Study on Bioequivalence of Acetylcysteine Granules in Chinese Healthy Volunteers / 医药导报

ABSTRACT

Objective To establish an analytical method for assessing acetylcysteine in human plasma and study the relative bioavailability and bioequivalence of acetylcysteine granules in Chinese healthy volunteers. Methods In the randomized crossover study, 24 healthy male volunteers received a single oral dose of 0. 6 g test acetylcysteine granules, reference acetylcysteine granules or no medication. The plasma concentration of acetylcysteine was determined by LC-MS/MS. Pharmacokinetic parameters were calculated and bioequivalence of two preparations were evaluated by DAS3. 0 software. Results The main pharmacokinetic parameters of the test and reference preparations were as followsAUC0→t was (8 547. 64± 2 860.04) and (8 783.07±4 042. 10) μg·h·L-1, respectively; AUC0→∞ was (9 481. 64±3 444. 76) and (9 540. 51± 4 239. 30) μg·h·L-1, respectively;Cmax was (1 994. 39±726. 42) and (2 090. 27±885. 46) μg·L-1, respectively;tmax was (1.18±0. 60) and (1. 13±0. 53) h, respectively; t1/2 was (8. 60±3. 76) and (7. 75±5. 01) h, respectively. The relative bioavailability F0→t and F0→∞ was ( 107. 0 ± 43. 3 )% and ( 106. 5 ± 40. 1 )%, respectively. Conclusion The results of statistical analysis indicate that the test and reference formulations are bioequivalent.