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Last Updated: September 21, 2021

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Claims for Patent: 9,925,147


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Summary for Patent: 9,925,147
Title:Method for treating secondary hyperparathyroidism in CKD
Abstract: A stable, controlled release formulation for oral dosing of vitamin D compounds is disclosed. The formulation is prepared by incorporating one or more vitamin D compounds into a solid or semi-solid mixture of waxy materials. Oral dosage forms can be prepared by melt-blending the components described herein and filling gelatin capsules with the formulation.
Inventor(s): Bishop; Charles W. (Miami Beach, FL), Tabash; Samir P. (Whitby, CA), Agudoawu; Sammy A. (Mississauga, CA), White; Jay A. (Newmarket, CA), Messner; Eric J. (Lake Forest, IL), Petkovich; P. Martin (Kingston, CA), Crawford; Keith H. (Lone Tree, CO)
Assignee: OPKO RENAL, LLC (Miami, FL) OPKO IRELAND GLOBAL HOLDINGS, LIMITED (Grand Cayman, KY)
Application Number:15/358,065
Patent Claims: 1. A method of treating secondary hyperparathyroidism in a human patient having Chronic Kidney Disease (CKD), comprising administering to the human patient having CKD an effective amount of a sustained release formulation of a 25-hydroxyvitamin D compound to treat the secondary hyperparathyroidism and reduce the patient's serum parathyroid hormone level, wherein the sustained release of the 25-hydroxyvitamin D compound is effected over a period of at least 10 hours.

2. The method of claim 1, wherein the sustained release of the 25-hydroxyvitamin D compound is effected over a period of at least 24 hours.

3. The method of claim 1, wherein the administration avoids transient increases in blood levels of 25-hydroxyvitamin D of greater than 3 ng/mL following a unit dose.

4. The method of claim 1, wherein the 25-hydrovitamin D compound is 25-hydroxyvitamin D.sub.2, 25-hydroxyvitamin D.sub.3, or a combination thereof.

5. The method of claim 1, wherein the sustained release formulation comprises 1 .mu.g to 1000 .mu.g 25-hydrovitamin D.sub.3 per unit dose.

6. The method of claim 5, wherein the sustained release formulation comprises 1 .mu.g to 100 .mu.g 25-hydrovitamin D.sub.3 per unit dose.

7. The method of claim 1, wherein the sustained release formulation comprises a waxy controlled release carrier.

8. The method of claim 1, wherein the sustained release formulation comprises a waxy controlled release carrier, a lipoidic agent, and an oily vehicle for the 25-hydroxyvitamin D compound.

9. The method of claim 1, comprising administering the sustained release formulation to deliver a dosage amount of the 25-hydroxyvitamin D compound from 1 to 100 .mu.g per day.

10. The method of claim 1, wherein the patient has CKD Stage 5.

11. The method of claim 1, wherein the patient has CKD Stage 1 or 2.

12. The method of claim 1, wherein the patient has CKD Stage 3 or 4.

13. A method of treating secondary hyperparathyroidism in a human patient having Chronic Kidney Disease (CKD), comprising administering to the human patient having CKD an effective amount of a sustained release formulation of a 25-hydroxyvitamin D compound to treat the secondary hyperparathyroidism and reduce the patient's serum parathyroid hormone level, such that the maximum serum concentration (Cmax) of 25-hydroxyvitamin D in a dose interval is reduced compared to the Cmax for an equivalent amount of the 25-hydroxyvitamin D compound administered by bolus IV injection and an equivalent amount of the 25-hydroxyvitamin D compound administered by immediate-release, oral dosing.

14. The method of claim 13, wherein the sustained release of the 25-hydroxyvitamin D compound is effected over a period of at least 10 hours.

15. The method of claim 13, wherein the sustained release of the 25-hydroxyvitamin D compound is effected over a period of at least 24 hours.

16. The method of claim 13, wherein the administration avoids transient increases in blood levels of 25-hydroxyvitamin D of greater than 3 ng/mL following a unit dose.

17. The method of claim 13, wherein the 25-hydrovitamin D compound is 25-hydroxyvitamin D.sub.2, 25-hydroxyvitamin D.sub.3, or a combination thereof.

18. The method of claim 13, wherein the sustained release formulation comprises 1 .mu.g to 1000 .mu.g 25-hydrovitamin D.sub.3 per unit dose.

19. The method of claim 18, wherein the sustained release formulation comprises 1 .mu.g to 100 .mu.g 25-hydrovitamin D.sub.3 per unit dose.

