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Claims for Patent: 8,586,084

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Claims for Patent: 8,586,084

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:13/167,281
Patent Claims: 1. A method for suppressing a rejection reaction by transplantation of an organ in a patient, the method comprising orally administering to the patient an extended release pharmaceutical composition comprising a therapeutically effective amount of tacrolimus and one or more modifying release agents, 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.

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

3. The method of claim 1, wherein the transplanted organ is a liver.

4. The method of claim 1, wherein at most 60% w/w of the tacrolimus in the pharmaceutical composition is released within 15 hours, when subjected to the in vitro dissolution test.

5. The method of claim 1, wherein at most 50% w/w of the tacrolimus in the pharmaceutical composition is released within 15 hours, when subjected to the in vitro dissolution test.

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

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

8. The method of claim 1, wherein the tacrolimus is dispersed or dissolved in a hydrophilic or water-miscible vehicle.

9. The method of claim 8, wherein the vehicle comprises poloxamer.

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

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

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

13. The method of claim 1, wherein the modifying release agent is a cellulose derivative 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 an extended release pharmaceutical composition comprising (a) a therapeutically effective amount of effective amount of tacrolimus dispersed or dissolved in a vehicle, and (b) one or more modifying release agents, 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 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, which delays release of the tacrolimus to the distal part of the duodenum thereby reducing tacrolimus induced gastrointestinal side effects and metabolism of tacrolimus by CYP3A4.

17. The method of claim 16, wherein the composition further comprises a solid carrier, and the vehicle further comprises polyethylene glycol having a molecular weight of from about 1,000 to about 35,000.
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