Pharmacokinetics, Bioequivalence, and Safety of Bromocriptine Mesylate Tablets in Healthy Chinese Subjects

Abstract To investigate the pharmacokinetic characteristics of bromocriptine mesylate tablets in healthy Chinese subjects and to assess their bioequivalence and safety. A randomized, open‐label, single‐dose, four‐period, two‐sequence, complete crossover study was conducted. Forty healthy volunteers were enrolled and administered a single oral dose of 2.5 mg of either the test formulation (T) or the reference formulation (R) of bromocriptine mesylate tablets under fed conditions, with a 7‐day washout period between treatments. Plasma concentrations of bromocriptine mesylate were measured using ultra‐performance liquid chromatography‐tandem mass spectrometry, and pharmacokinetic parameters were calculated using Phoenix WinNonlin software for bioequivalence evaluation. Geometric mean ratios of maximum concentration, the area under the concentration–time curve from time zero to the last measurable concentration, and the area under the concentration–time curve from time zero to infinity were calculated: maximum concentration by reference‐scaled average bioequivalence using a 95% upper confidence bound, and the area under the concentration‐time curve from time zero to the last measurable concentration and the area under the concentration‐time curve from time zero to infinity by average bioequivalence with 90% confidence intervals. Data from the fed trial met the bioequivalence criteria. No serious adverse reactions were observed, indicating that the test and reference bromocriptine mesylate tablets have similar safety profiles under fed conditions.