EP2167033A1 — Once daily oral dosage form comprising tacrolimus

USPTO 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. The dosage form releases the active substance over an extended period of time defined by a release of at the most 63.5% of the content of the active substance at the 12 hours time point defined by in vitro dissolution and when tested according to the USP Il dissolution test (paddle) or USP I dissolution test (basket) form in a medium at pH 4.5 and comprising 0.005% hydroxypropylcellulose and a rotation of 50 rpm. The extended release dosage form 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 dosage form.