伊曲康唑固体分散体制备及体外溶出实验

Preparation of itraconazole solid dispersion with PVP and dissolution experiment in vitro

目的 :运用固体分散体技术提高难溶性药物伊曲康唑的溶解度及体外溶出速率。方法 :选用聚乙烯吡咯烷酮 (PVPK30 )为载体 ,采用喷雾干燥法制备伊曲康唑固体分散体 ,通过差热分析及X射线衍射对固体分散体进行鉴定 ,比较考察伊曲康唑及其物理混合物和固体分散体的溶出特性。结果 :差热分析、X射线衍射图谱表明药物以无定形状态分散于载体中 ;体外溶出结果表明固体分散体能显著增加药物在水及人工胃液中的溶出度 (45min时 1∶4固体分散体体外溶出度为伊曲康唑的 1 1 .5倍。 1∶4固体分散体在 0 .1mol·L-1 盐酸中溶解度是伊曲康唑的 6 7倍 )。结论 :伊曲康唑固体分散体能明显提高伊曲康唑的溶解度及体外溶出速率。

OBJECTIVE The aim of present study is to improve the solubility and dissolution rate of itraconazole,which is sparingly soluble in water by a solid dispersion technique.METHODS Solid dispersion (SD) particles of itraconazole were prepared with PVP K30 by spray drying and were characterized by differential scanning calorimetry, powder X-ray diffraction.RESULTS The result of differential scanning calorimetry and powder X-ray diffraction test showed that spray drying resulted in the formation of an amorphous solid dispersion of itraconazole and PVP. Dissolution measurements demonstrated that a significantly increased dissolution rate was obtained with the amorphous solid dispersion compared to the physical mixture. Dissolution rate of itraconazole/PVP (1∶4 w/w) was 11.5 times than itraconazole powder at 45 min. Solubility of itraconazole in solid dispersion with PVP was 67 times than itraconazole.CONCLUSION Itraconazole solid dispersion can significantly increase it's solubility and dissolution rate.