Stefanova D, Daleva L, Nakova G, Peĭkova R, Ognianova V
Eksp Med Morfol. 1980;19(3):159-65.
The authors carried out studies on the preparation menilon in order to establish eventual correlations between some pharmacological and pharmakokinetic indices. For this purpose they examined the activity of menilon in rats and mice during electric shock and hypothermia and determined the concentrations of the preparation in plasma and brain in rats. The obtained results from the pharmacological investigation revealed manifested action against the seizures after electric shock in both groups of animals. It was established as early as 30 minutes after oral administration of the preparation reached maximal activity after 1-2 hours and disappeared after 6 hours. The authors found strong and continuous hypothermic activity. The hypothermic effect of the doses used was preserved up to the end the 24 th hour. The lowering of temperature in rats was comparatively weaker and shorter. The pharmacokinetic studies showed quick oral resportion of menilon. It was found in plasma and brain of the experimental animals on the 30 th minite after its administration, reached maximal concentration between the first and second hour and still was established on the 24 th hour after administration. The maximal level of the preparation in plasma and brain after oral administration correlated well with the time of maximal activity of its antiseizure and hypothermic effects. The preparation menilon was comparatively slightly toxic.
作者对美尼隆制剂进行了研究，以确定某些药理学和药代动力学指标之间可能存在的相关性。为此，他们研究了美尼隆在大鼠和小鼠遭受电击和低温时的活性，并测定了该制剂在大鼠血浆和大脑中的浓度。药理学研究所得结果显示，两组动物在遭受电击后，该制剂对癫痫发作均有明显作用。早在口服该制剂30分钟后即显示出活性，1 - 2小时后达到最大活性，6小时后活性消失。作者发现该制剂具有强烈且持续的降温活性。所用剂量的降温效果在24小时结束时仍存在。大鼠体温降低相对较弱且持续时间较短。药代动力学研究表明，美尼隆口服吸收迅速。给药后30分钟在实验动物的血浆和大脑中即可检测到，在第一和第二小时之间达到最大浓度，给药后24小时仍可检测到。口服给药后，该制剂在血浆和大脑中的最高水平与其抗癫痫和降温作用的最大活性时间密切相关。美尼隆制剂的毒性相对较小。
