TITLE:
Pharmacokinetics and Bioequivalence of Two Rivaroxaban Oral Formulations: A Randomized, Four-Period Crossover Study under Fasting and Fed Conditions
AUTHORS:
Evelyn Pena, Juan Chirinos, Alvaro Ortuño
KEYWORDS:
Pharmacokinetic, Rivaroxaban, Bioequivalence, Anticoagulant
JOURNAL NAME:
Journal of Biosciences and Medicines,
Vol.14 No.6,
June
26,
2026
ABSTRACT: Objective: This study aimed to compare the rate and extent of absorption of two oral rivaroxaban 20 mg formulations: Asarap? (Laboratorios Leti S.A.V.) as the test (T) and Xarelto? (Bayer A.G.) as the reference (R), in a randomized, single-dose, four-period, two-sequence crossover design. Methods: Healthy subjects received a single oral dose of T or R under fasting (n = 36) and fed (n = 40) conditions. A 5-day washout was applied between periods, for a total study duration of 19 days. Blood samples were collected pre-dose and up to 48 hours post-dose. Plasma rivaroxaban concentrations were determined using a validated LC-MS/MS method. Primary pharmacokinetic parameters included Cmax, AUC0–t, and AUC0–inf. Statistical analyses were performed using SAS? version 9.4. Results: Under fasting conditions, Geometric Mean Ratios (GMRs) (90% CI) were: Cmax 107.70% (99.85 - 116.17), AUC0–t 109.35% (102.52 - 116.63), and AUC0–inf 108.85% (102.48 - 115.60). Under fed conditions, GMRs were: Cmax 102.19% (97.87 - 106.70), AUC0–t 98.69% (95.37 - 102.13), and AUC0–inf 98.87% (95.67 - 102.18). All parameters met the predefined bioequivalence range (80% - 125%). No adverse events were reported. Conclusion: The test and reference formulations were bioequivalent under both fasting and fed conditions.