AUTHOR=Li Yinjuan , Qi Lu , Bai Haihong , Liu Ying , Fan Rongxia , Tu Yongrui , Sun Yongqiang , Wang Juxiang , Qi Qi , Feng Xiaohui , Zhou Da , Wang Xinghe 

TITLE=Pharmacokinetics and Bioequivalence of Rasagiline Tablets in Chinese Healthy Subjects Under Fasting and Fed Conditions: An Open, Randomized, Single-Dose, Double-Cycle, Two-Sequence, Crossover Trial

JOURNAL=Frontiers in Pharmacology

VOLUME=11

YEAR=2020

URL=https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2020.571747

DOI=10.3389/fphar.2020.571747

ISSN=1663-9812

ABSTRACT=<p><bold>Objective:</bold> This study evaluated the pharmacokinetics, safety, and bioequivalence (BE) of two formulations of rasagiline tablets in healthy Chinese subjects under fasting and fed conditions.</p><p><bold>Methods:</bold> An open, randomized, single-dose, double-cycle, two-sequence, self-crossover pharmacokinetic study in healthy Chinese subjects under fasting and high-fat postprandial conditions was performed. A total of 108 healthy subjects (36 in the fasting group and 72 in the postprandial group) were recruited. In each cycle of the study under both conditions, subjects received a single oral dose of 1 mg of a test or reference preparation of rasagiline tablets (1 mg each). A washout period of 3 days was observed. Blood samples were obtained up to 10 h post-intake. Primary endpoints were the BE of major pharmacokinetic parameters (AUC<sub>0–t</sub> and AUC<sub>0–∞</sub>) and the maximum observed serum concentration (C<sub>max</sub>). Secondary endpoints were safety parameters.</p><p><bold>Results:</bold> The 90% confidence interval (CI) of the geometric mean ratio (GMR) of the test drug vs. the reference drug for rasagiline was 94.16–105.35% for the AUC<sub>0–t</sub> under fasting conditions and 99.88–107.07% under postprandial conditions. The 90% CIs for the AUC<sub>0–∞</sub> were 93.55–105.01% and 99.59–107.05% under fasting and postprandial conditions, respectively. The 90% CIs for the C<sub>max</sub> were 88.26–108.46% and 89.54–118.23% under fasting and postprandial conditions, respectively. The 90% CIs for the test/reference AUC ratio and C<sub>max</sub> ratio were within the acceptable range (0.80–1.25) for BE. In this BE study, there were no serious adverse events (AEs).</p><p><bold>Conclusion:</bold> BE between the test and the reference products was established in both fasting and postprandial conditions. The two formulations of rasagiline showed good tolerability and a similar safety profile.</p><p><bold>Clinical Trial Registration:</bold><ext-link ext-link-type="uri" xlink:href="http://chinaDrugtrials.org.cn" xmlns:xlink="http://www.w3.org/1999/xlink">chinaDrugtrials.org.cn</ext-link>, identifier CTR20181466.</p>