School of Pharmacy, University of East Anglia, Norwich, NR4 7TJ, UK.
Pharm Res. 2011 Jul;28(7):1540-51. doi: 10.1007/s11095-011-0387-8. Epub 2011 Feb 24.
To investigate the physical processes involved in the emulsification of self-emulsifying drug delivery systems (SEDDSs) and the use of the Dynamic Gastric Model (DGM) as a characterisation tool.
SEDDSs based on soybean oil, Tween 80, Span 80 and ibuprofen were prepared and their equilibrium phase diagrams established. The emulsification behaviour in a range of media was studied using polarised light microscopy and particle sizing. The behaviour of the SEDDSs in the DGM and conventional testing equipment was assessed.
A range of liquid crystalline mesophases was observed, enhanced in the presence of the drug. Polarised light microscopy showed different emulsification processes in the presence and absence of the drug, which was also manifest in different droplet sizes. The droplet size distribution varied between the DGM and the USP II dissolution apparatus.
The model SEDDS displays complex liquid crystalline behaviour which may be intimately involved in the emulsification process, which in turn may alter particle size on emulsification, although there remains a question as to the in vivo significance of this effect. Furthermore, we demonstrate that the DGM represents a very promising new method of assessing the biological fate of SEDDSs.
研究自乳化药物传递系统（SEDDS）乳化过程中的物理过程，并将动态胃模型（DGM）用作特征化工具。
制备基于大豆油、吐温 80、司盘 80 和布洛芬的 SEDDS，并建立其平衡相图。使用偏光显微镜和粒度测定法研究了在一系列介质中的乳化行为。评估了 SEDDS 在 DGM 和常规测试设备中的行为。
观察到一系列液晶中间相，在药物存在下增强。偏光显微镜显示在药物存在和不存在的情况下存在不同的乳化过程，这也表现在不同的液滴尺寸上。DGM 和 USP II 溶解装置之间的液滴尺寸分布不同。
模型 SEDDS 显示出复杂的液晶行为，这可能与乳化过程密切相关，这反过来又可能在乳化时改变颗粒大小，尽管对于这种效应的体内意义仍存在疑问。此外，我们证明 DGM 代表了评估 SEDDS 生物学命运的一种很有前途的新方法。
