title: 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.
authors.affiliation: Department of Clinical and Bioequivalence Research, Cipla Ltd., Mumbai, India. siddharth.chachad@cipla.com
authors.forename: Siddarth
authors.initials: S
authors.lastname: Chachad
authors.forename: Amar
authors.initials: A
authors.lastname: Lulla
authors.forename: Geena
authors.initials: G
authors.lastname: Malhotra
authors.forename: Shrinivas
authors.initials: S
authors.lastname: Purandare
mesh_terms: D000328:Adult; D019380:Anti-HIV Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D019540:Area Under Curve; D002626:Chemistry, Pharmaceutical; D018592:Cross-Over Studies; D004311:Double-Blind Method; D005260:Female; D006801:Humans; D061466:Lopinavir; D008297:Male; D011744:Pyrimidinones / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D011786:Quality Control; D019438:Ritonavir / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D013607:Tablets; D013810:Therapeutic Equivalency
chemical_list: D019380:Anti-HIV Agents; D011744:Pyrimidinones; D013607:Tablets; D061466:Lopinavir; D019438:Ritonavir