Viukari M, Salo H, Lamminsivu U, Auvinen R, Gordin A
Acta Pharmacol Toxicol (Copenh). 1981 Jul;49(1):59-64. doi: 10.1111/j.1600-0773.1981.tb00870.x.
The pharmacokinetics of diazepam administered as suppositories or as a solution in rectal tubes were compared in six geriatric hospital patients. A single dose of 10 mg was administered in a cross-over study with a one week interval. There was no statistically significant difference in the bioavailability, the mean maximum serum concentration or the time of achievement of the maximum with these preparations. However, the peak serum concentration was somewhat higher with suppositories but the absorption was somewhat faster via rectal tubes. The serum N-desmethyldiazepam concentration increased during the whole 24 hour observation period, there was no difference between the preparations. Our results are in good agreement with most studies of the pharmacokinetics of diazepam. The basal substance of the suppository is of the utmost importance to the absorption of diazepam. The rectal tube for administration of diazepam did not have any advantage over the optimally formulated (a mixture of macrogols) suppository in geriatric patients. In fact, the use of rectal tubes is more expensive, the tube may not be completely emptied, and the solution may not be completely retained in the rectum.
在六名老年住院患者中比较了地西泮以栓剂形式或直肠管溶液形式给药后的药代动力学。在一项交叉研究中，以一周的间隔给予单次剂量10毫克。这些制剂在生物利用度、平均最大血清浓度或达到最大值的时间方面没有统计学上的显著差异。然而，栓剂的血清峰值浓度略高，但通过直肠管吸收略快。在整个24小时观察期内，血清N-去甲基地西泮浓度升高，制剂之间没有差异。我们的结果与大多数地西泮药代动力学研究结果高度一致。栓剂的基质对地西泮的吸收至关重要。在老年患者中，用于给药地西泮的直肠管相对于优化配方（聚乙二醇混合物）的栓剂没有任何优势。事实上，使用直肠管更昂贵，管子可能无法完全排空，溶液可能无法完全保留在直肠中。
