Greenblatt D J, Locniskar A, Shader R I
Psychopharmacology (Berl). 1983;80(2):178-80. doi: 10.1007/BF00427965.
Halazepam and its major metabolite desmethyldiazepam (DMDZ) can be reliably quantitated in human plasma following single doses of halazepam. After addition of appropriate internal standards, halazepam and DMDZ are extracted directly into an organic solvent at physiological pH. The organic extract is separated, evaporated to dryness, reconstituted, and directly chromatographed using a 50:50 methyl:phenyl silicone column (SP-2250) and an electron-capture detector. After a single 40 mg oral dose of halazepam, the parent compound appears in plasma only transiently and at low levels. DMDZ appears in higher concentrations and is slowly eliminated. During multiple-dose therapy with halazepam, DMDZ will be the major active substance in blood.
单次服用卤沙唑仑后,可在人血浆中可靠地定量测定卤沙唑仑及其主要代谢物去甲基地西泮(DMDZ)。加入适当的内标后,卤沙唑仑和DMDZ在生理pH值下直接萃取到有机溶剂中。将有机萃取物分离、蒸发至干、复溶,然后使用50:50甲基:苯基硅氧烷柱(SP-2250)和电子捕获检测器直接进行色谱分析。单次口服40mg卤沙唑仑后,母体化合物仅短暂且低水平地出现在血浆中。DMDZ以更高的浓度出现且消除缓慢。在卤沙唑仑多剂量治疗期间,DMDZ将成为血液中的主要活性物质。