Yigit Ugur Sezai, Lambrecht Fatma Yurt, Unak Perihan, Biber Fazilet Zümrüt, Medine Emin Ilker, Cetinkaya Berkan
Cigli High School, Izmir, Turkey.
Chem Pharm Bull (Tokyo). 2006 Jan;54(1):1-3. doi: 10.1248/cpb.54.1.
The aim of this study was to label ascorbic acid with (99m)Tc and to investigate its radiopharmaceutical potential in rats. Ascorbic acid was labeled with (99m)Tc using the stannous chloride method. The radiochemical purity of [(99m)Tc]ascorbic acid ((99m)Tc-AA) was determined by RTLC, paper electrophoresis, and RHPLC methods. The labeling yield was found to be 93+/-5.0%. The maximum labeling yield of (99m)Tc-AA was determined at pH 5 and 25 degrees C. The biodistribution studies related to (99m)Tc-AA were done in male albino Wistar rats. (99m)Tc-AA, which has a specific activity of 13.02 GBq/mmol, was administered into the tail vein of the rats. The rats were sacrificed at 15, 30, 60, and 120 min after the injection by heart puncture under ether anaesthesia. The organs were weighed after removal. Their activities were counted using a Cd(Te) detector equipped with a RAD 501 count system. The %ID/g (% of injected dose per gram of tissue weight) in each organ and in blood was calculated. Maximum uptake of (99m)Tc-AA was observed in prostate and kidneys at the 60th min. (99m)Tc-AA may be a promising radiopharmaceutical for the imaging of prostate and kidneys.
本研究的目的是用(99m)Tc标记抗坏血酸,并研究其在大鼠体内的放射性药物潜力。采用氯化亚锡法用(99m)Tc标记抗坏血酸。通过反相薄层色谱法(RTLC)、纸电泳法和反相高效液相色谱法(RHPLC)测定[(99m)Tc]抗坏血酸((99m)Tc-AA)的放射化学纯度。标记产率为93±5.0%。在pH 5和25℃条件下测定了(99m)Tc-AA的最大标记产率。在雄性白化Wistar大鼠中进行了与(99m)Tc-AA相关的生物分布研究。将比活度为13.02 GBq/mmol的(99m)Tc-AA经大鼠尾静脉注入。在乙醚麻醉下,通过心脏穿刺在注射后15、30、60和120分钟处死大鼠。取出器官后称重。使用配备RAD 501计数系统的碲化镉(Cd(Te))探测器对其放射性进行计数。计算每个器官和血液中的%ID/g(每克组织重量的注射剂量百分比)。在第60分钟时,在前列腺和肾脏中观察到(99m)Tc-AA的最大摄取量。(99m)Tc-AA可能是一种用于前列腺和肾脏成像的有前景的放射性药物。