IP Library Granted Patent US 9,498,486
Granted Patent B1
US 9,498,486 · App. 15/231,357 · Granted Nov 22, 2016

Method for controlled release oral dosage of a vitamin D compound

Inventors: Charles W. Bishop (Miami Beach, FL); Samir P. Tabash (Whitby, CA); Sammy A. Agudoawu (Mississauga, CA); Jay A. White (Newmarket, CA); Eric J. Messner (Lake Forest, IL); P. Martin Petkovich (Kingston, CA); Keith H. Crawford (Lone Tree, CO)
Assignees: OPKO RENAL, LLC; OPKO IRELAND GLOBAL HOLDINGS, LTD.
A61K31/593A61K9/0053A61K47/44
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Quick Facts
Patent No.
US 9,498,486
App. No.
15/231,357
Granted
Nov 22, 2016
Kind
B1
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.

Claims (31)

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, oral dosage form of 25-hydroxyvitamin D to treat the secondary hyperparathyroidism and reduce the patient's serum parathyroid hormone level, wherein the administration avoids transient increases in blood levels of 25-hydroxyvitamin D of greater than 3 ng/mL following a unit dose.

2. The method of claim 1 , comprising administering 30 μg or 60 μg of 25-hydroxyvitamin D 3 .

3. The method of claim 1 , wherein the sustained release, oral dosage form of 25-hydroxyvitamin D comprises a waxy controlled release carrier.

4. The method of claim 3 , wherein the sustained release, oral dosage form of 25-hydroxyvitamin D comprises a waxy controlled release carrier, a lipoidic agent, and an oily vehicle for the 25-hydroxyvitamin D compound.

5. The method of claim 1 , comprising administering said oral dosage on a schedule of once per day.

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

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

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

9. 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, oral dosage form of 25-hydroxyvitamin D to treat the secondary hyperparathyroidism and reduce the patient's serum parathyroid hormone level, wherein the sustained release is effected over a period of at least four hours.

10. The method of claim 9 , comprising administering 30 μg or 60 μg of 25-hydroxyvitamin D 3 .

11. The method of claim 9 , wherein the administration avoids transient increases in blood levels of 25-hydroxyvitamin D of greater than 3 ng/mL following a unit dose.

12. The method of claim 9 , wherein the sustained release, oral dosage form of 25-hydroxyvitamin D comprises a waxy controlled release carrier.

13. The method of claim 9 , comprising administering said oral dosage on a schedule of once per day.

14. The method of claim 9 , wherein the patient has CKD Stage 5.

15. The method of claim 9 , wherein the patient has CKD Stage 1 or 2.

16. The method of claim 9 , wherein the patient has CKD Stage 3 or 4.

17. 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, oral dosage form of 25-hydroxyvitamin D to treat the secondary hyperparathyroidism and reduce the patient's serum parathyroid hormone level, such that (a) the ratio of the maximum serum concentration within 24 hours after administration of the vitamin D compound to the concentration 24 hours after administration (Cmax 24hr /C 24hr ) is reduced as compared to an equivalent amount of the vitamin D compound administered by an immediate-release, oral dosage form and/or

(b) the time for the plasma concentration of the vitamin D compound to reach its maximum in a dose interval following administration (Tmax) is increased as compared to Tmax for an equivalent amount of the vitamin D compound administered by an equivalent immediate-release, oral dosage form, wherein the vitamin D compound comprises 25-hydroxyvitamin D 3 .

18. The method of claim 17 , comprising administering 30 μg or 60 μg of 25-hydroxyvitamin D 3 .

19. The method of claim 17 , wherein the administration avoids transient increases in blood levels of 25-hydroxyvitamin D of greater than 3 ng/mL following a unit dose.

20. The method of claim 17 , wherein the sustained release, oral dosage form of 25-hydroxyvitamin D comprises a waxy controlled release carrier.

21. The method of claim 17 , comprising administering said oral dosage on a schedule of once per day.

22. The method of claim 17 , wherein the patient has CKD Stage 5.

23. The method of claim 17 , wherein the patient has CKD Stage 1 or 2.

24. The method of claim 17 , wherein the patient has CKD Stage 3 or 4.

25. A method of treating a disease or condition, comprising administering to a human patient 30 μg or 60 μg of an extended release, oral dosage form of 25-hydroxyvitamin D 3 once daily, wherein the disease or condition is secondary hyperparathyroidism in an adult human patient having Chronic Kidney Disease (CKD) Stage 3 or 4 and serum total 25-hydroxyvitamin D levels less than 30 ng/mL.

26. The method of claim 25 , wherein the sustained release, oral dosage form of 25-hydroxyvitamin D comprises a waxy controlled release carrier.

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

28. The method of claim 25 , wherein the patient has CKD Stage 5.

29. The method of claim 25 , wherein the patient has CKD Stage 1 or 2.

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

Assignments (9)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 30, 2021
From: OPKO IRELAND GLOBAL HOLDINGS, LTD.
To: EIRGEN PHARMA LTD.
Reel/Frame 055765/0953 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 10, 2016
From: CYTOCHROMA INC.
To: CYTOCHROMA CAYMAN ISLANDS LTD.
Reel/Frame 040586/0889 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 14, 2016
From: BISHOP, CHARLES W.; CRAWFORD, KEITH H.; MESSNER, ERIC J.
To: PROVENTIV THERAPEUTICS, LLC
Reel/Frame 040019/0197 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 14, 2016
From: CYTOCHROMA INC.
To: CYTOCHROMA CAYMAN ISLANDS LTD.
Reel/Frame 040354/0542 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 14, 2016
From: PROVENTIV THERAPEUTICS, LLC
To: OPKO HEALTH, INC.
Reel/Frame 040019/0255 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 14, 2016
From: OPKO HEALTH, INC.
To: OPKO RENAL, LLC
Reel/Frame 040019/0274 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 14, 2016
From: OPKO IP HOLDINGS II, INC.
To: OPKO IRELAND GLOBAL HOLDINGS, LTD.
Reel/Frame 040019/0312 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 14, 2016
From: CYTOCHROMA CAYMAN ISLANDS LTD.
To: OPKO IP HOLDINGS II, INC.
Reel/Frame 040019/0208 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 14, 2016
From: TABASH, SAMIR P.; WHITE, JAY A.; AGUDOAWU, SAMMY A.; PETKOVICH, P. MARTIN
To: CYTOCHROMA INC.
Reel/Frame 040019/0169 →
Continuity (5)
Continuation 14690131 · Apr 17, 2015
Continuation 14305863 · Jun 16, 2014
Continuation 13746982 · Jan 22, 2013
Continuation 12109983 · Apr 25, 2008
Provisional Application 60913853 · Apr 25, 2007