Pharmacokinetic and Bioequivalence Study of Lisinopril/Hydrochlorothiazide Tablet Under Fasting and Postprandial Conditions in Healthy Chinese Subjects

Abstract

AbstractThe objective of this research was to evaluate and compare the pharmacokinetic profiles and safety of lisinopril/hydrochlorothiazide (10 mg/12.5 mg) tablets in the test and reference formulations administered to participants in both fasting and postprandial states and to evaluate the bioequivalence of the 2 products in healthy Chinese volunteers. This study employed a single‐center, randomized, open‐label, single‐dose dosing trial involving a cumulative 96 healthy adult participants (60 in the fasting group and 36 in the postprandial group). Each group comprised 2 sequence sets, and a 2‐week washout period was implemented. There were no statistically significant differences in time to maximum concentration and terminal elimination half‐life between the test and control groups under fasting and postprandial conditions (P > .05), and the 90% CIs for area under the plasma concentration–time curve and maximum plasma concentration were within the bioequivalence range of 80%‐125%. Pharmacokinetic results indicate a large food effect for lisinopril, meaning that there is a loss of approximately 20%‐25% of systemic exposure from fasting to postprandial administration for both preparations. The study demonstrated that a single oral dose of generic lisinopril/hydrochlorothiazide is bioequivalent to the reference product and well tolerated, with no significant adverse events observed, and that both products are similarly safe in a cohort of healthy Chinese male and female participants, following administration under fasting and postprandial conditions.