Huan Di, Yi Tao, Liu Ying, Xiao Lu, He Ji-kui
College of Pharmaceutical Sciences, Southwest University, Chongqing 400715, China.
Yao Xue Xue Bao. 2011 Apr;46(4):466-71.
Solid carriers had important effects on the properties of solid self-microemulsifying drug delivery systems (S-SMEDDS). In order to make the basis for further development of S-SMEDDS, the influences of silica on the absorption of S-SMEDDS were investigated. An in vitro lipolysis model was used to evaluate the influence of silica on self-microemulsifying drug delivery system digestion from intestinal tract. S-SMEDDS containing silica were prepared by extrusion/spheronization. The drug release and absorption were investigated. The results showed that lipolysis rate and drug concentration in aqueous phase after intestinal lipolysis both increased by adding silica, which was benefit to drug absorption. And silica was not benefit to absorption for slowing drug release. Consistently, there was no significant influence of silica on intestinal absorption. This study implied that the influences of silica on lipolysis rate and drug release were both amount dependent and it is suggested that silica could be used as the solid carrier but the proportion needs to be optimized.
固体载体对固体自微乳化药物传递系统(S-SMEDDS)的性质有重要影响。为了为S-SMEDDS的进一步发展奠定基础,研究了二氧化硅对S-SMEDDS吸收的影响。采用体外脂解模型评估二氧化硅对自微乳化药物传递系统从肠道消化的影响。通过挤出/滚圆法制备含二氧化硅的S-SMEDDS。考察了药物的释放和吸收情况。结果表明,添加二氧化硅后肠道脂解后的脂解速率和水相中药物浓度均增加,这有利于药物吸收。且二氧化硅不利于吸收,因其减缓了药物释放。一致地,二氧化硅对肠道吸收无显著影响。该研究表明,二氧化硅对脂解速率和药物释放的影响均与用量有关,建议二氧化硅可作为固体载体,但比例需要优化。