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为研究普拉西坦在犬和大鼠体内药代动力学规律,给犬灌服普拉西坦后,抽取不同时间的血液,分离血浆,用HPLC测定血浆中药物浓度,采用3p87 程序计算药代参数;应用HPLC测定大鼠灌服普拉西坦后各组织和胆汁、尿、粪中药物浓度。结果显示:血药浓度-时间曲线符合一室开放模型,其体内的T1/2为2.3~3.9 小时;大鼠灌服普拉西坦后3 小时各组织中有较高的浓度,以肾脏为最高,肝脏次之,依序为肠、肺、肌、心、生殖腺、脾、脂肪;脑组织也能测到一定的量。24小时从胆汁排泄原形药物占给药量的0.7% ,72小时从尿和粪中排出原形药物量分别占给药量的28.26% 和6.35% 。用平衡透析法测定普拉西坦的血浆蛋白结合率约为20.1% ~22.2% 。以上结果表明,普拉西坦吸收快,分布广,消除也快。
In order to study the pharmacokinetics of Pulsitin in dogs and rats, the dogs were fed with praticillin, blood was drawn at different times, plasma was separated, plasma concentration of the drug was measured by HPLC, 3p87 program was used to calculate the drug On behalf of the parameters; HPLC determination of rats fed with cortisol in tissues and bile, urine, feces in the drug concentration. The results showed that the plasma concentration-time curve conformed to the one-compartment open model with T1 / 2 of 2.3 to 3.9 hours in vivo and the higher concentration , With the kidney as the highest and the liver as the second, followed by the intestine, lung, muscle, heart, gonad, spleen, and fat; and the brain tissue could also measure a certain amount. 24 hours from the bile excretion of prototype drugs accounted for 0.7% of the dose, 72 hours from the urine and excretion of prototype drugs accounted for 28.26% and 6.35% of the dose. The plasma protein binding of procaterol was determined to be about 20.1% -22.2% by dialysis. The above results show that the rapid absorption of cortisol, widespread, eliminate quickly.