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目的 研究艾普斯特 (epristeride)在动物体内药代动力学 ,为临床试验提供依据。 方法 采用HPLC方法测定生物样品中药物浓度。结果 大鼠 poepristeride 10 ,2 0和 40mg·kg-1后 ,3个剂量的血清药物浓度出现明显双峰。Beagle犬 po 10mg·kg-1后血药浓度未出现明显双峰。大鼠 po 2 0mg·kg-1后 3h ,大部分组织中含量高于药后6h含量 ;药后 2 4h内尿和粪的排泄量分别占给药量的 0 0 9%和 42 9% ,12h内胆汁排泄的主要为代谢产物 ,原型药物仅为给药量的 0 14%。本品蛋白结合率为 92 3%。结论 Epristeride在 10～ 40mg·kg-1范围内呈现一级动力学特征 ,Cmax,AUC均与剂量呈正相关。药物在组织脏器中分布广泛 ,主要经粪和胆汁排泄。
Objective To study the pharmacokinetics of epristeride in animals and provide basis for clinical trials. Methods HPLC method was used to determine the drug concentration in biological samples. Results After three doses of poepristeride 10, 20 and 40 mg · kg-1, there were obvious double peaks in the serum drug concentration. Beagle dogs po po 10mg · kg-1 plasma concentrations did not appear obvious double peak. After 3 h of po 2 0 mg · kg -1, most of the tissue contents were higher than that of the 6 h after the drug injection. Urine and fecal excretion accounted for 0.09% and 42.9% 12h bile excretion of the main metabolites, the prototype drug only for the amount of 0 14%. This product protein binding rate of 92 3%. Conclusion Epristeride exhibits first-order kinetic characteristics in the range of 10-40 mg · kg-1, and Cmax and AUC are positively correlated with the dose. Drugs are widely distributed in tissues and organs and mainly excreted by excrement and bile.