^3H示踪法研究来乐司酮在动物体内的分布与排泄

The Study on Distribution and Excretion ofLyreston in Animals With 3H Tracer

进行了来乐司酮的氚标记,所得标记物的比活度为3.61TBq/g,纯化后放化纯度>95%;同时对该标记物在大白鼠体内的分布与排泄进行了研究。结果表明:来乐司酮能分布到大白鼠的各组织脏器中;其在卵巢中的分布量仅次于肝脏和肾上腺,其吸收量在0.5h时达到高峰,且在子宫中24h内可以保持一定的浓度,即可达到止早孕的目的;其在脊髓、脑和小脑中的分布较少,表明来乐司酮对中枢神经系统影响不大;来乐同酮主要经粪便排出,72h经粪和尿排出量占负荷量的62.84%,表明该药在体内没有积累致毒,可作为新药开发。

Lyrestone is labeled with 3H, the specific acitvity is 3.61 TBq/g and the radiochemical purity is over 95% after purification. Its distribuition and excretion in rats are studied at the same time. The results indicate that lyrestone can distribute the main organs. The absorption in ovary is only less than liver and suprarenal, and its maximum absorption is appeared at 0.5 hours.The concentration in uterus can keep a little varion within 24 hours. The absorption in spinal cord, brain and cerebellum is very little. So, lyrestone may be studied as a kind of new medicine.