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蒿甲醚自微乳化释药系统的制备及体外评价 被引量:3

Preparation and evaluation of self-microemulsifying drug delivery system for artemether in vitro
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摘要 目的研究蒿甲醚自微乳化释药系统处方组成和体外特性。方法通过溶解度实验、伪三元相图绘制和正交实验设计筛选优化蒿甲醚自微乳化处方。以自乳化速率、粒径、稳定性和体外溶出度为指标评价自乳化微乳系统体外特性。结果蒿甲醚自微乳化释药系统的最佳处方选择Lauroglycol 90为油相,Cremophor RH 40为乳化剂,Gelucire44/14为助乳化剂,最佳配比为4∶4∶2,其中蒿甲醚的载药量为80 mg/g。自制的ARM-SMEDDS均在2 min以内完成自微乳化,粒径为(61.50±8.66)nm,常温下3个月基本保持稳定,体外溶出度结果显示120 min即能达到>99.5%的溶出率,累积溶出百分率为原料药的7倍。结论所制备的ARM-SMEDDS外观和稳定性良好,能显著提高体外溶出度。 Objective To prepare and evaluate the self-microemulsifying drug delivery system(SMEDDS) of artemether(ARM) in vitro.Methods The preparation process of ARM-SMEDDS was optimized by solubility study,pseudo ternary phase diagrams and orthogonal design.Self-microemulsifying time,average particle size,stability and dissolution in vitro were evaluated.Results The optimized formation of ARM-SMEDDS were composed of ARM 80 mg/g,lauroglycol 90 as oil,cremophor RH 40 as surfactant and gelucire 44/14 as co-surfactant with a weight ratio of 4∶4∶2.The ARM-SMEDDS prepared above could selfmicroemulsify within 2 min,with a particle size of 61.50±8.66 nm.ARM-SMEDDS was found to be stable up to 3 months at room temperature.The percentage of accumulated dissolution was more than 99.5% within 120min which was 7 fold compared to ARM.Conclusion ARM-SMEDDS has good appearance and stability,and its dissolution in vitro is improved significantly.
出处 《第三军医大学学报》 CAS CSCD 北大核心 2013年第21期2348-2351,共4页 Journal of Third Military Medical University
基金 重庆市卫生局2012年医学科研计划项目(2012-2-261)~~
关键词 蒿甲醚 自微乳化释药系统 伪三元相图 体外评价 artemether self-microemulsifying drug delivery system pseudo-ternary phase diagrams in vitro evaluation
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