Bioequivalence Study of Atenolol Tablets in Healthy Chinese Subjects Under Fasting and Fed Conditions

Abstract

AbstractAtenolol, a cardioselective β1‐blocker, exhibits efficacy in treating cardiovascular diseases. We conducted a single‐center, randomized, open, single‐dose, 2‐preparation, 2‐cycle, 2‐sequence, double‐crossover trial with a 7‐day washout period to investigate the pharmacokinetics, bioequivalence (BE), and safety of test and reference atenolol tablets (25 mg) in healthy Chinese volunteers. Forty‐eight healthy participants were randomized into the fasting and fed arms. After administering a single oral dose of the test or reference formulation (25 mg), plasma atenolol concentrations were measured using liquid chromatography‐tandem mass spectrometry. Pharmacokinetic parameters were obtained from concentration‐time profiles. In total, 23 and 24 individuals were included in the fasting and fed arms, respectively. The mean concentration‐time profiles for both formulations were similar, and Cmax, AUC0‐t, and AUC0‐∞ were within the BE range of 80%‐125%. Thirteen adverse events (AEs) were observed in 7 participants in the fasting arm; 1 withdrew from the trial early owing to an AE. In the fed arm, 20 AEs were observed in 8 participants, and none withdrew from the trial. All adverse reactions were grade I, with no serious AEs or deaths. Therefore, the 2 tablets are bioequivalent in healthy Chinese individuals under fasting and fed conditions, supporting their further clinical development.