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Claims for Patent: 8,664,239

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Claims for Patent: 8,664,239

Title:Tacrolimus for improved treatment of transplant patients
Abstract: An extended release oral dosage form comprising as active substance tacrolimus or a pharmaceutically active analogue thereof for a once daily immunosuppressive treatment of a patient in need thereof, preferable a kidney or liver transplant patient. The dosage form releases the active substance over an extended period of time. It also provides improved pharmacokinetic parameters due to an extended and constant in vivo release including substantial decreased peak concentrations, despite increased bioavailability, substantial extended times for maximal concentration, and higher minimal concentrations when compared with conventional immediate release dosage forms and a recent modified release tacrolimus dosage form.
Inventor(s): Gordon; Robert D. (Sandy Springs, GA), Holm; Per (Vanlose, DK), Lademann; Anne-Marie (Klampenborg, DK), Norling; Tomas (Lyngby, DK)
Assignee: Veloxis Pharmaceuticals A/S (Horsholm, DK)
Application Number:13/167,420
Patent Claims: 1. A method of suppressing kidney rejection in a kidney transplant patient comprising orally administering once daily in the evening to the kidney transplant patient an extended release pharmaceutical composition comprising tacrolimus, wherein (i) the pharmaceutical composition provides a substantially zero order release profile, (ii) at least 8% of the tacrolimus in the composition is released at the 4 hour time point, (iii) at least 15% of the tacrolimus in the composition is released at the 8 hour time point, and (iv) less than 62% of the tacrolimus in the composition is released within 15 hours, when subjected to an in vitro dissolution test using the USP II Paddle method at a rotation speed of 50 ppm in a 900 mL aqueous dissolution medium at pH 4.5 with 0.005% hydroxypropylcellulose.

2. The method of claim 1, wherein the pharmaceutical composition releases (i) at most 20% of the tacrolimus in the composition within 4 hours, and (ii) at most 40% of the tacrolimus in the composition within 10 hours, when subjected to an in vitro dissolution test using the USP II Paddle method at a rotation speed of 50 ppm in a 900 mL aqueous dissolution medium at pH 4.5 with 0.005% hydroxypropylcellulose.

3. The method of claim 1, wherein the pharmaceutical composition is administered once daily for at least 7 days.

4. The method of claim 1, wherein the pharmaceutical composition administered comprises from 0.1 to 15 mg of tacrolimus.

5. The method of claim 1, wherein the pharmaceutical composition administered comprises from 0.5 to 5 mg of tacrolimus.

6. The method of claim 1, wherein the pharmaceutical composition administered comprises 1 mg of tacrolimus.

7. The method of claim 1, wherein the pharmaceutical composition is orally administered without simultaneous food intake.

8. The method of claim 1, wherein the patient is a de novo kidney transplant patient.

9. The method of claim 1, wherein the tacrolimus in the pharmaceutical composition is present in a hydrophilic or water-miscible vehicle.

10. The method of claim 9, wherein the vehicle is selected from a polyethylene glycol, a polyoxyethylene oxide, poloxamer, polyoxyethylene stearate, poly-epsilon caprolactone, polyglycolized glycerides, polyvinylpyrrolidone, polyvinyl-polyvinylacetate copolymer, polyvinyl alcohol, polymethacrylic polymer hydroxypropyl methylcellulose, hydroxypropyl cellulose, methylcellulose, sodium carboxymethylcellulose, hydroxyethyl cellulose, a pectin, a cyclodextrin, galactomannan, alginate, carragenate, xanthan gum, and mixtures thereof.

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

12. The method of claim 9, wherein the vehicle comprises a mixture of polyethylene glycol and poloxamer.
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