OBJECTIVE: 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 Cm,, 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.
RCT Entities:
OBJECTIVE: 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 Cm,, 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.
Authors: Jianyuan Deng; Xiao Zhu; Zongmeng Chen; Chun Ho Fan; Him Shek Kwan; Chi Ho Wong; Ka Yi Shek; Zhong Zuo; Tai Ning Lam Journal: Drugs Date: 2017-11 Impact factor: 9.546