Ahmed Muhammad Tauqeer, Yameen Muhammad, Munir Bushra, Asim Sadia, Usman Muhammad, Naqvi Syed Ali Raza, Gillani Jawad Akhtar Hussain, Rasheed Rashid, Shahzad Muhammad Adeel
Department of Chemistry, Government College University, Faisalabad, Pakistan.
Department of Biochemistry, Government College University, Faisalabad, Pakistan.
Pak J Pharm Sci. 2018 Jul;31(4(Supplementary)):1495-1499.
Bacterial infection is one of the vital sources of morbidity and mortality. The development of single photon emission computed tomography (SPECT) radiotracer agents using antibiotics, for targeting in-vivo bacteria, helps in antibiotic dose calibration, targeted infection therapy and reduction in mortality rate. The aim of this study was to appraised Tc-labeling sulfadiazine as a radiopharmaceutical for bacillus infections imaging. Radiolabeling of sulfadiazine with technetium-99m was carried out by subsequent addition of 1.5 mL aqueous solution of sulfadiazine (1mg/mL), 120µg stannous tartrate, gentistic acid as stabilizing agent and 185 MBq normal saline solution of TcO- (pertechnetate) at pH = 5. The reaction mixture was incubated for 40 min at room temperature with light stirring. The quality control analysis (ITLC-SG and paper chromatography analysis) revealed ~ 98% labeling yield. Biodistribution and scintigraphic study was carried using bacillus bacterial infection induced New Zealand white rabbits. Due to the ease of Tc-sulfadiazine conjugation method, high labeling efficiency, shelf stability (>95% up to 6h), blood serum stability (~90% up to 6h) and high uptake in the infected muscle (T/NT =2.21 at H), Tc-SDZ could be used as radiopharmaceutical of choice for further pre-clinical and clinical studies.
细菌感染是发病和死亡的重要原因之一。开发使用抗生素的单光子发射计算机断层扫描（SPECT）放射性示踪剂，用于体内细菌靶向，有助于抗生素剂量校准、靶向感染治疗和降低死亡率。本研究的目的是评估锝标记的磺胺嘧啶作为一种用于芽孢杆菌感染成像的放射性药物。磺胺嘧啶与99m锝的放射性标记是通过依次加入1.5 mL磺胺嘧啶水溶液（1mg/mL）、120μg酒石酸亚锡、作为稳定剂的龙胆酸和185 MBq pH = 5的高锝酸盐生理盐水溶液来进行的。反应混合物在室温下轻轻搅拌孵育40分钟。质量控制分析（ITLC-SG和纸色谱分析）显示标记产率约为98%。使用芽孢杆菌感染诱导的新西兰白兔进行生物分布和闪烁扫描研究。由于锝-磺胺嘧啶偶联方法简便、标记效率高、货架稳定性好（6小时内>95%）、血清稳定性高（6小时内约90%）以及在感染肌肉中的高摄取率（H时T/NT =2.21），锝-磺胺嘧啶可作为进一步临床前和临床研究的首选放射性药物。
