【摘要】 目的研制PEG修饰大蒜素长循环脂质体并进行家兔体内药物动力学研究。方法用聚乙二醇-2000单甲醚合成聚乙二醇单甲醚磷脂酰乙醇胺衍生物(PEG-PE),采用Szoka改进逆相蒸发技术,制备PEG修饰大蒜素长循环脂质体(PEG-DATS-LCL),以HPLC法测定大蒜素的包封率及家兔血浆中药物浓度。结果长循环脂质体的平均粒径为12·63μm,包封率为90·77%;长循环脂质体家兔静脉注射给药呈双室模型特征,t1/2β为41·04h,AUC为9·66μg·ml-1·h-1,均显著大于注射液和普通脂质体的t1/2β和AUC。结论本法制得的PEG修饰大蒜素长循环脂质体包封率高,且延长了在血液中的循环时间,可达缓释、长效。更多还原

【Abstract】 Objective To prepare long circulation allitridin PEG-liposomes(PEG-DATS-LCL) and study its pharmacokinetics.Methods To prepare PEG-PE with PEG2000-MM and DEEP.PEG-DATS-LCLs were prepared by Szoka converse vaporized mathod.To examine the entrapment efficiency of PEG-DATS-CLC.A methed to determine allitridin in rabbit plasma by high performance liguid chromatography (HPLC) was established.Results The mean diametre of PEG-DATS-LCL was 12.63μm.The entrapment efficiency was 90.77%.The pharmacokinetics was agreed to Two-Chamber Model.t_ 1/2 β of PEG-DATS-LCLwas 41.04h,AUC was 9.66μg·ml~ -1 ·h~ -1 .They obviously higher than those in injectins and commen liposomes.Conclusion By this way,the liposomes with high entrapment efficiency could be prepared.The liposomes were modified by PEG-PE could raise the AUC and prolong the resident time of the drug in the blood circulating system.更多还原