牡丹籽油自微乳化软胶囊内容物的制备工艺研究

Preparation technology of self-microemulsifying drug delivery soft capsules of Paeonia suffruticosa Andr.seed oil

研究牡丹籽油自微乳化软胶囊内容物(SMEDDS系统)的制备工艺。通过溶解度实验和体外自乳化实验对乳化剂和助乳化剂的种类及用量范围进行了筛选,并绘制了三元相图;以自乳化平衡时间和平均粒径为指标,筛选出牡丹籽油、乳化剂和助乳化剂的最佳配比;同时,对SMEDDS系统自乳化后的外观、自微乳化能力、粒度分布和稳定性进行了考察。结果表明,牡丹籽油SMEDDS系统中φ(牡丹籽油)=5%~10%、φ(聚山梨酯-80)=66%~78%、φ(PEG-400)=15%~27%;三者最佳配比为V(牡丹籽油)∶V(聚山梨酯-80)∶V(PEG-400)=2.12∶0.53∶0.3;牡丹籽油SMEDDS系统自微乳化平衡时间<1min,体外自乳化后呈蓝色乳光,粒度分布在1 000nm以下,平均粒径约为100nm,离心后未见分层,稳定性好。牡丹籽油SMEDDS系统自微乳化速度快,自微乳化能力强,自乳化后粒度达到了纳米级别,稳定性好。

To study the preparation technology of self-microemulsifying soft capsules of Paeonia suffruticosa Andr.seed oil(SMEDDS system).The types and dosage ranges of emulsifier and co-emulsifier were screened by the solubility test and the self-emulsification test in vitro,and the ternary phase diagrams was drawn.The optimum ratio of Paeonia suffruticosa Andr.seed oil,emulsifier and co-emulsifier was screened by self-emulsifying equilibrium time and average particle size.At the same time,the self-emulsifying appearance,self-microemulsifying ability,particle size distribution and stability after self-emulsification of SMEDDS system were investigated.The volume fraction of Paeonia suffruticosa Andr.seed oil in SMEDDS system accounted for 5% to 10%,polysorbate-80 accounted for 66% to 78%,PEG-400 accounted for 15% to 27%.The best ratio was V(Paeonia suffruticosa Andr.seed oil)∶V(polysorbate-80)∶V(PEG-400)=2.12∶0.53∶0.3.It's appearance was clear emulsified liquid with blue fluore scence after self-emulsification in vitro,it's particle size was distributed below 1 000 nm,and the average particle size about 100 nm.It can not be stratification after centrifugation.The self-microemulsification speed of Paeonia suffruticosa Andr.seed oil SMEDDS was very fast.It's microemulsification capacity was very strong.The particle size had reached the nanometer level after self-emulsification.It had a very strong stability.