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Claims for Patent: 8,623,411

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Claims for Patent: 8,623,411

Title:Modified release compositions comprising tacrolimus
Abstract: A modified release composition comprising tacrolimus releases less than 20% w/w of the active ingredient within 0.5 hours when subjected to an in vitro dissolution test using USP Paddle method and using 0.1 N HCl as dissolution medium and has increased bioavailability by effectively reducing or even avoiding the effects of CYP3A4 metabolism. The modified composition may be coated with an enteric coating; and/or may comprise a solid dispersion or a solid solution of tacrolimus in a hydrophilic or water-miscible vehicle and one or more modifying release agents; and/or may comprise a solid dispersion or a solid solution of tacrolimus in an amphiphilic or hydrophobic vehicle and optionally one or more modifying release agents.
Inventor(s): Holm; Per (Vanlose, DK), Norling; Tomas (Lyngby, DK)
Assignee: Veloxis Pharmaceuticals A/S (Horsholm, DK)
Application Number:13/167,334
Patent Claims: 1. A method for suppressing a rejection reaction by transplantation of an organ in a patient, the method comprising orally administering a therapeutically effective amount of one or more solid extended release pharmaceutical compositions, each solid extended release pharmaceutical composition comprising (i) tacrolimus dispersed or dissolved in a vehicle and (ii) one or more modifying release agents, wherein the pharmaceutical 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 in the patient.

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

3. The method of claim 1, wherein the pharmaceutical composition provides an AUC.sub.fed/AUC.sub.fasted of at least 0.9.

4. The method of claim 1, wherein the pharmaceutical composition provides pH independent release.

5. The method of claim 1, 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 Paddle method at a rotation speed of 50 rpm in a 900 mL aqueous dissolution medium with 0.005% hydroxypropylcellulose which has been adjusted to pH 4.5.

6. The method of claim 5, wherein at most 60% w/w of the tacrolimus in the composition is released within 15 hours, when subjected to the in vitro dissolution test.

7. The method of claim 5, wherein at most 50% w/w of the tacrolimus in the composition is released within 15 hours, when subjected to the in vitro dissolution test.

8. The method of claim 1, wherein the vehicle comprises polyethylene glycol and poloxamer.

9. The solid method of claim 8, wherein the polyethylene glycol and poloxamer are in a proportion by weight of between about 1:3 and about 10:1.

10. The method of claim 1, wherein the composition further comprises a solid carrier.

11. The method of claim 10, wherein the solid carrier is lactose.

12. The method of claim 1, wherein the composition further comprises a modifying release agent.

13. The method of claim 12, 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.

14. The method of claim 1, wherein the composition comprises tacrolimus-containing particles.

15. The method of claim 1, wherein the composition is in the form of a compressed tablet.

16. A method for suppressing a rejection reaction by transplantation of an organ in a patient, the method comprising orally administering to the patient a therapeutically effective amount of one or more extended release pharmaceutical compositions, each extended release pharmaceutical composition comprising tacrolimus particles, wherein (a) the particles contain (i) tacrolimus dispersed or dissolved in a vehicle and (ii) one or more modifying release agents, (b) the particles have a d.sub.gw of from about 100 to about 700 .mu.m, and (c) the pharmaceutical 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.

17. The method of claim 16, wherein the pharmaceutical composition provides an AUC.sub.fed/AUC.sub.fasted of at least 0.9.

18. The method of claim 16, wherein the pharmaceutical composition provides pH independent release.

19. The method of claim 16, 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 Paddle method at a rotation speed of 50 rpm in a 900 mL aqueous dissolution medium with 0.005% hydroxypropylcellulose which has been adjusted to pH 4.5.

20. The method 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 to the patient a therapeutically effective amount of one or more extended release pharmaceutical compositions, each solid extended release pharmaceutical composition comprising (i) tacrolimus particles, wherein the particles contain tacrolimus dispersed or dissolved in a vehicle and (ii) one or more modifying release agents, wherein the pharmaceutical composition provides pH independent release, and a W.sub.50 (the time where the plasma concentration is 50% or more of C.sub.max) of at least 14 hours in the patient, the pharmaceutical composition is free of organic solvent, and the tacrolimus particles have a d.sub.gw of from about 100 to about 700 .mu.m.

22. The method of claim 21, wherein the pharmaceutical composition provides an AUC.sub.fed/AUC.sub.fasted of at least 0.9.

23. The method of claim 21, 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 Paddle method at a rotation speed of 50 rpm in a 900 mL aqueous dissolution medium with 0.005% hydroxypropylcellulose which has been adjusted to pH 4.5.
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