Milligan N, Dhillon S, Oxley J, Richens A
Epilepsia. 1982 Jun;23(3):323-31. doi: 10.1111/j.1528-1157.1982.tb06198.x.
Rectal administration of several different preparations of diazepam to a group of adult volunteer patients with epilepsy produced variable rates of absorption. Peak serum concentrations following 10 mg, 20 mg, and 30 mg of diazepam solution were achieved between 13-60 min, 10-120 min, and 30-90 min respectively. An experimental diazepam "solid solution" suppository was found to have significantly better absorption characteristics compared with the commercially available Valium suppository. Diazepam solution 20 mg was administered rectally in 10 adult epileptic patients with frequent spontaneous interictal spikes in their EEGs. A highly significant reduction in spike frequency was seen compared with placebo. The effect was most marked 10-20 min after administration of diazepam, when the mean spike count fell to 39 +/- 35 SD percent of the control value (p less than 0.01), and this corresponded with a mean serum diazepam level of 210 +2- 125 ng/ml.
对一组成年癫痫志愿者患者经直肠给予几种不同制剂的地西泮,其吸收速率各不相同。给予10毫克、20毫克和30毫克地西泮溶液后,血清峰值浓度分别在13 - 60分钟、10 - 120分钟和30 - 90分钟达到。与市售的安定栓剂相比,一种实验性地西泮“固溶体”栓剂被发现具有明显更好的吸收特性。对10名脑电图中频繁出现自发发作间期棘波的成年癫痫患者经直肠给予20毫克地西泮溶液。与安慰剂相比,棘波频率显著降低。在给予地西泮后10 - 20分钟效果最为明显,此时平均棘波计数降至对照值的39±35标准差百分比(p<0.01),这与平均血清地西泮水平210±125纳克/毫升相对应。