乏氧组织显像剂^(99)Tc^m-HL91冻干药盒的研制  

Study on HL91 Single-kit Formulation Labelling With ^(99)Tc^m for Hypoxia Tissue Imaging

作　　者：国毓智 张志勇 朱霖[2] 张剑英[2] 汪建军[2] 李淑艳 

机构地区：[1]北京欣科思达医药科技有限公司,北京102600 [2]北京师范大学化学系,北京100875

出　　处：《同位素》2003年第3期171-174,共4页Journal of Isotopes

摘　　要：以酒石酸亚锡为还原剂,制备了无菌无热原的HL91药盒,并对药盒进行了99Tcm标记。条件实验结果显示:pH和酒石酸亚锡的量对99Tcm-HL91标记率的影响较大,pH为7～9时,标记率>90％,pH过高,HL91配体出现沉淀;酒石酸亚锡含量在5～30μg时,标记率>90％;HL91含量为1 mg。由此确定每支冻干品药盒中含有1 mg HL91、20μg酒石酸亚锡、pH 8～8.5。按照国家药典规定对药盒进行急性毒性实验、无菌和无热原检验合格;标记后的注射液室温5 h内稳定;冻干药盒室温保存1个月、冷冻保存3到6个月,标记后放化纯度仍大于90％。HL91 kit in lyophilized form is obtained by freeze-drying in the presence of stannous tar-trate as reductive agent, and labelled with 99Tcm. The optimal labelling condition is determined by pH and the content of stannous tartrate. Under the condition of pH7~9, 1 mg HL-91,5~30μg stannous tartrate, the labelling yield is above 90%. Every kit formulation contains 1 mg HL91, 20 μg stannous tartrate,pH8~8. 5. The kit is eligible according to acute toxicity,asepsis and pyrogen-free examinations. The labelled complex is stable in about 5 h at room temperature. Stability studies show that freeze-dried formulations stored at room temperature for 1 month and in refrigeratory from 3 to 6 months, the radiochemical purity are still above 90% .

关 键 词：乏氧组织显像剂 冻干药盒 酒石酸亚锡 还原剂 ^99TC^M 锝 

分 类 号：R81[医药卫生—放射医学] R981[医药卫生—临床医学]