^99mTc—谷胱甘肽药盒的制备和实验研究

目的：研制一种新型亲炎症或感染的99mTc标记谷胱甘肽（GSH）。报道其制备、质控及药代动力学。方法：用氯化亚锡作还原剂，制备冷冻干燥99mTc标记GSH一步法药盒，用纸层析法鉴定99mTc-GSH标记率及标记稳定性，测定标记产物99mtc-GSH的理化性质、生物学性质，初步试用于临床。结果：室温下该药盒与99mTcO4混合30分钟后，得标记率大于99％的99mTc-GSH，标记方法简便；标记后24小时测定其标记率仍大于98％，标记产物稳定性好；药盒放置6月后，标记率大于99％。99mTc-CSH生物分布显示血中清除快，主要经肾清除，其余器官浓聚少。松节油和金黄色葡萄球菌实验炎症模型显像，示踪剂定位明确，T／NT值高（3h为4．65）。药盒的各项技术指标符合药典体内诊断试剂的规定。结论：研制的99mTc-GSH药盒适合于临床探测炎症与感染，特别适合于我国国情。

PREPARATION AND EXPERIMENTAL STUDY OF ~(99m)TC LABELLED GLUTATHIONE KIT

Objective: 99mTc labelled glutathione is a novl agent for detecting infechon and inflammation.This paper reports the preparation, quality control, and phannaco kinetics of this imaging agent. Methods:One-step kit of glutathione was prepared by stannous chloride reduction method. Labelling yield and radiochemical purity were then determined by paper chromatography. Biological properties were evaluated by pharmacologic experiments. Results: 99mTc-GSH could be prepared by adding 99m TcO to the kit for 30min at room temperature and showd high radiochemical purity of 99% . More than 98% of radioactivity was retained after keeping Ihe labelled product 24 hours post-labelling. The sheir life of the kit when kept refrigeratal was at least 6 months. Rapid blood clearane was observed.The main route of clarce was via the kidneys, with no significant accumulation in any other omps. Scintigraphic studies in experimental rats and rabbits demonstrated high levels of accumulation of 99mTc-GSH in turpentine- and staphylococcus aureus-induced inflammation (3 hour target- to -nontarget ratio 4. 65: 1). Conclusions: This study documents a new kit developed for the preparation of 99mTc-GSH suitable for the scintigraphic assessment of inflammation and infection.