^(188)Re(Ⅴ)-DMSA药盒制备及其质量评估  

Preparation and evaluation of ^(188)Re(V)-DMSA kit

作　　者：程竞仪[1] 章英剑[1] 施伟[1] 万丹晶[2] 潘禾戎[1] 蒋长英[1] 

机构地区：[1]复旦大学附属肿瘤医院核医学科,上海200032 [2]复旦大学药学院放射药学教研组

出　　处：《中华核医学杂志》2006年第2期118-119,共2页Chinese Journal of Nuclear Medicine

摘　　要：目的研制^(188)Re(V)-二巯基丁二酸(DMSA)标记配方并制备药盒,评价药盒的质量。方法酸性环境下,SnCl_2·2H_2O还原高价态 ReO_4^-为Ⅴ价,并与 DMSA 反应,制备药盒,以高压液相色谱仪(HPLC)测定该药盒的标记率、标记物的体外稳定性、药盒的稳定性,并与^(99)Tc^m(V)-DMSA在小鼠体内分布比较。结果药盒标记率为100%,标记物室温放置24 h 后标记率>97%;药盒置-20和4℃条件下3个月后,标记率>95%;^(188)Re(Ⅴ)-DMSA 与^(99)Tc^m(Ⅴ)-DMSA 在小鼠体内分布相似,在骨骼高浓聚,经肾脏排泄。结论 ^(188)Re(Ⅴ)-DMSA 药盒性能优良。Objective To study the preparation of ^188Re（Ⅴ）-dimercaptosuccinic acid （DMSA） and to evaluate the quality of^188Re（Ⅴ）-DMSA kit. Methods The complex was prepared by reducing ^188Re in the presence of DMSA with stannous chloride in acid medium at pH = 1.5. Excess stannous chloride was required and the presence of hydrochloric acid didn＇ t reduce the yield from 100%. A large dose of ascorbic acid was used to minimize auto-radiolysis. The labeled rate and stability of the kit and the labeled compound stability in vitro were analyzed by high-performance liquid chromatograms （ HPLC ）. Finally the biodistribution of ^188Re（Ⅴ）-DMSA and ^99Te^m （V）-DMSA in mice was compared. Results The labeled rate was 100% and yield was steady in vitro after the compound was kept in room temperature as long as 24 h （ 〉97% ）. Keeping the kit at -20 ℃ and 4 ℃ for3 months the labeled rate was still 〉95%. Compared with ^99Tc^m（ Ⅴ）-DMSA, the biodistribution of ^188Re（Ⅴ）-DMSA was similar. Both of them accumulated highest in bone and excreted from kidney. Conclusion The quality of ^188Re（Ⅴ） -DMSA kit is satisfactory.

关 键 词：二巯基琥珀酸 铼 放射性同位素 同位素标记 质量控制 

分 类 号：R817[医药卫生—影像医学与核医学]