Box Behnken响应面法优化氢氯噻嗪速释微丸的处方

Optimization of Immediate-release Pellets Formulation of Hydrochlorothiazide by Box Behnken Design

目的:筛选以挤出滚圆法制备氢氯噻嗪速释微丸的处方。方法:采用Box Behnken响应面法优化设计及Design Expert软件,对挤出滚圆法制备氢氯噻嗪为模型药的处方优化区域确定及优化处方验证。结果:最优处方为每单位剂量含氢氯噻嗪30%,淀粉64.53%,L-HPC5.27%,SLS 0.2%,PVP K30水溶液浓度为4.15%(w/w),微丸收率为90.2%,长径比为1.12,实测值与预测值相符。结论:用此处方,挤出滚圆法制备的氢氯噻嗪微丸表面光洁、圆整,溶出快、收率高。

Objective： To prepare immediate-release pellets of hydrochlorothiazide via extrusion/spheronisation. Methods： Hydrochlorothiazide was used as a model drug. Box Behnken design with three variables was used to optimise the formulation and to evaluate pellet yield and sphericity. Data analysing and response surface fitting was conducted by the Design Expert software. Results： The optimised formulation was as follows： HCT 30%,starch 64.53%,SLS 0.2% and L-HPC 5.27%. The concentration of PVP K30 solution was 4.15%. The yield and aspect ratio of pellets was 90.2% and 1.12,respectively. There was no significant difference between observed and predictive responses. Conclusion： Pellets with a high yield,acceptable sphericity and fast dissolution were obtained.