基于体内自组装胶束思维分析千金子脂肪油对4种千金子素的增溶作用

目的：通过模拟人体肠道环境，研究千金子脂肪油与肠液中胆盐所形成混合胶束对千金子素L₁，L₂，L₃，L₈的增溶作用。方法：制备不同千金子脂肪油加入量的混合胶束，采用透射电子显微镜观察胶束的形态，运用粒度仪测定其粒径和Zeta电位，利用HPLC考察混合胶束对4种千金子素溶解度的影响，同时考察放置时间对混合胶束稳定性的影响。结果：体外模拟形成的千金子脂肪油/胆盐混合胶束呈球形且粒径均一，Zeta电位绝对值均<20 mV；固定脱氧胆酸钠质量浓度为4.96 g·L^-1，4种千金子素在千金子脂肪油质量浓度为0.1~4 g·L^-1时的溶解度均显著大于不含千金子脂肪油时的溶解度，混合胶束中4种千金子素的溶解度为其在不含脂肪油胶束体系溶解度的1.3~4倍；该混合胶束可稳定存在36 h。结论：千金子脂肪油与脱氧胆酸钠所形成的混合胶束对千金子素L₁，L₂，L₃，L₈有显著的增溶作用，可为从药剂学角度阐释千金子去油制霜的减毒机制提供参考。

Analysis of Solubilization of Fatty Oil from Euphorbiae Semen on Four Euphorbia Factors Based on Thinking of Self-assembled Micelles in vivo

Objective: The solubilization of 4 compounds(Euphorbia factor L₁,L₂,L₃ and L₈),caused by mixed micelles self-assembled from fatty oil of Euphorbiae Semen and bile salt of intestinal juice,was researched in the simulated human intestinal environment. Method: The mixed micelles were prepared with different amounts of fatty oil of Euphorbiae Semen.The transmission electron microscope(TEM) was used to observe the morphology of the micelles.Particle size detector was used to determine the particle size and Zeta potential.HPLC was used to assay the solubility of these 4 compounds.The variation tendency of the total dissolution of these 4 compounds with the change of standing time was observed. Result: Particle size of the mixed micelles was uniform and its morphology was spherical.The absolute values of Zeta potential were less than 20 mV.When the amount of sodium deoxycholate was fixed 4.96 g·L^-1,the solubility of these 4 compounds with the concentration of fatty oil at 0.1-4 g·L^-1 were significantly greater than that at the dosage of 0 g·L^-1.The solubility of these 4 compounds in the micelles formed by fatty oil was 1.3 to 4 times as much as the micelles without fatty oil.The micelles was stable for 36 h. Conclusion: The micelles self-assembled from fatty oil of Euphorbiae Semen and bile salt of intestinal juice,have significant solubilization effect on Euphorbia factor L₁,L₂,L₃ and L₈.This research can lay the foundation for clarifying the detoxification mechanism of removing fatty oil and making frostlike powder from the perspective of pharmaceutics.