缬沙坦缓释骨架片处方响应面法优化和制备  

Preparation of matrix tablets of valsartan and optimization of formulation by response surface methodology

作　　者：卢靖[1] 杨文思[1] 高崇凯[1] 

机构地区：[1]广东药学院药剂系,广州510006

出　　处：《中国新药杂志》2016年第2期219-225,共7页Chinese Journal of New Drugs

摘　　要：目的:响应面法优化缬沙坦骨架片处方,并进行体外释药评价。方法:以羟丙甲纤维素(hydroxypropyl methylcellulose,HPMC)为骨架材料,结合其他辅料制备缬沙坦骨架片。单因素实验考察处方因素对药物释放的影响,Box-Behnken响应面法(Box-Behnken design-response surface methodology,BBD-RSM)对处方进行优化,并对优化处方体外释药数据进行数学模型拟合。结果:优化后的缬沙坦骨架片体外释放性能良好,可持续释药12 h,药物释放符合Ritger-peppas模型。结论:通过BBD-RSM建立的模型可用于缬沙坦骨架片的处方优化,达到缬沙坦缓释骨架片设计要求。Objective： Optimization of valsartan matrix tablets prescription by response surface method,and to evaluate in vitro release. Methods： Hydroxypropyl methylcellulose（ HPMC） as matrix material,in combination with other materials for preparing valsartan matrix tablets. Effect of drug release of formulation factors were investigated through a single factor test and Box-Behnken design-response surface methodology were applied to optimize the formulation. The drug released mechanism of the tablet were studied by Model-fitted of drug released with different equations. Results： Optimized valsartan matrix tablets has a good performance in vitro release,sustainable release 12 h,drug release in line with Ritger-peppas model. Conclusion： The model established by Box-Behnken response surface methodology can be used to optimize the prescription valsartan matrix tablets,which achieved the design requirements.

关 键 词：缬沙坦 骨架片 BOX-BEHNKEN设计 响应面法 

分 类 号：R943.41[医药卫生—药剂学] R972.4[医药卫生—药学]