Evaluation of the bioequivalence and pharmacokinetics of two lisinopril tablet formulations after single oral administration in healthy volunteers.
An open, two-period, randomized, crossover trial of two lisinopril (1-[N2-[(S)-1-carboxyl-3-phenylpropyl]-L-lysil]-L-proline, CAS 76547-98-3) formulations (Adicanil as test and another commercially available preparation as reference) was performed in 24 healthy volunteers. A single 20 mg oral dose of lisinopril was administrated and pharmacokinetic parameters were compared. Lisinopril plasma concentrations were measured by a fully validated LC-MS method. The parametric 90% confidence intervals of the geometric mean values of the test/reference ratios were 95.38% to 105.94% (point estimate: 100.52%) for AUC(0-last), 94.01% to 103.47% (point estimate: 98.63%) for AUC(0-infinity) and 92.34% to 103.97% (point estimate: 97.98%) for Cmax, being within the acceptance criteria for bioequivalence (80%-125%). T(1/2), k(el) and Tmax values were also tested and the difference was not statistically significant. Therefore, it is concluded that the test and the reference lisinopril formulations are bioequivalent both in the extent and the rate of absorption.
Georgarakis
Manolis
M
Laboratory of Pharmaceutics and Drug Control, Department of Pharmacy, Aristotle University of Thessaloniki, Thessaloniki, Greece. mgeorgara@hotmail.com
Tsakalof
Andreas
A
Zougrou
Fotini
F
Kontopoulos
Georgios
G
Tsiptsios
Iakovos
I
D000328:Adult; D000806:Angiotensin-Converting Enzyme Inhibitors / Q000008:administration & dosage / Q000493:pharmacokinetics*; D019540:Area Under Curve; D002851:Chromatography, High Pressure Liquid; D018592:Cross-Over Studies; D005260:Female; D006207:Half-Life; D006801:Humans; D017706:Lisinopril / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008297:Male; D013058:Mass Spectrometry; D013607:Tablets; D013810:Therapeutic Equivalency
D000806:Angiotensin-Converting Enzyme Inhibitors; D013607:Tablets; D017706:Lisinopril