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


CONCLUSIONS
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.
Center of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing, P. R. China.
Qing-Hua
QH
Zhang
Jin
J
Yang
Ying
Y
He
Fang
F
Liu
Ji-Ping
JP
Wang
Andrew K
AK
Davey
D000284:Administration, Oral; D000328:Adult; D000998:Antiviral Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001682:Biological Availability; D002138:Calibration; D002851:Chromatography, High Pressure Liquid; D018592:Cross-Over Studies; D005215:Fasting / Q000378:metabolism; D005260:Female; D018565:Food-Drug Interactions; D015774:Ganciclovir / Q000493:pharmacokinetics; D006147:Guanine / Q000008:administration & dosage / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D006801:Humans; D008297:Male; D013058:Mass Spectrometry; D015203:Reproducibility of Results; D013607:Tablets; D055815:Young Adult
D000998:Antiviral Agents; D013607:Tablets; C413685:entecavir; D006147:Guanine; D015774:Ganciclovir