辐射法制备喃氟啶植入剂的家兔药物动力学

The pharmacokinetics in rabbits of the fluorofur implants made by irradiation-induced polymerization

目的:用辐射法制备喃氟啶植入剂,并对其体外溶出和家兔体内药物动力学进行研究。方法:用辐射法制备以聚甲基丙烯酸羟乙酯[Poly(2-hydroxyelthylmethacrylate),p(HEMA)]和胶原蛋白(Collagen)复合物[以下简称p-(HEMA)-胶原]为基质的喃氟啶缓释植入剂,并做体外溶出和家兔体内药物动力学研究,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,体外溶出指数为t1/2=99h,t09=327h,家兔体内药动学参数为:AUC=268666h·μg/ml,MRT=41704h,ka=0334/h。结论:用辐射法制备的p-(HEMA)-胶原可以作为抗癌药物的植入缓释载体进一步探索研究。

OBJECTIVE:To investigate the in vitro release and the pharmacokinetics in rabbits of the fluorofur implants.METHODS:The implant,poly(2-hydroxyelthyl methacrylate)[poly(HEMA)]-collagen composite,made by irradiation-induced polymerization,was implanted in the spinalis thoracis muscle of the rabbits and contrasted by fluorofur injection.RESULTS:The release profiles in vitro conformed to Higuchi kinetics.The release index of the implant was t 1/2 =9.9h, t 0 9 =32.7h.The pharmacokinetic parameters in rabbits were: AUC =268.666h·μg/ml, MRT =41 704h, k a =0 334/h.CONCLUSION:The results clearly indicated that the poly(HEMA)-collagen hydrogel made by irradiation-induced polymerization offers excellent potential as a carrier for the sustained release implant of anticancer drugs.