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放射治療與腫瘤學

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篇名 肝癌治療核醫藥物[?I/[fef3]]Iododeoxyuridine 之合成與配方研究
卷期 5:4
並列篇名 The Preparation and Formulation Study on [?I/[fef3]]Iododeoxyuridine Radiopharmaceutical for Hepatoma Therapy
作者 王信二季匡華顏上惠陳富都周衛樂黃廣良魏孝萍丁幹
頁次 285-291
關鍵字 核醫藥物腫瘤治療RadiopharmaceuticalCancer therapy5-iodo-2'-deoxyuridineLipiodolTSCI
出刊日期 199812

中文摘要

     目的:肝癌是目前臺灣男性惡性腫瘤死亡率最高的癌症,本文敘述肝癌放射治療藥物 [ ?哈? ]UdR 之治療機制、製備方法及安定性分析。 材料與方法:本研究以自行合成之5-tributylstannyl-2'-deoxyuridine (Bu ?? SnUdR) 為前驅物進行放射性碘標幟,反應完成後加入適量 gentisic acid,再經冷凍濃縮純化即得到 [ ?哈? / ?鞷? ]UdR 凍晶小瓶成品。 結果: 自製之 [ ?哈? / ?鞷? ]UdR 凍晶小瓶, 於使用前加入適量生理食鹽水或lipiodol 溶液配成所需之放射活性濃度,即可供肝癌或其他惡性腫瘤治療研究之用。 二種配方之溶液放射化學純度均可達 97% 以上。 本研究進行一系列之 [ ?哈? / ?鞷? ]UdR 安定性試驗, 結果顯示添加 gentisic acid 對 [ ?哈? / ?鞷? ]UdR 溶液或凍晶成品均可明顯增加其貯存安定性, 而凍晶成品之安定性遠優於溶液成品。 結論:本研究製備完成之 [?哈? / ?鞷? ]UdR 核醫藥物,放射化學純度高且安定性佳, 可提供國人進行肝癌或其他惡性腫瘤治療研究之用。

英文摘要

     Purpose:Hepatoma is one of the most prevalent male cancers in Taiwan.This paper investigates the interaction mechanism, preparation, formulation andstability of 5-[ ?哈? / ?鞷? ]-iodo-2'-deoxyuridine as a potentialradiopharmaceutical for hepatoma and cancers treatment. Materials andMethods:The self-synthesized 5-tributylstanny-2'-deoxyuridine (Bu ?? SnUdR),used as a precursor, was radioiodinated to produced [ ?哈? / ?鞷? ]IUdR. Afteradding the stabilizer, gentisic acid, the resultant reaction mixture wasdispensed and lyophilized to give the [ ?哈? / ?鞷? ]IUdR hot kits. Results:Thelyophilized [ ?哈? / ?鞷? ]IUdR hot kit was added with an appropriate amount ofnormal saline or lipiodol prior to preclinical hepatoma treatment studies. Theradiochemical purity for the studied formulation was higher than 97%. Whengentisic acid was used as a stabilizer, the stability of [ ?哈? / ?鞷? ]IUdR wassignificantly increased, and the stability of lyophilized form is far betterthan that of solution form. Conclusion:A stable radiopharmaceutical [ ?哈? / ??Ⅰ ]IUdR with high radiochemical purity and specific activity was prepared inthis study. Its use for preclinical and clinical studies on hepatoma and cancerstherapy will be carried out in the further investigation.

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