摘要
目的 制备穿心莲内酯自微乳给药系统.方法 根据平衡溶解度、辅料配伍、伪三元相图确定辅料比例范围.以广藿香油占比、Labrasol ALF与Tween 80 比例、Km 为影响因素,平衡溶解度为评价指标,星点设计-响应面法优化处方,再进行体外评价.结果 最优处方为广藿香油、Labrasol ALF、Tween 80、Transcutol HP 占比 10.45%、13.28%、9.82%、66.44%,平衡溶解度为(11.95±0.04)mg/g.质量参数分别为乳化时间(20.22±0.38)s,粒径(51.70±2.91)nm,多分散指数 0.27±0.02,透光率(91.21±1.58)%.自微乳给药系统冻融稳定性良好,稀释倍数、分散介质对其粒径无明显影响,在磷酸盐缓冲液(pH 6.8)中溶出迅速.结论 自微乳给药系统可提高穿心莲内酯溶解度、溶出速率.
Abstract
AIM To prepare andrographolide self-microemulsifying drug delivery system.METHODS The range of excipient ratio was determined according to equilibrium solubility,excipient compatibility and pseudo-ternary phase diagram.With Pogostemon cablin oil proportion,Labrasol ALF-Tween 80 ratio and Km as influencing factors,drug loading as an evaluation index,the formulation was optimized by central composite design-response surface method,after which in vitro evaluation was performed.RESULTS The optimized formulation was determined to be 10.45%,13.28%,9.82%,66.44%for Pogostemon cablin oil,Labrasol ALF,Tween 80,Transcutol HP proportions,the equilibrium solubility was(11.95±0.04)mg/g.The quality parameters were(20.22±0.38)s for emulsification time,(51.70±2.91)nm for particle size,0.27±0.02 for polydispersity index,and(91.21±1.58)%for light transmission rate,respectively.The self-microemulsion drug delivery system demonstrated good freeze-thaw stability,whose particle size was not obviously influenced by dilution times and dispersion medium,and was rapidly dissolved in phosphate buffer solution(pH 6.8).CONCLUSION Self-microemulsifying drug delivery system can enhance the solubility and dissolution rate of andrographolide.
维普
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