基于喹啉型配体的99mTc-和99mtcn -放射性药物的制备、高效液相色谱研究及其生物学行为

John Baldas, John Bonnyman
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引用次数: 1

摘要

通过配体交换99mTcNCl4−和亚铁还原99mTcO4−制备了氧(ox)、硫氧(tox)和8-羟基-5-喹啉磺酸(HQS)的99mtc -配合物。HPLC研究表明,99mTcN-tox制剂几乎为纯TcN(tox)2。99mTc(Sn)-ox在HPLC上产生了多个峰,其中主峰为TcO(ox)2Cl。未发现其他色谱峰的tc配合物。小鼠的生物分布研究表明,除99mTc-HQS外,所有复合物基本上都通过肝胆途径被清除。99mTc-HQS制剂由于喹啉环上磺酸基的存在增加了配合物的水溶性,肾脏清除率增加。
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Preparation, HPLC studies and biological behaviour of 99mTc- and 99mTcN-radiopharmaceuticals based on quinoline type ligands

99mTc-Complexes of oxine (ox), thiooxine (tox) and 8-hydroxy-5-quinolinesulphonic acid (HQS) were prepared by ligand exchange of 99mTcNCl4 and by stannous and dithionite reduction of 99mTcO4. HPLC studies showed that the 99mTcN-tox preparation was almost pure TcN(tox)2. 99mTc(Sn)-ox yielded a number of peaks upon HPLC with the major peak being identified as TcO(ox)2Cl. No other Tc-complexes responsible for other chromatographic peaks were identified. Biodistribution studies in mice showed that all complexes except 99mTc-HQS were cleared essentially by the hepatobiliary pathway. The 99mTc-HQS preparations showed increased renal clearance due to the increased aqueous solubility of the complexes resulting from the presence of the sulphonate group on the quinoline ring.

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