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(99m)锝-盐酸多西环素:一种用于细菌感染成像的新型放射性标记抗生素。

(99m) Tc-Doxycycline hyclate: a new radiolabeled antibiotic for bacterial infection imaging.

作者信息

Ïlem-Özdemir Derya, Asikoglu Makbule, Ozkilic Hayal, Yilmaz Ferda, Hosgor-Limoncu Mine, Ayhan Semin

机构信息

Faculty of Pharmacy, Department of Radiopharmacy, Ege University, Bornova, Izmir, Turkey.

出版信息

J Labelled Comp Radiopharm. 2014 Jan;57(1):36-41. doi: 10.1002/jlcr.3135. Epub 2013 Nov 21.

Abstract

Radiolabeled antibiotics are promising radiopharmaceuticals for the precise diagnosis and detection of infectious lesions. Doxycycline Hyclate (DOX) was chosen to investigate new (99m) Tc-labeled antibacterial agent. Ready to use freeze dry kits were formulated with optimum labeling conditions. Human serum stability, sterility, and pyrogenicity of kits were estimated, and gamma scintigraphy, in vivo biodistribution, and histopathological studies with bacterial infected rats were performed. DOX were successfully labeled by (99m) Tc with high radiochemical purity, and the labeled compound was stable in human serum. Kits were sterile, pyrogen-free, and stable up to 6 months. Static images depicted rapid distribution throughout the body and high uptake in bacterial infected thigh muscle. The uptake ratios of radiopharmaceuticals in infected thigh muscle were found above 2 up to 5 h. Five hours after injection, the rats were sacrificed, and biodistribution was determined. Samples of bacterial infected muscle, healthy muscle, blood, liver, spleen, lung, kidney, stomach, intestine, urine and heart were weighed, and the radioactivity was measured by using a gamma counter. The %ID/g of (99m) Tc-DOX was found 0.23 ± 0.06 for infected thigh muscle. According to the imaging, biodistribution, and histopathological studies, the promising characteristics of (99m) Tc-DOX make the new radiopharmaceutical valuable to examine for future studies.

摘要

放射性标记抗生素是用于精确诊断和检测感染性病变的有前景的放射性药物。选择盐酸多西环素(DOX)来研究新型(99m)Tc标记的抗菌剂。用最佳标记条件配制即用型冻干试剂盒。评估了试剂盒的人血清稳定性、无菌性和热原性,并对细菌感染的大鼠进行了γ闪烁显像、体内生物分布和组织病理学研究。DOX成功地被(99m)Tc标记,具有高放射化学纯度,且标记化合物在人血清中稳定。试剂盒无菌、无热原,在6个月内稳定。静态图像显示其在全身快速分布,在细菌感染的大腿肌肉中摄取较高。发现放射性药物在感染的大腿肌肉中的摄取率在2以上,持续5小时。注射后5小时,处死大鼠并测定生物分布。称取细菌感染的肌肉、健康肌肉、血液、肝脏、脾脏、肺、肾脏、胃、肠道、尿液和心脏的样本,并用γ计数器测量放射性。发现(99m)Tc-DOX在感染大腿肌肉中的%ID/g为0.23±0.06。根据成像、生物分布和组织病理学研究,(99m)Tc-DOX的良好特性使这种新型放射性药物对未来研究具有重要价值。

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