目的采用多元定位釋藥技術制備舒胸緩釋膠囊.方法將處方藥材精制后制備成舒胸微丸,然后分別采用HPMC、Eudragit L30D-55、Eudragit L100-Eudragit S100混合物(1:5)制備成3種包衣微丸,并按-定比例混合裝入膠囊中.結(jié)果HPMC包衣微丸在任何pH值條件下均可釋藥,Eudragit L30D-55包衣微丸在pH≥5.5時開始釋藥, Eudragit L100-Eudragit S100(1:5)包衣微丸在pH≥6.8時開始釋藥.由3種包衣微丸混合制備而成的緩釋膠囊,在模擬人體胃腸道pH變化條件下,呈現(xiàn)出-種pH依賴型梯度緩釋特征,而且處方中的主要成分三七總皂苷、紅花黃色素、阿魏酸、川芎嗪的釋放度差異無顯著性.結(jié)論采用定位釋藥技術制備而成的舒胸緩釋膠囊中理化性質(zhì)不同的各成分在緩釋的同時可以達到同步釋放,遵循了中藥制劑復方配伍的整體觀和用藥思想.

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.

國家自然科學基金資助項目(30200363);遼寧省博士啟動基金資助項目(2001102042)