A Bioequivalence Trial of Dienogest in Healthy Chinese Participants Under Fed Conditions.

Abstract

This trial was a randomized, open-label, single-dose, 2-treatment, 2-period, crossover study to evaluate the pharmacokinetic (PK) profile, bioequivalence, and safety of test formulation and reference formulation of 2-mg dienogest tablets in healthy Chinese participants. Eligible participants were randomly administered a single 2-mg dose of either the test formulation or the reference formulation orally under fed conditions, followed by a 1-week washout period and the administration of the other formulation. Samples of blood were collected until 48hours following administration. The main PK parameters were calculated using noncompartmental analysis techniques. The main PK parameters included maximum plasma concentration, area under the plasma concentration-time curve (AUC) from time zero to the last quantifiable concentration, and AUC from time zero to infinity. The bioequivalence of test and reference dienogest tablets was determined if the 90% confidence intervals of the geometric mean ratio of the test to reference formulations were within the predefined range of 80%-125%. The safety assessment included incidence of adverse events and serious adverse events and others. Twenty-four healthy Chinese participants were enrolled in this trial. The geometric mean ratios of maximum plasma concentration, AUC from time zero to the last quantifiable concentration, and AUC from time zero to infinity between the 2 formulations, and corresponding 90% confidence intervals, all fell within the range of 80%-125% under fed conditions. The test and reference dienogest tablets were well tolerated, and no severe adverse events were reported in the trial. It was shown that the test and the reference dienogest tablets were bioequivalent and well tolerated under fed conditions in healthy Chinese female participants.