Pharmacokinetics, bioequivalence, and food effect assessment of enteric-coated aspirin tablets: a randomized, single-dose, four-period crossover study in Chinese healthy subjects.

This study assessed the pharmacokinetics, bioequivalence, and food effect of two enteric-coated aspirin tablets (100 mg) in healthy Chinese subjects. Ninety subjects were enrolled and divided into fasted (n = 42) and fed cohorts (n = 48) in a single-center, randomized, open-label, single-dose, four-period, two-sequence and crossover study. The pharmacokinetic characteristics of acetylsalicylic acid (aspirin) and its metabolite salicylic acid, including C and AUC, were compared after subjects received single oral doses of enteric-coated aspirin tablet using a validated LC-MS/MS method. Bioequivalence was evaluated using the reference-scaled average bioequivalence (RSABE) approach when the within-subject standard deviation of the reference product (S) exceeded 0.29, while the average bioequivalence (ABE) method was applied for S values below 0.29. Pharmacokinetic profiles of two enteric-coated aspirin tablets were comparable after single-dose administration. The mean T, C, and AUC0-t were 5.5 h, 603.97 ng/mL and 786.47 h·ng/mL for acetylsalicylic acid, and 6.50 h, 4033.66 ng/mL, and 20,115.18 h·ng/mL for salicylic acid, respectively. Food delayed the T and increased the C but had no effect on the aspirin's overall exposure. 90% CI of geometric mean ratios (GMRs) of C, AUC, and AUC of acetylsalicylic acid and salicylic acid of two enteric-coated aspirin tablets fell within the predefined bioequivalence range of 80.0-125.0% under both fasted and fed conditions. Safety assessments revealed that all treatments were safe and well tolerated. Two enteric-coated aspirin tablets were bioequivalent in Chinese healthy subjects under both fasted and fed condition. All treatments were well tolerated.