Goeckeler W F, Stoneburner L K, Kasi L P, Fossella F V, Price D R, Fordyce W A
Central Research and Development, Dow Chemical Company, Midland, MI.
Nucl Med Biol. 1993 Jul;20(5):657-61. doi: 10.1016/0969-8051(93)90036-t.
153Sm-EDTMP is currently undergoing clinical evaluation as a radiotherapeutic agent for the relief of pain associated with cancer metastatic to bone. These clinical studies have demonstrated biodistributions similar to those seen earlier in animals, namely, rapid clearance from blood, selective uptake in bone and in particular metastatic bone lesions. The radioactivity not deposited in bone is cleared through the kidneys into the urine. In this study, urine samples collected from 9 patients injected with 153Sm-EDTMP underwent complexation analysis via Pharmacia SP-Sephadex C25 cation exchange chromatography. The results showed 96.9 +/- 1.7% of the radioactivity in the urine to be present as a complex of 153Sm. An HPLC method was developed and it was demonstrated that different complexes of 153Sm could be separated. A non-radioactive analytical standard of the Sm-EDTMP chelate was synthesized, characterized and shown to have the same HPLC retention profile as the 153Sm-EDTMP drug product. HPLC analysis was performed on six urine samples and in each case a single radioactivity peak with an elution profile the same as that of a 153Sm-EDTMP standard was observed. These results indicate that the 153Sm-EDTMP chelate is excreted intact in the urine of patients.
153钐-乙二胺四甲撑膦酸（153Sm-EDTMP）目前正作为一种放射治疗药物进行临床评估，用于缓解与骨转移癌相关的疼痛。这些临床研究表明，其生物分布与早期在动物身上观察到的相似，即从血液中快速清除，在骨骼尤其是转移性骨病变中选择性摄取。未沉积在骨骼中的放射性物质通过肾脏清除到尿液中。在本研究中，对9例注射153Sm-EDTMP的患者收集的尿液样本，通过Pharmacia SP-葡聚糖凝胶C25阳离子交换色谱法进行络合分析。结果显示，尿液中96.9±1.7%的放射性物质以153Sm的络合物形式存在。开发了一种高效液相色谱（HPLC）方法，并证明可以分离153Sm的不同络合物。合成了Sm-EDTMP螯合物的非放射性分析标准品，对其进行了表征，结果表明其具有与153Sm-EDTMP药品相同的HPLC保留图谱。对六个尿液样本进行了HPLC分析，在每个样本中均观察到一个单一的放射性峰，其洗脱图谱与153Sm-EDTMP标准品相同。这些结果表明，153Sm-EDTMP螯合物在患者尿液中完整排泄。
