冬凌草甲素长循环胶束的制备及药动学性质的考察  

Preparation of long-circulating oridion-containing micelle and its pharmacokinetics

作　　者：何晴[1] 杨琴[1] 龚涛[1] 张志荣[1] 邓黎[1] 张彦[2] 

机构地区：[1]四川大学华西药学院靶向药物重点实验室,四川成都610041 [2]重庆药友制药有限责任公司,重庆401121

出　　处：《华西药学杂志》2012年第1期48-50,共3页West China Journal of Pharmaceutical Sciences

摘　　要：目的制备冬凌草甲素长循环胶束,对比普通冬凌草甲素磷脂/胆盐混合胶束和冬凌草甲素长循环胶束在大鼠体内的药动学差异。方法用薄膜分散法制备冬凌草甲素长循环胶束和普通冬凌草甲素磷脂/胆盐混合胶束,测定粒径,HPLC法测定血浆中冬凌草甲素的浓度,并用DAS2.0软件计算药动学参数。结果胶束粒径为14.53±1.19 nm,PDI为0.28±0.06。冬凌草甲素长循环胶束的体内T1/2为125.25±40.78 h,是普通胶束的12.8倍,AUC为168.04±39.01μg.L-1.h-1,为普通胶束的5.8倍(P<0.05)。结论所制备的冬凌草甲素长循环胶束与普通磷脂/胆盐混合胶束相比,其体内半衰期明显延长,生物利用度显著提高,具有长循环的效果。OBJECTIVE To prepare the Long-circulating oridion-containing micelle and compare the pharmacokinetics between Long-circulating micelle and general PC/BS-MMS.METHODS The Long-circulating oridion-containing micelle were prepared by film dispersion method.The concentration of oridion in rats＇ plasma was determined by HPLC,and the parameters were calculated with DAS2.0.RESULTS The mean diameter of Long-circulating micelle was 14.53±1.19 nm,PDI was 0.28±0.06,the pharmacokinetic parameters of Long-circulating oridion-containing micelle were 125.245±40.783 h for T1/2 and 168.04 ±39.01 μg·L-1·h-1 for AUC.CONCLUSION Compared with genernal PC/BS-MMS,the Long-circulating oridion-containing micelle can prolong the T1/2,and improve the bioavailability of oridion.It can achieve the long-circulation profile.

关 键 词：冬凌草甲素 长循环胶束 药物动力学 薄膜分散法 

分 类 号：R94[医药卫生—药剂学]