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目的:优选甘草总黄酮微海绵的制备工艺并考察其体外释放度。方法:利用类乳剂溶媒扩散法制备甘草总黄酮微海绵,以微海绵得率、包封率及分散系数为指标,通过星点设计-效应面法考察聚乙烯醇用量、药物与乙基纤维素的比例、搅拌速度对甘草总黄酮微海绵制备工艺的影响。利用紫外分光光度法测定甘草总黄酮微海绵的包封率,检测波长335 nm;建立HPLC同时测定甘草总黄酮中甘草苷、异甘草苷、甘草素、异甘草素、甘草查尔酮A和光甘草定的含量,检测波长300 nm,流动相乙腈-甲醇-0.2%磷酸水溶液梯度洗脱;利用透析法比较甘草总黄酮及甘草总黄酮微海绵中6个成分的体外释放度。结果:甘草总黄酮微海绵的最佳制备工艺为聚乙烯醇用量2.69%,药物-乙基纤维素(6∶1),搅拌速度1 100 r·min~(-1),搅拌时间4 h。8 h内甘草总黄酮中甘草苷、异甘草苷、甘草素、异甘草素、甘草查尔酮A和光甘草定的累积释放度分别为87.47%,86.83%,76.98%,78.48%,86.58%和56.58%,24 h内甘草总黄酮微海绵中这6个成分的累积释放度分别为91.45%,89.74%,77.57%,82.64%,87.74%和67.74%。结论:利用类乳剂溶媒扩散法制备的甘草总黄酮微海绵粒径大小均匀、工艺稳定且操作简便。甘草总黄酮微海绵具有明显的缓释作用。
Objective: To optimize the preparation process of licorice flavonoids micro sponges and investigate its in vitro release. Methods: Microemulsions of licorice flavonoids were prepared by emulsion-solvent diffusion method. With the rate of micro-sponge, entrapment efficiency and dispersion coefficient as indices, the amount of polyvinyl alcohol Of the ratio of stirring speed on the preparation of flavonoids glycyrrhiza flavonoids. The encapsulation efficiency of glycyrrhiza flavonoids micro sponge was detected by UV spectrophotometry at a wavelength of 335 nm. HPLC was used to determine the contents of glycyrrhizin, isoliquiritin, glycyrrhizin, isoliquiritigenin, licochalcone A and licorice root The detection wavelength was set at 300 nm and the mobile phase was eluted with a gradient of acetonitrile-methanol-0.2% phosphoric acid. The dialysis method was used to compare the in vitro release of six components of total flavonoids from licorice root and micro-sponge of licorice flavonoids. Results: The optimal preparation technology of total flavone micro-sponge of licorice root was 2.69% of polyvinyl alcohol, 6:1 of drug-ethylcellulose, the stirring speed was 1 100 r · min -1 and the stirring time was 4 h. The cumulative release of glycyrrhizin, isoliquiritin, glycyrrhizin, isoliquiritigenin, licochalcone A and glabridin in the total flavones of licorice root in 8 h were 87.47%, 86.83%, 76.98%, 78.48%, 86.58% and 56.58%. The cumulative release of these six components in licorice flavonoids micro-sponge was 91.45%, 89.74%, 77.57%, 82.64%, 87.74% and 67.74% respectively within 24 h. Conclusion: The glycyrrhiza flavonoids micro-sponge particle size prepared by the emulsion-like solvent diffusion method is uniform in size, stable in process and easy to operate. Licorice flavonoids micro sponge has a significant sustained release effect.