用于治疗应用的钬-乙二胺四甲叉膦酸（Ho-EDTMP）的生产、质量控制和药代动力学研究。

Production, quality control and pharmacokinetic studies of Ho-EDTMP for therapeutic applications.

作者信息

Bahrami-Samani Ali, Bagheri Reza, Jalilian Amir R, Shirvani-Arani Simindokht, Ghannadi-Maragheh Mohammad, Shamsaee Mojtaba

机构信息

Radiopharmaceutical Research and Development Lab (RRDL), Nuclear Science and Technology Research Institute (NSTRI), Tehran, Postal code: 14155-1339, Iran.

出版信息

Sci Pharm. 2010 Jul-Sep;78(3):423-33. doi: 10.3797/scipharm.1004-21. Epub 2010 Jun 9.

(166)Ho-EDTMP is a major therapeutic agent which is widely used in bone palliation therapy. In this study, a (166)Ho-EDTMP complex was prepared successfully using an in-house synthesized EDTMP ligand and (166)HoCl(3). Ho-166 chloride was obtained by thermal neutron irradiation (1 Ã 10(13) ncm(â2)s(â1)) of natural Ho(NO(3))(3) samples (specific activity = 3â5 GBq/mg), dissolved in acidic media. The radiochemical purity of (166)Ho-EDTMP was checked by ITLC (>99%) and stability studies in presence of human serum and final preparation were performed. The biodistribution of (166)Ho-EDTMP and (166)HoCl(3) in wild-type rats was checked by scarification. SPECT imaging of (166)Ho-EDTMP was also performed in wild-type rats. A comparative accumulation study for (166)Ho-EDTMP and (166)HoCl(3) was performed for vital organs up to 48h. Significant bone accumulation (>70%) of the tracer in 48h was observed.

（166）钬-乙二胺四甲基膦酸是一种广泛用于骨姑息治疗的主要治疗剂。在本研究中，使用自行合成的乙二胺四甲基膦酸配体和（166）HoCl₃成功制备了（166）钬-乙二胺四甲基膦酸配合物。通过对天然Ho(NO₃)₃样品（比活度 = 3 - 5 GBq/mg）进行热中子辐照（1×10¹³ n/cm²·s）获得氯化钬-166，将其溶解在酸性介质中。通过薄层色谱法（>99%）检查（166）钬-乙二胺四甲基膦酸的放射化学纯度，并在人血清存在下进行稳定性研究及最终制剂的制备。通过放血法检查（166）钬-乙二胺四甲基膦酸和（166）HoCl₃在野生型大鼠体内的生物分布。还在野生型大鼠中进行了（166）钬-乙二胺四甲基膦酸的单光子发射计算机断层扫描成像。对（166）钬-乙二胺四甲基膦酸和（166）HoCl₃在重要器官中长达48小时的累积进行了比较研究。观察到48小时内示踪剂在骨中的显著累积（>70%）。