Kuz'mitskiĭ B B, Stoma O V, Slepneva L M, Mashkovich A E, Nasek V M
Farmakol Toksikol. 1989 Mar-Apr;52(2):71-4.
The pharmacokinetic investigation and the study of metabolism of an immunostimulator of 8-azasteroid series were performed on a single-compartment model. The main pharmacokinetic parameters of the immunomodulator in mice were established using different routes of administration. The maximal accumulation of tritium-labeled 8-azasteroid was recorded in the kidneys, liver and lung. The character of distribution changes with time. The half-life period is in the range of from 0.69 to 1.4 hours at different routes of administration. The total clearance is 0.49 ml/min, the area under the pharmacokinetic curve--3.8-8.1 micrograms/h/ml. On the model of the monooxygenase cytochrome P-450-containing system of the liver microsomes there was confirmed the formation of two metabolites preliminarily isolated from the mouse urine. By the character of resorption, distribution, elimination this 8-azasteroid immunoactivator is close to the agents of glucocorticoid series.
在单室模型上对8-氮杂甾体系列免疫刺激剂进行了药代动力学研究和代谢研究。通过不同给药途径确定了该免疫调节剂在小鼠体内的主要药代动力学参数。氚标记的8-氮杂甾体在肾脏、肝脏和肺中的积累量最大。分布特征随时间变化。不同给药途径下的半衰期在0.69至1.4小时范围内。总清除率为0.49 ml/min,药代动力学曲线下面积为3.8 - 8.1微克/小时/毫升。在肝微粒体含单加氧酶细胞色素P - 450系统的模型上,证实了从小鼠尿液中初步分离出的两种代谢产物的形成。从吸收、分布、消除特征来看,这种8-氮杂甾体免疫激活剂与糖皮质激素系列药物相近。