The Bioequivalence of Rasagiline Tablets in Chinese Healthy Subjects
Under Fasting and Fed Conditions
Objective This study aims to evaluate the bioequivalence of 2
formulations of rasagiline tablet (1mg) in Chinese healthy subjects.
Methods 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 of the two study periods under both
conditions, subjects received a single oral dose of 1 mg test or a
reference rasagiline (1 mg each). There was a 3-day washout period.
Blood samples were obtained up to 10 hours post-intake. Several
pharmacokinetic parameters were estimated based on the concentrations of
rasagiline measured in plasma by means of LC-MS/MS. Results The
geometric mean ratio (90% CI) of the test drug versus reference drug
for rasagiline was 94.16% to 105.35% for AUC0-t under fasting
conditions and 99.88% to 107.07% under postprandial conditions. The
AUC0-∞s were 93.55% to 105.01% and 99.59% to 107.05% under fasting
and postprandial conditions, respectively. The Cmax values were 88.26%
to 108.46% and 89.54% to 118.23% under two conditions, respectively.
The 90% CIs for test/reference AUC ratio and Cmax ratio were within the
acceptable range (0.80–1.25) for BE. There were no serious adverse
events (AEs) encountered during this BE study. Conclusion Bioequivalence
between the test and the reference products was established in both
fasting and postprandial conditions. The two types of rasagiline showed
good tolerability and a similar safety profile.