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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。
The enantiomers of seven kinds of aryloxylalcohol beta-blockers (atenolol, sotalol, celiprolol, carvedilol, metoprolol, , Propafenone) by reversed-phase high performance liquid chromatography. After liquid-liquid extraction, 100 μL GITC acetonitrile solution (1.0 mg / mL) was used for chiral derivatization and C_8 column separation. The mobile phase consisted of acetonitrile-0.01 mol / L potassium dihydrogen phosphate buffer ( pH 3.5). The specificity of this method was better. The absolute recoveries of enantiomers and internal standards were both> 78%. The relative recoveries of enantiomers were about 100%. The intra- and inter-day precision were all <15%. The results show that the method is simple, rapid, reproducible, and can be applied to the stereoselective studies of the seven drugs in monolayer transport of Caco-2 cells.