夏枯草有效组分结肠靶向微丸的制备及其体外释药行为

摘要

AIM To prepare colon-targeted pellets of Prunellae Spica effective components and to evaluate the in vitro drug-release behaviors.METHODS Fluidized bed coating method was adopted in the preparation of pellets.With in vitro accumulative release rate as an evaluation index,hydroxypropyl methyl cellulose (HMPC),polyacrylic resin (Eudragit S100) and triethyl citrate (TEC) amounts as influencing factors,orthogonal test was applied to optimizing the formulation.The in vitro drug-release behaviors were evaluated with rosmarinic acid content as an index.RESULTS The optimal formulation was determined to be 5％ for HPMC amount,70％ for Eudragit S100 amount,and 20％ for TEC amount.The obtained pellets attained an accumulative release rate of more than 90％ in pH 7.6 PBS (transportation for 2 h),while no drug dissolution was found in pH 1.0 HCl (transportation for 2 h) or pH 6.8 PBS (transportation for 3 h).CONCLUSION Colon-targeted pellets of Prunellae Spica effective components can achieve in vitro colon-targeted effect.%目的 制备夏枯草有效组分结肠靶向微丸,并评价其体外释药行为.方法 流化床包衣法制备微丸.以体外累积释放率为评价指标,羟丙基甲基纤维素(HPMC)、聚丙烯酸树脂(Eudragit S100)、枸橼酸三乙酯(TEC)用量为影响因素,正交试验优化处方.以迷迭香酸含有量为指标,评价体外释药行为.结果 最佳处方为HPMC用量5％,Eudragit S100用量70％,TEC用量20％,所得微丸在pH 7.6 PBS(转运2h)中累积释放率达90％以上,而在pH 1.0HCl(转运2 h)、pH 6.8 PBS(转运3h)中未溶出药物.结论 夏枯草有效组分结肠靶向微丸可达到体外结肠靶向效果.