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提取小鼠肝P450酶,建立咪达唑仑的体外代谢模型。确定了其在体内的主要代谢产物的结构;通过优化药物体外代谢的条件,获得了较高纯度的咪达唑仑代谢物(α-OH咪达唑仑)对照品。通过志愿者实验,考察了咪达唑仑在体内的代谢过程和咪达唑仑及其代谢物α-OH咪达唑仑在体内的消除过程。结果表明以代谢物α-OH咪达唑仑作为分析目标物,建立灵敏、快速的分析方法,可使体内咪达唑仑检测的检出时限从6h延长至48h.该研究结果可满足实际检案需要,并可为分析结果的评价提供依据。
Mouse liver P450 enzyme was extracted to establish the in vitro metabolism model of midazolam. The structure of its major metabolites in the body was determined. The midazolam metabolite (α-OH midazolam) reference substance with higher purity was obtained by optimizing the in vitro metabolism of the drug. Through volunteer experiments, we investigated the metabolic process of midazolam in vivo and the elimination process of midazolam and its metabolite α-OH midazolam in vivo. The results showed that the detection of midazolam in vivo could be extended from 6h to 48h by using the midazolam metabolite α-OH as the analytic target, and the sensitive and rapid analytical method was established. The case needs, and can provide the basis for the analysis of the results of the evaluation.