二氢吡啶类钙离子拮抗药物手性分析及其立体选择性药动学研究进展

Advances in chiral analysis and stereoselective pharmacokinetics of dihydropyridine calcium antagonists

手性药物与安全有效用药的关系密切,大多数二氢吡啶类药物具有手性碳原子,以消旋体入药,进入体内后产生立体选择性处置特征,可能影响用药的安全有效。该研究围绕该类药物手性拆分及药动学特点,综述了近年来该类药物的手性高效液相色谱法(HPLC)和手性毛细管电泳法(CE)方法选择规律及体内分析应用;列举并比较了该类药物间的立体选择性药动学研究情况,发现该类药物部分具有明显的立体选择性差异,体内药效和毒性也随之不同。

Chiral drugs are closely related to the safety and effectiveness of drug use.Most dihydropyridine drugs have chiral carbon atoms,which are used as racemes and produce stereoselective disposal characteristics after entering the body,and may affect the safety and effectiveness of drugs.Therefore,based on the chiral resolution and pharmacokinetic characteristics of this class of drugs,the selection rules of chiral HPLC and CE methods and in vivo analysis applications of this class of drugs in recent years were reviewed.The stereoselective pharmacokinetics of this class of drugs were listed and compared.It was found that some of these drugs had obvious differences in stereoselective pharmacokinetics,and the pharmacokinetics and toxicity in vivo were also different.