Bioequivalence study of abacavir 300 mg tablets in healthy Thai male volunteers under fasting conditions

Abstract

© 2014 Faculty of Pharmaceutical Sciences, Chulalongkorn University. All rights reserved. Abacavir is an antiretroviral drug that can be prescribed in single dose or in fixed-dose combination formulations to make adherence easier. Due to this advantage, a generic product of abacavir of GPO has been developed with lower price and would be benefit for HIV patients. A comparative randomized, single dose, two-way crossover, open-label bioequivalence study of the generic abacavir, Abacavir GPO 300 mg tablets, and the reference, Ziagenavir™ 300 mg tablets, after oral administration to 50 healthy, Thai volunteers under fasting conditions with 7 days washout period was carried out. Blood samples wer e collected at predefined time points up to 12 hours. Plasma concentrations of abacavir were analyzed using a validated liquid chromatography tandem mass spectrometry. Non-compartmental model was used for ph armacokinetic analysis. The mean values (± SD) of pharmacokinetic parameters (test vs. reference) were AUC0 -tlast (7114.645 ± 1701.7843 vs 6878.453 ± 1553.6328 ng.hr/mL), AUC0-8 (7161.443 ± 1713.3557 vs 6923.175 ± 15 66.9145 ng.hr/mL) and Cmax (3238.786 ± 1075.6341 vs 3181.232 ± 1072.4422 ng/mL). The 90 % confidence intervals for the ratios of mean AUC0-tlast, AUC0-8 and Cmax for the test/reference were 103.1 (100.83-105.51), 103.2 (100.84 -105.53) and 101.3 (94.05-109.03), respectively. These values were within the acceptable range of 80.00-125.00. Both the formulations were well tolerated. No clinically significant or serious ADRs were observed. By conclusion, two formulations of abacavir, Abacavir GPO and Ziagenavir‒, were bioequivalent and can be used interchangeably