格列吡嗪控释微球的制备及体外释药性质

为研究口服药物控释微球的制备及其体外释药性质,以格列吡嗪为模型药物,采用喷雾干燥法制备具有恒速释药性质的微球.通过考察微球的收率、包封率以及体外释放特性,研究了载体材料、材料与药物比例以及药物释放环境对格列吡嗪控释微球释药性质的影响.结果表明,采用醋酸纤维素为载体材料,选用合适的配方,可制得具有零级释药动力学的格列吡嗪控释微球制剂,并且该制剂可以根据需要的条件在12 h或24 h内释放完毕.不同条件下微球的药物释放曲线线性拟合的相关系数在0.981～0.999之间.

Preparation and in vitro release of glipizide loaded controlled release microspheres

Controlled release microspheres of glipizide were prepared by spray drying of polymer solutions containing the drug and other additives. The microspheres were characterized by a series of pharmaceutical properties, including microsphere morphology, microencapsulation efficiency and yield. Then drug release kinetics were investigated in vitro for various formulations and process parameters to optimize release profiles. The results suggest that the polymer matrix, function, and release media can affect the microsphere release properties. Zero-order release of glipizide in 12 h or 24 h could be achieved with cellulose acetate as the matrix in the optional formulation. For the various conditions, the release curves were approximately linear with correlation coefficients from 0.981~0.999.