Food effects on the human pharmacokinetics of rasagiline mesylate

To evaluate the effects of high-fat diet on the pharmacokinetic profile of rasagiline in healthy Chinese volunteers，an open-label,randomized,crossover study was conducted.12 Healthy Chinese volunteers were given a single oral dose of 1 mg rasagiline mesylate tablets after an over-night fast or after a high-fat breakfast.The rasagiline concentrations in plasma and urine were determined by validated LC-MS/MS methods.The pharmacokinetic parameters were estimated by DAS 2.1 software.The calibration curves of rasagiline in both plasma and urine were linear over the range of 0.006 4 to 12.8 ng/mL.The main pharmacokinetic parameters of rasagiline under fast and high fat postprandial were as follows:c_max （3.93±1.55） and （1.58±0.75）ng/mL;t_max (0.5±0.2) and (0.9±0.8) h;t_1/2 (1.08±0.78) and (1.51±0.63) h;AUC_{0-8 h} (2.81±0.92) and (2.43±0.77) ng ·h/mL,respectively,with the urine excretion of the unchanged form within 24 h as (0.20±0.12)% and (0.20±0.09)% of the oral dose of rasagiline.The results showed that high fat postprandial has obvious effects on the absorption rate of rasagiline,but no effect on the absorption amount and cumulative excretion.