替米考星β-环糊精聚合物微球的制备与表征

Preparation and Characterization of Tilmicosin β-Cyclodextrin Polymer Microspheres Inclusion Compound

[目的]优化替米考星β-环糊精聚合物(β-CDP)微球的制备工艺。[方法]采用共沉淀法制备替米考星β-CDP微球,以包封率和产率的回归分析综合得分为指标,通过L9(34)正交试验设计对制备工艺进行优化;采用扫描电镜、激光粒度分布仪、红外光谱仪和综合热分析仪对替米考星β-CDP微球进行表征。[结果]最佳工艺条件为:β-CDP微球3 g、替米考星0.25 g、反应温度50℃、反应时间1 h、搅拌速度600 r/min;在最佳工艺条件下:产率为83.32%,包封率为67.61%。以优化工艺制备的载药微球形态良好,平均粒径为161.35μm;替米考星进入到β-CDP微球中的内部,且以无定形的状态分散在聚合物载体中,具有较好的热稳定性。[结论]替米考星β-CDP微球制备方法合理可行。

[Objective]To optimize the preparation technology of Tilmicosin β-cyclodextrin polymer micro-spheres inclusion compound.[Method]Tilmicosin β-cyclodextrin polymer microspheres inclusion compound was prepared by coprecipitation method.The preparation process was optimized through the L9（34） orthogonal experimental design,the regression analysis was based on the evaluation indicators of drug produce and encapsulation efficiency.Tilmicosin β-cyclodextrin polymer microspheres inclusion compound was characterized by SEM,laser particle analyzer,FT-IR spectroscopy and thermo gravimetric analysis（TGA）.[Result]The best technological conditions were showed as following： the quantity of β-cyclodextrin polymer microspheres,Tilmicosin were 3 g,0.25 g respectively,the reacting temperature was 50 ℃,the reacting time was 3 h,stirring speed was 600 r/min.Under optimum conditions,the produce and drug encapsulation efficiency were 83.32% and 67.61% respectively.Through optimizing the preparation process,the loaded microspheres were endowed with good shape,and the average diameter of microparticle was 161.35 μm.Tilmicosin was dispersed with amorphous in microspheres,and it was ensured with good thermal stability.[Conclusion]The preparation method was reasonable and feasible.