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对８名健康志愿者进行９９ｍＴｃｔｅｔｒｏｆｏｓｍｉｎ的临床前试验。采用一天或两天显像方案，行９９ｍＴｃｔｅｔｒｏｆｏｓｍｉｎ运动负荷和静息显像。通过采血和留尿测定药代动力学参数；采用全身扫描及感兴趣区等技术进行人体分布、靶／非靶比值、有效显像剂量和显像方案研究；依ＭＩＲＤ法估算各种用药情况下的内照射吸收剂量，进行辐射安全评价。结果：９９ｍＴｃｔｅｔｒｏｆｏｓｍｉｎ符合一次静脉给药的药代动力学二室模型，血药总清除率为１２７０ｍｌ／ｍｉｎ；心肌摄取较高，以百分注射剂量（％ＩＤ）为单位，给药后５分钟和６０分钟，运动负荷显像分别为３４０±０１３和２３６±０１９，静息显像则为３１１±１０２和２２２±０６８，前者摄取略高；在２７０～９２５ＭＢｑ给药剂量范围内，一天或两天方案的平面及ＳＰＥＣＴ显像图同样清晰，肝和肺本底低；内照射吸收剂量符合安全标准。临床前试验证明，９９ｍＴｃｔｅｔｒｏｆｏｓｍｉｎ安全有效，这为临床应用提供了依据。
Pre-clinical trials of 99mTc-tetrofosmin were performed on eight healthy volunteers. Using one or two days imaging program, 99mTc trufosmin exercise load and resting imaging. Pharmacokinetic parameters were determined by blood sampling and urinary retention; studies of body distribution, target / non-target ratio, effective imaging dose and imaging protocols were performed using whole body scanning and ROI techniques; Of the internal radiation absorbed dose, radiation safety assessment. Results: 99mTctetrofosmin was consistent with a intravenous pharmacokinetic two-compartment model, the total blood clearance of 1270ml / min; higher myocardial uptake, the percentage of injection (% ID) as a unit, the administration After 5 minutes and 60 minutes, exercise load imaging were 3 40 ± 0 13 and 2 36 ± 0 19, resting imaging was 3 11 ± 1 02 and 2 22 0 68 , The former intake slightly higher; in the dose range of 270 ~ 925MBq, one day or two days plans planar and SPECT imaging clear, liver and lung background is low; internal dose absorbed dose in line with safety standards. Preclinical testing proves that 99mTctetrofosmin is safe and effective, which provides the basis for clinical application.