Prandial effect on the systemic exposure of amisulpride

Abstract

A substituted benzamide, amisulpride is an atypical antipsychotic and a specific antagonist for dopamine D₂ and D₃ receptors. The prandial effect on amisulpride absorption remains unclear, therefore, this study was designed to investigate the effect of food on the systemic exposure to amisulpride in healthy volunteers. The study was a randomized, two-way crossed trial in which a single oral dose of amisulpride was administered on two occasions, with 7-days washout period between each drug administration. The volunteers were randomly divided into two groups and received amisulpride (50 mg) with Korean traditional food or under fasting state. Blood was serially taken, and the plasma amisulpride concentrations were measured by LC/MS/MS. At fasting state, amisulpride reached the first peak (37.1 ± 13.3 ng/ml) at ~2.3 h, and decreased down to 19.4 ± 4.3 ng/ml until 3.5 h, and then again went up to the second peak (25.3 ± 5.8 ng/ml) at 5 h followed by a slow decay with 10.6 h of half-life. In contrast, no double peaks were shown when the drug was given with meal. The maximum concentration of amisulpride (56.0 ± 12.7 ng/ml) was increased by a 1.5-fold compared with that under fasting (p > 0.05), and the time to peak shortened a little (1.7 ± 0.6 h).