Arndts D, Rominger K L
Arzneimittelforschung. 1978;28(11a):1951-60.
Only very minute concentrations of metabolites of highly effective and consequently low dosed drugs can be detected in urine. In order to identify the structure of these compounds they must be concentrated by a factor up to 1:10(6). Isolation of metabolites, especially when present as conjugates, becomes more complicated the greater the polarity. In this paper some methods for isolation are presented using column- and thin-layer chromatography as well as extraction and dialysis, finally their practical application and their most effective combination are described. Priority must be given to solving two problems: firstly, a rough pre-purification is necessary to eliminate physiological components from the urine such as salts, urea, etc., and secondly, the mixture of metabolites has to be separated into single metabolites. Examples are given to demonstrate the practicability of these methods for the isolation and structural identification of metabolites belonging to varying structural classes.
在尿液中只能检测到极微量的高效低剂量药物代谢物。为了确定这些化合物的结构,必须将它们浓缩1000000倍。代谢物的分离,尤其是以结合物形式存在时,极性越大就越复杂。本文介绍了一些使用柱色谱法、薄层色谱法以及萃取和透析法进行分离的方法,最后描述了它们的实际应用及其最有效的组合方式。必须优先解决两个问题:第一,需要进行粗预纯化以去除尿液中的生理成分,如盐、尿素等;第二,必须将代谢物混合物分离成单一的代谢物。文中给出了一些例子,以证明这些方法对于分离和鉴定不同结构类别的代谢物结构的实用性。