灯盏花素脂质体/水分配系数的研究与应用

Study on the liposome/water partition coefficient for breviscapine and its application

目的应用脂质体 /水分配系数 ,初步揭示灯盏花素与磷脂分子间相互的作用机理 ,探讨灯盏花素口服吸收机制 ,并且解释一些因素影响灯盏花素脂质体包封率的规律。方法采用平衡透析法测定灯盏花素的脂质体 /水分布系数。结果与灯盏花素的油 /水分配系数随着 pH值的增加而减小相反 ,脂质体 /水分配系数随着pH值的增加而增大 ;磷脂浓度增大 ,脂质体 /水分配系数有增大的趋势。结论药物与磷脂膜的作用除疏水相互作用 (hydrophobicinteraction)外 ,离子间静电、氢键等相互作用占了很大比例 ;初步推测灯盏花素的吸收差可能是因为其吸收有除简单的被动转运外的其它机制 ;实验结果可以用来解释包封率影响因素的一些规律。

Objective To illuminate the mechanism of molecular interaction of breviscapine with the lecithin membrane,its oral absorption mechanism,and explain the factors which influence the entrapment efficiency of liposomal breviscapine.Methods The liposome/water partition coefficient (P lip/W) of breviscapine was determinated by equilibrium dialysis.Results The P lip/W of breviscapine increases with the increase of pH,which is different from the P O/W.Meanwhile,P lip/W becomes larger when lecithin concentration increases.Conclusions The other interaction besides hydrophobic interaction,such as ionic interaction,hydrogen bond etc,play a main role in the molecular interaction between breviscapine and lecithin membrance.The possible reason of the poor oral absorption of breviscapine is due to the other oral absorption mechanism of breviscapine besides the simple passive transportation.And the results can explain the fact that the entrapment efficiency of the liposomal breviscapine increases with the increasing concentration of the lecithin in the formulation.