Eisenhut M, Berberich R, Kimmig B, Oberhausen E
J Nucl Med. 1986 Aug;27(8):1255-61.
The kinetics, dosimetry, and response of iodine-131 alpha-amino-(4-hydroxybenzylidene)-diphosphonate ([131I]BDP3) treatment were investigated with patients who had pain symptoms from bone metastases of various primary carcinoma. The blood clearance of [131I]BDP3 was rapid. More than 90% disappeared from the blood pool at 2 hr after injection. The excretion of the activity occurred solely through the kidneys and mean total-body retention at 48 hr was 48.6%. The urinary activity showed a metabolite which must be formed by an in vivo cleavage reaction of a phosphorus-carbon bond. The uptake of in vivo cleaved [131I]iodide in the unblocked thyroid was approximately 0.5%. The effective half-life of [131I]BDP3 in metastatic bone (median 182 hr; range 177-205 hr) proved to be longer than in unaffected areas (145 hr; 140-165 hr). Palliative therapies were performed with 18 patients. They received doses ranging between 6 and 48 mCi [131I]BDP3. The response was 44% complete pain relief, 6% substantial pain relief, 22% minimal improvement, and 28% no change. The duration of response ranged between 1 and 8 wk.
对患有各种原发性癌骨转移疼痛症状的患者，研究了碘-131α-氨基-（4-羟基亚苄基）-二膦酸盐（[131I]BDP3）治疗的动力学、剂量学及反应。[131I]BDP3的血液清除迅速。注射后2小时，超过90%从血池消失。放射性仅通过肾脏排泄，48小时时全身平均滞留率为48.6%。尿液放射性显示出一种代谢产物，它必定是由磷-碳键的体内裂解反应形成的。未封闭甲状腺对体内裂解的[131I]碘的摄取约为0.5%。[131I]BDP3在转移性骨中的有效半衰期（中位数182小时；范围177 - 205小时）经证实比在未受影响区域（145小时；140 - 165小时）更长。对18例患者进行了姑息治疗。他们接受的[131I]BDP3剂量在6至48毫居里之间。反应情况为：44%完全缓解疼痛，6%显著缓解疼痛，22%稍有改善，28%无变化。反应持续时间在1至8周之间。
