pharmacokinetics and bioequivalence of two formulations of apixaban tablets: a double-blind, single-dose, crossover study in healthy subjects

Background :the present study aimed to determine the pharmacokinetic parameters and bioequivalence of the test medicinal product, apixaban 5 mg tablet, and its reference product, eliquis®, in healthy male and female subjects under a fasted state. methods :before in vivo evaluation, the quality control parameters of the products were evaluated and compared. this study was a single-dose, double-blind, 2-sequence, crossover, 2-period, randomized bioequivalence and pharmacokinetic study in 24 healthy individuals with a two-week washout period between doses. a series of blood samples were obtained over 48 hours after dose administration, and the samples were analyzed for their apixaban content using a validated liquid chromatography-tandem mass spectrometry (lc-ms/ms) technique. the pharmacokinetic parameters were computed using non-compartmental analysis. results :both products passed the in vitro quality control criteria. following administration of the apixaban tablet, the area under curve (auc)0-t, auc0-∞, and maximum plasma concentration (cmax) mean values for the test product were 1284.0 ng.h/ml, 1368.2 ng.h/ml, and 157.4 ng/ml, respectively, and for the reference product were 1310.6 ng.h/ml, 1406.5 ng.h/ml, and 157.6 ng/ml, respectively. the 90% confidence intervals (ci) of the geometric mean ratio for auc0-t (91.4 - 105.9), auc0-∞ (92.9 - 106.9), and cmax (87.1 - 101.9) fell within the predefined accepted range of 80% - 125%. no serious adverse events were observed. conclusions :the test product (apixaban 5 mg tablet) and reference product (eliquis®) achieved regulatory requirements for bioequivalence in healthy individuals under a fasted state.