新型心肌灌注显像剂^99mTc—Q3的标记方法学研究

为获得高质量的心肌灌注显像剂,作者进行了９９ｍＴｃ－Ｎ,Ｎ'－亚乙基－二（乙酰丙 酮亚胺）二「三（３－甲氧基－１－丙基）膦」（＾９９ｍＴｃ－Ｑ３）的制备方法学研究。采用多元正交试验法进行了制备＾９９ｍＴｃ－Ｑ３最佳配方的筛选;用氯化亚锡化学还原法制备＾９９ｍＴｃ－Ｑ３;用柱沉析法进行＾９９ｍＴｃ－Ｑ３的分离和纯化、质量控制及体外稳定性试验;完成了无菌、热原、安全试验及家兔显像验证。制备９９ｍＴｃ－Ｑ

Methodological study on preparation of a novel myocardial perfusion imaging agent: 99mTc-Q3]

This study was intended to explore the methods of preparing technetium-99m-N, N'-ethylenebis (acetylacetoneiminato) bis tris (3-methoxy-1-propyl) phosphine] (99mTc-Q3) as a newer cationic myocardial perfusion imaging agent. The optimum scheme of technetium labeling on the basis of exploring the effects of differently labeled conditions on radiochemical purity was established by a multivariate orthogonal experimental design. A newer agent for myocardial perfusion imaging was developed based on the optimum scheme by a stannous chloride reduction method. Preparation, separation, purification and quality control were performed by a chromatography. Experiments for stability (in vitro), sterility, apyrogen, safeness, and for imaging in animals were carried out. "A2B2C2" was chosen as the optimum scheme of this labeled complex. There each of A, B and C factors has significant effect on the radiochemical purity, and there is no one-class cross effect on the radiochemical purity between them. The labeling efficiency and radiochemical purity were measured over 99% labeled 10 min later (at R. T.). The stability (in vitro) was good and kept up to 4 hr or testing (range: 92%-99.37%). The prepared product was sterile, apyrogenic and safe. The scintigraphic imaging in rabbits demonstrated that the tracer accumulated early in the heart and the myocardial imaging displayed clearly up to 3 hr. The results of this methodological study demonstrate that not only high quality 99mTc-Q3 can be obtained but also a standardized procedure for labeling all kinds of 99mTc-agents can be set up, and on this basis, the one-step kit of 99mTc-Q3 may be developed.