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目的:优化鞣花酸微球的制备工艺并考察其体外释药机制,为该制剂的体内药物动力学研究提供参考。方法:采用HPLC测定鞣花酸含量,流动相乙腈-0.1%磷酸水(23∶77),检测波长254 nm。以微球释放度为考察指标,通过正交试验考察海藻酸钠、壳聚糖、氯化钙质量分数及海藻酸钠-药物质量比对鞣花酸微球处方工艺的影响,利用零级动力学方程、一级动力学方程和Higuchi方程进行体外释放度拟合。结果:最佳处方工艺为海藻酸钠-鞣花酸(3∶1),海藻酸钠2%,氯化钙2%,壳聚糖0.1%;微球在48 h内平均释放度80.14%,体外释放符合Higuchi方程Q=0.131t1/2-0.046 9(r=0.966 4)。结论:该处方工艺稳定可行、重复性好。鞣花酸微球体外释放具有缓释性能。
OBJECTIVE: To optimize the preparation process of ellagic acid microspheres and study its in vitro drug release mechanism, and to provide a reference for pharmacokinetics of ellagic acid microspheres in vivo. Methods: The ellagic acid was determined by HPLC. The mobile phase was acetonitrile - 0.1% phosphoric acid (23:77). The detection wavelength was 254 nm. Taking the release degree of microspheres as the index, the effects of sodium alginate, chitosan, calcium chloride mass fraction and sodium alginate-drug mass ratio on the prescription of ellagic acid microspheres were investigated by orthogonal experiments. Learning equation, first-order kinetic equation and Higuchi equation for in vitro release fitting. Results: The optimal prescription was sodium alginate - ellagic acid (3:1), sodium alginate 2%, calcium chloride 2% and chitosan 0.1%. The mean release of microspheres was 80.14% within 48 h, In vitro release was in accordance with the Higuchi equation Q = 0.131t1 / 2-0.046 9 (r = 0.966 4). Conclusion: The prescription process is stable and reproducible. Ellagic acid microspheres in vitro release with sustained-release properties.