目的以99m锝(99mTc)标记钆双胺(Gd-DTPA-BMA)制备99mTc-Gd-DTPA-BMA并对其基本生物学分布特征进行研究,旨在为SPECT-MRI双模式显像剂的应用提供依据。方法以氯化亚锡为还原剂,采用一步法以99mTc分别标记Gd-DTPA-BMA、二乙三胺五乙酸(DTPA),纸层析法测定两标记物标记率、不同pH值及室温下观察稳定性;将99mTc-Gd-DTPA-BMA用生理盐水稀释后注射至小鼠尾静脉,记录注药后1~240 min每克组织百分注射剂量率(%ID/g);取家兔3只耳缘静脉分别弹丸注射99mTc-Gd-DTPA-BMA和99mTc-DTPA,采用SPECT仪以肾动态显像模式行双时相采集,记录分肾摄取百分比(Uptake%)、达高峰时间(Tmax)、半排时间(T1/2)。结果 99mTc-Gd-DTPA-BMA标记率和稳定性均较高,通过静脉注入小鼠体内后主要分布于肾脏;99mTc-Gd-DTPA-BMA和99mTc-DTPA均经家兔肾脏排泄,其他脏器摄取率较低,但前者Tmax及T1/2显著大于后者(P〈0.05)。结论 99mTc标记Gd-DTPA-BMA具有标记率和稳定性较高等优点,所得99mTc-Gd-DTPA-BMA静脉注入体内后主要分布于肾脏并经肾脏排泄;此为SPECT-MRI双模式显像剂的制备及应用提供了依据。
Objective To prepare 99mTc-Gd-DTPA-BMA and investigate its biologic characteristics,and to provide the basis of 99mTc-Gd-DTPA-BMA using as a SPECT-MRI dual-modality agent.Methods Both Gd-DTPA-BMA and DTPA were synthesized,labeled with 99mTc by a stannous chloride reduction method.The radiochemical purity was determined by paper chromatography.Its stability was observed at room temperature and different values of pH.The 99mTc-Gd-DTPA-BMA diluted with normal saline,was injected into mice intravenous.The percentage of the injected dose per gram of tissues mass(% ID/g) was measured at 1to 240 mins after injection;Three rabbits were injected 99mTc-Gd-DTPA-BMA and 99mTc-DTPA through auricular vein,and the dynamic scintigraphy in rabbits were performed by SPECT after injection,the uptake percentage(Uptake%),time to peak(Tmax) and time from peak to 1/2 peak(T1/2) were observed respectively.Results Both labeling efficiency and stability of 99mTc-Gd-DTPA-BMA were high.The highest uptake after injection is kidney.Two labeled compounds were excreted by the kidney,but Tmax and T1/2 of 99mTc-Gd-DTPA-BMA were longer than 99mTc-DTPA(P0.05).Other organs have a little distribution of radiopharmaceuticals.Conclusions The methods of 99mTc labeled Gd-DTPA-BMA have high labeling efficiency and stability.99mTc-Gd-DTPA-BMA was major excreted by the kidney.It is expected to provide the basic information for the further study of SPECT-MRI dual-modality imaging agent.