Pharmacokinetics and Bioequivalence of 2 Safinamide Tablets in Healthy Chinese Volunteers Under Fasting and Fed Conditions.

Abstract

To assess the bioequivalence of a generic safinamide tablet (test) vs a brand-name safinamide tablet (reference) and effects of food on the pharmacokinetics of safinamide in healthy Chinese subjects, a single-center, single-dose, randomized, open-label, 2-preparation, 2-period study with a 15-day washout period was undertaken. A total of 56 healthy subjects were recruited in this study (fasting, n = 28; fed, n = 28). A single dose of a 100-mg test or reference safinamide tablet was administered to each subject in a randomized sequence. Blood samples were obtained at 5minutes before drug administration and during the 120hours after dosing. The safinamide concentration in plasma was determined by high-performance liquid chromatography-tandem mass spectrometry. Pharmacokinetic parameters were analyzed with noncompartmental methods. Safety was also monitored. The major pharmacokinetic parameters including maximum plasma drug concentration, area under plasma concentration-time curve (AUC) from zero to time t (AUC0-t ), and AUC from time 0 to infinity (AUC0-∞ ) were similar between the test and reference tablets under fasting and fed conditions. The 90% CIs of the test/reference ratios of log-transformed maximum plasma drug concentration, AUC from zero to time t, and AUC from time 0 to infinity all fell within the equivalence interval (80.0%-125%) whether under fasting condition or fed condition. In conclusion, the 2 formulations of safinamide tablets were bioequivalent and well tolerated under both fasting and fed conditions in healthy Chinese volunteers. High-fat food delayed the absorption of safinamide but did not affect the final bioavailability.