Simultaneous determination of tianeptine and its active metabolite tianeptine MC5 in rat plasma and brain tissue using high performance liquid chromatography/electrospray ionization tandem mass spectrometry (LC-ESI-MS/MS)

摘要

A selective and sensitive method was developed to simultaneously quantify tianeptine and its main active metabolite tianeptine MC5 in rat plasma and brain tissue. A one-step liquid–liquid extraction was developed for sample preparation. The linear range for plasma was from 1.0–500.0 ng mL?1 and for brain tissue it was from 1.0–500.0 ng g?1. The method was validated in accordance with US FDA guidelines (precision within 15% relative standard deviation (RSD) and accuracy within 15% relative error (RE) with a consistent recovery). Stable isotope-labeled tianeptine and tianeptine MC5 (tianeptine-D4 and tianeptine MC5-D4) were used as the internal standards achieving good reproducibility while reducing the matrix effects. This method was successfully applied to a preclinical study for the simultaneous determination of tianeptine and tianeptine MC5 in rat plasma and brain tissue.