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[一种用于骨关节炎软骨成像的新型放射性药物:99mTc-CS的制备及动物实验]

[A new radiopharmaceutical for osteoarthral cartilage imaging: preparation and animals experiment of 99mTc-CS].

作者信息

Xie Peng, Qing Chun, Deng Houfu

机构信息

Department of Nuclear Medicine, West China Hospital of Sichuan Uniwrsity, Chengdu 610041, China.

出版信息

Sheng Wu Yi Xue Gong Cheng Xue Za Zhi. 2009 Aug;26(4):799-802.

Abstract

The objective of this research work is to prepare a new and reliable radiopharmaceutical for osteoarthral cartilage imaging. Chondroitin sulfate (CS) was labeled directly with 99mTc by "pretinning" method, the labeling efficiency was 79.30% +/- 1.72% and radiochemical purity was 90.12% +/- 1l.23% after filtration by use of asepsis filter membrane. The biodistribution of 99Tc-CS was studied at 10, 30 min and 1, 2, 3, 4, 5, 6, 7, 8, 9 h respectively after caudal vein injection in normal mice,which showed that the radiolabeled product was washed out from blood quickly, and it was mainly excreted through kidney, but 99mTc-CS had distinctive characteristic of philo- cartilage. Scintigraphy of 99mTc-CS was performed on the rabbit with ostarthritis at 5 h after intravenous injection; the scintigram was clear,and the focus showed increased radiopharmaceutical uptake. The radioactivity ratio of the injured/uninjured side (T/NT) calculated over the region of interest (ROI) was 3.0 +/- 0.6 (P < 0.05). These results indicate that 99mTc-CS is an easily prepared compound with the characteristic of high philo-cartilage and it may be a new ideal cartilage imaging agent.

摘要

本研究工作的目的是制备一种用于骨关节炎软骨成像的新型可靠放射性药物。采用“预锡化”法将硫酸软骨素(CS)直接用99mTc标记,经无菌滤膜过滤后,标记率为79.30%±1.72%,放射化学纯度为90.12%±1.23%。分别于尾静脉注射后10、30分钟及1、2、3、4、5、6、7、8、9小时研究了99mTc-CS在正常小鼠体内的生物分布,结果表明放射性标记产物从血液中快速清除,主要经肾脏排泄,但99mTc-CS具有明显的亲软骨特性。于静脉注射后5小时对兔骨关节炎模型进行99mTc-CS的闪烁显像;闪烁图清晰,病灶处放射性药物摄取增加。在感兴趣区(ROI)计算的损伤侧/未损伤侧放射性比值(T/NT)为3.0±0.6(P<0.05)。这些结果表明,99mTc-CS是一种易于制备的化合物,具有高亲软骨特性,可能是一种新型理想的软骨显像剂。

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