Pharmacokinetics and bioequivalence of acetylcysteine granules among Chinese healthy volunteers under fasting and postprandial conditions.

Abstract

This study aimed to evaluate the pharmacokinetics, bioequivalence, and safety for two formulations of acetylcysteine granules in healthy Chinese subjects under fasting and postprandial conditions. A single-center, randomized, open-label, single-dose, two-period, two-sequence crossover study was performed. 34 and 38 healthy Chinese volunteers were enrolled in the fasting and postprandial groups, respectively. Each subject received a single oral dose (0.2 g) of acetylcysteine granules per period either as the test (T) or reference (R) formulation, followed by a 5-day washout interval. Serial blood samples were collected for up to 24 h post-dose in each period, and plasma concentration of acetylcysteine was detected using high performance liquid chromatography tandem mass spectrometry (HPLC-MS/MS). Whether under fasting or postprandial conditions, all the 90% confidence intervals (CIs) of the geometric mean ratios (GMRs) for maximum concentration (C_max), area under the curve from time 0 to the time of the last measurable concentration (AUC_{0- t}), and area under the curve from time 0 to infinity (AUC_0-∞) were all found to fall within the bioequivalence range of 80.00-125.00%. Only mild adverse events (AEs) were observed. In the study, the two formulations of acetylcysteine granules were bioequivalent and safe.