Preparation and biodistribution of 186,188Re—HEDP for bone tumor therapy

Radionuclides^186,188Re,suitable for tumor therapy and with high specific activity,are prepared through irradiating natural metallic rhenium,instead of costly enriched target,Complexation of rhenium with HEDP(1-hydroxy ethylidene diphosphonate)is mainly dependent on pH values and the reductant concentrations in the medium,and the yield is not less than 0.95 in pH2.0-4.0 and SnⅡconcentration of 0.012-0.018mol/L.The 186,188ReHEDP complex has high stability in vitro and in vivo in the presence of protecting agent,and gives superior biological properties in small animals,similar to those of ^153Sm-EDTMP including faster blood clearance,lower soft tissue residue and higher skeletal uptake with the peak of 0.2576 ID/g at 1h post injection(overseas report 0.0101 ID/g)comparable to that of 153m-EDTMP(0.2644ID/g) at 3h post injection.     

^188Re—硫化铼混悬液药盒的研制

研制了一种药盒,能简单、快速、有效地制备     

Synthesis of highly concentrated,carrier free ^188Re—mercaptoacetyltriglycine

Chelation of ^188Re to compounds such as MAG3 will further reduce the radiation dose to the patient in case of balloon rupture through the rapid excretion from the body.In order to prepae highly concentrated,carrier free ^188Re-MAG3,Sbenzoyl mercaptoacetyltriglycine(S-Bz-MAG3) was synthesized.labeled with carrier free ^188Re.the overall yield of S-Bz-MAG3 is higher than those published in the literature,Dependence of the labeling yield of ^188Re-MAG3 upon concentrations of reducing agent,pH,reaction time,etc.was examined and optimum conditions were confirmed.The concentration procedure was succeeded with Sep-Pak C18 cartridge to obtain highly concentrated ^188Re-MAG3.In the case of optimun conditions.the labeling yield of 188Re-MAG3 was more than 98%.Radiochemical purity of ^188ReMAG3 was more than 92% after 24 hour storage at room temperature.     

^186Re（Sn）—HEDP药盒中冻干品的研究

研究＾１８６Ｒｅ（Ｓｎ）＝ＨＥＤＰ药盒中冻干品的制备，以及冻干品各成份的有效含量的测定，以实现质量控制。同时，研究了反应温度和反应时间对药盒标记的影响以及＾１８６Ｒｅ（Ｓｎ）－ＨＥＤＰ在动物体内的分布情况。初步的动物实验结果表明：＾１８６Ｒｅ（Ｓｎ）－ＨＥＤＰ骨组织吸收高，在血液中的清除速度快。     

Peptides radiolabeled with Re-186/188 and Tc-99m as potential diagnostic and therapeutic agents

Small peptide-based compounds have attracted an enormous interest as carrier molecules to selectively deliver radionuclides to target tissues, sparing critical normal organs. When looking for ＂matched pairs＂ of radionuclides, suitable for radiolabeling of peptides for diagnosis and therapy, technetium and rhenium represent an almost ideal constellation. The important role of technetium-99m and Re-186/188 is based on the decay characteristics, suitable for tumor diagnosis and therapy. Tc-99m and Re-188 are readily available by either a ^99Mo/^99mTc or the ^188w/^188Re radionuclide generator system Furthermore, technetium and rhenium are chemically related and share structural as well as reactive similarities, which prompt an attractive ＂matched-pair＂ situation. This article shows an overview of ^99mTc- and ^186/188Re-radiolabeled peptides that have been tested for their potential use as imaging and therapeutic agents in oncological diseases.     

居里级的^188W—^188Re发生器的研制

在逐步放大试验和钨装载量模拟试验的基础上,成功地制备了数个居里级的     

188Re间接标记单克隆抗体的研究

采用先标记后偶联的方法,以NHS－MAG3为双功能连接剂,研究了用^188Re标记单克隆抗体的各种实验条件,得到了最佳标记方法和偶联方法。标记抗体^188Re-NHS-MAG3-IgG体外稳定性良好。完成了^188Re-NHS-MAG3-GL3在小鼠体内的生物分布实验,结果表明该配合物在体内稳定性良好。     

^153Sm—盐酸平阳霉素的标记及在小鼠体内的分布

研究了     

186W(d,2n)186Re反应制备无载体186Re

１８６Ｒｅ的半衰期为９０．６ｈ,β~－粒子能量中等（最大能量为１．０７ＭｅＶ）,伴随发射可用于显像的１３７ｋｅＶ（９．２％）的γ射线。就核性质而言,１８６Ｒｅ最适宜标记单抗［１］,但遗憾的是,目前市场上可以获得的均为由反应堆生产的有载体中等比活度的１?..     

188Re(Sn)-HEDP药盒的质量和稳定性研究

建立了^188Re(Sn)-HEDP药盒主要成分HEDP(1-hydroxy ethylidene diphosphonic acid)和氯化亚锡含量的分析方法。以标记率、HEDP和氯化亚锡的含量、无菌和内毒素检查为测试项目,按照中国药典对^188Re(Sn)-HEDP药盒进行了影响因素试验(强光、高温和高湿度)和低温保存有效期试验等稳定性研究。