绿原酸自微乳给药系统的处方设计与体外评价

Preparation and quality valuation of chlorogenic acid self-microemulsion drug delivery system

目的制备绿原酸自微乳制剂并评价其质量。方法通过绘制伪三元相图筛选自微乳的最佳处方,在此基础上制备绿原酸自微乳制剂;对自微乳的乳化速率、乳滴形态、粒径大小、稳定性以及释放度进行了研究。结果自微乳的最佳配比为油酸乙酯∶吐温-80∶甘油=1∶3∶6,绿原酸最大载药量为0.067 8 g。所得绿原酸预微乳浓缩液遇水能够迅速乳化成无色澄明的O/W型纳米乳,乳滴呈圆球形,粒径为16 nm,分布均匀,稳定性良好。自微乳释放度受介质影响小,能够延缓绿原酸的释放。结论所制备的绿原酸自微乳工艺简单可行、性质稳定,为进一步研究绿原酸自微乳的体内吸收奠定了良好的基础。

Objective To prepare chlorogenic acid（ CHA） self- microemulsifying drug delivery system（ SMEDDS） and evaluate its quality. Methods The optimal formulation of CHA- SMEDDS was studied by drawing pseudo- ternary phase diagrams. The self- emulsifying rate,morphology appearance,particle size,stability and dissolution of the optimal formulation were determined. Results The optimal formulation and matching ratio of CHA- SMEDDS were ethylis oleas ∶ tween- 80 ∶ glycerol（ 1 ∶ 3 ∶ 6） with the largest drug loadings of 0. 067 8gram. The obtained O / W CHA- SMEDDS was a translucent and achromatous solution with good stability. After100- fold dilution with water,CHA- SMEDDS consisted of small spherical drops with the mean size of 16 nm.The release of CHA was not influenced by the dissolution medium. Conclusion CHA- SMEDDS is easy to prepare,the stability is satisfactory and the quality is easy to control,which provided a good foundation for further study on CHA- SMEDDS in vivo.