四乙酰基葛根素固体自微乳化双层片的研究  

Preparation of bi-layered solid self-microemulsifying tablets of tetra-acetylated puerarin

作　　者：谢欢[1] 周伟[1] 刘姹[1] 杨大坚[1] 

机构地区：[1]香港理工大学现代中药研究所暨深圳市中药药学及分子药理学研究重点实验室,深圳518057

出　　处：《中国新药杂志》2011年第9期837-843,共7页Chinese Journal of New Drugs

基　　金：深圳市深港创新圈专项资助计划(SG200710190095A)

摘　　要：目的:探索固体自微乳化释药系统,制备四乙酰基葛根素固体自微乳化双层片。方法:考察各吸附材料对自微乳化液的吸附能力;以片剂外观、硬度、崩解时限等为指标筛选速释层处方;采用相似因子(f2)法评价双层片释药曲线的相似性,通过单因素考察,确定影响药物释放的主要因素;利用中心复合设计法对双层片处方进行优化,以HPMC K100LV和PEO400用量的各水平分别进行多元线性回归和二项式方程拟合,用效应面法预测最佳处方。结果:速释层的最佳处方为10%四乙酰基葛根素,30%自微乳化液,15%微粉硅胶,15%微晶纤维素,30%交联聚维酮,粘合剂为20%淀粉浆。缓释层中HPMC K100LV用量是影响药物释放的主要因素。中心复合设计优化处方的体外释放度预测值与实验值很接近。结论:中心复合设计法优化的固体自乳化双层片处方良好,双层片体外释放度达到了设计要求。Objective：To investigate solid self-microemulsifying drug delivery systems and prepare bi-layered solid self-microemulsifying tablets of tetra-acetylated puerarin.Methods：The adsorption capacity of different absorbents on microemulsion was evaluated.The formulation of rapid-release layer was selected according to appearance,hardness,friability and disintegration,etc.The similarity of the drug release curve was evaluated by similarity factor method（f2）.The formulation was developed based on a single-factor test,which was carried out to screen the critical influencing factors for the release rate.The optimal formulation was obtained by a central composite design,the response variables were the amount of HPMC K100LV,PEO400.A desirability function that combines these two response variables was constructed.A second-order polynomial equation was fitted to the data and the resulting equation was used to predict the responses in the optimal region.Results：The optimal formulation of the rapid-release layer was 10% tetra-acetylated puerarin,30% self-microemulsifying drug delivery systems,15% aerosil,15% microcrystalline cellulose,30% crospovidone,and 20% starch slurry as adhesive.The main factor affecting drug release was the amount of HPMC K100LV.The prediction of the cumulative release showed good agreement with the experimental results.Conclusion：The central composite design is able to optimize the formulation of the bi-layered solid self-microemulsifying tablets,and the cumulative release of the optimized bi-layered tablets is up to the standard of the design.

关 键 词：四乙酰基葛根素 固体自微乳化 双层片 中心复合设计 

分 类 号：R943.41[医药卫生—药剂学] R972[医药卫生—药学]