Abstract
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。
Purpose:Hepatoma is one of the most prevalent male cancers in Taiwan. This paper investigates the interaction mechanism, preparation, formulation and stability of 5-[ ?哈? / ?鞷? ]-iodo-2'-deoxyuridine as a potential radiopharmaceutical for hepatoma and cancers treatment. Materials and Methods:The self-synthesized 5-tributylstanny-2'-deoxyuridine (Bu ?? SnUdR), used as a precursor, was radioiodinated to produced [ ?哈? / ?鞷? ]IUdR. After adding the stabilizer, gentisic acid, the resultant reaction mixture was dispensed and lyophilized to give the [ ?哈? / ?鞷? ]IUdR hot kits. Results:The lyophilized [ ?哈? / ?鞷? ]IUdR hot kit was added with an appropriate amount of normal saline or lipiodol prior to preclinical 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 [ ?哈? / ?鞷? ]IUdR was significantly increased, and the stability of lyophilized form is far better than that of solution form. Conclusion:A stable radiopharmaceutical [ ?哈? / ?? Ⅰ ]IUdR with high radiochemical purity and specific activity was prepared in this study. Its use for preclinical and clinical studies on hepatoma and cancers therapy will be carried out in the further investigation.
Purpose:Hepatoma is one of the most prevalent male cancers in Taiwan. This paper investigates the interaction mechanism, preparation, formulation and stability of 5-[ ?哈? / ?鞷? ]-iodo-2'-deoxyuridine as a potential radiopharmaceutical for hepatoma and cancers treatment. Materials and Methods:The self-synthesized 5-tributylstanny-2'-deoxyuridine (Bu ?? SnUdR), used as a precursor, was radioiodinated to produced [ ?哈? / ?鞷? ]IUdR. After adding the stabilizer, gentisic acid, the resultant reaction mixture was dispensed and lyophilized to give the [ ?哈? / ?鞷? ]IUdR hot kits. Results:The lyophilized [ ?哈? / ?鞷? ]IUdR hot kit was added with an appropriate amount of normal saline or lipiodol prior to preclinical 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 [ ?哈? / ?鞷? ]IUdR was significantly increased, and the stability of lyophilized form is far better than that of solution form. Conclusion:A stable radiopharmaceutical [ ?哈? / ?? Ⅰ ]IUdR with high radiochemical purity and specific activity was prepared in this study. Its use for preclinical and clinical studies on hepatoma and cancers therapy will be carried out in the further investigation.
| Original language | Chinese (Traditional) |
|---|---|
| Pages (from-to) | 285-291 |
| Journal | 放射治療與腫瘤學 |
| Volume | 5 |
| Issue number | 4 |
| State | Published - 1998 |