Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Medicine, Romania.
Department of Analytical Chemistry and Drug Analysis, Faculty of Pharmacy, University of Medicine, Romania.
Chirality. 2020 Jan;32(1):32-41. doi: 10.1002/chir.23139. Epub 2019 Nov 8.
Citalopram (CIT) is a highly selective serotonin reuptake inhibitor (SSRI) frequently used in the treatment of major depressive disorders. It has a chiral centre in its structure and is used in therapy both as a racemic mixture (R,S-CIT) and a pure enantiomer (S-CIT). The differences between the pharmacokinetic and pharmacological profiles of the two enantiomers are well established. Consequently, the development of new efficient chiral analysis methods for their enantiomeric separation is a topic of great actuality. CIT metabolism is stereoselective as it is metabolized in chiral active metabolites, which retain considerable SSRI activity and contribute to the pharmacological effect. Chiral analytical methods are employed for the determination of enantiomeric ratio in pharmaceutical preparations and for monitoring the enantiomer levels in biological samples for therapeutic and toxicologic purposes. The current study reviews the published literature for the chiral analysis of CIT and its metabolites based on chromatographic and electrophoretic methods coupled with UV, fluorescence and mass spectrometry detectors.
西酞普兰（CIT）是一种高度选择性的 5-羟色胺再摄取抑制剂（SSRI），常用于治疗重度抑郁症。它的结构中有一个手性中心，在治疗中既作为外消旋混合物（R，S-CIT），也作为纯对映异构体（S-CIT）使用。两种对映异构体在药代动力学和药理学特征方面的差异已得到充分证实。因此，开发新的高效手性分析方法来对它们进行对映体分离是一个具有重要现实意义的课题。CIT 的代谢具有立体选择性，因为它会代谢成具有手性活性的代谢物，这些代谢物保留相当大的 SSRI 活性，并有助于发挥药理作用。手性分析方法用于测定药物制剂中的对映体比例，以及用于监测生物样本中的对映体水平，以达到治疗和毒理学目的。本研究综述了基于色谱和电泳方法与紫外、荧光和质谱检测器相结合的 CIT 及其代谢物的手性分析的文献。
