according to claim 3, wherein the hydrocolloid gum is, by weight/volume (g/100 mL), 0.23% to 0.45%.

9. The aqueous pharmaceutical suspension according to claim 3, wherein the hydrocolloid gum is, by weight/volume (g/100 mL), 0.35% to 0.45%.

10. The aqueous pharmaceutical suspension according to claim 3, wherein the hydrocolloid gum is xanthan gum.

11. The aqueous pharmaceutical suspension according to claim 3, wherein the hydroxyethylcellulose is, by weight/volume (g/100 mL), 0.2% to 0.4%.

12. The aqueous pharmaceutical suspension according to claim 3, wherein the hydroxyethylcellulose is, by weight/volume (g/100 mL), 0.2% to 0.3%.

13. The aqueous pharmaceutical suspension according to claim 3, wherein the xylitol, sorbitol or sorbitol solution, or maltitol solution is, by weight/volume (g/100 mL), 5% to 20%.

14. The aqueous pharmaceutical suspension according to claim 3, wherein the xylitol, sorbitol or sorbitol solution, or maltitol solution is, by weight/volume (g/100 mL), 10% to 20%.

15. The aqueous pharmaceutical suspension according to claim 3, wherein the xylitol, sorbitol or sorbitol solution, or maltitol solution is, by weight/volume (g/100 mL), 10%.

16. The aqueous pharmaceutical suspension according to claim 3, wherein the sucrose or invert sucrose is, by weight/volume (g/100 mL), 10% to 40%.

17. The aqueous pharmaceutical suspension according to claim 3, wherein the sucrose or invert sucrose is, by weight/volume (g/100 mL), 10% to 20%.

18. The aqueous pharmaceutical suspension according to claim 3, wherein the sucrose or invert sucrose is, by weight/volume (g/100 mL), 20%.

19. The aqueous pharmaceutical suspension according to claim 3, wherein the sweetener system comprises xylitol and sucrose.

20. The aqueous pharmaceutical suspension according to claim 3, wherein the sweetener system comprises xylitol and sucrose, and the ratio of the amount of sucrose : xylitol is 2:1.

21. The aqueous pharmaceutical suspension according to claim 3, wherein the sweetener system comprises, by weight/volume (g/100 mL), 0% to 20% of xylitol, and 10% to 40% of sucrose.

22. The aqueous pharmaceutical suspension according to claim 3, wherein the sweetener system comprises, by weight/volume (g/100 mL), 10% to 20% of xylitol, and 10% to 20% of sucrose.

23. The aqueous pharmaceutical suspension according to claim 3, wherein the sweetener system comprises, by weight/volume (g/100 mL), 20% of sucrose and 10% of xylitol.

24. The aqueous pharmaceutical suspension according to claim 3, the ratio of the amount of (sucrose or invert sucrose):(xylitol, sorbitol or sorbitol solution, or maltitol solution) is 2:1.

25. The aqueous pharmaceutical suspension according to claim 3, wherein the propylparaben, sodium propylparaben, or potassium propylparaben is, by weight/volume (g/100 mL), 0.014% to 0.048%.

26. The aqueous pharmaceutical suspension according to claim 3, wherein the propylparaben, sodium propylparaben, or potassium propylparaben is, by weight/volume (g/100 mL), 0.027% to 0.040%.

27. The aqueous pharmaceutical suspension according to claim 3, wherein the butylparaben, or sodium butylparaben is, by weight/volume (g/100 mL), 0.0008% to 0.0240%.

28. The aqueous pharmaceutical suspension according to claim 3, wherein the butylparaben, or sodium butylparaben is, by weight/volume (g/100 mL), 0.014% to 0.020%.

29. The aqueous pharmaceutical suspension according to claim 3, wherein the edetate disodium is, by weight/volume (g/100 mL), 0.10% to 0.18%.

30. The aqueous pharmaceutical suspension according to claim 3, wherein the edetate disodium is, by weight/volume (g/100 mL), 0.12% to 0.18%.

31. The aqueous pharmaceutical suspension according to claim 3, wherein the preservative system comprises propylparaben, butylparaben and edetate disodium.

32. The aqueous pharmaceutical suspension according to claim 3, wherein the benzoic acid or sodium benzoate is, by weight/volume (g/100 mL), 0.10% to 0.20%.

33. The aqueous pharmaceutical suspension according to claim 3, wherein the benzoic acid or sodium benzoate is, by weight/volume (g/100 mL), 0.12% to 0.18%.

