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Last Updated: September 21, 2021

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Claims for Patent: 9,763,920


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Summary for Patent: 9,763,920
Title:Solid dispersions comprising tacrolimus
Abstract: A pharmaceutical composition comprising tacrolimus (FK-506) dissolved and/or dispersed in a hydrophilic or water-miscible vehicle to form a solid dispersion or solid solution at ambient temperature have improved bioavailability.
Inventor(s): Holm; Per (Vanlose, DK)
Assignee: VELOXIS PHARMACEUTICALS A/S (Kobenhavn, DK)
Application Number:14/934,908
Patent Claims: 1. A solid pharmaceutical composition comprising (i) a solid carrier, and (ii) tacrolimus in a mixture of at least two hydrophilic or water-miscible vehicles having a melting point between 30.degree. C. and the melting point of tacrolimus, wherein the tacrolimus is present in the composition at a concentration of between 0.01 w/w % and 15 w/w %.

2. The solid pharmaceutical composition of claim 1, wherein the hydrophilic or water-miscible vehicles have a melting point between 40.degree. C. and the melting point of tacrolimus.

3. The solid pharmaceutical composition of claim 1, wherein the hydrophilic or water-miscible vehicles have a melting point between 50.degree. C. and the melting point of tacrolimus.

4. The solid pharmaceutical composition of claim 1, wherein one hydrophilic or water-miscible vehicle is a poloxamer.

5. The solid pharmaceutical composition of claim 4, wherein the poloxamer is poloxamer 188.

6. The solid pharmaceutical composition of claim 1, wherein one hydrophilic or water-miscible vehicle is polyethylene glycol.

7. The solid pharmaceutical composition of claim 6, wherein the polyethylene glycol has an average molecular weight of at least 1500.

8. The solid pharmaceutical composition of claim 1, wherein the composition further comprises a release-modifying agent.

9. The solid pharmaceutical composition of claim 8, wherein the composition provides a W.sub.50 (the time where the plasma concentration is 50% or more of C.sub.max) of at least 12 hours.

10. The solid pharmaceutical composition of claim 9, wherein the composition provides a W.sub.50 (the time where the plasma concentration is 50% or more of C.sub.max) of at least 14 hours.

11. A solid pharmaceutical composition comprising agglomerated particles comprising a solid carrier and tacrolimus dispersed or dissolved in a mixture of at least two hydrophilic or water-miscible vehicles having a melting point between 30.degree. C. and the melting point of tacrolimus, wherein (i) the tacrolimus is present in the composition at a concentration of between about 0.01 w/w % and about 15 w/w %, and (ii) the particles have a geometric weight mean diameter d.sub.gw of from 100 to 1000 .mu.m.

12. The solid pharmaceutical composition of claim 11, wherein the hydrophilic or water-miscible vehicles have a melting point between 40.degree. C. and the melting point of tacrolimus.

13. The solid pharmaceutical composition of claim 11, wherein the hydrophilic or water-miscible vehicles have a melting point between 50.degree. C. and the melting point of tacrolimus.

14. The solid pharmaceutical composition of claim 11, wherein one hydrophilic or water-miscible vehicle is a poloxamer.

15. The solid pharmaceutical composition of claim 14, wherein the poloxamer is poloxamer 188.

16. The solid pharmaceutical composition of claim 11, wherein one hydrophilic or water-miscible vehicle is polyethylene glycol.

17. The solid pharmaceutical composition of claim 16, wherein the polyethylene glycol has an average molecular weight of at least 1500.

18. The solid pharmaceutical composition of claim 11, wherein the composition further comprises a release-modifying agent.

19. The solid pharmaceutical composition of claim 18, wherein the composition provides a W.sub.50 (the time where the plasma concentration is 50% or more of C.sub.max) of at least 12 hours.

20. The solid pharmaceutical composition of claim 19, wherein the composition provides a W.sub.50 (the time where the plasma concentration is 50% or more of C.sub.max) of at least 14 hours.

21. A solid pharmaceutical composition prepared by a process comprising the steps of: (a) spraying a solid carrier with tacrolimus dispersed or dissolved in a melted mixture of two hydrophilic or water-miscible vehicles, the vehicles having a melting point between 30.degree. C. and the melting point of tacrolimus, (b) mechanically working the product from step (a) to form agglomerated particles having a geometric weight mean diameter d.sub.gw of from 100 to 1000 .mu.m, and (c) compressing the agglomerated particles, wherein the tacrolimus is present in the composition at a concentration of between about 0.01 w/w % and about 15 w/w %.

22. The solid pharmaceutical composition of claim 21, wherein the hydrophilic or water-miscible vehicles have a melting point between 40.degree. C. and the melting point of tacrolimus.

23. The solid pharmaceutical composition of claim 21, wherein the hydrophilic or water-miscible vehicles have a melting point between 50.degree. C. and the melting point of tacrolimus.

24. The solid pharmaceutical composition of claim 21, wherein one hydrophilic or water-miscible vehicle is a poloxamer.

25. The solid pharmaceutical composition of claim 24, wherein the poloxamer is poloxamer 188.

26. The solid pharmaceutical composition of claim 21, wherein one hydrophilic or water-miscible vehicle is polyethylene glycol.

27. The solid pharmaceutical composition of claim 26, wherein the polyethylene glycol has an average molecular weight of at least 1500.

28. The solid pharmaceutical composition of claim 21, wherein the composition further comprises a release-modifying agent.

29. The solid pharmaceutical composition of claim 28, wherein the composition provides a W.sub.50 (the time where the plasma concentration is 50% or more of C.sub.max) of at least 12 hours.

30. The solid pharmaceutical composition of claim 29, wherein the composition provides a W.sub.50 (the time where the plasma concentration is 50% or more of C.sub.max) of at least 14 hours.

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