- 期刊
肝癌治療核醫藥物[(上標 125)I/(上標 131)I]Iododeoxyuridine之合成與配方研究
The Preparation and formulation Study on [(superscript 125)I/(superscript 131)I]- Iododeoxyuridine Radiopharmaceutical for Hepatoma Therapy
摘要
目的：肝癌是目前台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少[(上標 125)I]IUdR之治療機制、製備方法及安定性分析。 材料與去法：本研究以自行合成之5-tributylstannyl-2'-deoxyuridine(Bu3SnUdR) 為前驅物進行放射性碘標幟，反應完成後加入適量gentlsic acid，再經冷凍濃縮純化即得到[(上標 125)I/(上標 131)I]lUdR凍晶小瓶成品。 結果：自製之[(上標 125)I/(上標 131)I]IUdR 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[(上標125)I/(上標 131)I]IUdR安定性試驗，結果顯示添加gntsic acid對[(上標 125)I/(上標 131)l]IUdR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擾於溶液成品。 結論：本研究製備完成之[(上標 125)I/(上標 131)I]IUdR 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。
並列摘要
Purpose: Hepatoma is one of the most prevalent male cancers in Taiwan. This paper investigates the interaction mechanism, preparation, formulation and stability of 5-[(superscript 125)I/(superscript131)I]-iodo-2'-deoxyuridine as a potential radiopharmaceutical for hepatoma and cancers treatment. Materials and Methods: The self-synthesized 5-ributylstannyl-2’-deoxyuridine (Bu3SnUdR), used as a precursor, was radioiodinated to produce [(superscript 125)I/(superscript 131)I]IUdR. After adding the stabilizer, gentisic acid, the resultant reaction mixture was dispensed and lyophilized to give the [(superscrip 125)I/(superscrip 131)I]IUdR hot kits. Results: The lyophilized [(superscript 125)I/(superscript 131)I]IUdR hot kit was added with an appropriate amount of normal saline or lipiodol prior to preclinieal hepatoma treatment studies. The radiochemical purity for the studied formulation was higher than 97%. When gentisic acid was used as a stabilizer, the stability of [(superscript 125)I/(superscript 131)I]IUdR was significantly increased, and the stability of lyophilized form is far better than that of solution form. Conclusion: A stable radiopharmaceutical [(superscript 125)I/(superscript 131)I]IUdR with high radioehemical purity and specific activity was prepared in this study. Its use for preclinieal and clinical studies on hepatoma and cancers therapy will be carried out in the further investigation.
被引用紀錄
延伸閱讀
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