^(188)Re-TTHMP的合成及其在小鼠体内分布的研究  

Preparation and Bio-Distribution of 188Re-TTHMP

作　　者：蒋树斌[1] 刘业兵[1] 罗顺忠[1] 刘国平[1] 

机构地区：[1]中国工程物理研究院核物理与化学研究所,四川绵阳621900

出　　处：《四川大学学报（自然科学版）》2004年第3期623-627,共5页Journal of Sichuan University(Natural Science Edition)

基　　金：国家自然科学基金(29771027);中国工程物理研究院科学基金(20020537)

摘　　要：作者合成了氨基甲撑膦酸配体三乙烯四胺六甲撑膦酸.以龙胆酸与抗坏血酸为保护剂、通过SnCl2还原188ReO-4制备了188Re TTHMP.研究表明,当还原剂SnCl2用量大于0.5mg及制备体系pH为1.5～3.5和配体TTHMP用量大于25mg时,通过温水浴(85℃)反应30min即可制得标记率高于95%的188Re TTHMP,标记物在体外4d内的放化纯高于92%.由正常小鼠体内分布研究表明,当将放射性注入鼠体1h后,188Re TTHMP能迅速浓集在其骨骼系统内,其峰值达(19.81±3.83)%/g,之后骨骼所摄取的放射性迅速下降,到48h时,其骨骼内的放射性仅保留(6.23±1.52)%/g.TTHMP (triethylenetetraaminehexamethylenephosphonic acid) was synthesized and labeled with 188Re. Also, the stability in vitro and bio-distribution in normal mice of 188Re-TTHMP were investigated. The labelling efficiency of 188Re was more than 95% on the conditions of SnCl2 of more than 0.5mg, TTHMP of more than 25 mg and at the pH value 1.5 to 3.5.188Re-TTHMP was stable in vitro with radiochemical purity of more than 92% in 4d. Bio-distribution experiment indicated that 188Re-TTHMP was principally incepted by bone of mice and the radioactivity got its peak value, (19.81±3.83)×10-2g-1, at 1 h post-injection.However, the retention of 188Re-TTHMP at bone was un-satisfied in that the bone uptake reduced to (6.23±1.52)×10-2g-1 at 48 h post-injection.

关 键 词：^188RE TTHMP 生物分布 标记 

分 类 号：R979[医药卫生—药品] R817[医药卫生—药学]