芪麝丸体外释放度研究  

In vitro dissolution of Qishe Pills

作　　者：李秋芬[1] 杜思邈[1] 周永全[1] 张忠亮[1] 潘一峰 张宁[1] 

机构地区：[1]上海中医药大学,上海201203 [2]上海现代中医药股份有限公司,上海200051

出　　处：《中草药》2013年第13期1748-1755,共8页Chinese Traditional and Herbal Drugs

基　　金：上海教育委员会重点学科资助项目(J50302);高等学校博士学科点专项科研基金(20123107110007)

摘　　要：目的研究芪麝丸在2种溶出介质中的溶出特性,为建立以溶出法评价该制剂质量方法奠定基础。方法采用浆法,以1%聚山梨酯80水溶液和0.5%十二烷基硫酸钠(SDS)水溶液为溶出介质,以HPLC法测定的毛蕊异黄酮、毛蕊异黄酮葡萄糖苷、芒柄花素、芒柄花苷、洋川芎内酯I、洋川芎内酯A、青藤碱为指标,考察芪麝丸在不同时间的累积溶出度,同时比较采用不同溶出介质时的各成分释放情况,拟合其溶出模型,求算溶出参数。结果青藤碱、毛蕊异黄酮葡萄糖苷、洋川芎内酯I、芒柄花苷、毛蕊异黄酮、芒柄花素、洋川芎内酯A分别在0.718～10.770、0.190～2.850、0.100～1.500μg、31.4～471.0、34.0～510.0、33.6～504.0、40.0～600.0 ng呈良好线性关系,以1%聚山梨酯80水溶液为溶出介质时,在45 min时各指标成分的累计溶出率均达到90%以上(毛蕊异黄酮葡萄糖苷除外),以0.5%SDS水溶液为溶出介质时,各指标成分溶出均较缓慢。在2种介质中Weibull模型拟合芪麝丸中7种指标成分均较好,但个别成分在不同种介质中的其他模型拟合相关性更高。f2相似因子法作为模型比较表明芪麝丸中同种成分在2种不同溶出介质下的溶出不具有相似性。结论各指标成分在1%聚山梨酯80水溶液中的溶出速率明显快于0.5%SDS水溶液;以1%聚山梨酯80水溶液为溶出介质时,各指标成分的溶出具有相似性,释放具有同步性。芪麝丸溶出研究适合在1%聚山梨酯80水溶液的介质中进行。Objective To study the dissolution characteristics of Qishe Pills in two kinds of media and to lay the foundation for the establishment of quality evaluation methods by stripping method. Methods With 1% Polysorbate 80 solution and 0.5% sodium dodecyl sulfate （SDS） as media, the sinomenine, calycosin-7-glucoside, senkyunolide I, ononin, calycosin, formononetin, and senkyunolide A, determined by HPLC, were used as indexes. The cumulative dissolution of Qishe Pills at different time was investigated, and the dissolvable situation of respective components in the different media was compared simultaneously. The dissolution models were fit and the dissolution parameters were obtained. Results The linear ranges of sinomenine, calycosin-7-glucoside, senkyunolide I, ononin, calycosin, formononetin, and senkyunolide A were 0.718-10.770, 0.190-2.850, 0.100-1.500μg, 31.4-471.0, 34.0-510.0, 33.6-504.0, and 40.0-600.0 ng. In 45 min, the cumulative dissolving rates of the respective components were above 90% （calycosin-7-glucoside excepted） with 1% Polysorbate 80 solution as medium, while they were slower with 0.5% SDS as medium. The Weibull model of the seven components was good in the two kinds of media, while other model of the individual components had higher correlation in the different media. The f2 similarity factor method indicated that the dissolution of the same component of Qishe Pills has no similarity in the two different media. Conclusion The dissolvable speed of each component with 1% Polysorbate 80 as medium was faster than that with 0.5% SDS as medium obviously. With 1% Polysorbate 80 as medium, the dissolution of each component had similarity and synchronism. Using 1% Polysorbate 80 solution as medium is applicable to research the dissolution of Qishe Pills.

关 键 词：芪麝丸 溶出模型 相似度 毛蕊异黄酮 芒柄花苷 洋川芎内酯A 

分 类 号：R283.6[医药卫生—中药学] R286.02[医药卫生—中医学]