20. The method of claim 13, wherein the sustained release formulation comprises a waxy controlled release carrier.

21. The method of claim 13, wherein the sustained release formulation comprises a waxy controlled release carrier, a lipoidic agent, and an oily vehicle for the 25-hydroxyvitamin D compound.

22. The method of claim 13, comprising administering the sustained release formulation to deliver a dosage amount of the 25-hydroxyvitamin D compound from 1 to 100 .mu.g per day.

23. The method of claim 13, wherein the patient has CKD Stage 5.

24. The method of claim 13, wherein the patient has CKD Stage 1 or 2.

25. The method of claim 13, wherein the patient has CKD Stage 3 or 4.

26. A method of treating secondary hyperparathyroidism in a human patient having Chronic Kidney Disease (CKD), comprising administering to the human patient having CKD an effective amount of a sustained release formulation of a 25-hydroxyvitamin D compound to treat the secondary hyperparathyroidism and reduce the patient's serum parathyroid hormone level, such that the maximum change in serum concentration of 25-hydroxyvitamin D in a dose interval is reduced compared to the maximum change in serum concentration of 25-hydroxyvitamin D for an equivalent amount of the 25-hydroxyvitamin D compound administered by bolus IV injection and an equivalent amount of the 25-hydroxyvitamin D compound administered by immediate-release, oral dosing.

27. The method of claim 26, wherein the sustained release of the 25-hydroxyvitamin D compound is effected over a period of at least 10 hours.

28. The method of claim 26, wherein the sustained release of the 25-hydroxyvitamin D compound is effected over a period of at least 24 hours.

29. The method of claim 26, wherein the administration avoids transient increases in blood levels of 25-hydroxyvitamin D of greater than 3 ng/mL following a unit dose.

30. The method of claim 26, wherein the 25-hydrovitamin D compound is 25-hydroxyvitamin D.sub.2, 25-hydroxyvitamin D.sub.3, or a combination thereof.

31. The method of claim 26, wherein the sustained release formulation comprises 1 .mu.g to 1000 .mu.g 25-hydrovitamin D.sub.3 per unit dose.

32. The method of claim 31, wherein the sustained release formulation comprises 1 .mu.g to 100 .mu.g 25-hydrovitamin D.sub.3 per unit dose.

33. The method of claim 26, wherein the sustained release formulation comprises a waxy controlled release carrier.

34. The method of claim 26, wherein the sustained release formulation comprises a waxy controlled release carrier, a lipoidic agent, and an oily vehicle for the 25-hydroxyvitamin D compound.

35. The method of claim 26, comprising administering the sustained release formulation to deliver a dosage amount of the 25-hydroxyvitamin D compound from 1 to 100 .mu.g per day.

36. The method of claim 26, wherein the patient has CKD Stage 5.

37. The method of claim 26, wherein the patient has CKD Stage 1 or 2.

38. The method of claim 26, wherein the patient has CKD Stage 3 or 4.

39. A method of treating secondary hyperparathyroidism in a human patient having Chronic Kidney Disease (CKD), comprising administering to the human patient having CKD an effective amount of a sustained release formulation of a 25-hydroxyvitamin D compound to treat the secondary hyperparathyroidism and reduce the patient's serum parathyroid hormone level, such that the maximum serum concentration within 24 hours after administration of the 25-hydroxyvitamin D compound to the concentration 24 hours after administration (Cmax.sub.24hr/C.sub.24hr) is reduced compared to the Cmax.sub.24hr/C.sub.24hr for an equivalent amount of the 25-hydroxyvitamin D compound administered by bolus IV injection and an equivalent amount of the 25-hydroxyvitamin D compound administered by immediate-release, oral dosing.

40. The method of claim 39, wherein the sustained release of the 25-hydroxyvitamin D compound is effected over a period of at least 10 hours.

41. The method of claim 39, wherein the sustained release of the 25-hydroxyvitamin D compound is effected over a period of at least 24 hours.

42. The method of claim 39, wherein the administration avoids transient increases in blood levels of 25-hydroxyvitamin D of greater than 3 ng/mL following a unit dose.

43. The method of claim 39, wherein the 25-hydrovitamin D compound is 25-hydroxyvitamin D.sub.2, 25-hydroxyvitamin D.sub.3, or a combination thereof.

44. The method of claim 39, wherein the sustained release formulation comprises 1 .mu.g to 1000 .mu.g 25-hydrovitamin D.sub.3 per unit dose.

45. The method of claim 44, wherein the sustained release formulation comprises 1 .mu.g to 100 .mu.g 25-hydrovitamin D.sub.3 per unit dose.

