Chan K, Lau O W, Wong Y C
Department of Pharmacology, Chinese University of Hong Kong, Shatin, N.T.
J Chromatogr. 1991 Apr 19;565(1-2):247-54.
Procedures based on gas chromatography were established to determine pethidine and its major metabolites in human urine. The chromatographic system consisted of a glass column packed with 3% (w/w) SP2250 on Chromosorb W (80-100 mesh) linked to a nitrogen-phosphorus detector. Diethyl ether was used as the extraction solvent. Pethidinic and norpethidinic acids, and their conjugated metabolites (after beta-glucuronidase treatment) were determined after conversion into pethidine and norpethidine by acid-catalysed esterification. The retention times of pethidine, norpethidine and chlorpheniramine (internal standard) were 3.3, 4.5 and 7.5 min, respectively. The amount of unchanged drugs and metabolites excreted varied considerably among the subjects. The mean 24-h urinary recoveries in eight patients of pethidine, norpethidine, pethidinic acid, norpethidinic acid, and the glucuronides of pethidinic and norpethidinic acids were 6.62 +/- 5.05, 4.33 +/- 1.19, 18.9 +/- 6.29, 9.10 +/- 4.26, 15.1 +/- 3.02 and 7.57 +/- 2.28%, respectively. This indicates that the major metyabolic pathways of pethidine in the eight patients were hydrolysis followed by conjugation. Over 60% of the dose was accounted for in 24 h after intramuscular administration of 1 mg/kg pethidine.
建立了基于气相色谱法的程序来测定人尿中的哌替啶及其主要代谢物。色谱系统由一根填充有3%（w/w）SP2250的Chromosorb W（80 - 100目）玻璃柱与氮磷检测器相连组成。使用乙醚作为萃取溶剂。哌替啶酸和去甲哌替啶酸及其结合代谢物（经β-葡萄糖醛酸酶处理后）在通过酸催化酯化转化为哌替啶和去甲哌替啶后进行测定。哌替啶、去甲哌替啶和氯苯那敏（内标）的保留时间分别为3.3、4.5和7.5分钟。排泄的未变化药物和代谢物的量在受试者之间差异很大。8名患者中哌替啶、去甲哌替啶、哌替啶酸、去甲哌替啶酸以及哌替啶酸和去甲哌替啶酸的葡萄糖醛酸苷的24小时尿回收率平均值分别为6.62±5.05、4.33±1.19、18.9±6.29、9.10±4.26、15.1±3.02和7.57±2.28%。这表明这8名患者中哌替啶的主要代谢途径是水解后结合。肌肉注射1mg/kg哌替啶后24小时内超过60%的剂量得以说明。
