乳酸环丙沙星淀粉微球的体外释药研究

目的：制备乳酸环丙沙星淀粉微球并对其体外释放行为进行考察。方法：采用反相乳液聚合法结合包埋载药法制备乳酸环丙沙星淀粉微球，应用体外恒温透析法考察其释药行为及影响因素，以紫外可见分光光度法测定并计算累积释药百分数。使用origin软件，将微球释药数据与载药微粒的主要释药方程进行拟合，以找出最佳拟合释药方程。结果：制备的乳酸环丙沙星淀粉微球置于生理盐水中约5小时后达到释放平衡，其释放行为受处方中球-药比和交联剂用量及释放介质的影响。该载药淀粉微球的释药行为最符合双指数双相动力学方程，即呈双相释放，前期为快速释放相，后期（5小时后）为缓慢释放相。结论：本制剂工艺切实可行，所得乳酸环丙沙星淀粉微球具有明显的缓释制剂特征。

The Release Profile of Ciprofloxacin Lactate Starch Microspheres in vitro

Objective： To prepare ciprofloxacin lactate starch microspheres（CFL-SM ） and to investigate the release profile of the microspheres in vitro. Methods： CFL-SM were prepared by inverse emulsion polymerization and encapsulation. The homeothermia dialysis system and UV method for the determination of accumulated release percentage were used to investigate in vitro release of these microspheres and the impact factors thereof. The release data of CFL-SM were fitted with main drug-release equations for drug-loaded micmparticles using origin software to find the optimal fitting release equation. Results：The prepared CFL-SM showed a stable release in NS after 5 n, of which the release behavior was related to microsphere-drug ratio and crosslinker content in the formulation and release medium. The release behavior of CFL-SM was well-fitted to ambiexponent equation, with diphasic release including early rapid release and late（after 5 h） slow release. Conclusion： The preparation process is feasible, and CFL-SM prepared possess the properties of sustained release formalotion.