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.

This study evaluated the pharmacokinetics, safety, and bioequivalence (BE) of two formulations of rasagiline tablets in healthy Chinese subjects under fasting and fed conditions. 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 and AUC) and the maximum observed serum concentration (C). Secondary endpoints were safety parameters. 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 under fasting conditions and 99.88-107.07% under postprandial conditions. The 90% CIs for the AUC were 93.55-105.01% and 99.59-107.05% under fasting and postprandial conditions, respectively. The 90% CIs for the C 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 ratio were within the acceptable range (0.80-1.25) for BE. In this BE study, there were no serious adverse events (AEs). 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. chinaDrugtrials.org.cn, identifier CTR20181466.