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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。
Objective: To develop a new type of pro-inflammatory or infected 99mTc-labeled glutathione (GSH). Reported its preparation, quality control and pharmacokinetics. Methods: Stannous chloride was used as reducing agent to prepare freeze-dried 99mTc labeled GSH one-step kit. The 99mTc-GSH labeling rate and labeling stability were identified by paper chromatography. The physicochemical properties of 99mtTc-GSH, Nature, preliminary trial in clinical. Results: 99mTc-GSH with 99mTc-4 labeling rate was obtained after the kit was mixed with 99mTcO4 for 30 minutes at room temperature. The labeling method was simple. The labeling rate was still above 98% at 24 hours after labeling. The stability of the labeled product was good. After placing for 6 months, the marking rate is greater than 99%. 99mTc-CSH biodistribution showed rapid clearance of blood, mainly by the kidneys, the remaining organs less concentrated. Turpentine and Staphylococcus aureus experimental inflammatory model imaging, tracer positioning clear, T / NT value is high (3h 4.65). The kit’s technical indicators in line with pharmacopoeia diagnostic reagents in the provisions. Conclusion: 99mTc-GSH kit developed for clinical detection of inflammation and infection, especially for our national conditions.