34. The aqueous pharmaceutical suspension according to claim 3, wherein the sorbic acid or potassium sorbate is, by weight/volume (g/100 mL), 0.10% to 0.22%.

35. The aqueous pharmaceutical suspension according to claim 3, wherein the sorbic acid or potassium sorbate is, by weight/volume (g/100 mL), 0.12% to 0.20%.

36. The aqueous pharmaceutical suspension according to claim 3, wherein the benzyl alcohol is, by weight/volume (g/100 mL), 0.25% to 1.00%.

37. The aqueous pharmaceutical suspension according to claim 3, wherein the benzyl alcohol is, by weight/volume (g/100 mL), 0.24% to 0.50%.

38. The aqueous pharmaceutical suspension according to claim 3, wherein the buffering uses a buffer system comprising, by weight/volume (g/100 mL), 0.75% of sodium phosphate monobasic or a corresponding equivalent amount of a sodium phosphate monobasic hydrate, or 0.89% of potassium phosphate monobasic; and 1.25% of sodium phosphate dibasic or a corresponding equivalent amount of a sodium phosphate dibasic hydrate, or 1.86% of potassium phosphate dibasic or a corresponding equivalent amount of a potassium phosphate dibasic hydrate.

39. The aqueous pharmaceutical suspension according to claim 6, wherein the buffering uses a buffer system comprising, by weight/volume (g/100 mL), 0.75% of sodium phosphate monobasic or a corresponding equivalent amount of a sodium phosphate monobasic hydrate; and 1.25% of sodium phosphate dibasic or a corresponding equivalent amount of a sodium phosphate dibasic hydrate.

40. The aqueous pharmaceutical suspension according to claim 3, wherein the wetting agent is nonionic.

41. The aqueous pharmaceutical suspension according to claim 3, wherein the wetting agent is Poloxamer 407 or Poloxamer 188.

42. The aqueous pharmaceutical suspension according to claim 3, wherein the wetting agent is Poloxamer 407.

43. The aqueous pharmaceutical suspension according to claim 3, further comprising, by weight/volume (g/100 mL), 0.1% to 3.0% of microcrystalline cellulose.

44. The aqueous pharmaceutical suspension according to claim 3, further comprising, by weight/volume (g/100 mL), 1.0% to 2.0% of microcrystalline cellulose.

45. The aqueous pharmaceutical suspension according to claim 3, further comprising, by weight/volume (g/100 mL), 1.5% to 2.0% of microcrystalline cellulose.

46. The aqueous pharmaceutical suspension according to claim 3, further comprising, by weight/volume (g/100 mL), 0.01% to 0.20% of saccharin.

47. The aqueous pharmaceutical suspension according to claim 3, further comprising, by weight/volume (g/100 mL), 0.012% to 0.130% of saccharin.

48. The aqueous pharmaceutical suspension according to claim 3, further comprising, by weight/volume (g/100 mL), 0.05% to 0.10% of saccharin.

49. The aqueous pharmaceutical suspension according to claim 3, further comprising, by weight/volume (g/100 mL), 0.01% to 1.00% of acesulfame potassium or sucralose.

50. The aqueous pharmaceutical suspension according to claim 3, further comprising, by weight/volume (g/100 mL), 0.01% to 0.50% of acesulfame potassium or sucralose.

51. The aqueous pharmaceutical suspension according to claim 3, further comprising, by weight/volume (g/100 mL), 0.01% to 0.10% of acesulfame potassium or sucralose.

52. The aqueous pharmaceutical suspension according to claim 3, further comprising, by weight/volume (g/100 mL), 0.1% to 15.0% of propylene glycol.

53. The aqueous pharmaceutical suspension according to claim 3, further comprising, by weight/volume (g/100 mL), 1.0% to 10.0% of propylene glycol.

54. The aqueous pharmaceutical suspension according to claim 3, further comprising, by weight/volume (g/100 mL), 2.5% to 5.0% of propylene glycol.

55. The aqueous pharmaceutical suspension according to claim 3, further comprising, by weight/volume (g/100 mL), 0% to 4% of polyethylene glycol 200, polyethylene glycol 300 or polyethylene glycol 400.

56. The aqueous pharmaceutical suspension according to claim 3, further comprising, by weight/volume (g/100 mL), 0% to 2% of polyethylene glycol 200, polyethylene glycol 300 or polyethylene glycol 400.

