Effects of Food on the Pharmacokinetics and Bioequivalence of Oseltamivir Phosphate for Suspension and TAMIFLU® in Healthy Chinese Subjects：A randomized, open-label Clinical Trial.

Abstract

Abstract Purpose Oseltamivir is mainly used for the treatment and prevention of influenza. The study was aimed at evaluating the bioequivalence and safety of oseltamivir phosphate suspension (Oselavir®), provided by Shenzhen Beimei Pharmaceutical Co.Ltd. and manufactured by Hetero Labs Limited, and the reference product TAMIFLU®in healthy Chinese subjects. Methods A single-dose, randomized, open-label, two-phase, two-sequence, self-crossed model was adopted. Among 80 healthy subjects, 40 were maintain an empty stomach before took medication while the other 40 had the opposite. Subjects were randomized into the above two groups according to the proportion of 1:1, administered 75 mg/12.5 mL Oselavir® or TAMIFLU®, and cross-administered after 7 days. Results The Tmaxof two oseltamivir products in the fasting group were 1.50 h and 1.25 h, and t1/2were 3.34 h and 3.67 h, respectively. The Tmax of two oseltamivir products in the fed group were both 1.25 h, and t1/2 were 6.18 h and 7.23 h, respectively. Geometrically adjusted mean ratios of the PK parameters (Cmax, AUC0-t, AUC0-∞) of Oselavir® along with TAMIFLU® under fasting and postprandial conditions were in the range of 80.00-125.00% at the 90% confidence interval. Among the subjects on medication, a total of 18 subjects reported 27 adverse events (AEs), all of which were treatment-emergent adverse events (TEAEs), six of these TEAEs were rated as grade 2 in severity and the rest were as grade 1. Conclusion Two Oseltamivir phosphate suspensions are safe and bioequivalent as food had no effect on the pharmacokinetics and bioequivalence in healthy subjects.