目的采用多元定位释药技术制备舒胸缓释胶囊.方法将处方药材精制后制备成舒胸微丸,然后分别采用HPMC、Eudragit L30D-55、Eudragit L100-Eudragit S100混合物(1:5)制备成3种包衣微丸,并按-定比例混合装入胶囊中.结果HPMC包衣微丸在任何pH值条件下均可释药,Eudragit L30D-55包衣微丸在pH≥5.5时开始释药, Eudragit L100-Eudragit S100(1:5)包衣微丸在pH≥6.8时开始释药.由3种包衣微丸混合制备而成的缓释胶囊,在模拟人体胃肠道pH变化条件下,呈现出-种pH依赖型梯度缓释特征,而且处方中的主要成分三七总皂苷、红花黄色素、阿魏酸、川芎嗪的释放度差异无显著性.结论采用定位释药技术制备而成的舒胸缓释胶囊中理化性质不同的各成分在缓释的同时可以达到同步释放,遵循了中药制剂复方配伍的整体观和用药思想.

Objective To prepare Shuxiong Sustained-release Capsule by multiparticulate site-controlled release technique.Methods First,Shuxiong pellets were prepared with the refined medicinal materials containing in the recipe of Shuxiong Tablets.Then,three kinds of coated pellets were prepared by HPMC,Eudragit L-30D-55,and Eudragit L100-Eudragit S100 combinations(1:5)as coater,respecti-vely.Finally,Shuxiong Sustained～release Capsules were developed by encapsulating the above three kinds of coated pellets as certain ratio in hard gelatin capsules.Results The three kinds of pellets coated with HPMC,Eudragit L-30D-55 and Eudragit L100-Eudra-git S100 combinations(1:5)could dissolve in any pH condition water,at pH value 5.5 or above and at pH value 6.8 or higher,respecti-vely. The release profiles of notoginseng saponin,safflower yellow,ferulic acid,and tetramethylpyzine from Shuxiong Sustained-rele-ase Capsules showed a characteristic of pH-dependent gradient-release in the simulated gastrointestinal pH conditions and no signi-ficant difference among them.Conclusion The results indicate that the multiparticulate site-controlled release technique makes it possible that various components with extremely different physicochemical properties in sustained-release formulations of traditional Chinese medicinal eompound recipe could release synchronously while sustained-releasing.That complies with the whole conception of formulated compatibility of traditional Chinese medicinal compound recipe.

国家自然科学基金资助项目(30200363);辽宁省博士启动基金资助项目(2001102042)