Bioequivalence Study of Two Fixed Dose Combination Tablet Formulations of Lopinavir and Ritonavir in Healthy Volunteers

Abstract

The study was designed to compare the rate and extent of absorption of two fixed dose combination tablet formulations of lopinavir (CAS 192725-17-0) and ritonavir (CAS 155213-67-5). This bioequivalence study was conducted using a standard preparation as reference and a generic alternative as test in 72 adult healthy volunteers within 18-45 years of age who received a single dose of the test or reference product under fasting conditions. A washout period of 10 d was maintained between period I and period II dosing. After dosing, blood samples were collected from 0 h (pre-dose) to 72 h postdose administration. Lopinavir and ritonavir were quantified using a validated LC-MS/MS method. The data obtained for each subject was evaluated for primary pharmacokinetic variables C(max), AUC(0-72), and AUC(0-Inf) with respect to % ratio and 90% confidence interval for log-transformed data. The 90% confidence intervals (obtained by analysis of variance, ANOVA) were well within the bioequivalence acceptance range of 80% to 125%. Thus, it can be concluded that the evaluated formulations are bioequivalent in terms of rate and extent of absorption. The safety profiles of both the test and reference formulations were comparable.