99mTc-地高辛作为潜在心脏成像剂的合成、优化及生物学评价

Synthesis, optimization and biological evaluation of 99mTc-digoxin as possible cardiac imaging agent.

作者信息

Bokhari Tanveer Hussain, Roohi Samina, Hina Saira, Saeed Shabana

机构信息

Department of Chemistry, Government College University, Faisalabad, Pakistan.

Isotope Production Division, Pakistan Institute of Nuclear Science and Technology, P.O. Nilore, Islamabad, Pakistan.

出版信息

Pak J Pharm Sci. 2018 Jan;31(1):19-24.

PMID:29348079

Abstract

Heart imaging radiopharmaceuticals could improve the diagnostic value of routine heart scanning for detecting cardiac disorders. The aim of the study was to prepare high radiochemical purity 99mTc-Digoxin in a yield of about 98%. The optimal conditions for labelling were as follows: 100μg of Digoxin, 2μg of SnCl2•2H2O, room temperature (25±1°C), reaction retention time of 30 min at pH 7. Under these conditions, the radiochemical yield of Tc-Digoxin reaches 98%. In vivo bio distribution was performed in normal Swiss Albino mice at different time intervals after administration of Tc-Digoxin.Scintigraphic study of Tc-Digoxin was performed in rabbits. The heart uptake of Tc-Digoxin was sufficiently high and thus may be a potential myocardial imaging radiopharmaceutical applicable in cardiology.

摘要

心脏成像放射性药物可以提高常规心脏扫描检测心脏疾病的诊断价值。本研究的目的是以约98%的产率制备高放射化学纯度的99mTc-地高辛。标记的最佳条件如下：100μg地高辛、2μg SnCl₂•2H₂O、室温（25±1°C）、pH值为7时反应保留时间30分钟。在这些条件下，Tc-地高辛的放射化学产率达到98%。在给予Tc-地高辛后的不同时间间隔，对正常瑞士白化小鼠进行了体内生物分布研究。对兔子进行了Tc-地高辛的闪烁扫描研究。Tc-地高辛在心脏的摄取足够高，因此可能是一种适用于心脏病学的潜在心肌成像放射性药物。