^(99m)Tc(V)-DMSA大鼠体内药代动力学

Pharmacokinetic studies on ^(99m)Tc(V )-DMSA in rats

用改良方法成功制备了五价锝标记的二巯基丁二酸（９９ｍＴｃ（Ｖ）－ＤＭＳＡ）。根据血样时间－放射性曲线，该药在大鼠体内的代谢符合开放型二房室模型。主要动力学参数为Ｔ１／２（α）＝３．４ｍｉｎ，Ｔ１／２（β）＝７０．９ｍｉｎ，Ｖ（ｃ）＝２７２ｍｌ，Ｋ２１＝０．０５８ｍｉｌ－１，Ｋ１０＝０．０３４ｍｉｎ－１，Ｋ１２＝０．１２２ｍｉｎ－１。结果表明，９９ｍＴＣ（Ｖ）－ＤＭＳＡ从血液向组织的分布速度快，分布范围极广，体内消除迅速，基本从血中清除仅需６—７ｈ．为该显像剂的临床应用提供了实验基础。还研究了该药在大鼠血中的存在形式。

Six normal rats were injected intravenously with 99mTc(V )-DMSA. The blood radioactivity vs. time curve showed that pharmacokinetics of 99mTc(V )-DMSA accorded with the two compartment open model. The important kinetic parameters were as follows:T1/2(α )= 3.4min, T1/2(β) = 70.9min, V(c) = 272ml, K21 = 0.058min-1,K10= 0.034min-1 and K12= 0.122min-1. These results indicated the drug was distributed very rapidly and widely from blood to tissues, and its e1Anination was also rapid, eg. an almost complete elimination from blood need only 6-7h. The drug's existing form in rat blood was studied as well.