盐酸普萘洛尔延时脉冲微丸的制备与体外释放研究  

Preparation and in vitro dissolution of pulsatile release pellets of propranolol hydrochloride

作　　者：蔡丹宁 吴瑞[1] 胡晓[1] 宗莉[1] CAI Dan-ning;WU Rui;HU Xiao;ZONG Li(Department of Pharmaceutics,China Pharmaceutical University,Jiangsu Nanling 210009,China;Hubei Institute of Drug Control,Hubei Wuhan 430075,China)

机构地区：[1]中国药科大学药剂系,江苏南京210009 [2]湖北省药品监督检验研究院,湖北武汉430075

出　　处：《中国医院药学杂志》2018年第24期2537-2541,共5页Chinese Journal of Hospital Pharmacy

摘　　要：目的:基于有机酸诱导原理制备盐酸普萘洛尔延时脉冲微丸,并研究其体外释药行为。方法:以低渗型丙烯酸树脂为包衣材料,采用空白丸心上药法制备含有机酸的载药微丸,考察处方因素对药物释放的影响,应用Box-Behnken效应面设计优化处方。通过有机酸与包衣膜相互作用试验探索其体外释药机制。结果:药物与琥珀酸分层的微丸具有较理想的脉冲释药特征,最优处方体外释药时滞约为4h,时滞后2h累积释放量90%以上,其体外释放曲线符合logistic模型。有机酸能够降低衣膜的玻璃化转变温度并促进其水化,从而提高包衣膜渗透性而加速释放。结论:所得微丸具有良好的体外脉冲释放效果。OBJECTIVE To prepare pulsatile release pellets of propranolol hydrochloride with proper lag time based on or-ganic acid induction,and investigate the in vitro drug release.METHODS Pulsatile release pellets were prepared by coating the blank seeds with drug and organic acid,followed by coating with Eudragit^■ RS.The effect of pellet formulation on in vitro release was evaluated.The formula was then optimized by Box-Behnken design.The release mechanism was explored by investigating the organic acid-film interactions.RESULTS Pellets with drug and succinic acid in separate layers showed ideal pulsa-tile release characteristics.The optimized pellets showed a lag time of about 4hand a cumulative release of over 90% at 6h. Logistic model could be used to fit the release profile.Organic acid increased the permeability of the outer coating and thus the drug release,by promoting film hydration and reducing T g .CONCLUSION The obtained pellets display good pulsatile release behavior in vitro .

关 键 词：脉冲微丸 有机酸诱导 体外释放 BOX-BEHNKEN设计 

分 类 号：R944[医药卫生—药剂学]