辐射聚合制备止痛药DHP缓释制剂的研究

Study on Slow Release Analgesic Prepared by Radiation Induced Polymerization

报告了甲基丙烯酸β－羟乙酯（ＨＥＭＡ）在室温下进行辐射聚合制备双氢埃托啡（ＤＨＰ）缓释制剂的研究，结果表明：药物接受１６．７５ｋＧｙ照射后其红外紫外光谱未见明显改变，说明ＤＨＰ受１８．７５ｋＧｙ以下的辐射对其结构没有影响。ＨＥＭＡ所固化的ＤＨＰ体外释放稳定而持久，小鼠皮下包埋实验显示出数日的止痛效果，小鼠皮肤病理表明仅有轻微的异物反应．

In this study, the analgesic dithydroetorphine hydrochloride (DHP) with controlledalow release was made by radiation induced polymerization of monomers at room temperature.The radiation effect on the actiyity of DHP was investigated before immobilizing. The differencebetween UV spectrum and IR spectrum of radiation drug was not obvious when samples wereradiated with doses less than 16.75 kGy. It is found that the structure of drugs did not changewhen radiation doses were less than 16.75 kGy at room temperature. The DHP can be used forimmobilization. In vitro the rate of drug release remained stable. In vivo test in the mouseshowed that the rate of analgesic was retarded for many days. The pathologic findings of thetissue surrounding the copolymers were also investigated by microscopy.