| 赵岩,杨夏,何丽萌,刘楠,邓嘉,陈跃,张伟.国产177Lu标记DOTATATE最佳条件及其产物的性质[J].中国医学影像技术,2023,39(8):1147~1152 |
| 国产177Lu标记DOTATATE最佳条件及其产物的性质 |
| Optimal conditions of labelling DOTATATE with domestic-made 177Lu and properties of the product |
| 投稿时间：2022-12-15 修订日期：2023-03-30 |
| DOI：10.13929/j.issn.1003-3289.2023.08.007 |
| 中文关键词: 小鼠 镥 奥曲肽 体层摄影术,发射型计算机,单光子 |
| 英文关键词:mice lutetium octreotide tomography, emission-computed, single-photon |
| 基金项目:四川省自然科学基金(23NSFSC0635)。 |
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| 中文摘要: |
| 目的 观察以国产177Lu标记DOTATATE的最佳条件及其产物的性质。方法 采用国产177Lu标记DOTATATE,观察DOTATATE用量、pH、反应温度及反应时间对标记产物177Lu-DOTATATE的影响,以确定最佳标记条件;检测最佳标记条件下产物177Lu-DOTATATE的放射化学纯度(简称放化纯度)、其在小鼠体内外的稳定性、于小鼠体内分布特征及SPECT显像特点。结果 国产177Lu标记DOTATATE最佳条件为以1 μg/μl DOTATATE 20 μl、37 MBq/μl 国产177LuCl3原溶液40 μl、醋酸(0.5 mol/L)-醋酸钠(0.5 mol/L)缓冲液40μl及生理盐水200 μl于80℃恒温条件下反应30 min;上述条件下产物177Lu-DOTATATE的放化纯度＞99%、比活度4.9 MBq/μl,在小鼠体内外稳定性良好;对小鼠注射后主要滞留于其肝脏及肾脏,并经肾脏排泄。结论 采用国产177Lu标记DOTATATE时,以醋酸(0.5 mol/L)-醋酸钠(0.5 mol/L)缓冲液代替0.25 mol/L醋酸钠缓冲液可提高标记效率,其产物177Lu-DOTATATE的放化纯度、比活度及稳定性均较佳,且对小鼠注射后主要滞留于其肝、肾并经肾脏排泄。 |
| 英文摘要: |
| Objective To explore the optimal conditions of labelling DOTATATE with domestic-made 177Lu, and to observe the properties of the product. Methods DOTATATE was labeled with domestic-made 177Lu, and the influence of DOTATATE dosage, pH, reaction temperature and reaction time on product 177Lu-DOTATATE were observed to screen the optimal labelling conditions. Under the optimal labelling conditions, the radiochemical purity, stability in vivo and in vitro of mice, distribution characteristics in vivo of mice and SPECT characteristics of 177Lu-DOTATATE were analyzed. Results The optimized labeling conditions of labeling DOTATATE with domestic-made 177Lu were as mix of 1 μg/μl DOTATATE 20 μl, 37 MBq/μl domestic-made 177LuCl3 40 μl, acetic acid (0.5 mol/L)-sodium acetate (0.5 mol/L) buffer 40μl and physiological saline 200 μl and react for 30 min at constant temperature of 80℃. Under the above conditions, the radiochemical purity of 177Lu-DOTATATE was ＞99%, specific activity was 4.9 MBq/μl, with good stability in vivo and in vitro of mice. Experiments and SPECT imaging showed that after injection, 177Lu-DOTATATE mainly remained in liver and kidneys of mice and excreted through the kidneys. Conclusion For labelling of DOTATATE with domestic-made 177Lu, replacing acetic acid (0.5 mol/L)-sodium acetate (0.5 mol/L) buffer with 0.25 mol/L sodium acetate buffer could improve labelling efficiency, and the product 177Lu-DOTATATE had good radiochemical purity, specific activity and stability, which mainly remained in the liver and kidneys of mice after injection and excreted through the kidneys. |
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