论文部分内容阅读
目的制备氨基修饰有序介孔硅(amino-modified ordered mesoporous silica,NH2-OMS)并考察其作为水难溶性药物载体的载药及体外释放性能。方法以十六烷基三甲基溴化铵为模板合成了有序介孔硅(OMS),并以3-氨丙基三甲氧基硅烷对其表面进行修饰,以槲皮素为模型药物,并利用N2吸附-脱附、X-射线衍射、热重分析等方法对载药前后的氨基修饰有序介孔硅进行表征。考察氨基修饰有序介孔硅的载药性能及药物的体外释放行为。结果当槲皮素浓度为4 mmol.L-1、载药24 h、50℃时,氨基修饰有序介孔硅对槲皮素的载药量为21.0%,包封率为58.2%。槲皮素氨基修饰有序介孔硅药粒在模拟肠液和模拟胃液中的药物释放量分别是槲皮素原料药溶解量的13和27倍。结论氨基修饰有序介孔硅作为水难溶性药物槲皮素的载体可以明显改善其水溶性及在胃肠道中的溶出度。
OBJECTIVE To prepare amino-modified ordered mesoporous silica (NH2-OMS) and study its drug release and in vitro release as a poorly water-soluble drug carrier. Methods The ordered mesoporous silica (OMS) was synthesized by using cetyltrimethylammonium bromide as template. The surface of the mesoporous silica was modified with 3-aminopropyltrimethoxysilane. Quercetin was used as model drug, The amino-modified ordered mesoporous silica was characterized by N2 adsorption-desorption, X-ray diffraction and thermogravimetric analysis before and after drug loading. To investigate the drug-loading properties of amino-modified ordered mesoporous silicon and the drug release in vitro. Results When the concentration of quercetin was 4 mmol.L-1, the drug loading was 24 h and the temperature was 50 ℃, the drug loaded amount of amino-modified ordered mesoporous silica on quercetin was 21.0% and the entrapment efficiency was 58.2%. Quercetin amino modified ordered mesoporous silica particles in the simulated intestinal fluid and simulated gastric fluid drug release were quercetin API dissolved amount of 13 and 27 times. Conclusion Amino-modified ordered mesoporous silica as a poorly water-soluble drug carrier can significantly improve its water solubility and dissolution in the gastrointestinal tract.