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。
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. t1/2 β of PEG - D ATS - LCLwas 41.04h, A UC 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.
出处
《实用心脑肺血管病杂志》
2006年第6期454-456,共3页
Practical Journal of Cardiac Cerebral Pneumal and Vascular Disease
