鎝-99m標誌錯合物應用於缺氧細胞造影劑之合成、鑑定及生物分佈研究

• Main Authors: Han-Wen Cheng, 鄭涵文
• Other Authors: 羅建苗
• Format: Others
• Language: en_US
• Published: 2001
• Online Access: http://ndltd.ncl.edu.tw/handle/23064810513723969866

碩士 === 國立清華大學 === 原子科學系 === 89 === Syntheses, radiochemical characterization and biologic evaluation of 99m'Tc labeled 2-keto-3-ethoxybutyraldehyde bis (thiosemicarbazone) complexes have been investigated in this study. One of the precursors, kethoxal, which is not commercially available, was prepared by the SeO2 oxidation of crotonaldehyde in C2H5OH. The selenium and its by-product were removed by filtrating with Celite as a solid absorbent. Then the filtrate was purified by fractional distillation under reduced pressure, and the product collected at 80ºC. KTS and KTSM2 were obtained by reaction of kethoxal with thiosemicarbazide and 4,4-dimethythiosemicarbazide, respectively. After purification, 5´ 10-4 M of KTS and KTSM2 in ethanol was prepared for 99mTc labeling. The 99mTc labeling was performed under different pH condition and in the presence of a certain amount of saturated stannous tartrate solution. Solvent extraction, thin layer chromatography and electrophoresis were employed for the radiochemical characterization for the 99mTc-KTS and 99mTc-KTSM2 preparations. From the results, it is indicated that 99mTc-KTS presents a highest extraction efficiency (i.e., 69%) in the preparation under pH5 and 0.2 mL of saturated stannous tartrate solution, whereas 99mTc-KTSM2 displays extraction efficiency as high as 90% under pH4 and 0.3 mL of saturated stannous tartrate solution. According to the result of TLC test, no 99mTcO4- is present in the 99mTc-complex preparations. The lipophilicity of 99mTc-KTSM2 is apparently higher than 99mTc-KTS. From the result of electrophoresis, both 99mTc-KTS and 99mTc-KTSM2 are mainly of neutral species. The biodistribution study was carried out for 99mTc-KTSM2 by normal C3H/HeN mice and the Nfsa tumor bearing mice. The clearance from the blood and other organs or tissues are generally very fast either in the normal C3H/HeN mice or in the Nfsa tumor bearing mice. 99mTc-KTSM2 complex is highly retained in intestine at 2 hr postinjection. The radioactivity uptake in tumor seems to be very low. In a preliminary study for autoradiography by 99mTc-KTS and 99mTc-KTSM2, both of the images in tumors in the mice were not obvious probably due to a low-radioactivity injection.