摘要
根据溶解度和伪三元相图结果,结合星点设计-效应面法,以牛蒡子苷(1)在不同空白处方中的平衡溶解度和粒径为指标,优化1自微乳化给药系统(SMEDDS)处方。所得优化处方为1∶辛癸酸甘油酯∶聚氧乙烯氢化蓖麻油∶二乙二醇单乙基醚=4∶19∶54∶27。测得制品中1的含量为(40.09±0.06)mg/g;乳化后平均粒径为(26.65±0.57)nm。载药自微乳在p H 6.8磷酸盐缓冲液、水和0.1 mol/L盐酸中的释放行为相似;用恒温磁力搅拌器和恒温气浴振荡仪测得的释放行为也相似。与1原药相比,制品在0.1 mol/L盐酸中释放速率加快。
Based on the analysis of solubility test and pseudoternary phase diagrams, the formulation of self- emulsifying drug delivery system （SMEDDS） loaded with arctiin （1） was further optimized by central composite design and response surface methodology with the equilibrium solubility of 1 in blank SMEDDS and particle size as indexes. The optimum formulation of 1-SMEDDS contained 1, octyl and decyl glycerate, Cremophor RH40 and Transcutol-P with the weight ratio of 4 ： 19 ： 54 ： 27. The content ofl in SMEDDS was （40.09±0.06） mg/g, and the particle size of the product after microemulsion was （26.65±0.57） nm. The release behaviors of 1 from SMEDDS in different release media （pH 6.8 phosphate buffer, water and 0.1 mol/L hydrochloric acid） and using different machines （constant temperature magnetic stirrer and constant temperature bath shaker） were similar. Compared with the bulk drug, the release rate of 1-SMEDDS was accelerated in 0.1 mol/L hydrochloric acid.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2015年第3期248-253,共6页
Chinese Journal of Pharmaceuticals
基金
重庆市卫生局中医药科技项目(2012-2-25)
关键词
牛蒡子苷
自微乳给药系统
处方优化
体外释放
arctiin
self-emulsifying drug delivery system
formulation optimization
in vitro release
