Shimada K, Tanaka M, Nambara T, Imai Y
J Pharm Sci. 1984 Jan;73(1):119-21. doi: 10.1002/jps.2600730133.
A sensitive method has been developed for the determination of a new antihypertensive agent, (2R,4R)-2-(2-hydroxyphenyl)-3-(3-mercaptopropionyl)-4-thiazolidinecar boxylic acid (I), in human blood. Because the drug is unstable in biological fluids, it was immediately derivatized by treating the freshly drawn blood specimens with N-(4-anilinophenyl)maleimide. The adduct was separated and determined by high-performance liquid chromatography with electrochemical detection on a reverse-phase column. The assay method was satisfactory with respect to the sensitivity and precision, providing a quantitation limit of 2 ng/ml and coefficient of variation of 3%. Preliminary pharmacokinetic data were obtained by orally administering I to two patients with essential hypertension.
已开发出一种灵敏的方法用于测定人血中一种新型抗高血压药物(2R,4R)-2-(2-羟苯基)-3-(3-巯基丙酰基)-4-噻唑烷羧酸(I)。由于该药物在生物流体中不稳定,因此通过用N-(4-苯胺基苯基)马来酰亚胺处理刚采集的血样立即进行衍生化。加合物通过反相柱上的高效液相色谱-电化学检测进行分离和测定。该测定方法在灵敏度和精密度方面令人满意,定量限为2 ng/ml,变异系数为3%。通过对两名原发性高血压患者口服I获得了初步的药代动力学数据。