Objective To determine whether the anti-inflammatory properties of Shuxiong Tablet (SXT) and the effective components group of SXT (ECGS) are equivalent and to assess the formulary rationality. Methods ECGS consisted ...Objective To determine whether the anti-inflammatory properties of Shuxiong Tablet (SXT) and the effective components group of SXT (ECGS) are equivalent and to assess the formulary rationality. Methods ECGS consisted of Panax notoginsen saponion (PNS), hydroxysafflor yellow A, and ferulic acid plus volatile oil of Ligusticum chuanxiong, which was based on the active ingredients and their ratios in SXT. We compared the anti-inflammatory actions of ECGS and SXT using the xylene-induced edema model and the carrageenan-induced edema model, as well as the analgesic activity of them using the acetic acid-induced writhing model. Moreover, cultured macrophages were incubated with media containing serum isolated from SXT-, ECGS-, or every component of ECGS-treated rats, to compare the depress effects on lipopolysaccharide (LPS)-stimulated NO production and inducible nitric oxide synthase (iNOS) expression. Results ECGS and SXT had equivalent anti-inflammatory actions and analgesic effects at an equipotent dosage in a dose-dependent manner. The drug-containing media could inhibit the LPS-stimulated NO production and iNOS expression in cultured macrophages. A 2 × 2 × 2 ANOVA revealed that three effective components could produce synergistic effect on the inhibition of NO production, and PNS was the capital component. Conclusion ECGS and SXT display an equivalent anti-inflammatory effect, and the formula follows traditional Chinese medicine compatibility principle, which shows obvious formulary rationality.展开更多
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HPM C、Eudrag it L 30D-55、Eudrag it L 100-Eudrag it S100混合物(1∶5)制备成3种包衣微丸,并按一定比例混合装入胶囊中。结果HPM C包...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HPM C、Eudrag it L 30D-55、Eudrag it L 100-Eudrag it S100混合物(1∶5)制备成3种包衣微丸,并按一定比例混合装入胶囊中。结果HPM C包衣微丸在任何pH值条件下均可释药,Eudrag it L 30D-55包衣微丸在pH≥5.5时开始释药,Eudrag it L 100-Eudrag it 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,呈现出一种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。展开更多
目的制备复方中药舒胸速释微丸,筛选速释微丸的最佳制备工艺和处方,使理化性质差异较大的各成分达到同步释放。方法采用挤出滚圆法制备复方中药舒胸速释微丸,以阿魏酸、红花黄色素、三七总皂苷为体外溶出考察的主要指标性成分,对微丸中...目的制备复方中药舒胸速释微丸,筛选速释微丸的最佳制备工艺和处方,使理化性质差异较大的各成分达到同步释放。方法采用挤出滚圆法制备复方中药舒胸速释微丸,以阿魏酸、红花黄色素、三七总皂苷为体外溶出考察的主要指标性成分,对微丸中加入的崩解剂种类和用量、粘合剂和表面活性剂等处方因素进行筛选,并采用正交设计试验以筛选最优处方。结果在处方中加入复合崩解剂(20%泡腾崩解剂、5%羧甲基淀粉钠),以70%乙醇(含2%十二烷基硫酸钠)为粘合剂,可使制备的舒胸速释微丸在1 m in内迅速崩解。在模拟人体胃肠道生理条件下,舒胸速释微丸中红花黄色素和三七总皂苷体外释放的f2值为77.34,红花黄色素和阿魏酸的f2值为58.67,三七总皂苷与阿魏酸的f2值为67.83,表明三者的释放度差异无显著性。结论通过加入复合崩解剂,可以使采用挤出滚圆法制备的舒胸速释微丸迅速崩解,从而使复方中药中理化性质差异较大的各种成分达到同步释放。展开更多
基金National Natural Science Foundation of China (30430790)
文摘Objective To determine whether the anti-inflammatory properties of Shuxiong Tablet (SXT) and the effective components group of SXT (ECGS) are equivalent and to assess the formulary rationality. Methods ECGS consisted of Panax notoginsen saponion (PNS), hydroxysafflor yellow A, and ferulic acid plus volatile oil of Ligusticum chuanxiong, which was based on the active ingredients and their ratios in SXT. We compared the anti-inflammatory actions of ECGS and SXT using the xylene-induced edema model and the carrageenan-induced edema model, as well as the analgesic activity of them using the acetic acid-induced writhing model. Moreover, cultured macrophages were incubated with media containing serum isolated from SXT-, ECGS-, or every component of ECGS-treated rats, to compare the depress effects on lipopolysaccharide (LPS)-stimulated NO production and inducible nitric oxide synthase (iNOS) expression. Results ECGS and SXT had equivalent anti-inflammatory actions and analgesic effects at an equipotent dosage in a dose-dependent manner. The drug-containing media could inhibit the LPS-stimulated NO production and iNOS expression in cultured macrophages. A 2 × 2 × 2 ANOVA revealed that three effective components could produce synergistic effect on the inhibition of NO production, and PNS was the capital component. Conclusion ECGS and SXT display an equivalent anti-inflammatory effect, and the formula follows traditional Chinese medicine compatibility principle, which shows obvious formulary rationality.
文摘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HPM C、Eudrag it L 30D-55、Eudrag it L 100-Eudrag it S100混合物(1∶5)制备成3种包衣微丸,并按一定比例混合装入胶囊中。结果HPM C包衣微丸在任何pH值条件下均可释药,Eudrag it L 30D-55包衣微丸在pH≥5.5时开始释药,Eudrag it L 100-Eudrag it 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,呈现出一种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。
文摘目的制备复方中药舒胸速释微丸,筛选速释微丸的最佳制备工艺和处方,使理化性质差异较大的各成分达到同步释放。方法采用挤出滚圆法制备复方中药舒胸速释微丸,以阿魏酸、红花黄色素、三七总皂苷为体外溶出考察的主要指标性成分,对微丸中加入的崩解剂种类和用量、粘合剂和表面活性剂等处方因素进行筛选,并采用正交设计试验以筛选最优处方。结果在处方中加入复合崩解剂(20%泡腾崩解剂、5%羧甲基淀粉钠),以70%乙醇(含2%十二烷基硫酸钠)为粘合剂,可使制备的舒胸速释微丸在1 m in内迅速崩解。在模拟人体胃肠道生理条件下,舒胸速释微丸中红花黄色素和三七总皂苷体外释放的f2值为77.34,红花黄色素和阿魏酸的f2值为58.67,三七总皂苷与阿魏酸的f2值为67.83,表明三者的释放度差异无显著性。结论通过加入复合崩解剂,可以使采用挤出滚圆法制备的舒胸速释微丸迅速崩解,从而使复方中药中理化性质差异较大的各种成分达到同步释放。
