DTPA-2SN的合成及其99Tcm标记

合成了DTPA-2SN（二乙烯三胺二乙酰二磺胺），并对其化学结构进行了鉴定；制备了DTPA双酸酐（DTPAA），通过DTPAA与磺胺反应合成DTPA-2SN，并对其进行了99Tcm标记。采用n(K222):n( K2CO3)薄层层析法测定标记率，Sep-Pak C18小柱纯化，鉴定放化纯度。并观察其体外稳定性。结果显示DTPAA产率为85%，DTPA-2SN的产率为80%，二者经鉴定与其化学结构式相符。DTPA-2SN易于被99Tcm标记，标记率可达90%±3%。连续观察4h 99Tcm-DTPA-2SN放化纯度均大于90%，稳定性良好。     

125I标记紫杉醇的方法

摘要:采用改良的氯胺T法,先用稳定的NaI与紫杉醇作用,再以放射性Na125I标记紫杉醇(paclitaxel),建立了125I标记紫杉醇的方法。采用纸层析及HPLC测定标记产物的标记率、纯化后放射化学纯度,采用纸层析测定标记产物在不同温度、储存溶剂条件下的体外稳定性,红外光谱鉴定产物。改良Ch-T法所得标记产物的标记率与硝酸氧化法和传统氯胺T法相比较。结果显示,采用改良氯胺T法标记率约63.1%±5.7%,放射化学纯度约96.3%±1.3%;标记物储存于4℃生理盐水或乙醇储存体系中24h、120h,放化纯度分别＞95%和约90%;在血浆中稳定性也较好,在4℃ 、37℃放置24h,放化纯度分别为92.3%±0.4%、89.5%±0.6% 。以上结果表明,改良氯胺T法标记紫杉醇方法简便,标记率高,标记产物稳定性较好,能够满足放射性示踪实验的要求。     

在柱水解法自动化合成18F-氟代乙酸盐

采用 TRACERlab FXF-N 自动化合成仪,以溴代乙酸苄酯为前体,经亲核氟化、在柱水解两步反应及Sep-Pak小柱分离纯化制备18F-FAC注射液.总合成时间＜20 min,未校正放化产率达60%,放化纯度＞95%.在柱水解法适于商售2-18F-2-脱氧-D-葡萄糖(18F-FDG)全自动化合成模块自动化合成18BF-FAC.     

外周苯二氮卓受体示踪剂131I-CLINDE的合成和标记

本文报道CLINDE改进的合成方法及其同位素131I-标记.标记前体由5-氯-2-氨基吡啶与溴代酮酰胺缩合制得.标记产物经三烷基锡化、过氧化氢-碘脱锡化而得.产物经反向HPLC分离纯化.结果显示,标记前体总收率30.8%,标记物放化得率80%,TLC和HPLC检测放化纯度大于98%.表明该法简便易行,放化得率好,产物纯度(包括放射化学纯度)高.     

11C/18F-乙酸盐在CFN-MPS200上的自动合成

采用CFN-MPS200多功能合成模块分别进行11C-乙酸盐(11C-Acetate)和18F-乙酸盐(18F-Acatate)合成,并用TLC法和HPLC法进行质量分析。将11CO2释放到1.0 mol/L甲基溴化镁的四氢呋喃溶液中,2 min后用1 mol/L盐酸水解,反应液经ON Guard-Ag、ON Guard-H柱纯化后,再经PS-OH柱吸附,用生理盐水淋洗,最后由CM柱纯化并经无菌滤膜过滤得到11C-乙酸盐;合成时间约为10 min,不校正放化合成产率(53.5±5)%(n=6)。18F-与溴代乙酸苄酯发生取代反应,经C-18柱吸附去除杂质后洗脱,碱水解后经IC-H、PS-2、氧化铝柱纯化后通过无菌滤膜得到产品18F-乙酸盐;合成时间为40 min,不校正放化合成产率(20.2±5)%(n=5)。分别对两类化合物进行TLC和HPLC分析,以95%乙腈水溶液(V∶V)为TLC的展开剂,比移值Rf分别为0.31 min与0.60 min,放化纯度大于99%;HPLC进样质控,紫外检测器和放射性检测器的出峰时间均在2.3~2.4 min之间,化学纯度和放化纯度大于99%。11C-乙酸盐和18F-乙酸盐的合成均由CFN-MPS200多功能合成模块自动合成,过程简单,合成产率稳定,放化纯度和化学纯度高,可以满足临床使用。     

