【摘要】 目的 制备pH依赖型梯度释药的双黄连微丸，以实现药物在体内的梯度脉冲释放。方法将酸中溶解度低的指标性成分黄芩苷制备成固体分散体，采用挤出滚圆法分别制备双黄连素丸和双黄连固体分散体微丸，选择Eudragit L30D-55和Eudragit L100/S100为包衣材料，采用流化床进行包衣。将固体分散体微丸、Eudragit L30D-55包衣微丸和Eudragit L100/S100包衣微丸按照比例混合即得。结果 双黄连固体分散体微丸在pH> 1.2的介质中释药，Eudragit L30D-55包衣微丸在pH> 5.5的介质中开始释药，Eudragit L100/S100包衣微丸在pH> 6.8的介质中开始释药。三种微丸按照比例混合之后在模拟人体胃肠道pH环境变化的体外释放介质中呈现良好的pH依赖型释药特性，且指标性成分黄芩苷和绿原酸的体外释放行为相似。结论 利用人体胃肠道pH变化，采用多元定位释药技术制备的双黄连pH依赖性梯度释药微丸可以在长效释放的同时达到同步释放，满足中医药理论下的用药思想和整体观念。更多还原

【Abstract】 Objective To prepare Shuanghuanglian pH-dependent gradient-release pellets to achieve gradient pulse release in the body. Methods To prepare baicalins with low solubility in acid into solid dispersion. Shuanghuanglian and Shuanghuanglian solid dispersion pellets were prepared with extrusion roller. Eudragit L30D-55 and Eudragit L100/S100 were used as coating in fluidized beds. Solid dispersion pellets, Eudragit L30D-55 coated pellets and Eudragit L100/S100 coated pellets were mixed in proportion. Results Shuanghuanglian solid dispersion pellets were released medium with in pH > 1.2, and Eudragit L30D-55 coated pellets started to release in the medium with pH > 5.5, and Eudragit L100/S100 coated pellets in the medium with pH >6.8. After mixing the three pellets, a good pH-dependent release property was present in an in vitro release medium that simulated the changes of human gastrointestinal pH. The in vitro release behavior of the chlorogenic acid and baicalin of the indicator component was similar. Conclusion Shuanghuanglian pH-dependent gradient-release pellets prepared with human gastrointestinal pH, and multiparticulate site-controlled release technology improve the modification of index components, can synchronously release with gradient at long term. That complies with the organic whole conception of compatibility of traditional Chinese medicinal compound recipe.更多还原