水飞蓟素自微乳的研制

目的筛选水飞蓟素自微乳的处方并对其体外溶出及稳定性进行考察。方法通过溶解度实验、正交设计及伪三元相图的建立,筛选水飞蓟素自微乳的组成。采用HPLC法测定处方中的药物含量,并对照市售制剂考察其溶出度及稳定性。结果水飞蓟素自微乳化系统的组成为水飞蓟素、油酸乙酯、聚氧乙烯氢化蓖麻油(Cremophor EL)和乙二醇单乙基醚(transcutol)的质量比为0.07∶0.45∶0.45∶0.1;自微乳的平均粒径为72.1 nm;于4种溶出介质中均完全溶出,且溶出曲线明显高于市售制剂;强光照射(4 500 lx)、高温(60℃)及高低温循环实验(40℃和4℃)结果表明,该自微乳性状、含量均无明显变化。结论水飞蓟素自微乳粒径小,溶出度及稳定性良好。

Silymarin self-microemulsifying drug delivery systems(SMEDDS)

Objective To design the formulation for silymarin self-emulsifying microemulsion and evaluate its dissolution and stability.Methods The formulation was established through solubility experiments,orthogonal design and pseudo-ternary phase diagrams.The dissolution and stability were evaluated by HPLC assay.Results The optimal formulation was composed of silymarin,ethyl oleate,Cremophor EL and transcutol,with the ratio of 0.07∶0.45∶0.45∶0.1.The average particle size was 72.1 nm.Silymarin from SMEDDS was completely and rapidly dissolved in four different buffer media and obtained a higher dissolution profile compared with commercial preparations.The appearance and average silybin content of SM-SMEDDS were of no significant changes after 10 days of illumination(4 500 lx),high temperature(60 ℃) and temperature cycling tests(40 ℃,4 ℃).Conclusions The acquired microemulsion is stable,with small particle size and good dissolution.