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DOI: 10.1055/s-0031-1297964
Bioequivalence Evaluation of 2 Tablet Formulations of Entecavir in Healthy Chinese Volunteers: A Single-Dose, Randomized-Sequence, Open-Label Crossover Study
Publication History
received 08 November 2011
accepted 22 November 2011
Publication Date:
20 January 2012 (online)
![](https://www.thieme-connect.de/media/amf/201203/lookinside/thumbnails/10.1055-s-0031-1297964-1.jpg)
Abstract
A randomized, 2-way crossover study was conducted in healthy Chinese male volunteers to evaluate the bioequivalence of a new generic formulation of entecavir (CAS 142217-69-4) tablets (test) and the available branded formulation (reference) to meet the requirements for marketing the test product in China. Test and reference tablets were administered as a single dose on 2 treatment days separated by a 2-week washout period. Blood samples were collected for a period of 24 h following drug administration. Plasma concentration of entecavir was determined by a liquid chromatography-tandem mass spectrometry (LC/MS/MS) method. Pharmacokinetic parameters were calculated using a noncompartmental model. Bioequivalence was determined by calculating 90% CIs for the ratios of Cmax, AUC0–t and AUC0–∞ values for the test and reference products. Tolerability was assessed by monitoring vital signs, laboratory tests and interviews with the volunteers before administration and every 2 h during the study. The 90% CIs of entecavir for Cmax, AUC0–t and AUC0–∞ were 95.2–106.9%, 98.4–104.6% and 97.3–104.4%, respectively, which fell within the interval of 80–125%. No clinically important adverse effects were reported. These results suggested that the test formulation of entecavir tablets met the regulatory criterion for bioequivalence to the reference formulation.
Key words
bioequivalence - pharmacokinetics - entecavir - CAS 142217-69-4 - LC-MS/MS - healthy volunteers* Co-first authors
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