Becker-Scharfenkamp U, Blaschke G
Institute of Pharmaceutical Chemistry, University of Münster, Germany.
J Chromatogr. 1993 Nov 24;621(2):199-207. doi: 10.1016/0378-4347(93)80096-m.
The enantiomers of the racemic analgesic drug etodolac have been resolved by fractional crystallization of the diastereomeric salts with optically active 1-phenylethylamine. A high-performance liquid chromatographic method to determine racemic etodolac (assay I) and its major metabolites (assay II) in urine using a conventional reverse-phase column is described. The determination of the enantiomeric ratios of etodolac and the two metabolites 7-hydroxyetodolac and 8-(1'-hydroxyethyl)etodolac was achieved using different protein-bonded chiral stationary phases. The urinary data for five volunteers are presented and show a marked stereoselectivity of the metabolism of etodolac in humans.
通过外消旋镇痛药物依托度酸与旋光性1-苯乙胺形成的非对映体盐的分步结晶，拆分了其对映体。描述了一种使用常规反相柱测定尿液中消旋依托度酸（测定方法I）及其主要代谢物（测定方法II）的高效液相色谱法。使用不同的蛋白质键合手性固定相，实现了依托度酸及其两种代谢物7-羟基依托度酸和8-（1'-羟乙基）依托度酸对映体比例的测定。给出了五名志愿者的尿液数据，显示了依托度酸在人体内代谢具有显著的立体选择性。
