Plasma Pharmacokinetics of Idarubicin and its 13-Hydroxymetabolite after Intravenous and Oral Administration under Fasting and Non-Fasting Conditions

Abstract

The plasma pharmacokinetics of Idarubicin and its 13-hydroxymetabolite have been studied in 10 patients with solid tumours after intravenous and oral administration under fasting and non-fasting conditions in a randomized cross-over design. The plasma concentration time curves of Idarubicin after intravenous administration could be described by the open two or three compartment models. No pharmacokinetic modelling of Idarubicin was possible after oral administration. After oral administration of Idarubicin, the amount of intact drug was higher under non-fasting conditions. The extensive and long-lasting appearance of Idarubicinol suggests that this cytotoxic metabolite is of major clinical importance in i.v. and oral therapy with Idarubicin. The pharmacokinetics of Idarubicinol was not affected by food intake.