摘要
目的:制备载灯盏花素介孔二氧化硅(BRE-MSN)以提高药物的体外溶出度。方法:以吸附法将灯盏花素负载于介孔二氧化硅,通过氮气吸附-解吸试验、透射电镜(TEM)、差示扫描量热(DSC)、X-射线衍射(XRD)分析对其进行性质表征,同时对制剂的稳定性和释药行为进行考察。结果:所制BRE-MSN的载药量为(37.47±1.38)%;空白MSN的比表面积为1139.8m2·g-1,BRE-MSN的比表面积为521.9 m2·g-1;药物以无定形态存在于载体中,且拥有较好的稳定性;体外释放试验显示,累计溶出率最高达到了93.74%。结论:本方法成功制备得到了载药量高、性质稳定的BRE-MSN且显著提高了BRE的水溶性和溶出速率,为解决BRE的水难溶性提供了一种有效的方法。
Objective:To prepare mesoporous silica nanoparticles(MSN)loading breviscapine(BRE-MSN)to improve the dissolution of breviscapine.Methods:MSN was used as the carrier to load BRE by the adsorption method.BRE-MSN was characterized by nitrogen adsorption test,transmission electron microscope,differential scanning calorimetry and X-ray diffraction.And then,stability and in vitro dissolution study of BRE-MSN were performed.Results:The drug loading of BRE-MSN was(37.47±1.38)%.The specific surface area of the blank MSN and BRE-MSN was 1139.8 m2·g-1 and 521.9 m2·g-1,respectively.BRE-MSN had good stability and the drug state in the MSN was not crystal.The accumulate release rate of BRE-MSN could achieve to 93.74%.Conclusion:BRE-MSN with high drug loading and good stability was prepared successfully,which can significantly improve the solubility and dissolution rate of BRE.The study provides an effective method for solving the water-insolubility of BRE.
作者
陈敏燕
杨刚
吴飞华
原永芳
Chen Minyan;Yang Gang;Wu Feihua;Yuan Yongfang(Department of Pharmacy,the Ninth People’s Hospital Affiliated to Medical School,Shanghai Jiao Tong University,Shanghai 200011,China)
出处
《中国药师》
CAS
2020年第3期457-461,共5页
China Pharmacist
基金
上海交通大学“医工交叉基金项目”(编号:YG2016QN08).
关键词
灯盏花素
介孔二氧化硅
稳定性
体外溶出
Breviscapine
Mesoporous silica nanoparticles
Stability
In vitro release