双氯芬酸钠自乳化给药系统的研制

Preparation of self-microemulsifying drug delivery system for diclofenac sodium

目的研制双氯芬酸钠自乳化给药系统。方法通过测定双氯芬酸钠在各种溶剂中的平衡溶解度,选择适宜油相、乳化剂、助乳化剂,并在此基础上绘制伪三元相图。通过对各处方比例的筛选,结合各处方载药量以及所形成微乳的稳定性,确定最佳处方。结果以油相为三辛酸/癸酸甘油酯,乳化剂为Cremophor EL,助乳化剂为丙二醇,Km1为4∶1,Km2为1∶9,双氯芬酸钠在微乳中的质量浓度为25g.L-1,该处方为最佳处方。结论所研制的自乳化给药系统具有粒径小、载药量高、性质稳定的优势,可作为进一步研究的基础。

Objective To develop the formulation of diclofenac sodium self-microemulsifying drug delivery system{ SEDDS）. Methods Through solubility experiment,the stability of microemulsion and drug loading, the optimum formulation was selected by pseudot- ernary phase diagrams. Results In the selected formulation,octyl decyl acid triglycerate, cremophor EL and propylene glycol were screened as the oil phase,emulsifier and co-emulsifier,respectively. Km1 is 4：1 and Km2 is 1 ：9. The microemulsion contains 25 g·L-1 diclofenac sodium. Conclusion The self-microemulsifying drug delivery system was sucessfully prepared with a high drug loading.