药学学报, 2011, 46(4): 466-471
引用本文:
宦 娣 易 涛 刘 颖 肖 璐 何吉奎. 微粉硅胶对固体自微乳化给药系统小肠吸收的影响[J]. 药学学报, 2011, 46(4): 466-471.
HUAN Di, Yi- Chao, Liu- Ying, Xiao- Lu, He-Ji-Kui. Influence of silica on intestinal absorption of solid self-microemulsifying drug delivery systems[J]. Acta Pharmaceutica Sinica, 2011, 46(4): 466-471.

微粉硅胶对固体自微乳化给药系统小肠吸收的影响
宦  娣1, 易  涛1, 2*, 刘  颖1, 肖  璐1, 何吉奎1
(1. 西南大学药学院, 重庆 400715; 2. 澳门科技大学澳门药物及健康应用研究所, 澳门 000853)
摘要:

固体载体对固体自微乳化给药系统 (solid self-microemulsifying drug delivery systems, S-SMEDDS) 的体内外性质有重要影响。本文探讨微粉硅胶对S-SMEDDS药物吸收的影响, 为选择适宜固体载体提供依据。通过研究微粉硅胶对小肠脂解和S-SMEDDS体外释放的影响, 并采用新型体外脂解-吸收模型研究微粉硅胶对S-SMEDDS离体小肠吸收的影响。结果发现微粉硅胶既能提高脂解速率, 增加脂解后水性分散相中药物分配, 促进药物吸收; 又会延缓S-SMEDDS体外释药, 影响药物的吸收速度; 最终导致对S-SMEDDS的离体小肠吸收没有显著性影响。而且微粉硅胶对脂解和释药的影响都与其用量有关, 这提示微粉硅胶适合作为S-SMEDDS的固体载体, 其用量需要进一步筛选优化。

关键词:   
Influence of silica on intestinal absorption of solid self-microemulsifying drug delivery systems
Abstract:

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.

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