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目的 进行新型乏氧组织显像剂DTPA 甲硝唑的化学合成、药盒制备、99Tcm 标记、质量控制以及药理研究。方法 合成的DTPA 甲硝唑用氯化亚锡作还原剂 ,99Tcm 标记 ,用多元正交法确立99Tcm 标记一步法药盒的最佳配方。纸层析法鉴定99Tcm DTPA 甲硝唑的标记率、标记稳定性 ,完成了H2 2肝癌小鼠体内生物分布实验及显像研究。结果 DTPA 甲硝唑一步法药盒与99TcmO-4 混合 ,沸水浴反应 10min ,放化纯度大于 99%。H2 2肝癌小鼠生物分布显示 ,肿瘤 /血液比值 1、2h分别为3 43、6 40 ,肿瘤 /肌肉比值 1、2h分别为 5 2 4、7 42 ;注射血管舒张药肼苯哒嗪组肿瘤组织摄取明显高于对照组 (P <0 0 1)。结论 研制的99Tcm DTPA 甲硝唑有望成为一种新型的肿瘤乏氧组织显像剂。
Objective To study the chemical synthesis of DTPA metronidazole, kit preparation, 99Tcm labeling, quality control and pharmacological studies. Methods DTPA metronidazole was synthesized with stannous chloride as reducing agent and labeled with 99Tcm. The optimal formulation of 99Tcm labeled one-step kit was established by multiplex orthogonal method. Paper chromatography identification of 99Tcm DTPA metronidazole labeling rate, labeling stability, completed the H2B mice in vivo biodistribution experiments and imaging studies. Results The DTPA metronidazole one-step kit was mixed with 99TcmO-4. The reaction was carried out in a boiling water bath for 10 minutes and the radiochemical purity was over 99%. The biodistribution of H2-HCC mice showed that the tumor-blood ratio was 436, 40 and 1,24, respectively, with a tumor-to-muscle ratio of 52.42 and 42.22, respectively. The injection of the vasodilator hydralazine group Tissue uptake was significantly higher than that in the control group (P <0.01). Conclusion 99Tcm DTPA metronidazole is expected to become a new imaging agent of tumor hypoxia.