Modified release compositions comprising tacrolimus
AssigneeLifeCycle Pharma A/S
InventorsPer HOLM, Tomas Norling
Life of this patent
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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.
Claims23
1-53. (canceled)
A method for suppressing a rejection reaction by transplantation of an organ in a patient, the method comprising orally administering a solid extended release pharmaceutical composition comprising from about 0.5 to about 5% by weight of tacrolimus dispersed or dissolved in a vehicle comprising poloxamer, based upon 100% total weight of vehicle, wherein the pharmaceutical composition provides a W50 (the time where the plasma concentration is 50% or more of Cmax) of at least 14 hours in the patient.
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 tacrolimus particles, wherein (i) the particles contain from about 0.5 to about 5% by weight of tacrolimus dispersed or dissolved in a vehicle comprising poloxamer, based upon 100% total weight of vehicle, (ii) the particles have a dgw of from about 100 to about 700 μm, and (iii) the pharmaceutical composition provides a W50 (the time where the plasma concentration is 50% or more of Cmax) of at least 14 hours.
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 tacrolimus particles, wherein the particles contain from about 0.5 to about 5% by weight of tacrolimus dispersed or dissolved in a vehicle comprising poloxamer, based upon 100% total weight of vehicle, wherein
- the pharmaceutical composition provides pH independent release, a W50 (the time where the plasma concentration is 50% or more of Cmax) of at least 14 hours in the patient,
- the pharmaceutical composition is free of organic solvent, and
- the tacrolimus particles have a dgw of from about 100 to about 700 μm.
Dependencies are inferred from the claim text.