微粉硅胶对固体自微乳化给药系统小肠吸收的影响  

Influence of silica on intestinal absorption of solid self-microemulsifying drug delivery systems

作　　者：宦娣[1] 易涛[1,2] 刘颖[1] 肖璐[1] 何吉奎[1] 

机构地区：[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

出　　处：《药学学报》2011年第4期466-471,共6页Acta Pharmaceutica Sinica

基　　金：重庆市自然科学基金资助项目(CSTC2009BB5106);重庆高校优秀成果转化资助项目(KJ08B06);中央高校基本科研业务费专项资金项目(XDJK2009C076);西南大学博士基金项目(SWUB2008032)

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。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.

关 键 词：微粉硅胶 自微乳化给药系统 小肠吸收 体外脂解模型 吲哚美辛 

分 类 号：R943[医药卫生—药剂学]