Abstract：
Enantioseparation and determination of chiral drugs are of vital importance in biochemical and pharmaceutical research due to the different biological activity, mechanism, and toxicity of individual enantiomers. As a second-generation H(1)-antagonist, cetirizine\'s pharmaceutical activity is mainly derived from the levocetirizine while the dextro-enantiomer is ineffective and even associated with side effects. Herein, the enantiomers of cetirizine were separated by capillary electrophoresis and identified by electronic circular dichroism. Satisfactory linear relationship was found between the circular dichroism signal at λmax and the electrophoretic peak area difference in the nonracemic mixture of enantiomers. It made possible identification and quantification of cetirizine enantiomers independent of single enantiomer standards. The method\'s feasibility was demonstrated on the enantiomeric excess experiments of oral drugs measured in human blank urine. Additionally, the separation and determination of cetirizine in human urine after administration were also realized by capillary electrophoresis, indicating the method was sensitive enough for pharmacokinetic study.
摘要：
手性药物的对映体分离和测定在生化和药物研究中至关重要。由于不同的生物活性，机制，和单个对映异构体的毒性。作为第二代H（1）-拮抗剂，西替利嗪的药物活性主要来自左西替利嗪，而右旋对映体无效，甚至伴有副作用。在这里，西替利嗪的对映体通过CE分离，并通过电子圆二色性鉴定。在λmax处的圆二色性信号与对映异构体的非外消旋混合物中的电泳峰面积差之间发现了令人满意的线性关系。它使独立于单一对映体标准的西替利嗪对映体的鉴定和定量成为可能。在人空白尿中测定口服药物对映体过量的实验中证明了该方法的可行性。此外,CE还实现了给药后人尿液中西替利嗪的分离和测定，表明该方法对药代动力学研究足够灵敏。本文受版权保护。保留所有权利。
