Comparative Randomized, Single Dose, Two-Way Crossover, Open-Label Study to Determine the Bioequivalence of Irbesartan Formulation, Irbesartan GPO 150 mg Tablets and Aprovel® 150 mg Tablets, after Oral Administration to Healthy Thai Volunteers under Fasti

Abstract

Background: Irbesartan is a vasodilator indicated for the treatment of hypertension with high efficacy and rapid absorption. A generic product, Irbesartan GPO has been developed with lower price, to provide an alternative choice for physicians and patients to access the lower price medicines with the same quality and safety as in the originals.

Methods: A comparative randomized, single dose, two-way crossover, open-label study to determine the bioequivalence of Irbesartan GPO 150 mg tablets and Aprovel^® 150 mg tablets, after oral administration to healthy volunteers under fasting conditions, with 7 days washout period, was carried out. Blood samples were collected at predefined time points up to 72 hours. Plasma concentrations of irbesartan were analyzed using validated liquid chromatography tandem mass spectrometry
(LC-MS/MS). Non-compartmental model was used for pharmacokinetic analysis.

Results: The mean values ± SD of pharmacokinetic parameters (test vs. reference) of area under the plasma concentration versus time curve from time zero to the last measurable concentration (AUC_0-tlast), the area under the plasma concentration versus time curve from time zero to the time infinity (AUC_0-∞) and maximum plasma concentration (C_max) were 9507.632±2400.764 vs 9003.785±2136.219 ng.hr/mL, 9925.103±2378.850 vs 9469.099±2127.933 ng.hr/mL and 2373.466±585.390 vs 2373.054±584.536 ng/mL, respectively. The 90% Confidence Interval of AUC_0-tlast, AUC_0-∞ and C_max were within the bioequivalence range of 80.00 - 125.00. Both products were well tolerated and there were no significant adverse drug reactions (ADRs).

Conclusion: Irbesartan GPO and Aprovel^® were bioequivalent in terms of rate and extent of absorption.