57. The aqueous pharmaceutical suspension according to claim 3, further comprising, by weight/volume (g/100 mL), 0% to 1% of polyethylene glycol 200, polyethylene glycol 300 or polyethylene glycol 400.

58. The aqueous pharmaceutical suspension according to claim 3, further comprising, by weight/volume (g/100 mL), 0% to 0.50% of an opacifying agent.

59. The aqueous pharmaceutical suspension according to claim 3, further comprising, by weight/volume (g/100 mL), 0% to 0.10% of an opacifying agent.

60. The aqueous pharmaceutical suspension according to claim 3, further comprising, by weight/volume (g/100 mL), 0.05% to 0.10% of an opacifying agent.

61. The aqueous pharmaceutical suspension according to claim 58, wherein the opacifying agent is titanium dioxide.

62. The aqueous pharmaceutical suspension according to claim 59, wherein the opacifying agent is titanium dioxide.

63. The aqueous pharmaceutical suspension according to claim 60, wherein the opacifying agent is Titanium dioxide.

64. The aqueous pharmaceutical suspension according to claim 3, further comprising, by weight/volume (g/100 mL), 0.20% to 0.70% of a flavoring agent.

65. The aqueous pharmaceutical suspension according to claim 3, further comprising, by weight/volume (g/100 mL), 0.30% to 0.45% of a flavoring agent.

66. The aqueous pharmaceutical suspension according to claim 3, further comprising, by weight/volume (g/100 mL), 0.40% to 0.45% of a flavoring agent.

67. The aqueous pharmaceutical suspension according to claim 66, wherein the flavoring agent is artificial raspberry cream flavor or artificial orange cream flavor.

68. The aqueous pharmaceutical suspension according to claim 67, wherein the flavoring agent is artificial raspberry cream flavor or artificial orange cream flavor.

69. The aqueous pharmaceutical suspension according to claim 68, wherein the flavoring agent is artificial raspberry cream flavor or artificial orange cream flavor.

70. The aqueous pharmaceutical suspension according to claim 3, comprising, by weight/volume (g/100 mL), 0.60% of fexofenadine zwitterionic dihydrate Form I, 2.5% of propylene glycol, 0.15% of edetate disodium, 0.034% of propylparaben, 0.017% of butylparaben, 0.35% of xanthan gum, 0.05% of Poloxamer 407, 1.25% of sodium phosphate dibasic heptahydrate, 0.75% of sodium phosphate monobasic monohydrate, 20% of sucrose, and 10% of xylitol.

71. The aqueous pharmaceutical suspension according to claim 70, further comprising, by weight/volume (g/100 mL), 0.1% of titanium dioxide.

72. The aqueous pharmaceutical suspension according to claim 71, further comprising, by weight/volume (g/100 mL), 0.4% of raspberry cream flavor.

73. The aqueous pharmaceutical suspension according to claim 3, comprising, by weight/volume (g/100 mL), 0.60% of fexofenadine zwitterionic dihydrate Form I, 2.5% of propylene glycol, 0.15% of edetate disodium, 0.034% of propylparaben, 0.017% of butylparaben, 0.35% of xanthan gum, 0.05% of Poloxamer 407, 1.25% of sodium phosphate dibasic heptahydrate, 0.75% of sodium phosphate monobasic monohydrate, 10% of sucrose, and 10% of xylitol.

74. The aqueous pharmaceutical suspension according to claim 73, further comprising, by weight/volume (g/100 mL), 0.1% of titanium dioxide.

75. The aqueous pharmaceutical suspension according to claim 74, further comprising, by weight/volume (g/100 mL), 0.4% of raspberry cream flavor.

76. The aqueous pharmaceutical suspension according to claim 3, comprising, by weight/volume (g/100 mL), 0.60% of fexofenadine zwitterionic dihydrate Form I, 2.5% of propylene glycol, 0.15% of edetate disodium, 0.034% of propylparaben, 0.017% of butylparaben, 0.35% of xanthan gum, 0.05% of Poloxamer 407, 1.25% of sodium phosphate dibasic heptahydrate, 0.75% of sodium phosphate monobasic monohydrate, 20% of sucrose, and 10% of sorbitol solution.

77. The aqueous pharmaceutical suspension according to claim 76, further comprising, by weight/volume (g/100 mL), 0.1% of titanium dioxide.

