Seung-Hyun Jeong, Ji-Hun Jang, Hea‐Young Cho
Apr 17, 2020
Citations
0
Influential Citations
2
Citations
Journal
Biomedical chromatography : BMC
Abstract
Epinastine is an antiallergic drug with high selectivity for histamine receptors. It has been reported that 9,13b-dehydroepinastine is present as a metabolite in vivo in humans, but there was little information about their pharmacokinetics (PKs) in humans. Although several analytical methods have been reported for epinastine analysis in different matrices, none are available for its metabolite. Therefore, purpose of this study was to develop an analytical method to simultaneously measure epinastine and its metabolite, 9,13b-dehydroepinastine, in human plasma samples using ultra-performance liquid chromatography-tandem mass spectrometer. Analytes were separated in a C18 -column. Quantifying of this analysis was performed on a triple-quadrupole mass spectrometer. Chromatograms showed high sensitivity, selectivity, and resolution with no interference with plasma constituents. Calibration curves for both epinastine and 9,13b-dehydroepinastine in human plasma were 0.1-50 ng/mL and displayed excellent linearity with correlation coefficients (r2 ) greater than 0.99. Developed analytical method satisfied the criteria of international guidance and was validated. Method could be successfully applied to PK studies of epinastine and, for the first time, metabolite kinetics of epinastine to 9,13b-dehydroepinastine in humans after oral administration of 20 mg epinastine hydrochloride tablets. Our study is expected to be useful in future studies such as dosage settings and clinical pharmacotherapy.