李青松;王新;王鹤霖;徐璐;孙进;

• 1:沈阳药科大学无涯学院

摘要(Abstract)：

目的探索基于马来酰亚胺与肠道黏蛋白共价结合的肠道黏附纳米粒对药物口服生物利用度的影响,构建新型纳米载体用于增强药物口服吸收。方法通过乳化溶剂挥发法制备包载荧光剂香豆素6的马来酰亚胺肠道黏附纳米粒,对制备的黏附纳米粒与非黏附聚乳酸-羟基乙酸共聚物[poly(lactic-co-glycolic acid),PLGA]纳米粒的外观、粒径进行了表征,通过香豆素6考察了纳米粒的体外释放、肠灌流及体内药动学。结果制备的马来酰亚胺肠道黏附纳米粒呈类球形,粒径为(139.8±2.650)nm,PDI为(0.071±0.062),Zeta电位为(-5.793±0.737)mV。在4℃条件下放置30 d稳定性良好,体外释放实验表明马来酰亚胺纳米粒释放缓慢,没有突释效应。药动学实验表明香豆素6马来酰亚胺纳米粒的体内消除半衰期(t_(1/2))和药时曲线下面积(AUC_(0-t))分别是香豆素6非黏附对照纳米粒组的1.17倍和1.42倍,药时曲线下面积(AUC_(0-t))是香豆素6溶液剂的1.76倍。结论基于马来酰亚胺与肠道黏蛋白共价结合的肠道黏附纳米粒能延长药物肠道滞留时间,增加口服吸收,提高药物口服生物利用度。

关键词(KeyWords)： 药剂学;马来酰亚胺纳米粒;肠道黏附;生物利用度;香豆素6

Abstract:

Keywords:

基金项目(Foundation): 国家自然科学基金资助项目(81473164)

作者(Author): 李青松;王新;王鹤霖;徐璐;孙进;

Email:

DOI: 10.14066/j.cnki.cn21-1349/r.2019.0142

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