46. The method of claim 39, wherein the sustained release formulation comprises a waxy controlled release carrier.

47. The method of claim 39, wherein the sustained release formulation comprises a waxy controlled release carrier, a lipoidic agent, and an oily vehicle for the 25-hydroxyvitamin D compound.

48. The method of claim 39, comprising administering the sustained release formulation to deliver a dosage amount of the 25-hydroxyvitamin D compound from 1 to 100 .mu.g per day.

49. The method of claim 39, wherein the patient has CKD Stage 5.

50. The method of claim 39, wherein the patient has CKD Stage 1 or 2.

51. The method of claim 39, wherein the patient has CKD Stage 3 or 4.

52. A method of treating secondary hyperparathyroidism in a human patient having Chronic Kidney Disease (CKD), comprising administering to the human patient having CKD an effective amount of a sustained release formulation of a 25-hydroxyvitamin D compound to treat the secondary hyperparathyroidism and reduce the patient's serum parathyroid hormone level, such that the elimination half-life (t.sub.1/2) of the 25-hydroxyvitamin D compound is increased compared to the t.sub.1/2 for an equivalent amount of the 25-hydroxyvitamin D compound administered by bolus IV injection and an equivalent amount of the 25-hydroxyvitamin D compound administered by immediate-release, oral dosing.

53. The method of claim 52, wherein the sustained release of the 25-hydroxyvitamin D compound is effected over a period of at least 10 hours.

54. The method of claim 52, wherein the sustained release of the 25-hydroxyvitamin D compound is effected over a period of at least 24 hours.

55. The method of claim 52, wherein the administration avoids transient increases in blood levels of 25-hydroxyvitamin D of greater than 3 ng/mL following a unit dose.

56. The method of claim 52, wherein the 25-hydrovitamin D compound is 25-hydroxyvitamin D.sub.2, 25-hydroxyvitamin D.sub.3, or a combination thereof.

57. The method of claim 52, wherein the sustained release formulation comprises 1 .mu.g to 1000 .mu.g 25-hydrovitamin D.sub.3 per unit dose.

58. The method of claim 57, wherein the sustained release formulation comprises 1 .mu.g to 100 .mu.g 25-hydrovitamin D.sub.3 per unit dose.

59. The method of claim 52, wherein the sustained release formulation comprises a waxy controlled release carrier.

60. The method of claim 52, wherein the sustained release formulation comprises a waxy controlled release carrier, a lipoidic agent, and an oily vehicle for the 25-hydroxyvitamin D compound.

61. The method of claim 52, comprising administering the sustained release formulation to deliver a dosage amount of the 25-hydroxyvitamin D compound from 1 to 100 .mu.g per day.

62. The method of claim 52, wherein the patient has CKD Stage 5.

63. The method of claim 52, wherein the patient has CKD Stage 1 or 2.

64. The method of claim 52, wherein the patient has CKD Stage 3 or 4.

65. A method of treating secondary hyperparathyroidism in a human patient having Chronic Kidney Disease (CKD), comprising administering to the human patient having CKD an effective amount of a sustained release formulation of a 25-hydroxyvitamin D compound to treat the secondary hyperparathyroidism and reduce the patient's serum parathyroid hormone level, such that the time for the plasma concentration of the 25-hydroxyvitamin D compound to reach its maximum in a dose interval following administration (Tmax) is increased compared to the Tmax for an equivalent amount of the 25-hydroxyvitamin D compound administered by bolus IV injection and an equivalent amount of the 25-hydroxyvitamin D compound administered by immediate-release, oral dosing.

66. The method of claim 65, wherein the sustained release of the 25-hydroxyvitamin D compound is effected over a period of at least 10 hours.

67. The method of claim 65, wherein the sustained release of the 25-hydroxyvitamin D compound is effected over a period of at least 24 hours.

68. The method of claim 65, wherein the administration avoids transient increases in blood levels of 25-hydroxyvitamin D of greater than 3 ng/mL following a unit dose.

69. The method of claim 65, wherein the 25-hydrovitamin D compound is 25-hydroxyvitamin D.sub.2, 25-hydroxyvitamin D.sub.3, or a combination thereof.

70. The method of claim 65, wherein the sustained release formulation comprises 1 .mu.g to 1000 .mu.g 25-hydrovitamin D.sub.3 per unit dose.

71. The method of claim 70, wherein the sustained release formulation comprises 1 .mu.g to 100 .mu.g 25-hydrovitamin D.sub.3 per unit dose.

