论文摘要
Time-sensitive and pH-dependent polymers are generally employed to prepare colon-site delivery system, and their coating thickness and order are very important in controlling the drug release. The traditional colon-site delivery systems consist of time-dependent polymers as inner layer and pH-sensitive polymers as outer layer. However, they suffer from low drug-loading rate and immature drug release. In this study, total alkaloids of sophora alopecuroides（TASA）-loaded pellets were prepared by extrusion-spheronization method and coated with Eudragit RS30D and Eudragit S100. Pellets using Eudragit RS30D as inner layer and Eudragit S100 as outer layer were named as ERS-ES100 TCO, while pellets with Eudragit S100 as inner layer and Eudragit RS30D as outer layer were ES100-ERS NCO. Both types of formulations with varying coating ratios and orders of Eudragit S100 and Eudragit RS30D were designed and prepared. The following in vitro drug release and SEM studies indicated that ERS-ES100 TCO（F2） with 12.8% Eudragit RS30D as inner layer and 21% Eudragit S100 as outer layer released up to 42% drug in 5 h. Interestingly, ES100-ERS NCO（F4） coated with 12.8% Eudragit S100 and 14.8% Eudragit RS30D showed optimal drug release in colon. In conclusion, ES100-ERS NCO colonic delivery system achieved reduced coating thickness and improved colonic targeting compared with traditional delivery system（ERS-ES100 TCO）. In addition, the similarity factors（ f 2） value of sophoridine and matrine for investigated formulation were within 50–100 and > 80, demonstrating that sophoridine and matrine in all formulations achieved a synchronous release.
论文目录
文章来源
类型: 期刊论文
作者: Lijun Song,Liping Liang,Xiaoying Shi,Honglang Chen,Shumin Zhao,Wenfeng Chen,Ruoxia Zhou,Wenchang Zhao
来源: Asian Journal of Pharmaceutical Sciences 2019年04期
年度: 2019
分类: 医药卫生科技,工程科技Ⅰ辑
专业: 有机化工,药学
单位: School of Pharmacy, Guangdong Medical University,Guangdong Key Laboratory for Research and Development of Natural Drugs, Guangdong Medical University
基金: supposed by major science and technology projects of Guangdong province,China(2013A022100039),science innovation projects of higher school(2012KJCX0060),the technology bureau of Zhanjiang,Guangdong,China (2011C3108015),Guangdong province sail plan project of high level talents in 2014,the National Natural Science Foundation of China (81473401),Guangdong provincial innovation and entrepreneurship training program for college students in 2016 no.196
分类号: R943
页码: 413-422
总页数: 10
文件大小: 1573K
下载量: 13
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