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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。
Objective To prepare chlorogenic acid bioadhesive microspheres and study its in vitro release and adhesion. Methods Chlorogenic acid bioadhesive microspheres were prepared by liquid-drying method. The best formulation and technology were selected by single factor in combination with the release behavior of microspheres. The in vitro release properties were investigated by HPLC, and the retention rate was taken as the index to evaluate the adhesion . Results The average loading rate of chlorogenic acid bioadhesive microspheres under the optimal prescription was 17.25% and the average entrapment efficiency was 57.25%. The microspheres released 92.07% after 12 h in vitro, and the in vitro release was in accordance with Weibull model: ln The average retention rate of mucosa in vitro was 78.54% and the average retention rate of mucosa in vivo was 30.23% [(1n (1-Q)]] = 0.6376lnt-0.4373 (r = 0.9819) Conclusion The preparation process is stable and feasible. The prepared microspheres have obvious sustained release effect.