三羰基锝([99mTc(CO)3(OH2)3]+)标记 Morpholino寡核苷酸

采用三羰基锝药盒制备三羰基锝([99mTc(CO)3(OH2)3]+),并以DTPA作为双功能螯合剂,标记人工合成的Morpholino寡核苷酸.高效液相色谱(HPLC)证实,此方法三羰基锝产率大于90%,且产率稳定;Morpholino 寡核苷酸的标记率为(63±7)%,纯化后比活度为(9.62±1.26)GBq/μg;标记的Morpholino寡核苷酸在生理盐水及新鲜人血清中经过48 h仍保持其稳定性(＞90%),并保持与其互补链的杂交特性.总之,药盒法制备三羰基锝是一种简单而可靠的方法.Morpholino可以被三羰基锝成功标记并保持其生物活性.     

表皮生长因子受体显像剂~(18)F-FEA-Erlotinib的自动化合成

通过"点击化学"方法尝试埃罗替尼(Erlotinib)的~(18)F标记,探索其全自动放化标记并进行初步评价。使用国产PET-MF-2V-IT-I合成模块,以2-~(18)F-氟叠氮乙烷(~(18)F-FEA)为放射化学反应中间体,通过"点击化学"反应制备~(18)F-FEA-Erlotinib,产物经半制备高效液相色谱(High Performance Liquid Chromatography,HPLC)分离、C-18柱富集,最后经乙醇淋洗即得。~(18)F-FEA-Erlotinib自动化合成时间70 min,总放射化学产率为(54±2)%(n5,衰变校正),放射化学纯度大于99%,放射性比活度高于200 MBq·μmol~(-1),K2.2.2含量低于10 mg·L~(-1),无菌无热原符合要求,体外稳定性好,具有和Erlotinib相似的亲脂性。自动化合成~(18)F-FEA-Erlotinib操作简便,高效可靠,质量控制符合要求,能满足科研及临床用药要求,本工作为进一步研究~(18)F-FEA-Erlotinib靶向表皮生长因子受体(Epithelial Growth Factor Receptor,EGFR)的肿瘤正电子断层扫描(Positron Emission Tomography,PET)显像奠定了良好基础。     

乏氧组织显像剂99Tcm-HL91冻干药盒的研制

以酒石酸亚锡为还原剂,制备了无菌无热原的HL91药盒,并对药盒进行了99Tcm标记.条件实验结果显示:pH和酒石酸亚锡的量对99Tcm-HL91标记率的影响较大,pH为7～9时,标记率＞90%,pH过高,HL91配体出现沉淀;酒石酸亚锡含量在5～30 μg时,标记率＞90%;HL91含量为1 mg.由此确定每支冻干品药盒中含有1 mg HL91、20 μg酒石酸亚锡、pH 8～8.5.按照国家药典规定对药盒进行急性毒性实验、无菌和无热原检验合格;标记后的注射液室温5 h内稳定;冻干药盒室温保存1个月、冷冻保存3到6个月,标记后放化纯度仍大于90%.     

125I示踪法检测西夫韦肽在生物体内的代谢过程

采用 Iodogen法标记了西夫韦肽(sifuvirtide)，并用S-100 HR凝胶柱分离纯化标记物。125I-sifuvirtide放化纯度＞99.0%，比活为3.9 GBq•g-1；标记后的蛋白仍具有一定生物活性。三氯醋酸(TCA)沉淀法测定125I-sifuvirtide在生物样品中含量，血浆中125I-sifuvirtide 的放射性活度为286.5-26125.5 Bq•mL-1时，线性为0.9998±0.0005，回收率为72.3%±6.9%。猕猴静脉和皮下推注125I-sifuvirtide后，血浆TCA酸沉放射性浓度时间曲线符合二房室模型；皮下给药后平均消除半衰期为95.83 h，达峰时间平均为3.35 h，平均绝对生物利用度为85.2%。     

β-榄香烯三羰基铼衍生物的放射化学合成

本文报道了β-榄香烯三羰基铼衍生物的合成及其同位素188Re标记.标记配体由β-榄香烯与双功能螯合剂二(2-吡啶甲基)-胺反应制得.标记产物直接由配体与fac-[188Re(CO)3(H2O)3] 制得,并经反向HPLC分离纯化.结果显示,标记配体收率为64%,标记产物放化产率40%,经HPLC分离后放化纯度达到95%以上.表明该法简单易行,其标记化合物有可能发展成为一种新的放射性药物.     

