茶碱β-环糊精聚合物微球的制备与缓释性能

Preparation and Sustained Release of Theophylline β-Cyclodextrin Polymer Microspheres Inclusion Compound

目的:以β-环糊精为原料,采用共沉淀法制备茶碱β环糊精聚合物(CDP)微球。方法:通过L9(34)正交试验设计对制备工艺进行了优化,并采用体外动态释药法评价其释药特征。分别用激光粒度分布仪、红外光谱仪、综合热分析仪、X射线衍射仪对茶碱β-CDP载药微球进行表征。结果:最佳工艺条件是β-CDP微球1 g、茶碱0.02 g、蒸馏水30 mL、反应时间3h、温度60℃。合成的载药微球形态良好,平均粒径为162.35μm,载药量为1.79%,包封率为89.50%。茶碱β-CDP微球体外释药规律符合一级释放方程和Korsmeyer-Peppas模型方程。结论:茶碱载药微球具有一定缓释效果,其制备方法合理可行。

Objective：Theophylline β-cyclodextrin polymer（β-CDP） microspheres inclusion compound was prepared with β-cyclodextrin as material by coprecipitation method.Method：The preparation process was optimized through the L9（34） orthogonal experimental design and theophylline release from theophylline β-cyclodextrin polymer microspheres was evaluated in vitro.Theophylline β-cyclodextrin polymer microspheres was characterized by laser particle analyzer,FT-IR spectroscopy,thermogravimetric analysis（TGA） and X-ray diffraction（XRD）.Result：The optimal procedure was β-CDP microspheres 1 g,theophylline 0.02 g,water 30 mL,time 3 h,and inclusion temperature 60 ℃.Average diameter of optimized products was 162.35 μm and the drug loading and drug encapsulation efficiency were 1.79% and 89.50% respectively.The drug release profile could be described by first-order release equation and Korsmeyer-Peppas equation.Conclusion：The sustained release microspheres had determinate effects be observed and this preparation method was reasonable and feasible.