de Klerk J M, van Dijk A, van het Schip A D, Zonnenberg B A, van Rijk P P
Department of Nuclear Medicine, University Hospital Utrecht, The Netherlands.
J Nucl Med. 1992 May;33(5):646-51.
The pharmacokinetics of 186Re-HEDP, a radiopharmaceutical for palliative treatment of metastatic bone pain, was investigated in 11 patients (17 studies) who suffered from metastatic breast or prostate cancer. Half-life times of 186Re in three blood fractions (whole blood, plasma and plasma water) were 40.1 +/- 5.0, 41.0 +/- 6.0 and 29.5 +/- 6.4 hr, respectively. Time-dependent increase in plasma-protein binding was observed, probably caused by in vivo decomposition of 186Re-HEDP. Total urinary 186Re excretion was 69% +/- 15%, of which 71% +/- 6% was excreted in the first 24 hr after injection. The BSI (i.e., fraction of the skeleton showing scintigraphic evidence of metastatic disease) closely correlated with the fraction of dose non-renally cleared (r = 0.98). This implies that the amount of radioactivity taken up by the skeleton and hence the bone marrow absorbed dose can be predicted from a diagnostic pre-therapy 99mTc-HDP scintigram. The pharmacokinetic behavior indicates that 186Re-HEDP has suitable properties to justify its application.
对11例转移性乳腺癌或前列腺癌患者（共进行17项研究），研究了用于转移性骨痛姑息治疗的放射性药物186Re-HEDP的药代动力学。186Re在全血、血浆和血浆水这三个血液组分中的半衰期分别为40.1±5.0小时、41.0±6.0小时和29.5±6.4小时。观察到血浆蛋白结合随时间增加，这可能是由于186Re-HEDP在体内分解所致。186Re经尿液的总排泄量为69%±15%，其中71%±6%在注射后24小时内排出。骨转移指数（即显示骨转移疾病闪烁显像证据的骨骼部分）与非肾清除剂量部分密切相关（r = 0.98）。这意味着可以根据治疗前的诊断性99mTc-HDP闪烁显像预测骨骼摄取的放射性活度以及骨髓吸收剂量。药代动力学行为表明，186Re-HEDP具有适合应用的特性。
