替米考星β-CDP载药微球的制备及释药性能研究

Study on Preparation and Drug Release of Tilmicosin β-Cyclodextrin Polymer Microspheres

采用共沉淀法制备了替米考星β-CDP载药微球,讨论了投药比、反应时间、反应温度对替米考星β-CDP载药微球的影响,并探讨了其体外释药情况,运用红外光谱仪、电镜、粒度分析仪对产物进行了表征。结果表明,在β-CDP微球质量为3g、替米考星质量为0.25g、反应温度为50℃、反应时间为1.0h、搅拌速度为400r.min-1的条件下制得的载药微球的产率为81.60%、包封率为66.05%。替米考星β-CDP载药微球粒径分布均匀,外观圆整,在pH值为7.4的PBS中释药效果较好。载药微球释药与Korsmeyer-Peppas方程有较好拟合。

Tilmicosin β-cyclodextrin polymer （β-CDP） mierospheres was prepared by coprecipitation method. The influence of preparation conditions on tilrnicosin β-CDP microspheres and its drug release in vitro were investigated. Fourier transform infrared spectroscopy （IR）,scanning electron microscopy （SEM） and granularity analyaer were used to character tilmicosin β-CDP. The results showed that the optimum prepa- ration conditions were as follows： the quantity of fl-CDP was 3 g, the quantity of tilmicosin was 0.25 g, the reaction temperature was 50 ℃,the reaction time was 1.0 h,the stirring speed was 400 r· min^-1. The yield and drug encapsulation rate were 81.60% and 66.05%, respectively under above conditions. The tilmicosin β-CDP microspheres was uniform in particle size distribution,was round in appearance,and had a good drug release in PBS（pH=7.4）. And Korsmeyer-Peppas equation was adapted for its drug release characteristic.