骨肿瘤治疗药物的研究Ⅱ.￣153Sm-EDTMP的生物性质评价

摘要: 全面评价了￣１５３Ｓｍ－ＥＤＴＭＰ（乙二胺四甲撑膦酸）的生物学性质。对大鼠注入１６８ＭＢｑ￣１５３Ｓｍ－ＥＤＴＭＰ（相当于人体用量１８．５ＭＢｑ／ｋｇ的６４倍），未观察到毒副作用，血象无明显改变，组织病理学检验主要脏器正常。在小鼠体内，注入后３ｈ，骨胳摄取率达峰值（２６．４４％／ｇ±２．５３％／ｇ），肝脏及其它软组织摄取很低；血清除快，优于临床骨显像剂￣９９Ｔｃ￣ｍ－ＭＤＰ（甲撑二膦酸）和￣９９Ｔｃ￣ｍ－ＰＹＰ（焦膦酸）；动物骨显像清晰，可与￣９９Ｔｃ￣ｍ－ＭＤＰ媲美；￣１５３Ｓｍ－ＥＤＴＭＰ能高度浓集于骨损伤部位。在大鼠体内，骨损伤部位的放射性与正常部位之比值为１２．４（８．６－１５．５）。实验结果表明：￣１８５Ｓｍ－ＥＤＴＭＰ具有优良的生物学性质，值得作深入、广泛研究，以尽快用于人类骨癌的治疗。

Abstract: STUDIES ON BONE TUMOR THERAPEUTIC RADIOPHARMACEUTICALSⅡ．BIOLOGICAL EVALUATION OF ~(153)Sm-EDTMPLUO SHUNZHONG；PU MANFEI；QIAO JIAN；LIU ZHONGLIN；ZHANG CHANYING；ZHAO PENGJI；FU YIBEI（Institute of Southwest Nrclear Physics and Chemmistry, Chengdu，610003）DENG HOUFU（Department of Nuclear Medicine，the First Affiliated Hospital of Huaxi Medical College，Chengdu，610041）ABSTRACT~(153)Sm-EDTMP （ethylene diamine tetramethylene phosphonic acid），a promising therapeuticagent for pain dissemination of bone tumor，has been recently synthesized in our laboratory. Thispaper deals with its behavior in animals. Biodistribution studies on rats demonstrate that~(153)Sm-EDTMP has a high skeletal uptake（bonic peak value 63． 04％±8． 10％at 3h post-injec-tion），a long term retention in bone（over 4 days）but a much lower uptake of liver and othersoft-tissues. The blood clearance of ~(153)Sm-EDTMP iS faster than that of both ~(99)Tc~m-MDP（methylene diphosphonic acid ） and ~(99)Tc~m-PYP（pyrophosphonic acid），which have been widelyused as bone scaning agents in clinic.It＇s imaging in rabbits is execllent，comparing favorably withthat of ~(99)Tc~m-MDP. No toxicity is observed when ~(153)Sm-EDTMP is injected in mice with a dosageup to 11． 1 GBq／kg，60 times of that of a 50kg patient．The ratio of the lesion to the normal bonein mice is 12．4（ranging from 8． 6 to 15． 5）． The above experimental results on animals providethe scientific basis for treating bone tumor in human beings with ~(153)Sm-EDTMP.Key words Bone tumor therapeutic agents ~(153)Sm-EDTMP BiodistributionBlood clearance Bone image