186,188Re-SZ39的药学性能研究

本工作对单克隆抗体ＭＡｂ－ＳＺ３９的铼标记物进行动物体内稳定性、免疫活性、细胞杀伤能力及对荷人脑胶质瘤裸鼠的抑制离等测试。结果表明标记物细胞杀伤能力强,体内较稳定,且能明显抑制肿瘤的生长,作为一种免疫治疗剂具有良好的应用前景。     

^188Re—labeled McAb 3H11 used as preventive for the peritoneal micrometasis of gastric cancer

In advancing gastric cancer, especially when the serous is invaded, the plantation of cancer cells in peritoneal is common and it affects patients' survival time severely. Based on successfully labeled McAb (monoclonal antibody) 3H11 with ~(188)Re, we investigated the effect of RIT (Radioimmuno-Therapy) with ~(188)Re-3H11 on preventing the peritoneal micrometastasis of gastric cancer cells in nude micc to increase the survival time. After 1×10~6 BGC-823 gastric cancer cells were injected into the peritoneal cavity of each mouse, 45BABL/C nude mice were divided into 9 groups. Each group received different doses of ~(188)Re-3H11 or ~(188)Re-IgG, or saline I.P.16 hours postoperation. The injected volume of each mouse was 1.0mL. The results showed that the survival time depended on the injected doses during 0 to 37 MBq. The survival time was 170±25.3d after 37MBq ~(188)Re-3H11 were treated. It was over 5 times more than that for the saline group and about 3 times more than that for 37 MBq ~(188)-Re IgG gro     

凝聚法和分散法制备^188Re—硫化铼混悬液的比较研究

对聚法和分散法备＾１８８Ｒｅ－硫化铼混悬液的条件进行了比较。条件试验结果表明，凝聚法的最佳条件为Ｎａ２Ｓ２Ｏ３和ＫＲｅＯ４的摩尔比３５：１，反应时间７－８ｍｉｎ；而分散法分别为７０：１和３０ｍｉｎ。随着超声时间的加长，硫化铼的颗粒逐渐变小。从而得出结论：聚凝法虽然比较简单，但标记率不高（约７０％），颗粒小，稳定性差：而分散法的标记率大于９６％，颗粒较大，且７２ｈ内均十分稳定。     

^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 and radioiodinated labeling of p—iodophenyl pentadecanoic acid

A new method for the preparation of p-iodophenyl pentadecanoic acid(IPPA) has been developed.The synthesis are described,and physical properties of IPPA are characterized by IR,1HNMR,elementary analysis and MS.^125I-IPPA can be easily prepared by two methods:direct labeling and solid-phase iodo-exchange labeling,and the yields of labeling are 80% and 65%,respectively,The radiochemical purities are higher than 98% after being extracted with chloroform and hexane.     

186Re对抗人脑胶质瘤单克隆抗体的标记条件及其体外稳定性研究

用＾１８６Ｒｅ对抗人脑胶质瘤单克隆抗体（ＭＡｂ ＳＺ３９）进行了标记。研究了影响标记率的多种因素：如不同转移螯合剂、不同反应时间、ｐＨ及不同的ＳＺ３９还原剂等,最终找到了最佳反应条件,选用低ｐＨ的葡萄糖酸钠－盐酸缓冲溶液,标记率高达９６．２％。通过测量相同反应条件下标记率,发现＾１８６Ｒｅ比活度太阳明显降低标记率。标记物进行了高效液相分离与纯化,并对纯化物作了体个稳定性测试,测定了不同条件下放化纯     

放射性药物~(188)Re标记DTPA的制备和在大鼠体内的分布

球囊导管内充盈β放射性核素防治经皮冠状动脉成形术(PTCA)后再狭窄是一种崭新的技术, 其中,188Re是一种常用的放射性核素。为了尽可能降低在万一球囊破裂的情况下高剂量放射性对人体的损害,利用二乙三胺五醋酸(DTPA)迅速从泌尿系统排出的特点,通过探索188Re标记DTPA的方法和条件,成功地制备了188Re-DTPA化合物,并研究出最佳的标记条件从而使标记产率达到90%以上。188Re-DTPA和188ReO4-在大鼠体内分布的研究结果显示,甲状腺和胃肠道的放射性水平188Re-DTPA组明显低于188ReO4-组,188Re-DTPA经肾脏排泄明显快于188ReO4-,用MIRDOSE 3.0软件估算体内重要脏器的吸收剂量同样也显示了这一结果。188Re-DTPA组和188ReO4-组甲状腺的吸收剂量分别为0.041 nGy/Bq和0.563 nGy/Bq,胃的吸收剂量分别为0.043 nGy/Bq和0.118 nGy/Bq。因此,实验结果认为在血管内照射治疗中188Re-DTPA明显优于188ReO4-。     

