Pharmacokinetics, bioequivalence, and safety studies of gefitinib tablet formulations: A randomized, open-label, two-period, two-sequence crossover study in Chinese healthy volunteers

Abstract

A randomized, open-label, two-period, two-sequence crossover study was carried out for evaluating the bioequivalence of test (T) and reference (R) formulation of gefitinib in healthy Chinese volunteers. A total of eighty subjects were enrolled and randomized into two sequence groups. All subjects were orally administered of T or R formulation at a dose of 250 mg. The plasma samples were obtained at before and after administration until 168 h post-dose, and the drug concentrations were analyzed using validated high-performance liquid chromatography-tandem mass spectrometry method. The 90% confidence interval of the geometric mean ratios were all within the range of 0.80–1.25 under fasting and fed conditions. As for the safety of both formulations, no serious or unexpected adverse events occurred during the study. Overall, the T formulation was bioequivalent with R formulation under fasting and fed conditions.