PHARMACOKINETICS AND BIOEQUIVALENCE ASSESSMENT OF ORAL RIVAROXABAN TABLET IN IRANIAN HEALTHY VOLUNTEERS

Rivaroxaban is utilized as a direct factor Xa inhibitor for the prevention and remedy of thromboembolic disorders. This study aimed to evaluate a generic version of rivaroxaban 10 mg tablet. Considering previous reports of safety and tolerability of a single dose (1.25-80 mg) of rivaroxaban, this study used a randomized, single-dose two-way crossover of rivaroxaban in 28 healthy volunteers, with a washout period of seven days. Analyses of blood samples were performed by a validated ultra-high performance liquid chromatography coupled with tandem mass spectrometry. An YMC-Pack ODS-AQ reversed-phase column with the mobile phase of acetonitrile and 10 mM ammonium acetate pH = 3 (70: 30, v/v) at a flow rate of 0.3 mL.min(-1) under isocratic elution was selected for the analysis. A range of 2.5-600 ng.mL(-1) was obtained for the calibration curve. Pharmacokinetic parameters were calculated for the bioequivalence assessment. The results showed that two formulations have similar pharmacokinetics. The 90% confidence interval of the mean ratios of the test versus reference formulation of Ln transformed AUC(0-30) (82.0-98.0), AUC(0-inf) (81.3-105.2), and Cmax (82.4-104.4) were within the acceptable range of 80-125%.