Unceta Nora, Goicolea M Aranzazu, Barrio Ramón J
Department of Analytical Chemistry, Faculty of Pharmacy, University of Basque Country, Paseo de la Universidad 7, 01006 Vitoria-Gasteiz, Spain.
Biomed Chromatogr. 2011 Jan;25(1-2):238-57. doi: 10.1002/bmc.1542. Epub 2010 Nov 5.
The antidepressant citalopram (CIT) is a potent and highly selective serotonin reuptake inhibitor (SSRI) which has been introduced in therapy as a racemic drug. CIT has been used to treat central nervous system affective disorders such as depression, anxiety, obsessive-compulsive disorders, various phobias, borderline personality disorders, bipolar disorders as well as indications wherein inhibition of serotonin reuptake is desired. CIT is demethylated to demethylcitalopram (DCIT) and didemethylcitalopram (DDCIT), which retain considerable activity as SSRIs. Therefore, in recent years, the monitoring of the levels of these analytes in biological fluids for toxicological and therapeutic purposes has been a target worthy of interest. In addition, the differences in activity between CIT enantiomers established the need to assess its behaviour in the field of pharmacological research. It is also necessary to develop analytical methodologies that make it possible to determine the levels of enantiomer concentrations. This review includes most of the published analytical methods for achiral assay of racemic CIT and its metabolites based on high-performance liquid chromatography coupled with UV, fluorescence and mass spectrometry detectors, capillary electrophoresis and gas chromatography with mass spectrometry detectors among others. With regard to the monitoring of enantiomers of CIT and of its metabolites, stereoselective methods based on chiral chromatographic columns, chiral additives in mobile phases and on the derivatization with a chiral reagent are also collected. In addition, different procedures of extraction are mentioned as well as liquid-liquid extraction, solid-phase extraction, solid-phase microextraction, automated online extraction or liquid-phase microextraction in different biological and environmental samples.
抗抑郁药西酞普兰（CIT）是一种强效且高度选择性的5-羟色胺再摄取抑制剂（SSRI），它作为消旋药物已被用于治疗。CIT已被用于治疗中枢神经系统情感障碍，如抑郁症、焦虑症、强迫症、各种恐惧症、边缘性人格障碍、双相情感障碍以及需要抑制5-羟色胺再摄取的适应症。CIT会脱甲基化为去甲基西酞普兰（DCIT）和双去甲基西酞普兰（DDCIT），它们作为SSRI仍保留相当的活性。因此，近年来，出于毒理学和治疗目的监测生物流体中这些分析物的水平一直是一个值得关注的目标。此外，CIT对映体之间活性的差异确定了在药理研究领域评估其行为的必要性。还需要开发能够测定对映体浓度水平的分析方法。本综述涵盖了基于高效液相色谱与紫外、荧光和质谱检测器联用、毛细管电泳以及气相色谱与质谱检测器联用等方法的大多数已发表的用于消旋CIT及其代谢物非手性测定的分析方法。关于CIT及其代谢物对映体的监测，还收集了基于手性色谱柱、流动相中的手性添加剂以及手性试剂衍生化的立体选择性方法。此外，还提到了不同的提取程序，以及在不同生物和环境样品中的液-液萃取、固相萃取、固相微萃取、自动在线萃取或液相微萃取。
