Pharmacokinetics and Bioequivalence of Ilaprazole Enteric‐Coated Tablets in Healthy Chinese Volunteers: A Two‐Sequence, Four‐Period, Fully Replicated Crossover Study

Ilaprazole enteric-coated tablets are a novel proton pump inhibitor primarily used for the treatment of gastroesophageal reflux disease, with metabolism not affected by CYP2C19 genetic polymorphism. This study evaluated the pharmacokinetics and bioequivalence of two formulations of ilaprazole enteric-coated tablets in Chinese healthy volunteers under fasting and fed conditions using a single-center, randomized, open-label, single-dose, two-formulation, four-period, two-sequence, fully replicated crossover design. A total of 72 volunteers were enrolled, with 36 in each group. In the fasting group, volunteers received a single dose of 5 mg of the test or reference formulation in each period, while in the fed group, a high-fat meal was consumed 30 min before drug administration. Blood samples were collected within 36 h postdose, and plasma concentrations of ilaprazole were analyzed using ultra-performance liquid chromatography-tandem mass spectrometry. The geometric means and 90% confidence intervals of AUC_0-t, AUC_0-∞, and C_max for both fasting and fed conditions were within the 80%-125% bioequivalence range, and the upper limit of the one-sided 95% confidence interval was ≤0. Both formulations demonstrated bioequivalence under these conditions, with no serious adverse reactions observed.