冬凌草甲素-介孔二氧化硅固体分散体的制备及体外性质评价

Preparation and in vitro evaluation of oridonin-mesoporous silica nanoparticle solid dispersion

目的以介孔二氧化硅为载体制备冬凌草甲素(ORI)-介孔二氧化硅固体分散体并研究其对ORI溶出度的影响。方法以吸附法将ORI负载于介孔二氧化硅中,采用透射电镜、X-射线衍射、差示扫描量热等手段表征载药固体分散体的物相变化,同时对载药固体分散体的稳定性和体外溶出行为进行考察。结果制备得到的载药介孔二氧化硅呈椭球状,载药量为26.47%;ORI 以无定形态存在于载体中,且稳定性良好;固体分散体中ORI的体外溶出度得到显著提升,在45 min内的累积溶出在80%以上。结论介孔二氧化硅固体分散体显著提高了ORI的溶出速率,为解决ORI的水难溶性问题提供了一条新途径。

Objective To prepare oridonin(ORI)-mesoporous silica nanoparticles(MSN)solid dispersion with MSN as the carrier and to determine their effect on the dissolution of ORI.Methods ORI was loaded into MSN solid dispersion by adsorption.Transmission electron microscopy,X-ray diffraction analysis and differential scanning valorimetry were used to characterize the phase change of the solid dispersion.The stability of the drug carrying solid dispersion and dissolution behaviors were also determined.Results The prepared drug-carrying mesoporous silica was ellipsoid,with the drug loading of 26.47%.ORI loaded in the carrier was amorphous with good stability.The in vitro dissolution of ORI in solid dispersion was significantly increased,and the cumulative dissolution rate reached over 80%within 45 min.Conclusion MSN solid dispersion greatly improves the dissolution rate of ORI,providing a new solution to the water insolubility of ORI.