格列齐特缓释微丸胶囊的制备及体外释放度考察

Study on Preparation and Dissolution Test in Vitro of Gliclazide Extended-release Pellet Capsule

目的对格列齐特缓释微丸胶囊的处方和工艺进行研究,并考察其体外释放度。方法以微丸成球性和释放度为评价指标,采用正交设计试验优化处方与工艺。结果格列齐特缓释微丸的最优处方为格列齐特15g,微晶纤维素25g,乙基纤维素3g,硬脂酸6g;最佳工艺为以水作黏合剂,用量35%,采用挤出滚圆法制备微丸,挤出转速30r/min,50r/min高速剪切1min,30r/min滚圆5min。所制微丸圆整度好,平面临界角12.1°,收率94.8%;释药行为符合Higuchi方程,具有明显的缓释特征。结论格列齐特缓释微丸胶囊具有良好的体外缓释效果,可进一步进行体内释药行为考察。

Objective To study prescription and technique of gliclazide extended-release pellet capsule（EPC） and to inspect release property in vitro. Methods The orthogonal experiment was designed to screen prescription and technique which were definited with the colligation evaluation of formation and release of pellets. Results The optimization of prescription and technique were definited： gliclazide 15g, MCC 25 g, EC 3 g, stearic acid 6 g, distilled water as adhesive and 35% in quantity. The pellets were prepared by extrusion/spheronization. Speed of extrusion： 30 r/min, speed of spheronization： 50 r/min, time of spheronization： 1 min, time of spheronization： 5 min. The pellets prepared had good spheronization. The critical angle of plan was 12.1°, the recovery rate was 94.8%. The release behavior of gliclazide EPC coincidented with Higuchi equation well and the character of extended- release was transparent. Conclusion Gliclazide EPC has good effect of extendedrelease in vitro and the release behavior in vivo need to be inspected.