茴拉西坦/MCM-48载体的制备及释药性能研究

Preparation and drug release performance of aniracetam/MCM-48 materials

为了提高难溶性药物的口服生物利用度,采用水热合成法制备了MCM-48介孔二氧化硅载体材料,利用浸渍法将水难溶性药物茴拉西坦负载于MCM-48载体上。利用扫描电子显微镜(SEM)、透射电子显微镜(TEM)、激光粒度仪、小角X射线衍射(XRD)、N2吸附-脱附、红外光谱(IR)、差热-热重(DTA-TG)对载药前后MCM-48的表面形貌、粒径、孔径、孔容、比表面积、晶胞参数等进行测试,结果表明,MCM-48外形为球形颗粒,介孔结构为三维立方结构,孔径3.55 nm,孔容及比表面积分别为0.86 cm^3/g和764 m^2/g;MCM-48负载茴拉西坦的载药量为16%,载药后药物以非晶态装载于介孔孔道中或吸附于载体表面,没有影响MCM-48的骨架结构,但使孔径、孔容及比表面积下降。通过在不同pH溶液中载药MCM-48与茴拉西坦原料药的溶出度比较发现,MCM-48载体能够提高茴拉西坦的溶出速率。

In order to improve the oral bioavailability of insoluble drugs,MCM-48 as mesoporous silica carrier was prepared by hydrothermal method.The poorly water-soluble drug Aniracetam was loaded on MCM-48 by dipping method.The surface morphology,particle size,pore size,pore volume,specific surface area and cell parameters of drug unloaded and loaded MCM-48 were investigated by SEM,TEM,laser particle size analyzer,XRD,N2 adsorption-desorption test,IR,DTA-TG.The results showed that MCM-48 with spherical shape was three-dimensional cubic structure with pore size of 3.55 nm,pore volume of 0.86 cm^3/g and specific surface area of 764 m^2/g.The drug loading of MCM-48 was 16%,and the drug with amorphous state loaded in the mesoporous pores or on the surface without any effect on the skeleton structure of MCM-48 which decreased pore size,pore volume and specific surface area.MCM-48 loaded with Aniracetam could enhance its dissolution rate comparing with unloaded Aniracetam in different pH solution.