基于星点设计-效应面法优化的曲美他嗪双层渗透泵控释片的制备及评价  

Preparation and evaluation of trimetazidine sustained-release tablets by central composite design and response surface methodology

作　　者：朱志红[1] 曲绪楷 梁静阁 张文骥[1] 江美增 王雨微[1] 王冠乔[1] 杨星钢[1] 潘卫三[1] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016 [2]天津药物研究院,天津300193

出　　处：《中国新药与临床杂志》2014年第8期599-603,共5页Chinese Journal of New Drugs and Clinical Remedies

基　　金：国家基础科学人才培养基金项目(J1103606);释药技术与药代动力学国家重点实验室开放课题(2012CB724000)

摘　　要：目的制备曲美他嗪双层渗透泵控释片并优化其处方。方法以含药层聚氧乙烯用量、助推层氯化钠用量、包衣增重为考察因素,药物的8 h累积释放度和0～8 h释放曲线的线性相关系数为考察指标,应用星点设计-效应面法对处方进行优化并验证。结果最优处方为含药层聚氧乙烯的用量86 mg,助推层氯化钠用量为25 mg,包衣增重7%。其释放曲线在0～8 h零级释放特征显著,8 h累积释放量达到89%以上,实测值与预测值无明显差异。结论采用星点设计-效应面法成功得到曲美他嗪双层渗透泵控释片的处方优化模型,实现了处方优化。AIM To prepare trimetazidine osmotic pump tablets and optimize its formulation by central composite design- response surface methodology （CCDRSM）. METHODS The amount of polyethylene oxide （PEO） which used as an adjuvant of trimetazidine pump tablets, the amount of NaC1, and the coating weight increase were used as three factors for investigation, and the cumulative release amount at 0 h to 8 h respectively, and the linear correlation coefficient （r） of the cumulative release amount versus time were taken as indexes. The formulation of trimetazidine was optimized by CCDRSM and the optimized formulation was verified. RESULTS The optimized formulation obtained was as follows： PEO 86 mg, NaCl 25 mg, and the coating weight increase 7%. A well zero-order release characteristic up to 0 - 8 h was achieved and cumulative release of TMZ was up to 89%. CONCLUSION The CCDRSM can be applied to optimize the formulation of trimetazidine and the established model is of satisfactory predictive value.

关 键 词：曲美他嗪 迟效制剂 星点设计-效应面法 评价研究 

分 类 号：R943[医药卫生—药剂学]