Na188ReO4、188Re-DTPA和188Re-MAG3的生物分布及排泄比较

为比较Na^188ReO4、^188Re-DTPA和^188Re-MAG3在冠状动脉再狭窄防治中的优劣,将这三种放射性药物注入到ICR小鼠和SD大鼠体内,观察其在小鼠体内的分布及在大鼠体内的排泄动力学.结果显示,^188Re-MAG3在小鼠体内的血液清除明显快于^188Re-DTPA和Na^188ReO4,并且在各主要组织脏器的吸收也明显低于^188Re-DTPA和Na^188ReO4.注射后2 h,77.28%的^188Re-MAG3经尿液排出体外,而此时^188Re-DTPA 和Na^188ReO4的尿液排出量不到注射剂量的50%.188Re-MAG3在动物体内的行为明显优于^188Re-DTPA和Na^188ReO4,更适于冠状动脉再狭窄的防治.     

Na188ReO4溶液活度测量的标准化研究

摘要：治疗用放射性药品活度与其用药安全性和有效直接相关。为了确保含188Re放射性药品用药安全有效,本工作利用Na188ReO4溶液,对使用活度计测量Na188ReO4 溶液活度的方法进行了标准化研究。利用4π液闪、4πβ-γ符合方法,通过三家单位4套装置测量,确定Na188ReO4溶液标准源的活度量值;再利用已知活度的标准源,对使用活度计测量Na188ReO4 溶液活度的方法进行了标准化研究,确定了测量条件;最后在三个地区的10台不同活度计上进行了活度测量比对试验,结果表明,利用CRC系列活度计测量Na188ReO4溶液活度,各测定值均在标准值的±3%以内。因此,进行标准化标定后,活度计适于测量Na188ReO4溶液的活度。     

~(188)Re诱发人离体外周血淋巴细胞染色体畸变的初步研究

将人离体外周血在不同剂量的188ReO- 4中培养 5 4h ,观察淋巴细胞有丝分裂中期的染色体型和单体型畸变 ,这两种类型的畸变均有随188Re活度的增高而增加的趋势 ,并与活度存在一定的依赖关系 ,染色体畸变以二次多项式的模式为佳。单体型畸变、畸变细胞、染色体断片也可配以直线回归。     

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.     

CR-39固体核径迹探测器的制备和蚀刻性能

用二甘醇双烯丙基碳酸脂(ADC)和过氧化苯甲酸(BPO),经本体热固聚合,研制了一种新型CR-39固体核径迹探测器,它的体蚀刻速度V_B=1.37μm/h,相对灵敏度V_a·V~(-1)_B=1.77,本底径迹密度B=9.8×10~(-5)径迹·mm~(-2)。它具有高灵敏度、低本底以及均匀、稳定的性能。     

国产CR-39记录高注量的He++和H+的蚀刻特性

研究了国产ＳＹ－１型ＣＲ－３９记录加速器加速的高注量的Ｈｅ＾＋＋和Ｈ＾＋的蚀刻特性,对辐照过程中靶室内的环境本底做了观察实验。结果表明,在靶室内直接照射束斑位置以及远至４０ｍｍ处仍能记录到与束斑处相同的离子,而且在高注量离子的束斑区蚀刻后几乎辨不出径迹。进行了刻度实验,给出了ＣＲ－３９记录不同能量的Ｈｅ＾＋＋和Ｈ＾＋的径迹直径响应蚀刻曲线,对高注量束斑区蚀刻后注入新离子的实验表明记录特性不改变。     

CEA、CA19-9、CA72-4、MG-Ag单项及联合检测对诊断胃癌的临床价值

选用CEA，CA19－9，CA72－4，MG－Ag四项肿瘤标志物，应用IRMA进行单项及联合检测，从而为胃癌的早期诊断提供依据，检测结果表明：单项检测阳性率均＞70％，但以MG－Ag阳性率最高（90．4％），次为CA72－4（84．2％），两两组合进行双项联合检测，按双阳性分析，结果显示MG＋CA72－4组合阳性率最高（70．6％），MG＋CA19－9组合次之（64．6％），因此，单项筛选检测，首先MG－Ag；双项组合检测首选MG＋CA72-4为宜，随访可按组织学类型选用适宜的双项组合检测法。