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研究盐酸他可林(THA)在大鼠体内的分布和排泄。方法大鼠以剂量8mg/kg灌胃给予盐酸他可林后,在规定时间摘取各脏器,收集尿粪,提取后用高效液相法测定浓度,分别计算药物在各组织的分布和排泄。结果69%的药物由尿排泄,24%的药物由粪排泄。在尿粪中原形药THA仅占3.1%。而1-OH-THA和2-OH-THA分别为42.0%和35.5%。结论盐酸他可林在大鼠体内的清除途径以羟代谢为主,药物在脑、肝、血、肾、脂肪、肺、脾、睾丸、胃、心、十二指肠、骨骼肌中的分布依次下降。
To study the distribution and excretion of THA in rats. Methods Rats were dosed with tacrine hydrochloride via intragastric administration at a dose of 8 mg / kg, and the organs were collected at regular time intervals to collect urine excrement. After concentration, the concentration of the drug was measured by HPLC. The distribution and excretion of drugs in each tissue were calculated . As a result, 69% of the drug was excreted in the urine and 24% of the drug excreted in the excrement. In the urine excretion prototype THA only accounted for 3.1%. While 1-OH-THA and 2-OH-THA were 42.0% and 35.5%, respectively. Conclusion The pathways of clearance of tacrine hydrochloride in rats are mainly in the form of hydroxyl metabolism. The distribution of drugs in the brain, liver, blood, kidney, fat, lung, spleen, testis, stomach, heart, duodenum and skeletal muscle In turn down.