Divoll M, Greenblatt D J
Pharmacology. 1981;22(4):263-8. doi: 10.1159/000137498.
A single 5-mg oral dose of diazepam was administered to 6 healthy volunteers on 3 occasions in a randomized 3-way crossover study. Modes of administration were: (A) (control): diazepam with 120 ml of water, preceded 30 min before with 120 ml of water; (B) diazepam with 120 ml water, preceded by 120 ml of a 50:50 vodka:water mixture, and (C) diazepam with 120 ml of the vodka mixture, preceded by 120 ml of water. Peak plasma diazepam levels averaged 166, 140 and 145 ng/ml in trials A, B and C, respectively; the time of peak concentration was 0.71, 2.1 and 1.5 h after the dose, respectively. Differences were not significant. Total areas under the plasma concentration curve were nearly identical (2.7, 2.8 and 2.9 micrograms/ml X h) among the 3 trials, as were values of diazepam elimination half-life (29, 36 and 35 h). The rate and extent of desmethyldiazepam formation also did not differ among trials. Thus, coadministration of diazepam with or shortly after a typical social cocktail tends to slow the rate of diazepam absorption, but does not influence the completeness of absorption or the rate of elimination.
在一项随机三交叉研究中，6名健康志愿者分3次接受了单次5毫克口服地西泮给药。给药方式如下：(A)（对照）：地西泮与120毫升水同服，服药前30分钟先服120毫升水；(B)地西泮与120毫升水同服，服药前先服120毫升50:50伏特加与水的混合液；(C)地西泮与120毫升伏特加混合液同服，服药前先服120毫升水。在试验A、B和C中，血浆地西泮峰值水平分别平均为166、140和145纳克/毫升；达峰时间分别为服药后0.71、2.1和1.5小时。差异不显著。3次试验中血浆浓度曲线下总面积几乎相同（2.7、2.8和2.9微克/毫升×小时），地西泮消除半衰期值也相同（29、36和35小时）。试验中去甲地西泮的生成速率和程度也没有差异。因此，地西泮与典型社交鸡尾酒同时服用或在其后不久服用往往会减缓地西泮的吸收速率，但不影响吸收的完全程度或消除速率。
