双氯芬酸钾延迟缓释微丸的制备及体外释放

Preparation and in vitro evaluation of diclofenac potassium delayed-sustained release pellets

以乙基纤维素水分散体为包衣材料,采用双层包衣法制备双氯芬酸钾延迟缓释微丸,考察释放条件及处方因素对释药行为的影响,并用星点设计-效应面法对处方进行优化。结果表明,微丸的体外释药受介质pH的影响较大,受介质黏度影响较小;内外层包衣增重比例和外层包衣中致孔剂用量可影响释药时滞、释药速度以及最终释药量;星点设计-效应面法可用于微丸处方的优化。

Diclofenac potassium delayed-sustained release pellets were prepared by double-layer coating method with ethylcellulose aqueous dispersion.The effects of release condition and pellet compositions on the in vitro drug release were evaluated.The formulation was optimized by the central composite design-response surface methodology.It was shown that the pH of the media greatly affected the in vitro drug release of the pellets while the viscosity of the media had little influence.Drug release from the pellets was related to the proportion of the inner coat to the outer coat and the amount of pore forming agent in the outer coat.The optimization of the formulation could be achieved by the central composite design-response surface methodology.