Identification of radiation treatment of wheat （Triticum aestivum. L）and rice （Oryza sativa. L） samples using thermoluminescence of contaminating minerals

Food irradiation is gaining popularity worldwide and this technology is important to improve quality and reduce the post harvest losses of food. Because of the rapid commercialization of irradiated foods throughout the world, compliance of different regulations relating to use of technology in different countries and demand of consumers for clear labelling of irradiated foods, there is need for the development of analytical methods to detect radiation treatment of food. Among several methods studied so far, thermoluminescence （TL） is an important method that can be used to find out the irradiation history of food that contain even a very minute amount of dust particles. In this study, the irradiated and unirradiated wheat and rice samples were analyzed using the TL method. The samples were purchased from the local market of Peshawar and irradiated to radiation doses of 0.5 and 1.0 kGy using Co-60 gamma irradiator at the Nuclear Institute for Food and Agriculture （NIFA）, Peshawar. The mineral contaminants were isolated by jet water, ultrasonic treatment, and density gradient. TL glow curves of the isolated minerals from irradiated and unirradiated samples were recorded between the temperature ranges of 50-500℃ using a TL reader. Generally, the glow curves for irradiated samples showed much higher TL intensities （TL1） than the unirradiated samples. The results were normalized by rerradiation of mineral samples to gamma-ray dose of 1.0 kGy followed by determination of the second glow curves （TL2）. The ratio of the area of first glow curve to that of second glow curve （TL1/TL2） was calculated for selected temperature intervals and compared with the recommended values for unirradiated and irradiated samples. Finally, the shapes of the glow curves for irradiated and unirradiated samples were also analyzed. On the basis of these results （comparison of TL-intensities, TL1/TL2 ratios and shapes of the glow curves）, all the irradiated and unirradiated samples of wheat and rice were unequivocally identified.     

Preparation of Zn/TiO2 powder and its photocatalytic performance for oxidation of P-nitrophenol

Zn-doped TiO2 catalysts were prepared using a sol-gel method and characterized by XPS,UV-Vis, BET, XRD in this study. Under the irradiation of simulant sunlight, the photocatalytic activity for the degradation of p-nitrophenol was studied too. After irradiation for 2.5 h, the degradation percentage of p-nitrophenol could rise to more than 80 %. The results showed that the spectrum absorption band edge of Zn/TiO2 powder does not broaden obviously comparing with pure TiO2 powder. Zinc exists as Zn （11）. When calcined at 973 K, there is a new phase as ZnTiO3 in Zn/TiO2 catalyst. The order of photocatalytic activity of Zn/TiO2 catalysts calcined at different temperatures for p-nitrophenol is 773 K 〉 673 K 〉 873 K 〉 573 K 〉 973 K and the photocatalytic activity of Zn/TiO2 catalyst calcined at 773 K is better than TiO2 catalysts heated at the same temperature, and outclasses that of commercial TiO2 catalyst. It also showed that the photocatalytic degradation of p-nitrophenol follows first-order kinetics under the irradiation of simulant sunlight.     

Current status of radiation therapy for prostate cancer

Radiotherapy for the treatment of prostate cancer has been extensively explored in the past. Along with the comprehensive understanding of the biology of prostate cancer and rapid advances in terms of technology, the out- come of treatment for the patients with prostate cancer has improved. The authors review radiotherapy as the primary treatment for the disease, with particular emphasis on the technological advances from both the radiobiological and radiophysics aspects. Nonconventional fractionated irradiation like hyper- or hypo-fractionation has been imple- mented in the clinic, the final results still need to be confirmed in the future. Technological advances like IMRT, IGRT, in the last two decades have significantly improved the delivery of external radiotherapy to the prostate. This has re- sulted in an overall increase in the total dose that can be safely delivered to the prostate, which has led to modest im- provements in the biochemical outcome. However, establishing the standard therapy for prostate cancer remains con- troversial. It is hoped that the next decades will bring continued advances in the development of biologicals that will further improve current clinical outcomes.     

