Box-Behnken响应面法优化去氧氟尿苷缓释片处方及其体外释放机制研究  

Optimization of the sustained-release tablets of doxifluridine using the Box-Behnken design and the study on the mechanism of in vitro drug release

作　　者：赵科[1] 刘源[1] 赖可[1] 任静[1] 

机构地区：[1]抗生素研究与再评价四川省重点实验室四川抗菌素工业研究所成都大学,成都610052

出　　处：《中国抗生素杂志》2018年第1期64-68,共5页Chinese Journal of Antibiotics

基　　金：四川省科技厅应用基础项目(No.2016JY0256);四川省教育厅科研项目(No.17ZB0118);成都大学校青年基金项目(No.2014XQCKS13)

摘　　要：目的响应面法优化去氧氟尿苷骨架片处方,并进行体外释放机制研究。方法以羟丙甲纤维素(HPMC K4M)为骨架材料,结合其他辅料混合均匀,以直接压片法制备去氧氟尿苷骨架缓释片。通过Box-Behnken响应面法(Box-Behnken designresponse surface methodology,BBD-RSM)对处方进行优化,研究优化处方的体外释药规律,并进行数学模型拟合。结果优化处方的去氧氟尿苷骨架缓释片体外释放性能良好,可持续释药24h,药物释放符合Ritger-peppas模型。结论通过BBD-RSM建立的模型可用于去氧氟尿苷骨架缓释片的处方优化,优化处方达到去氧氟尿苷缓释骨架片设计要求。Objective Optimization of the matrix tablets prescription of doxifluridine by the response surface method, and to research mechanism of in vitro release. Methods Hydroxypropyl methylcellulose （HPMC K4M） was used as the matrix material, using the method of direct tableting in combination with other materials for preparing the matrix sustained-release tablets of doxifluridine. The drug released mechanism of the tablets were studied by the model-fitting of drug release with different equations and the Box-Behnken design-response surface methodology was applied to optimize the formulation. Results Optimized the matrix sustained-release tablets of doxifluridine had a good performance in vitro release. It achevied sustainable release for 24h, and the drug release was in line with the ritger-peppas model. Conclusion The model established by the Box-Behnken response surface methodology can be used to optimize the prescription of the matrix sustained-release tablets of doxifluridine which achieved the design requirements.

关 键 词：去氧氟尿苷 骨架缓释片 Box-Behnken响应面法 体外释放机制 

分 类 号：R9[医药卫生—药学]