Lu J F, Wu M F, Chen G, Xiang B R, An D K
Department of Clinical Pharmacy of Jinling Hospital, Nanjing, China.
Zhongguo Yao Li Xue Bao. 1993 Nov;14(6):485-8.
Eight Chinese healthy male volunteers aged 27 +/- s 4 a were injected i.v. midazolam (Mid) 15 mg. Blood samples were collected at 0, 2, 5, 7, 10, 20, 30, 45, 60, 90, 120, 180, and 240 min. A HPLC method was established for determining the Mid concentrations in serum. The concentration-time data was fitted with biexponential curve. Pharmacokinetic parameters were: T1/2 alpha = 6.8 +2- 2.5 min, T1/2 beta = 118 +/- 27 min, Vc = 25 +/- 7 L, Cl = 393 +/- 79 ml.min-1, Vdss = 59 +/- 13 L, AUC0-infinity = 39.6 +/- 8.6 g.min.L-1. The electroencephalogram (EEG) showed a decrease in alpha activity and an increase in beta activity. The EEG pattern reverted toward baseline after 2-3 h. Pharmacokinetic and EEG findings suggest that Mid is a preferable anesthesia inducing agent.
八名年龄在27±4岁的中国健康男性志愿者静脉注射15毫克咪达唑仑（Mid）。在0、2、5、7、10、20、30、45、60、90、120、180和240分钟采集血样。建立了一种高效液相色谱法（HPLC）来测定血清中咪达唑仑的浓度。浓度-时间数据用双指数曲线拟合。药代动力学参数为：T1/2α = 6.8±2.5分钟，T1/2β = 118±27分钟，Vc = 25±7升，Cl = 393±79毫升·分钟-1，Vdss = 59±13升，AUC0-∞ = 39.6±8.6微克·分钟·升-1。脑电图（EEG）显示α波活动减少，β波活动增加。2至3小时后脑电图模式恢复到基线。药代动力学和脑电图结果表明，咪达唑仑是一种较好的麻醉诱导剂。
