喃氟啶植入剂的研究

 目的：制备以聚甲基丙烯酸羟乙酯〔poly(2-hydroxyethyl methacrylate)，P(HEMA)〕和胶原蛋白(colagen)复合物〔以下简称P-(HEMA)-胶原〕为基质的喃氟啶缓释植入剂，并对其体外溶出和家兔体内药动学进行研究。方法：可溶性胶原蛋白从小牛皮中提取，用胃蛋白酶处理而去除其抗原性。植入剂用引发剂引发聚合法制备。体外溶出在蒸馏水中进行37℃。将植入剂植入家兔胸肌棘内进行体内药动学研究，用注射剂作为对照。结果：植入剂的体外释药过程符合Higuchi动力学，其t_0.5=7.5h，t_0.9=23.9h。家兔体内药动学参数为：AUC=222.619h·μg·ml^-1，MRT=33.674h，K_a=0.537h^-1。结论：P-(HEMA)-胶原作为抗癌药物的植入缓释载体，是有潜力的，值得进一步探索研究。

Study on fluorofur implant of poly(HEMA)-collagen composite

OBJECTIVE:To make fluorofur implant of poly(2-hydroxyethyl methacrylate)[poly(HEMA)]-collagen composite and to investigate its in vitro release and the pharmaceutics in rabbits.METHODS:Soluble collagen was extracted from calf fetus skin and was made nonantigenic with pepsin.The implant was made by initiator induced polymerization.The in vitro release studies of fluorofur from the implant were carried out in distilled water at 37℃.To study the in vitro release,the implants were implanted in the spinalis thoracis muscle of rabbits with fluorofur injection as control.RESULTS:The release profiles in vitro conformed to Higuchi kinetics.Its release index was t_0.5=7.5h，t_0.9=23.9h.The pharmacokinetic parameters of fluorofur implant in rabbits were AUC=222.619h·μg·ml^-1，MRT=33.674h，K_a=0.537h^-1 CONCLUSION:The poly(HEMA) collagen hydrogel offers excellent potential as a carrier for the sustained release implant of anticancer drugs.