tacrolimus oral sustained release solid pharmaceutical composition in the form of a solid dispersion, dosage form and use of the pharmaceutical composition

摘要

"solid pharmaceutical composition, dosage form, use of the pharmaceutical composition, and method for preparing the composition". A modified release composition comprising tacrolimus releases less than 20 wt% active ingredient in 0.5 h 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 effective reduction 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 solid solution of tacrolimus in a hydrophilic or water miscible carrier and one or more release modifying agents; and / or may comprise a solid dispersion or solid solution of tacrolimus in an amphiphilic or hydrophobic vehicle and optionally one or more release modifying agents.