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

Qing-Hua Zhang; Jin Yang; Ying He; Fang Liu; Ji-Ping Wang; K Davey Andrew

doi:10.1055/s-0031-1296339

Arzneimittelforschung, Table of Contents

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

¹Center of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing, (P. R. China)

,

Jin Yang

¹Center of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing, (P. R. China)

,

Ying He

¹Center of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing, (P. R. China)

,

Fang Liu

²Jiangsu Province Hospital of TCM, Nanjing, (P. R. China)

,

Ji-Ping Wang

³Sansom Institute, School of Pharmacy and Medical Sciences, University of South Australia, Adelaide, SA, (Australia)

,

K Davey Andrew

¹Center of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing, (P. R. China)

› Author Affiliations

Abstract

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 C_max of 63%, a decrease in AUC_0–t of 22%, and a delay in T_max 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.

Key words

Antiviral agents - CAS 142217-69-4 - Entecavir, dispersible tablets, food effects, pharmacokinetics

Full Text

References

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