72. The method of claim 65, wherein the sustained release formulation comprises a waxy controlled release carrier.

73. The method of claim 65, wherein the sustained release formulation comprises a waxy controlled release carrier, a lipoidic agent, and an oily vehicle for the 25-hydroxyvitamin D compound.

74. The method of claim 65, comprising administering the sustained release formulation to deliver a dosage amount of the 25-hydroxyvitamin D compound from 1 to 100 .mu.g per day.

75. The method of claim 65, wherein the patient has CKD Stage 5.

76. The method of claim 65, wherein the patient has CKD Stage 1 or 2.

77. The method of claim 65, wherein the patient has CKD Stage 3 or 4.

78. A method of administering a 25-hydroxyvitamin D compound to a patient wherein the maximum serum concentration of 25-hydroxyvitamin D in a dose interval (Cmax) is reduced as compared to Cmax for both an equivalent amount of the 25-hydroxyvitamin D compound administered by bolus IV injection and an equivalent amount of the 25-hydroxyvitamin D compound administered by immediate-release, oral dosing; and wherein the maximum change in serum concentration of 25-hydroxyvitamin D in a dose interval is reduced as compared to the maximum change in serum concentration of 25-hydroxyvitamin D in a dose interval for both an equivalent amount of the 25-hydroxyvitamin D compound administered by bolus IV injection and an equivalent amount of the 25-hydroxyvitamin D compound administered by immediate-release, oral dosing; and wherein the time for the plasma concentration of the 25-hydroxyvitamin D compound to reach its maximum in a dose interval following administration (Tmax) is reduced as compared to Tmax for both an equivalent amount of the 25-hydroxyvitamin D compound administered by bolus IV injection and an equivalent amount of the 25-hydroxyvitamin D compound administered by immediate-release, oral dosing.

79. The method of claim 78, wherein the sustained release of the 25-hydroxyvitamin D compound is effected over a period of at least 10 hours.

80. The method of claim 78, wherein the sustained release of the 25-hydroxyvitamin D compound is effected over a period of at least 24 hours.

81. The method of claim 78, wherein the administration avoids transient increases in blood levels of 25-hydroxyvitamin D of greater than 3 ng/mL following a unit dose.

82. The method of claim 78, wherein the 25-hydrovitamin D compound is 25-hydroxyvitamin D.sub.2, 25-hydroxyvitamin D.sub.3, or a combination thereof.

83. The method of claim 78, wherein the sustained release formulation comprises 1 .mu.g to 1000 .mu.g 25-hydrovitamin D.sub.3 per unit dose.

84. The method of claim 83, wherein the sustained release formulation comprises 1 .mu.g to 100 .mu.g 25-hydrovitamin D.sub.3 per unit dose.

85. The method of claim 78, wherein the sustained release formulation comprises a waxy controlled release carrier.

86. The method of claim 78, wherein the sustained release formulation comprises a waxy controlled release carrier, a lipoidic agent, and an oily vehicle for the 25-hydroxyvitamin D compound.

87. The method of claim 78, comprising administering the sustained release formulation to deliver a dosage amount of the 25-hydroxyvitamin D compound from 1 to 100 .mu.g per day.

88. The method of claim 78, wherein the patient has CKD Stage 5.

89. The method of claim 78, wherein the patient has CKD Stage 1 or 2.

90. The method of claim 78, wherein the patient has CKD Stage 3 or 4.

91. A formulation for sustained release of a 25-hydroxyvitamin D compound, wherein release of the 25-hydroxyvitamin D compound from the formulation is sustained for at least four hours.

92. The formulation of claim 91, wherein the release of the 25-hydroxyvitamin D compound from the formulation is sustained for at least 10 hours.

93. The formulation of claim 91, wherein the release of the 25-hydroxyvitamin D compound from the formulation is sustained for at least 24 hours.

94. The formulation of claim 91, wherein the 25-hydrovitamin D compound is 25-hydroxyvitamin D.sub.2, 25-hydroxyvitamin D.sub.3, or a combination thereof.

95. The formulation of claim 91, comprising 1 .mu.g to 1000 .mu.g 25-hydrovitamin D.sub.3 per unit dose.

96. The formulation of claim 95, comprising 1 .mu.g to 100 .mu.g 25-hydrovitamin D.sub.3 per unit dose.

97. The formulation of claim 91, comprising a waxy controlled release carrier.

98. The formulation of claim 91, comprising a waxy controlled release carrier, a lipoidic agent, and an oily vehicle for the 25-hydroxyvitamin D compound.

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