他达那非固体分散体的制备和性质研究

目的制备他达那非(tadalafil,TD)固体分散体并进行性质研究。方法利用喷雾干燥法制备固体分散体,以表观溶解度和溶出度为指标筛选处方,采用差示扫描量热(DSC)、粉末X-射线衍射(PXRD)和接触角测定等技术研究药物的存在状态和润湿性等理化性质。结果固体分散体将他达那非的表观溶解度提高22.6倍;20min内药物的累积溶出超过90%;固体分散体药物以分子或无定形状态存在;接触角减小,润湿性增大。结论采用十二烷基硫酸钠(SDS)和介孔硅为载体制备的他达那非固体分散体,能明显提高药物的表观溶解度和溶出度。

Preparation and characteristics of tadalafil solid dispersions

Objective To prepare tadalafil(TD) solid dispersions and investigate the basic characteristics of the solid dispersion . Methods The solid dispersion was prepared by spray drying technology ,and an optimal formulation of the solid dispersion was screened by using apparent solubility and dissolution experiments as indexes .The characteristics including drug state in the disper‐sion and wettability of the dispersion were investigated by DSC ,PXRD and contact tangle examining technology .Results Through preparing the solid dispersions of TD ,the apparent solubility of TD was enhanced up to 22 .6 times;the drug release within 20 min exceeded 90% ;the drug state in dispersion was molecular state or amorphous form ;the contact angle decreased and the wettability of solid dispersion increased .Conclusion The apparent solubility and the dissolution of TD were improved by solid dispersion by u‐sing SDS and mesoporous silica as carriers .