2'-氯地西泮及其代谢物的药代动力学特征的LC/MS研究

目的利用液质联用法研究2’-氯地西泮及其代谢物在大鼠体内的药代动力学规律。方法SD大鼠经灌胃给药2’-氯地西泮2.625mg/kg,给药后采集不同时间的血样。蛋白沉淀法处理血浆样品后,进样分析。结果2’-氯地西泮及其代谢物在给药后1h均达到最高血药浓度。2’-氯地西泮在大鼠体内的半衰期约为93h,在给药后144h均能检测到。3种代谢产物地洛西泮、氯甲西泮、劳拉西泮在大鼠血浆的检出时限分别24h、144h、48h。结论2’-氯地西泮在大鼠体内吸收较快,半衰期较长,原体药物和代谢物在大鼠体内的检测窗口均较长。该研究可为临床救治2’-氯地西泮中毒患者以及相关案件的侦破提供一定的实验依据。

Study on the pharmacokinetics of diclazeapm and its metabolites by LC/MS

Objective To study the pharmacokinetics of diclazepam and its metabolites in rats by LC/MS.Methods The SD rats were given diclazepam 2.625 mg/kg by gavage,and plasma was collected at different times after administration.After processed by protein precipitation method,the samples were injected for analysis.Results Diclazepam and its metabolites reached the highest plasma concentration in 1 h after administration.The half-life of diclazepam in rats is about 93 h,and can be detected for 144 h after administration.The detection time limits in rats plasma of the three metabolites,delorazepam,lormetazepam,and lorazepam,were 24 h,144 h,and 48 h respectively.Conclusion Diclaepam is absorbed faster and has a longer half-life in rats,and the detection window of the original drug and metabolites in the plasma were also longer.This research can provide a certain experimental basis for the clinical treatment of diclazepam poisoning and the detection of related criminal cases.