Comparative pharmacokinetics and bioequivalence of two imatinib formulations as film-coated tablets, 400 mg

Abstract

The comparative pharmacokinetics and bioequivalence of imatinib formulations, as Genfatinib®, 400-mg film-coated tablets (Tutor Laboratories S.A.S.I.F.I.A., Varifarma Laboratories, S. A., Argentina) (test formulation) and Gleevec®, 400-mg film-coated tablets (Novartis Pharma Stein AG, Switzerland) (reference formulation) were studied after single oral doses in 24 male healthy volunteers aged 18 – 55 (mean 29.5) years in a randomized, open, cross-over trial. Plasma imatinib was assayed by LC/MS with prior sample preparation by acetonitrile protein precipitation. The following pharmacokinetic parameters were evaluated: C max, T max, AUC 0-t, AUC inf, and C max/AUC 0-t . Bioequivalence was assessed in compliance with the methodological recommendations of the Ministry of Health and Social Development of the Russian Federation, “Assessment of the Bioequivalence of Medicines,” 2008. Assessment of the relative bioequivalence (80 < f˝ (109%) < 125 and 75 < f˝ (102%) < 133) and analysis of variance of AUC 0 – 72, C max, and C max/AUC 0 – 72 values indicated that the two formulations were bioequivalent.