Hong Young-Don, Park Kyung-Bae, Jang Beom-Su, Choi Sun-Ju, Choi Sang-Moo, Kim Young-Mi
RI and Radiation Application Team, Korea Atomic Energy Research Institute, 150 Dukjin-dong, Yuseong-gu, 305-353 Daejeon, Republic of South Korea.
Nucl Med Biol. 2002 Nov;29(8):833-9. doi: 10.1016/s0969-8051(02)00329-3.
Liquid radiation sources with beta emitters have advantages of accurate positioning and uniform dose distribution to the vessel walls to prevent the restenosis of coronary artery. As a liquid radiation source, 166Ho-DTPA was prepared and evaluated its in-vivo pharmacokinetic behavior through animal studies.166Ho-DTPA was prepared by simple mixing the Holmium with DTPA at room temperature. The radiolabelling yield was 100% when the DTPA/Holmium molar ratio was >2. Radiolabelling of 166Ho-DTPA was not dependent on the pH range of 1.7-7.5. High radiochemical stability (>98%) was maintained over a period of 6 hours even with a radioactivity ( approximately 11.1 GBq/12 mg of DTPA) stored at room temperature. Biodistribution of 166Ho-DTPA in rats and gamma camera images in rabbits showed that 166Ho-DTPA was quickly excreted via the urinary system. The average of T(max) and T(1/2) of 166Ho-DTPA in the kidneys of rabbits were 3.71 +/- 1.18 min and 9.15 +/- 3.15 min. 166Ho-DTPA is a potential liquid radiation source for radiation brachytherapy to prevent the restenosis of the coronary artery using a liquid-filled balloon.
含β发射体的液体辐射源具有定位准确、血管壁剂量分布均匀的优点，可预防冠状动脉再狭窄。作为一种液体辐射源，制备了166Ho-DTPA，并通过动物研究评估其体内药代动力学行为。166Ho-DTPA是通过在室温下将钬与DTPA简单混合制备而成。当DTPA/钬摩尔比>2时，放射性标记产率为100%。166Ho-DTPA的放射性标记不依赖于1.7-7.5的pH范围。即使在室温下储存放射性（约11.1 GBq/12 mg DTPA）的情况下，6小时内仍保持高放射化学稳定性（>98%）。166Ho-DTPA在大鼠体内的生物分布及在兔体内的γ相机图像显示，166Ho-DTPA通过泌尿系统迅速排出。166Ho-DTPA在兔肾脏中的T(max)和T(1/2)平均值分别为3.71±1.18分钟和9.15±3.15分钟。166Ho-DTPA是一种潜在的液体辐射源，可用于通过充液球囊进行放射性近距离治疗以预防冠状动脉再狭窄。
