中华核医学杂志
中華覈醫學雜誌
중화핵의학잡지
CHINESE JOURNAL OF NUCLEAR MEDICINE
2008年
4期
231-233
,共3页
罗世能%郭雪花%叶万忠%谢敏浩%周莲%虞燕华%赵燕%曹国宪
囉世能%郭雪花%葉萬忠%謝敏浩%週蓮%虞燕華%趙燕%曹國憲
라세능%곽설화%협만충%사민호%주련%우연화%조연%조국헌
HMIBP%同位素标记%动物,实验%药代动力学%骨骼%放射性核素显像%MDP
HMIBP%同位素標記%動物,實驗%藥代動力學%骨骼%放射性覈素顯像%MDP
HMIBP%동위소표기%동물,실험%약대동역학%골격%방사성핵소현상%MDP
HMIBP%Isotope labeling%Animals,laboratory%Pharmacokineties%Skeleton%Radionuclide imaging%MDP
目的 通过99Tcm-1-羟基-2-(1-甲基咪唑-2-基)乙烷-1,1-二膦酸(HMIBP)和鲫99Tcm-亚甲基二膦酸盐(MDP)的骨显像质量比较,评价99Tcm-HMIBP作为骨显像剂的可能性.方法 制备HMIBP冻干药盒,对HMIBP及SnCl2-2H2O含量、放化纯、药盒pH值及在4℃下的稳定性等进行了研究.测定99Tcm-HMIBP在正辛醇/水相中的分配系数(P)及血浆蛋白结合率,计算血药清除动力学方程参数.同时研究了HMIBP的半数致死剂量(LD50).新西兰兔静脉注射99Tcm-HMIBP和99Tcm-MDP后同步显像比较.结果 99Tcm-HMIBP药盒含HMIBP 5 mg,SnCl2·2H2O 0.05 mg,药盒pH值为5,标记率和放化纯均为98%;在4℃下放置180 d后标记率为96%.在pH值为7.0和7.4时,P值分别为0.0125和0.0054,血浆蛋白结合率为44.77%.小鼠血药清除动力学方程为C=3.0979 e-0.0721t+0.1250 e-0.0076.HMIBP的LD50为8.2 mg/kg.兔骨显像表明,99Tcm-HMIBP和99Tcm-MDP在3 h时均可获得清晰的图像.结论 99Tcm-HMIBP生物学性能优良,显像效果与99Tcm-MDP相当,可能成为集显像与治疗于一体的骨显像剂.
目的 通過99Tcm-1-羥基-2-(1-甲基咪唑-2-基)乙烷-1,1-二膦痠(HMIBP)和鯽99Tcm-亞甲基二膦痠鹽(MDP)的骨顯像質量比較,評價99Tcm-HMIBP作為骨顯像劑的可能性.方法 製備HMIBP凍榦藥盒,對HMIBP及SnCl2-2H2O含量、放化純、藥盒pH值及在4℃下的穩定性等進行瞭研究.測定99Tcm-HMIBP在正辛醇/水相中的分配繫數(P)及血漿蛋白結閤率,計算血藥清除動力學方程參數.同時研究瞭HMIBP的半數緻死劑量(LD50).新西蘭兔靜脈註射99Tcm-HMIBP和99Tcm-MDP後同步顯像比較.結果 99Tcm-HMIBP藥盒含HMIBP 5 mg,SnCl2·2H2O 0.05 mg,藥盒pH值為5,標記率和放化純均為98%;在4℃下放置180 d後標記率為96%.在pH值為7.0和7.4時,P值分彆為0.0125和0.0054,血漿蛋白結閤率為44.77%.小鼠血藥清除動力學方程為C=3.0979 e-0.0721t+0.1250 e-0.0076.HMIBP的LD50為8.2 mg/kg.兔骨顯像錶明,99Tcm-HMIBP和99Tcm-MDP在3 h時均可穫得清晰的圖像.結論 99Tcm-HMIBP生物學性能優良,顯像效果與99Tcm-MDP相噹,可能成為集顯像與治療于一體的骨顯像劑.
목적 통과99Tcm-1-간기-2-(1-갑기미서-2-기)을완-1,1-이련산(HMIBP)화즉99Tcm-아갑기이련산염(MDP)적골현상질량비교,평개99Tcm-HMIBP작위골현상제적가능성.방법 제비HMIBP동간약합,대HMIBP급SnCl2-2H2O함량、방화순、약합pH치급재4℃하적은정성등진행료연구.측정99Tcm-HMIBP재정신순/수상중적분배계수(P)급혈장단백결합솔,계산혈약청제동역학방정삼수.동시연구료HMIBP적반수치사제량(LD50).신서란토정맥주사99Tcm-HMIBP화99Tcm-MDP후동보현상비교.결과 99Tcm-HMIBP약합함HMIBP 5 mg,SnCl2·2H2O 0.05 mg,약합pH치위5,표기솔화방화순균위98%;재4℃하방치180 d후표기솔위96%.재pH치위7.0화7.4시,P치분별위0.0125화0.0054,혈장단백결합솔위44.77%.소서혈약청제동역학방정위C=3.0979 e-0.0721t+0.1250 e-0.0076.HMIBP적LD50위8.2 mg/kg.토골현상표명,99Tcm-HMIBP화99Tcm-MDP재3 h시균가획득청석적도상.결론 99Tcm-HMIBP생물학성능우량,현상효과여99Tcm-MDP상당,가능성위집현상여치료우일체적골현상제.
Objective Zoledronate has been extensively used for the treatment of tumor-induced hypercalcemia and osteolytic bone metastases.1-hydroxy-2-(1-methylimidazol-2-yl)ethylidene-1,1-bisphos-phonic acid(HMIBP)with similar chemical structure as Zoledronate,was therefore considered to be useful as bone imaging agent.In this study the usefulness of 99Tcm labeled HMIBP for bone imaging was evaluated and the results with the well-established 99Tcm-methylene diphosphonic acid(MDP)imaging was compared.Methods Labeled with 99Tcm,the SnCl2·2H2O quantity,radiochemical purity,pH value and stability at 4℃ of 99Tcm-HMIBP were measured.Besides,the partition coefficient,plasma protein binding rate,hemody-namic parameters of 99Tcm-HMIBP and median lethal dose(LD50)of HMIBP were determined.99Tcm-HMIBP bone imaging was performed in normal New Zealand rabbits and compared with 99Tcm-MDP bone imaging.Results The kit composed of 5 mg HMIBP and 0.05 mg SnCl2·2H2O.The labeling rate was 96% after 180 d storage at 4℃.The radiochemical purity of 99Tcm-HMIBP was 98% at pH 5 and the partition coefficients were 0.0125 and 0.0054 at pH 7.0 and 7.4 respectively.The plasma protein binding rate of 99Tcm-HMIBP was 44.77%.The hemedynamic parameter C valued 3.0979 e-0.0721t+0.1250 e-0.0076 and LD50 was 8.2 mg/kg.The bone images of 99Tcm-HMIBP were fairly well 3 h after the injection.which was comparable to 99Tcm-MDP bone imaging.Conclusions 99Tcm-HMIBP had good biological properties and comparable bone imaging quality with 99Tcm-MDP.It might be a potential agent for both treatment and imaging.
