异丙氯肼的代谢产物对氯苯氧乙酰胺在人体中的鉴定及尿排泄情况。

Identification and urinary excretion of p-chlorophenoxyacetamide, a metabolite of iproclozide, in humans.

作者信息

De Sagher R M, De Leenheer A P, Cruyl A A, Claeys A E

出版信息

Drug Metab Dispos. 1975 Nov-Dec;3(6):423-9.

Abstract

The presence of p-chlorophenoxyacetamide was detected in the urine of man receiving iproclozide [1-(p-chlorophenoxyacetyl)-2-isopropylhydrazine]. This new metabolite was identified by combined gas-liquid chromatography-mass spectrometry and by comparison with the synthetic compound. An appropriate procedure for the extraction and quantitation of p-chlorophenoxyacetamide by gas-liquid chromatography on a 5% OV-225-packed column with the 2-butyl analog of iproclozide as an internal standard, has been developed. After 20- and 50-mg single dose oral administrations of iproclozide, 5.2 and 8.3% were slowly excreted in urine as p-chlorophenoxyacetamide within 30.5 and 36 hr. respectively. After 20-mg oral intakes by psychiatric patients, the 24-hr urinary excretion of p-chlorophenoxyacetamide amounted to about 2-4% of the iproclozide dose administered.

摘要

在服用氯哌齐特[1-(对氯苯氧基乙酰基)-2-异丙基肼]的人的尿液中检测到了对氯苯氧基乙酰胺。通过气液色谱-质谱联用以及与合成化合物进行比较，鉴定出了这种新的代谢产物。已开发出一种合适的方法，以异丙氯嗪的2-丁基类似物为内标，在5% OV-225填充柱上通过气液色谱法提取和定量对氯苯氧基乙酰胺。单次口服20毫克和50毫克氯哌齐特后，分别在30.5小时和36小时内，有5.2%和8.3%以对氯苯氧基乙酰胺的形式缓慢排泄到尿液中。精神科患者口服20毫克后，对氯苯氧基乙酰胺的24小时尿排泄量约为所服氯哌齐特剂量的2%-4%。