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给28名健康男性受试者,年龄22～30岁,体重55～70kg。按饭后服或静注,禁食后口服或静注,于上午9:30和下午9:30给安定5mg,随机分为4组,交叉连续使用3周,于给药前后不同时间采血样,用HPLC电子捕获检测器检测血药浓度(安定及其主要代谢产物N-去甲安定)。实验表明,(1)平均总血浆浓度上午服药组在0.5、1、1.5、6h 高于晚上服药组,峰浓度上午高于晚上,达峰时间上午服药组比晚上者短,但上午或晚上服药的β相半衰期及曲线下面积相似。(2)血浆去甲安定于3、6、10
To 28 healthy male subjects, aged 22 to 30 years old, weighing 55 to 70kg. After meals or intravenous injection, fasting oral or intravenous injection at 9:30 am and 9:30 pm to stability and 5mg, were randomly divided into 4 groups, cross-continuous use of 3 weeks, before and after administration of blood samples at different times The plasma concentration (diazepam and its major metabolite N-desmethyl) was measured by HPLC electron capture detector. The experimental results showed that: (1) The average total plasma concentration in the morning was higher than that in the evening at 0.5,1,1.5 and 6h, the peak concentration was higher in the morning than in the evening and the morning in the morning and the evening were shorter The beta phase half-life and area under the curve are similar. (2) plasma to a stable at 3,6,10