咪达唑仑：用于人体药代动力学研究的放射免疫测定法。

Midazolam: radioimmunoassay for pharmacokinetic studies in man.

作者信息

Dixon R, Lucek R, Todd D, Walser A

出版信息

Res Commun Chem Pathol Pharmacol. 1982 Jul;37(1):11-20.

Abstract

A specific radioimmunoassay (RIA) for the determination of the new short-acting water soluble imidazo-1,4-benzodiazepine, midazolam, directly in plasma has been developed. Employing 3H-midazolam as the radioligand and a rabbit antiserum to a diazo conjugate of 5'-aminomidazolam and albumin, the method has a limit of sensitivity of 2 ng/ml of midazolam using a 20 microliters sample of plasma. The intra- and inter-assay coefficients of variation ranged from 4 to 7% and 13 to 15%, respectively. The specificity of the RIA was established by demonstrating good agreement with both EC-GC and GC-MS procedures in the analysis of multiple clinical plasma samples. The utility of the RIA for the pharmacokinetic evaluation of midazolam is illustrated with plasma concentration profiles of the drug obtained in subjects who had received midazolam intravenously, intramuscularly and orally.

摘要

已开发出一种用于直接测定血浆中新的短效水溶性咪唑并-1,4-苯二氮䓬——咪达唑仑的特定放射免疫分析（RIA）方法。该方法以³H-咪达唑仑作为放射性配体，使用针对5'-氨基咪达唑仑与白蛋白的重氮共轭物的兔抗血清，采用20微升血浆样本时，对咪达唑仑的检测灵敏度极限为2纳克/毫升。批内和批间变异系数分别为4%至7%和13%至15%。通过在分析多个临床血浆样本时与气相色谱-电子捕获检测法（EC-GC）和气相色谱-质谱联用法（GC-MS）均显示出良好一致性，确定了该放射免疫分析的特异性。通过接受静脉、肌肉和口服咪达唑仑的受试者所获得的药物血浆浓度曲线，说明了该放射免疫分析在咪达唑仑药代动力学评估中的实用性。