绿原酸生物黏附微球的制备及其体外释放特性的研究

目的制备绿原酸生物黏附微球,并考察其体外释放规律和黏附性。方法采用液中干燥法制备绿原酸生物黏附微球,结合微球的释放行为,单因素筛选最佳处方和工艺;用HPLC法考察其体外释放性质,采用滞留率作为考察其黏附性的指标。结果绿原酸生物黏附微球在最佳处方条件下的平均载药量为17.25%,平均包封率为57.25%;微球在体外12 h可释放92.07%,体外释药符合Weibull模型:ln[ln[1/(1-Q)]]=0.6376lnt-0.4373(r=0.9819);体外黏膜平均滞留率为78.54%,体内黏膜平均滞留率为30.23%。结论所用制备工艺稳定可行,所制微球具有明显的缓释效果。

Preparation of chlorogenic acid loaded bioadhesive microspheres and its release profile in vitro

OBJECTIVE To prepare chlorogenic acid loaded bioadhesive microspheres and investigate its release profile in vitro and mucoadhesive characteristics.METHODS Chlorogenic acid loaded bioadhesive microspheres were prepared by solvent evaporation method.The formulations and the preparation methods were evaluated by single factor selecting experiment and the release profile.The drug release was analyzed by HPLC.Its mucoadhesive property was evaluated using stagnation percentage.RESULTS The average drug loading content and encapsulation efficiency of the optimum formulation of chlorogenic acid loaded bioadhesive microspheres were 17.25% and 57.25%.The microspheres could release 92.07% in vitro in 12 h.The release in vitro accorded to the Weibull order model:ln[ln[1/(1-Q)]]=0.6376lnt-0.4373(r=0.9819).The average stagnation percentage in vitro and vivo was 78.54% and 30.23%,respectively.CONCLUSION The preparation procedure was stable and practical,and the microspheres obtained showed a sustained-release character.