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Claims for Patent: 9,161,907

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Claims for Patent: 9,161,907

Title:Modified release compositions comprising tacrolimus
Abstract: A modified release composition comprising tacrolimus which is useful for the treatment or prevention of rejection reactions by transplantation of organs or tissues.
Inventor(s): Holm; Per (Vanlose, DK), Norling; Tomas (Lyngby, DK)
Assignee: VELOXIS PHARMACEUTICALS A/S (Horsholm, DK)
Application Number:14/079,443
Patent Claims: 1. An oral extended release pharmaceutical composition comprising tacrolimus, wherein the composition releases at most 62% of the tacrolimus in the composition within 15 hours when subjected to an in vitro dissolution test using USP Method A, delayed release articles (USP paddle method; rotation speed: 50 rpm; 37.degree. C.; after 2 hours in acidic medium, the medium is changed to phosphate buffer pH 6.8.).

2. The oral extended release pharmaceutical composition of claim 1, wherein at most 60% w/w of the tacrolimus in the composition is released within 15 hours.

3. The oral extended release pharmaceutical composition of claim 1, wherein at most 50% w/w of the tacrolimus in the composition is released within 15 hours.

4. The oral extended release pharmaceutical composition of claim 1, wherein the pharmaceutical composition provides an AUC.sub.fed/AUC.sub.fasted of at least 0.9.

5. The oral extended release pharmaceutical composition of claim 1, wherein the pharmaceutical composition provides pH independent release.

6. The oral extended release pharmaceutical composition of claim 1, wherein the tacrolimus is dispersed or dissolved in a hydrophilic or water-miscible vehicle.

7. The oral extended release pharmaceutical composition of claim 6, wherein the hydrophilic or water-miscible vehicle is selected from polyethylene glycol, polyoxyethylene oxide, poloxamer, polyoxyethylene stearate, poly-epsilon caprolactone, polyglycolized glyceride, and mixtures thereof.

8. The oral extended release pharmaceutical composition of claim 7, wherein the vehicle comprises poloxamer.

9. The oral extended release pharmaceutical composition of claim 7, wherein the vehicle comprises poloxamer and polyethylene glycol.

10. The oral extended release pharmaceutical composition of claim 9, wherein the polyethylene glycol and poloxamer are in a proportion by weight of between about 1:3 and about 10:1.

11. The oral extended release pharmaceutical composition of claim 1, further comprising a solid carrier.

12. The oral extended release pharmaceutical composition of claim 11, wherein the solid carrier is lactose.

13. The oral extended release pharmaceutical composition of claim 1, further comprising a modifying release agent.

14. The oral extended release pharmaceutical composition of claim 13, wherein the modifying release agent is selected from hydroxypropyl methylcellulose (HPMC), hydroxypropyl cellulose (HPC), methylcellulose, sodium carboxymethylcellulose, hydroxyethyl cellulose, poloxamers, polyoxyethylene stearates, poly-s-caprolactone, polyvinylpyrrolidone (PVP), polyvinylpyrrolidone-polyvinylacetate copolymer PVP-PVA, polymethacrylic polymers, polyvinyl alcohol (PVA), poly (ethylene oxide) (PED), and mixtures thereof.

15. The oral extended release pharmaceutical composition of claim 1, wherein the composition comprises tacrolimus-containing particles.

16. The oral extended release pharmaceutical composition of claim 1, in the form of a compressed tablet.

17. An oral extended release pharmaceutical composition comprising tacrolimus dispersed or dissolved in a vehicle, wherein (i) the vehicle comprises a poloxamer, and (ii) the composition releases at most 62% of the tacrolimus in the composition within 15 hours when subjected to an in vitro dissolution test using USP Method A, delayed release articles (USP paddle method; rotation speed: 50 rpm; 37.degree. C.; after 2 hours in acidic medium, the medium is changed to phosphate buffer pH 6.8.).

18. The oral extended release pharmaceutical composition of claim 17, wherein at most 60% w/w of the tacrolimus in the composition is released within 15 hours.

19. An oral extended release pharmaceutical composition comprising (a) tacrolimus dispersed or dissolved in a vehicle, and (b) a solid carrier, wherein (i) the vehicle comprises polyethylene glycol having a molecular weight of from about 1,000 to about 35,000 and a poloxamer, and (ii) the composition releases at most 62% of the tacrolimus in the composition within 15 hours when subjected to an in vitro dissolution test using USP Method A, delayed release articles (USP paddle method; rotation speed: 50 rpm; 37.degree. C.; after 2 hours in acidic medium, the medium is changed to phosphate buffer pH 6.8.).

20. The oral extended release pharmaceutical composition of claim 19, wherein at most 60% w/w of the tacrolimus in the composition is released within 15 hours.

21. A method for suppressing a rejection reaction by transplantation of an organ in a patient, the method comprising orally administering once daily to the patient an extended release pharmaceutical composition of claim 1.

22. The method of claim 1, wherein the transplanted organ is a kidney.

23. The method of claim 22, wherein at most 60% w/w of the tacrolimus in the composition is released within 15 hours.

24. The method of claim 22, wherein at most 50% w/w of the tacrolimus in the composition is released within 15 hours.
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