Establishment of reverse-phase high-performance liquid chromatography with chiral reagent derivatization for separation of fexofenadine enantiomers

VernacularTitle:非索非那定对映体柱前手性衍生化反相高效液相色谱分析方法的建立
Author: Qing-Qing YAO ¹ ; Bo-Xuan QU ; Quan ZHOU ; Su ZENG
Author Information

1. 浙江大学药学院药物分析与药物代谢研究室浙江省抗肿瘤药物临床前研究重点实验室
Keywords: Terfenadine/chemistry; Isocyanates; Stereoisomerism; Chromatography,high pressure liquid/methods; Indicators and reagents
From: Journal of Zhejiang University. Medical sciences 2014;(2):155-159
CountryChina
Language:Chinese
Abstract: Objective: To establish a precolumn chiral derivatization method for determination of fexofenadine enantiomers , a chiral substrate of OATP1B1, in cellular model.Methods: R-( +)-phenylethylisocyanate was selected as chiral derivatization reagent , which was reacted with fexofenadine to form carbamate derivatives . Enantiomers were identified by LC/MS and separated by RP-HPLC.Results:Under the experimental conditions , the fexofenadine enantiomers were separated completely .The standard curve was linear over the concentration range of 25-100 ng/ml (R2 =0.9992, 0.9989).Accuracy was 101.1%and 98.3%, intra-precision was 2.4%and 3.1%, inter-precision was 3.1% and 4.0% for D1 and D2, respectively.Conclusion: The method established is sensitive and accurate for determination of fexofenadine enantiomers in cells .