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目的研究脑局部缓释125碘标记的5-碘脱氧尿苷(IUdR)的作用。方法为了控制释放125碘-IUdR,合成了25μCi的羧基苯氧丙烷:癸二酸(PCPPSA)(2080)125碘-IUdR聚合体。体外将合成的三聚体缓释剂(10mgPCPPSA)置于37℃磷酸盐缓冲溶液(PBS)中孵育不同时间后移出溶剂并置换为新的PBS,将移出液于放射计数器上测量数值。在体研究采用雄性裸鼠(6周)颅内接种U251人恶性星形细胞瘤及皮下接种对比研究。将颅内荷瘤鼠瘤腔内及皮下接种肿瘤组织内分别应用三聚体缓释剂及空白缓释剂,于不同时间分别测量动物头颅及皮下结节的放射活性,间接定量研究缓释状况;采血了解全身代谢情况。对于多聚磷酸酯(PPE)缓释剂研究采用皮下肿瘤结节内局部应用并测量其缓释的方法,放射自显影研究及全身不同器官缓释剂的吸收代谢研究采用接种后2、4和8d收集标本,分别行切片放射自显影和器官放射活性测定。结果体内和体外研究均显示PCPP:SA缓释剂对125碘-IUdR的控制性释放作用,尤其在体研究分别显示颅内和皮下接种的肿瘤组织对标记的IUdR的释放程度存有极大的差异,提示颅内局部应用的优越性。放射自显影定性研究显示了随距离的增加被标记的IUdR的递减趋势,为确定缓释剂施放部位和间距提供了参考数据。各主要脏器放射性测定的结果显示早期小肠内放射性较高,其次为脾脏,提示IUdR主要的代谢渠道,为处理应用其而可能引发的其他脏器损害或作用提供了线索。结论放射标记的IUdR缓释剂主要集中在接种部位且缓释作用确切。
Objective To study the effect of 125 I-iododeoxyuridine (IUdR) on local slow release of brain. Methods To control the release of 125 iodine-IUdR, 25 μCi carboxyphenoxy propane: sebacic acid (PCPPSA) (2080) 125 iodine-IUdR polymer was synthesized. In vitro, the synthesized trimeric sustained-release agent (10 mgPCPPSA) was placed in phosphate buffered saline (PBS) at 37 ° C. for a different period of time and the solvent was removed and replaced with fresh PBS. The effluent was measured on a radio-frequency counter. A Comparative Study of Intracranial U251 Human Malignant Astrocytoma and Subcutaneous Inoculation in Male Nude Mice (6 weeks). The intracranial tumor bearing tumor in mice were inoculated intradermally and subcutaneously with trimeric sustained-release agents and blank sustained-release agents respectively at different times to measure the radioactivity of the skull and subcutaneous nodules in animals, ; Blood to understand the body’s metabolism. For polyphosphate (PPE) sustained-release agent study subcutaneous tumor nodules within the local application and measurement of its sustained release method, autoradiographic studies and systemic absorption of different organs and sustained-release agents study using 2, 4 and after inoculation 8d specimens were collected, autoradiography and organ radioactivity were measured. Results Both in vivo and in vitro studies showed a controlled release of 125 Iod-IUdR by PCPP: SA sustained-release agents. In particular, in vivo studies have shown that the intracranial and subcutaneous inoculation of tumor tissue has a very significant release of labeled IUdR Differences, suggesting the superiority of intracranial local application. A qualitative study of autoradiography shows a decreasing trend of IUdR labeled with increasing distance, providing reference data for determining the release site and spacing of the sustained-release agent. The results of radioactivity measurement of major organs showed that the radioactivity in the early small intestine was higher, followed by the spleen, suggesting that the main metabolic pathway of IUdR provided clues for handling the damage or action of other organs that may be caused by it. Conclusion The radiolabeled IUdR sustained-release agents are mainly concentrated in the inoculation sites and the sustained-release effect is definite.