特考韦瑞固体分散体的制备与表征

Preparation and characterization of tecovirimat solid dispersions

目的考察载体用量、制备工艺等对特考韦瑞固体分散体(T-SD)内在性质的影响。方法选择PVP K30为载体,分别以旋转蒸发法和冷冻干燥法制备T-SD,并通过扫描电镜(SEM)、粉末X射线衍射(PXRD)、差示扫描量热法(DSC)和傅里叶红外光谱(FTIR)进行表征。结果与特考韦瑞、物理混合物相比,T-SD显著改善了该药的体外溶出;且随载体用量的增加,T-SD的体外溶出有增加的趋势。冷冻干燥法制备所得固体分散体中药物虽以微晶形式存在,但其溶出度显著高于旋转蒸发法制备所得。结论增加载体用量、采用冷冻干燥法能显著改善难溶性药物特考韦瑞的溶出度,在选择制备工艺时应考虑固体分散体中药物的分散形式以及所得样品的粒径、多孔性和可润湿性等。

Objective To study the effects of carrier and preparation process on the properties of solid dispersions of poorly water-soluble tecovirimat.Methods Tecovirimat solid dispersions(T-SD)were prepared by rotary evaporation and freeze-drying using PVP K30 as the carrier,and characterized by scanning electron microscopy(SEM),powder X-ray diffraction(PXRD),differential scanning calorimetry(DSC)and Fourier infrared spectroscopy(FTIR).Results Compared with raw tecovirimat and the physical mixture,the dissolution of tecovirimat from T-SD was significantly increased with the increase of the amount of PVP K30.Although the drug in the solid dispersion prepared by freeze-drying existsed in a microcrystalline form,its dissolution rate was significantly higher than that of rotary evaporation.Conclusion Increasing the level of the carrier and adopting the freeze-drying method can significantly improve the dissolution of tecovirimat.The dispersion form of the drug in solid dispersion,particle size,porosity and wettability of the samples should be considered in the selection of the preparation process.