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Claims for Patent: 8,361,488

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Claims for Patent: 8,361,488

Title:Methods and compositions for controlled release oral dosage of a vitamin D compound
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. (Mount Horeb, WI), Tabash; Samir P. (Whitby, CA), Agudoawu; Sammy Asiamah (Mississauga, CA), White; Jay A. (Newmarket, CA), Crawford; Keith H. (Highlands Ranch, CO), Messner; Eric J. (Lake Forest, IL), Petkovich; P. Martin (Kingston, CA)
Assignee: Cytochroma Inc. (Markham, CA) Proventiv Therapeutics, LLC (Bannockburn, IL)
Application Number:12/109,983
Patent Claims: 1. A formulation for controlled release of a vitamin D compound in the gastrointestinal tract of a subject which ingests the formulation, comprising a solid or semi-solid, waxy mixture comprising a waxy controlled release carrier agent, a lipoidic agent, an oily vehicle for the vitamin D compound, and a vitamin D compound, wherein the vitamin D compound comprises a compound selected from the group consisting of 25-hydroxyvitamin D.sub.2, 25-hydroxyvitamin D.sub.3, or a combination thereof.

2. The formulation according to claim 1, wherein the mixture is solid or semi-solid at room temperature and semi-solid or liquid at body temperature.

3. The formulation according to claim 1, wherein the waxy controlled release carrier agent comprises a non-digestible wax.

4. The formulation according to claim 3, wherein the non-digestible wax comprises paraffin wax.

5. The formulation according to claim 1, wherein the waxy controlled release carrier agent is present in an amount in a range of 5 wt % to 35 wt %.

6. The formulation according to claim 1, wherein the lipoidic agent has a HLB in a range of about 13 to about 18.

7. The formulation according to claim 1, wherein the lipoidic agent is an emulsifier having a HLB less than 7.

8. The formulation according to claim 1, wherein the lipoidic agent comprises a polyglycolized glyceride.

9. The formulation according to claim 8, wherein the polyglycolized glyceride is characterized by a melting point of about 44.degree. C. and a HLB of about 14.

10. The formulation according to claim 1, wherein the lipoidic agent includes a mixture of a lipophilic emulsifier which has an HLB of less than 7 and an absorption enhancer that preferably has an HLB value from 13 to 18.

11. The formulation according to claim 1, wherein the oily vehicle comprises a non-digestible oil.

12. A controlled-release oral dosage formulation of a vitamin D compound, comprising a pharmacologically active amount of a vitamin D compound and a release-modifying agent in an amount effective to control the release rate of the vitamin D compound from the dosage form to reduce the maximum serum concentration of the vitamin D compound in a dose interval (Cmax) and/or reduce the maximum change in serum concentration of the vitamin D compound and/or increase the time for the plasma concentration of the vitamin D compound to reach its maximum in a dose interval following administration (Tmax) and/or decrease a ratio of the maximum serum concentration of the vitamin D compound within 24 hours after administration to the concentration 24 hours after administration (Cmax.sub.24hr/C.sub.24hr), as compared to either or both of (a) an equivalent amount of the vitamin D compound administered by bolus IV injection and (b) the same dosage form omitting the effective amount of the release-modifying agent, wherein the vitamin D compound comprises a compound selected from the group consisting of 25-hydroxyvitamin D.sub.2, 25-hydroxyvitamin D.sub.3, or a combination thereof.

13. The formulation according to claim 12, wherein the dosage form is characterized by both reduced Cmax and increased Tmax.

14. The formulation according to claim 12, wherein the vitamin D compound comprises 25-hydroxyvitamin D.sub.3.

15. The formulation according to claim 1, wherein the vitamin D compound comprises 25-hydroxyvitamin D.sub.3.

16. A formulation for controlled release of a vitamin D compound in the gastrointestinal tract of a subject which ingests the formulation, comprising a solid or semi-solid, waxy mixture comprising a waxy controlled release carrier agent, a lipoidic agent, an oily vehicle for the vitamin D compound, and a vitamin D compound, wherein the mixture is solid or semi-solid at room temperature and semi-solid or liquid at body temperature, and wherein the vitamin D compound comprises a compound selected from the group consisting of 25-hydroxyvitamin D.sub.2, 25-hydroxyvitamin D.sub.3, or a combination thereof.

17. A formulation for controlled release of a vitamin D compound in the gastrointestinal tract of a subject which ingests the formulation, comprising a solid or semi-solid, waxy mixture comprising a waxy controlled release carrier agent, a lipoidic agent, an oily vehicle for the vitamin D compound, and a vitamin D compound, wherein the oily vehicle comprises a non-digestible oil, and wherein the vitamin D compound comprises a compound selected from the group consisting of 25-hydroxyvitamin D.sub.2, 25-hydroxyvitamin D.sub.3, or a combination thereof.

18. A formulation for controlled release of a vitamin D compound in the gastrointestinal tract of a subject which ingests the formulation, comprising a solid or semi-solid, waxy mixture comprising paraffin wax, fatty acid mono- and di-glycerides, a mineral oil, a polyglycolized glyceride, and a vitamin D compound selected from the group consisting of 25-hydroxyvitamin D.sub.2, 25-hydroxyvitamin D.sub.3, or a combination thereof.

19. The formulation according to claim 12, wherein the reduction in Cmax is of at least 20%.

20. The formulation according to claim 19, wherein the reduction in Cmax is of at least 70%.

21. The formulation according to claim 19, wherein the increase in Tmax is of at least 100%.

22. The formulation according to claim 12, wherein the reduction of the maximum change in serum concentration of the vitamin D compound is of at least 20%.

23. The formulation according to claim 22, wherein the reduction of the maximum change in serum concentration of the vitamin D compound is of at least 70%.

24. The formulation according to claim 22, wherein the increase in Tmax is of at least 100%.

25. The formulation according to claim 12, wherein the decrease in Cmax.sub.24hr/C.sub.24 hr is of at least 20%.

26. The formulation according to claim 25, wherein the decrease in Cmax.sub.24hr/C.sub.24 hr is of at least 30%.

27. The formulation according to claim 25, wherein the increase in Tmax is of at least 100%.

28. The formulation according to claim 12, wherein the increase in Tmax is of at least 100%.

29. The formulation according to claim 28, wherein the increase in Tmax is of at least 150%.
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