Arzneimittelforschung 2010; 60(10): 640-644
DOI: 10.1055/s-0031-1296339
Antibiotics · Antimycotics · Antiparasitics · Antiviral Drugs · Chemotherapeutics · Cytostatics
Editio Cantor Verlag Aulendorf (Germany)

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

Qing-Hua Zhang
1   Center of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing, (P. R. China)
Jin Yang
1   Center of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing, (P. R. China)
Ying He
1   Center of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing, (P. R. China)
Fang Liu
2   Jiangsu Province Hospital of TCM, Nanjing, (P. R. China)
Ji-Ping Wang
3   Sansom Institute, School of Pharmacy and Medical Sciences, University of South Australia, Adelaide, SA, (Australia)
K Davey Andrew
1   Center of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing, (P. R. China)
› Author Affiliations
Further Information

Publication History

Publication Date:
03 December 2011 (online)



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.


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.


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.


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.

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