矽宁的药物代谢动力学研究

Studies on the Pharmacokinetics of Xinin

利用燐光分析法研究了矽宁在动物体内的药代动力学及其吸收、分布和排泄的特点∈蠊辔覆煌亮课?血药浓度-时间的动力学过程均符合一级吸收二室开放模型;吸收速度较快且完全,分布广泛,在组织中有一定的蓄积性;经小鼠、大鼠的尿、粪便及胆汁中以原形物排出很少。

Xinin is an analogous Tilorone. It possesses significant curative effect on the experimental silicosis in rats. The pharmacokinetics of Xinin were carried out after oral administration in mice. A method of phosphorimetric analysis for the determination of Xinin in biological samples was developed. The blood drug concentration-time curve was found to fit a two compartment model with the following pharmacokinetic parameters.t1/2α=5.22～6.68min, T1/2β=46.37～55.23min,Vb=11.6～16.61 L/kg, C1=182.45～252.99ml/kg.min,after oral administration of Xinin from 20mg/kg to 60mg/kg. After oral administration of Xinin 40mg/kg to mice, absorption was shown to be rapid and complete. At 2 hours the concentration of Xinin in spleen, liver, kidney and adrenal was higher than that in the other tissues. After oral administration of Xinin in a dose of 40mg/kg to mice, 4.4% of the dose was found in the mouse urine and 2.52% of the dose was recovered in the mouse faeces within 72 hours. 0.13% of the dose was found in the rat bile within 24 hours. The results indicate that most of drug may be converted.