78. The aqueous pharmaceutical suspension according to claim 77, further comprising, by weight/volume (g/100 mL), 0.4% of raspberry cream flavor.

79. The aqueous pharmaceutical suspension according to claim 4, comprising, by weight/volume (g/100 mL), 0.60% of fexofenadine zwitterionic dihydrate Form I, 2.5% of propylene glycol, 0.15% of edentate disodium, 0.034% of propylparaben 0.017% of butylparaben, 0.35% of xanthan gum, 0.05% of Poloxamer 407, 1.25% of sodium phosphate dibasic heptahydrate, 0.75% of sodium phosphate monobasic monohydrate, 20% of sucrose, and 10% of sorbitol solution.

80. The aqueous pharmaceutical suspension according to claim 79, further comprising, by weight/volume (g/100 mL), 0.1% of titanium dioxide.

81. The aqueous pharmaceutical suspension according to claim 80, further comprising, by weight/volume (g/100 mL), 0.4% of raspberry cream flavor.

82. The aqueous pharmaceutical suspension according to claim 1, comprising, by weight/volume (g/100 mL), 0.60% of fexofenadine zwitterionic dihydrate Form I, 2.5% of propylene glycol, 0.042% of propylparaben 0.021% of butylparaben, 0.35% of xanthan gum, 0.05% of Poloxamer 407, 1.25% of sodium phosphate dibasic heptahydrate, 0.75% of sodium phosphate monobasic monohydrate, 10% of sucrose, and 10% of xylitol.

83. The aqueous pharmaceutical suspension according to claim 1, comprising, by weight/volume (g/100 mL), 0.60% of fexofenadine zwitterionic dihydrate Form I, 2.5% of propylene glycol, 0.042% of propylparaben 0.021% of butylparaben, 0.35% of xanthan gum, 0.05% of Poloxamer 407, 1.25% of sodium phosphate dibasic heptahydrate, 0.75% of sodium phosphate monobasic monohydrate, 20% of sucrose, and 10% of xylitol.

84. The aqueous pharmaceutical suspension according to claim 1, wherein the sweetener system comprises, by weight/volume (g/100 mL), 10% to 40% sucrose; and 20% xylitol.

85. The aqueous pharmaceutical suspension according to claim 1, wherein the sweetener system comprises, by weight/volume (g/100 mL), 10% to 20% sucrose, and 10% to 20% xylitol.

86. An aqueous pharmaceutical suspension, having a pH 5.8 to 7.0 adjusted by a buffer system, wherein the suspension comprises, by weight/volume (g/100 mL), 0.60% of fexofenadine zwitterionic dihydrate Form I of formula (I) having a particle size of less than 40 .mu.m for at least 90% of the fexofenadine zwitterionic dihydrate Form I; ##STR00003## 0.01% to 0.20% of a wetting agent; a suspending agent selected from 0.10% to 0.50% of a hydrocolloid gum, or 0.1% to 1.0% of hydroxyethylcellulose; a sweetener system comprising 10% to 40% of sucrose or invert sucrose; and 10% to 20% of xylitol, sorbitol or sorbitol solution, or maltitol solution; provided that the ratio of the amount of (sucrose or invert sucrose):(xylitol, sorbitol or sorbitol solution, or maltitol solution) is 1:1 to 2:1; and a preservative system comprising 0.010% to 0.058% of propylparaben, sodium propylparaben or potassium propylparaben; 0.0005% to 0.0350% of butylparaben or sodium butylparaben; and 0.06% to 0.26% of edetate disodium, 0.01% to 0.27% of benzoic acid or sodium benzoate, 0.01% to 0.30% of sorbic acid or potassium sorbate or 0.10% to 1.50% of benzyl alcohol.

87. The aqueous pharmaceutical suspension according to claim 86, comprising, by weight/volume (g/100 mL), 2.5% of propylene glycol; 0.05% of Poloxamer 407; 0.35% of xanthan gum; 10% to 20% of sucrose; 10% of xylitol or sorbitol; 0.034% of propylparaben; 0.017% of butylparaben; 0.15% of edetate disodium; and wherein the buffer system comprises, by weight/volume (g/100 mL), 1.25% of sodium phosphate dibasic heptahydrate and 0.75% of sodium phosphate monobasic monohydrate.

88. The aqueous pharmaceutical suspension according to claim 86, comprising, by weight/volume (g/100 mL), 20% of sucrose and 10% of xylitol.
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