Reversed-phase high-performance liquid chromatographic analysis of seven pairs of chiral drug enantiomers in transport medium after chiral derivatization  

柱前手性衍生化反相高效液相色谱法测定转运液中7种芳氧丙醇胺类β受体阻断剂对映体的含量(英文)

作　　者：贺瑛[1] 柴晓鹃[1] 曾苏[1] 

机构地区：[1]浙江大学药学院药物分析与药物代谢研究室,浙江杭州310058

出　　处：《Journal of Chinese Pharmaceutical Sciences》2010年第2期104-109,共6页中国药学（英文版）

基　　金：National Key Project of China(Grant No. 2009ZX09304-003).

摘　　要：A reversed-phase high-performance liquid chromatographic （RP-HPLC） method was established for the determination of the enantiomers of 7 aryloxy aminopropanol drugs （atenolol, sotalol, celiprolol, carvedilol, metoprolol, propranolol and propafenone） in transport medium. The method involved liquid-liquid extraction of chiral drugs from transport medium, and employed 2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyl isothiocyanate （GITC, 1.0 mg/mL in acetonitrile） as a pre-column chiral derivatization reagent. After derivatization, the products were separated on an Agilent Zorbax C8 column （150 min×4.6 mm, 5 μm） at 25 ℃. The mobile phase consisted of a mixture of acetonitrile and 0.01 M phosphate buffer （pH 3.5）. The present methods were specific for the determination of enantiomers of each chiral drug. The absolute recoveries of the enantiomers and internal standards were 〉78%. The relative recoveries of the enantiomers were approximately 100%. The intra- and inter-day variations were 〈 15%. The method was reproducible and sufficiently sensitive to determine the enantiomers of seven aryloxy aminopropanol drugs in transport medium. The method could be used to study the transport of atenolol, sotalol, celiprolol, carvedilol, metoprolol, propranolol and propafenone.建立转运液中7种芳氧内醇胺类β受体阻断剂对映体(阿替洛尔、索他洛尔、塞利洛尔、卡维地洛、美托洛尔、普萘洛尔、普罗帕酮)的反相高效液相色谱测定法。转运液中药物经液液萃取后,加入100μL GITC乙腈液(1.0 mg/mL)进行手性衍生化,再用C_8柱进行分离,流动相为乙腈-0.01 mol/L磷酸二氢钾缓冲盐(pH 3.5)。本方法专属性较好,对映体和内标的绝对回收率均>78%,对映体的相对回收率约为100%,日间和日内精密度均<15%。结果表明本方法简做便、快速、重现性好,可应用于这7种药物在Caco-2细胞单层转运中的立体选择性研究。

关 键 词：Enantiomer separation Aryloxy aminopropanol drugs RP-HPLC Pre-column derivatization 

分 类 号：R917[医药卫生—药物分析学]