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用发生器产生的188Re对碘油进行放射性标记用于肝脏肿瘤治疗。

Radiolabelling of Lipiodol with generator-produced 188Re for hepatic tumor therapy.

作者信息

Wang S J, Lin W Y, Chen M N, Hsieh B T, Shen L H, Tsai Z T, Ting G, Knapp F F

机构信息

Department of Nuclear Medicine, Veterans General Hospital-Taichung, Taiwan.

出版信息

Appl Radiat Isot. 1996 Mar;47(3):267-71. doi: 10.1016/0969-8043(95)00300-2.

Abstract

In this study we prepared and analyzed the biodistribution of 188Re-labelled Lipiodol ([188Re]-Lipiodol) in rats after intrahepatic arterial injection. EDTB was synthesized by condensation of 1,2-benzenediamine and ethylenediaminetetraacetic acid (EDTA). The labelling efficiency of [188Re] Lipiodol was determined to be greater than 97% by ITLC developed with n-hexane. Following incubation of the [188Re] Lipiodol with an equal volume of serum at 37 degrees C for 48 h, ITLC indicated good in vitro stability. Approximately 7.4 MBq [188Re] Lipiodol was injected in each rat via the hepatic artery and samples of liver, spleen, muscle, lung, kidney, bone, whole blood and testis were obtained. [188Re] Lipiodol tissue concentrations showed that after 1 h intrahepatic injection most of the radiotracer was retained in the liver, and was eliminated slowly with a biological half-life of 33.5 h. Radioactvity levels in the lung, kidney and blood were moderate at 1 h, and declined rapidly over time. In the spleen, muscle, testis and bone, radiation levels were insignificant. These initial results indicate that -188Re- Lipiodol may be a potential radiopharmaceutical agent for the treatment of liver tumors.

摘要

在本研究中,我们制备并分析了肝动脉内注射后188Re标记的碘油([188Re]-碘油)在大鼠体内的生物分布。乙二硫丁二胺(EDTB)由1,2-苯二胺与乙二胺四乙酸(EDTA)缩合而成。用正己烷展开的ITLC法测定[188Re]碘油的标记率大于97%。将[188Re]碘油与等体积血清在37℃孵育48小时后,ITLC显示其体外稳定性良好。每只大鼠经肝动脉注射约7.4 MBq的[188Re]碘油,并获取肝脏、脾脏、肌肉、肺、肾、骨、全血和睾丸的样本。[188Re]碘油的组织浓度显示,肝内注射1小时后,大部分放射性示踪剂保留在肝脏中,并以33.5小时的生物半衰期缓慢消除。1小时时,肺、肾和血液中的放射性水平适中,并随时间迅速下降。在脾脏、肌肉、睾丸和骨骼中,辐射水平微不足道。这些初步结果表明,188Re-碘油可能是一种治疗肝肿瘤的潜在放射性药物。

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