Greenblatt D J, Locniskar A, Shader R I
Sleep. 1983;6(1):72-6. doi: 10.1093/sleep/6.1.72.
Brotizolam, a thienodiazepine hypnotic, can be reliably and sensitively quantitated in human plasma using gas chromatography with electron-capture detection. After addition of an internal standard, samples are directly extracted into an organic solvent, evaporated, reconstituted, and chromatographed at 290 degrees C on a 1% OV-17 column. Sensitivity limits are 0.25 ng of brotizolam/ml of plasma. Six volunteers ingested single 0.25- and 0.5-mg doses of brotizolam on two occasions, and brotizolam concentrations were measured in plasma samples drawn during 24 h after each dose. Peak concentrations averaged 5.5 and 9.2 ng/ml at the two dose levels, and were always attained within 1.5 h after dosage. Elimination half-life averaged 4.4 h (range 2.6-6.9 h) and was independent of dose. Thus brotizolam is a rapidly absorbed hypnotic drug with a short elimination half-life.
溴替唑仑是一种噻吩二氮卓类催眠药，采用带电子捕获检测的气相色谱法可对人血浆中的溴替唑仑进行可靠且灵敏的定量分析。加入内标后，将样品直接萃取到有机溶剂中，蒸发、复溶，然后在290℃下于1% OV - 17柱上进行色谱分析。检测限为0.25纳克溴替唑仑/毫升血浆。六名志愿者分两次服用了单次0.25毫克和0.5毫克剂量的溴替唑仑，并在每次服药后24小时内采集的血浆样本中测定溴替唑仑浓度。在两个剂量水平下，峰值浓度平均分别为5.5纳克/毫升和9.2纳克/毫升，且总是在服药后1.5小时内达到。消除半衰期平均为4.4小时（范围为2.6 - 6.9小时），且与剂量无关。因此，溴替唑仑是一种吸收迅速、消除半衰期短的催眠药。
