A Bioequivalence Study of Azilsartan in Healthy Chinese Subjects

Abstract

Azilsartan is an angiotensin II receptor blocker used for treating adult hypertension. It significantly improves cardiovascular outcomes in patients with high‐risk hypertension, heart failure, and diabetic nephropathy. A single‐center, randomized, open‐label, single‐dose, dual‐cycle, dual‐crossover clinical trial was conducted to evaluate the bioequivalence of azilsartan under fasting and postprandial conditions in 60 Chinese healthy volunteers. Thirty healthy subjects were enrolled in each test group, with random cross‐administration for fasting and postprandial tests. The concentration of azilsartan in human plasma was evaluated using liquid chromatography‐tandem mass spectrometry after a single oral administration of test and reference preparations, each at a dose of 20 mg (1 tablet). Pharmacokinetic parameters were determined using WinNonlin8.2 software, and bioequivalence was evaluated using SAS 9.4 software. The geometric mean ratios and 90% confidence intervals for maximum concentration, area under the plasma concentration‐time curve from time 0 to the time of last measurable concentration, and area under the plasma concentration‐time curve from time 0 to infinity of the test and reference preparations in the fasting and postprandial test groups were in the range of 80%‐125%. The incidence of adverse events in the fasting and postprandial test groups was 30% (9/30) and 33.3% (10/30), respectively. No serious adverse events or unexpected adverse drug reactions were observed. In conclusion, the test and reference preparations of azilsartan tablets demonstrate bioequivalence and good safety in healthy Chinese subjects under fasting and postprandial conditions.