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本文采用同位素示踪法研究尾静脉注射131I-标记大黄素在大鼠体内的药物动力学和小鼠体内的组织分布.在NBS催化剂作用下,将131I-NaI与大黄素反应得到产物2-131I-大黄素,放射性化学产率为96%,放射性化学纯度>95%,且标记物在大鼠血浆中24h内稳定.131I-标记大黄素在大鼠体内的药物动力学过程符合一室模型,半衰期(t1/2)为0.25h,清除率(CL)为0.007L/(h·kg).小鼠的组织分布特征为肺部和肾脏最高,脑组织最低,其它组织水平基本相似.研究结果表明静脉注射131I-标记大黄素后在体内分布和清除速度较快,主要经过肾脏排泄,且不易透过血脑屏障.
In this paper, the isotope tracer method was used to study the pharmacokinetics of 131I-labeled emodin in the tail vein and the tissue distribution in mice.Under the action of NBS catalyst, 131I-NaI was reacted with emodin to obtain the product 2-131I - Emodin with a radiochemical yield of 96% and a radiochemical purity of> 95%, and the marker is stable in rat plasma within 24 h. The pharmacokinetics of 131I-labeled emodin in rats is consistent with a one-compartment model, The half-life (t1 / 2) was 0.25h, and the clearance rate (CL) was 0.007L / (h · kg) .The distribution of the mice was the highest in the lungs and kidneys with the lowest in the brain and the rest in other tissues. The results showed that intravenous injection of 131I-labeled emodin rapidly distributed and cleared in vivo, mainly excreted by the kidneys and not easily penetrated the blood-brain barrier.