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Claims for Patent: 8,617,599

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Claims for Patent: 8,617,599

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:13/167,095
Patent Claims: 1. An oral 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 900mL aqueous dissolution medium with 0.005% hydroxypropylcellulose which has been adjusted to pH 4.5.

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

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

16. An oral extended release pharmaceutical composition comprising (a) a therapeutically 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 900mL aqueous dissolution medium with 0.005% hydroxypropylcellulose which has been adjusted to pH 4.5.

17. The oral extended release pharmaceutical composition of claim 16, wherein at most 60% w/w of the tacrolimus in the composition is released within 15 hours.

18. An oral extended release pharmaceutical composition comprising (a) a therapeutically effective amount of tacrolimus dispersed or dissolved in a vehicle, (b) one or more modifying release agents, and (c) 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 Paddle method at a rotation speed of 50 rpm in a 900mL aqueous dissolution medium with 0.005% hydroxypropylcellulose which has been adjusted to pH 4.5.

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