Ohtake T, Watanabe T, Kosaka N, Momose T, Nishikawa J, Sasaki Y, Iio M, Saihara S, Sugimoto T
Department of Radiology, Faculty of Medicine, University of Tokyo.
Kaku Igaku. 1991 Jan;28(1):71-82.
99mTc-SQ30217 555 MBq (15 mCi) was intravenously injected to 6 healthy subjects to study its safety, pharmacokinetics and the imaging time. Neither side effects nor abnormalities in physical findings, hemato-biochemical tests, urinary test, etc. caused by this agent were observed in any case and its safety was suggested. Radiation dose estimates over the entire body was 4.88 mGy/1,110 MBq (0.488 rad) and that over the major organs was less than 10 mGy and they were within the allowable ranges. 99mTc-SQ30217 showed biphasic disappearance curve in blood with the half-life of alpha-phase 0.02 hour and that of beta-phase 10.14 hours. 99mTc-SQ30217 was considered to show characteristic pharmacokinetics in that the myocardial accumulation was high in an early stage of the administration, but it rapidly decreased. Both heart to liver ratio and heart to lung ratio were high within 10 minutes, but they decreased after 15 minutes. As a result of SPECT imaging of 4 patients with ischemic cardiac disease, the images obtained with 99mTc-SQ30217 at an early period after the administration was as good as those with 201Tl and the appearance of defects in the images with both agents was similar. 99mTc-SQ30217 was considered to be sufficiently useful as a 99mTc-labelled agent for myocardial blood flow.
将99mTc-SQ30217 555兆贝可（15毫居里）静脉注射给6名健康受试者，以研究其安全性、药代动力学和显像时间。在任何情况下均未观察到该药物引起的副作用，也未发现体格检查、血液生化检查、尿液检查等方面的异常，提示其安全性良好。全身辐射剂量估计为4.88毫戈瑞/1110兆贝可（0.488拉德），主要器官的辐射剂量小于10毫戈瑞，均在允许范围内。99mTc-SQ30217在血液中呈现双相消失曲线，α相半衰期为0.02小时，β相半衰期为10.14小时。99mTc-SQ30217被认为具有特征性药代动力学，即给药早期心肌摄取较高，但迅速下降。给药后10分钟内心脏与肝脏比值和心脏与肺比值均较高，但15分钟后下降。对4例缺血性心脏病患者进行单光子发射计算机断层显像（SPECT）成像的结果显示，给药后早期用99mTc-SQ30217获得的图像与用201铊获得的图像质量相当，两种药物图像中缺损的表现相似。99mTc-SQ30217被认为作为一种99mTc标记的心肌血流显像剂具有足够的实用性。