水平管内含空气蒸汽强制对流冷凝换热模型研究

为研究含空气蒸汽在水平管内强制对流冷凝换热特性,基于对传热传质过程的分析,建立了管内为环状流与波状流条件下的流动冷凝换热模型。从潜热、显热和液膜3个环节对整个换热过程进行建模,最终得到计算局部冷凝换热系数的理论关系式。模型预测结果与实验数据的对比表明,二者相对偏差在±20%以内,验证了该换热模型的准确性与适用性。通过进一步的研究发现：从换热管入口至出口,随着冷凝的进行,管内换热主要热阻由液膜热阻向气液界面的凝结热阻转变;主流气体对流换热过程基本可忽略。     

The preclinical pharmacological study of dopamine transporter imaging agent 18F-FP-β-CIT

The paper is to study pharmacologic characteristics of 18F-FP-β-CIT (18F-N-(3-fluoropropyl)-2β- carbomethoxy-3β- (4-iodophenyl)nortropane) as an imaging agent for dopamine transporter. The radiochemical purity of 18F-FP-β-CIT in aqueous solution was over 95% after standing at room temperature for 4h. Biodistribution displayed rapid uptake in rat brain (1.375 %ID/organ at 5min and 0.100 %ID/organ at 180 min) and the striatal uptake was 1.444,0.731, 0.397, 0.230 and 0.146 %ID/g at 5, 30, 60, 120 and 180 min, respectively. The values of striatum/cerebellum,striatum/frontal cortex and striatum / hippocampus in rat's brain at 30 min were 3.38, 2.17 and 2.40 respectively. The uptake in striatum can be blocked by β-CFT, suggesting that 18F-FP-β-CIT binds to DAT peculiarly. The compound was rapidly cleared from monkey's blood. The striatal uptake was bilaterally decreased in the left-sided lesioned PD rats, compared with normal control. Brain PET imaging studies in normal monkey showed that 18F-FP-β-CIT was concentrated in striatum. The test of undue toxicity showed that the dose received by mice was 1250 times as by human, which indicates that 18F-FP-β-CIT is very safe. So 18F-FP-β-CIT is a promising PET imaging agent for DAT with safety and validity.     

Web Services interface of SSRF archive data analysis system

Accelerator database stores various static parameters and real-time data of accelerator. SSRF (Shanghai Synchrotron Radiation Facility) adopts relational database to save the data. We developed a data retrieval system based on XML Web Services for accessing the archive data. It includes a bottom layer interface and an interface applicable for accelerator physics. Client samples exemplifying how to consume the interface are given. The users can browse, retrieve and plot data by the client samples. Also, we give a method to test its stability. The test result and performance are described.     

Investigations on landmine detection by BF3 detector

Experiments were carried out to investigate the possible use of neutron backscattering for the detection of polyethylene (PE) sample buried in the soil. In detection of landmine by neutrons, the neutron detector and its shield play an important role. In this paper, the effects of graphite, heavy water, polyethylene and boric acid moderators on the flux of back scattered neutrons were investigated. We have also experimentally verified the effect of BF3 detector shield and obtained good agreement with theory.     

PLASMA SCIENCE AND TECHNOLOGY AUTHOR INDEX TO VOLUME 16(2014)

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Radioactivity levels in soil of salt field area,Kelambakkam,Tamilnadu,India

Soil samples in and around salt field area have been analyzed for natural radioactivity concentration using gamma ray spectrometer.The activity concentration for ~(232)Th,~(238)U and ~(40)K are ranged from 27.88 to 45.27 Bq/kg, from BDL to 13.30 Bq/kg,and from 135.54 to 381.28 Bq/kg,respectively.The measured activity concentrations for these radionuclides were compared with world average activity of soil.The average activity concentration of ~(232)Th in the present study is 1.19 times higher than world median value while the activity of ~(238)U and ~(40)K is found to be lower. The absorbed dose rates due to these radionuclides were calculated.The average absorbed gamma dose rate due to the presence of ~(232)Th,~(238)U and ~(40)K in soil samples is 36.99 nGy·h~(-1).These results indicate no radiological anomaly. The data presented in this study will serve as a base line survey for primordial radionuclides concentration in the study area.     

Preparation and properties of 117m Sn(IV)-TTHMP in in-vitro and in small animals

In this work,TTHMP was synthesized and labelled with 117m Sn.The preparation conditions,stability and lipophilicity of 117m Sn(IV)-TTHMP were investigated.Biodistribution of the complex in rabbits and mice was studied.It was found that the quantity of TTHMP and pH value of the prepararion solution had vital effects on the labeling yield of 117m Sn(IV)-TTHMP.It was also found that 117m Sn(IV)-TTHMP was hydrophilic and stable at room temperature and 37℃ in open air 117m Sn(IV)-TTHMP showed unexpectedly high bone uptake and bone-to-blood ratio in the animals.This made it potentially useful as an reagent for skeletal scintigraphy and radiotherapy of bone tumors.