Food effect on the pharmacokinetics of entecavir from dispersible tablets following oral administration in healthy Chinese volunteers

Abstract

The aim of the present study was to assess the effect of food on the pharmacokinetics of entecavir (CAS 142217-69-4) from dispersible tablets. Methods: In an open-label, two-way crossover study, 12 healthy Chinese volunteers randomly received a single oral dose of 1 mg entecavir dispersible tablets under fasted and fed conditions. Blood samples were collected and determined for pharmacokinetic analyses. A solid phase extraction for sample preparation and a LC/MS method were developed and validated for determination of entecavir in human plasma. Results: The absorption of entecavir from dispersible tablets was altered significantly with food intake, as evidenced by a decrease in Cmax of 63 %, a decrease in AUC0―t of 22 %, and a delay in Tmax of 1.5 h. The calibration curve was linear from 0.2 to 25 ng/mL, with a lower limit of quantitation (LLOQ) of 0.2 ng/mL. Conclusion: Food intake has an obvious effect on the absorption of entecavir from dispersible tablets. It is better to take entecavir dispersible tablets on an empty stomach.