淫羊藿总黄酮纳米混悬剂的制备及体外评价  

Preparation and in vitro Evaluation of Total Flavones of Epimedium Nanosuspensions

作　　者：丁志远 杨娟 谢燕 DING Zhiyuan;YANG Juan;XIE Yan(School of Public Health,Shanghai University of Traditional Chinese Medicine,Shanghai 201203;Jiangsu Kanion Pharmaceutical Co.,Ltd.,Lianyungang 222001;State Key Lab.of New-tech for Chinese Medicine Pharmaceutical Process,Lianyungang 222001)

机构地区：[1]上海中医药大学公共健康学院,上海201203 [2]江苏康缘药业股份有限公司,江苏连云港222001 [3]中药制药过程新技术国家重点实验室,江苏连云港222001

出　　处：《中国医药工业杂志》2023年第3期395-403,共9页Chinese Journal of Pharmaceuticals

基　　金：中药制药过程新技术国家重点实验室开放基金(SKL2020Z0204)给予资助。

摘　　要：为提高淫羊藿总黄酮(1)的溶解度和溶出度,该研究分别采用微型化介质研磨法和沉淀-高压均质法,以十二烷基硫酸钠(SDS)和聚乙烯己内酰胺-聚乙酸乙烯酯-聚乙二醇接枝共聚物(Soluplus)为稳定剂,制备了3种淫羊藿总黄酮纳米混悬剂(1-NSps)。表征结果显示,3种1-NSps粒径均在200 nm以下,在4℃下具有良好的物理稳定性。并且,1制成纳米混悬剂后,其中各成分的分子结构未发生改变,少量晶型化合物在稳定剂为Soluplus的纳米混悬剂中晶型衍射峰减弱、结晶度降低,但在稳定剂为SDS的纳米混悬剂中以无定形状态存在。3种1-NSps中淫羊藿苷和淫羊藿次苷Ⅱ的饱和溶解度与稳定剂种类相关。相较于原料药,3种1-NSps中总黄酮的溶出速率和溶出程度均明显增加,在水中180 min时的溶出率分别为75.77%、76.26%和84.36%;与微型化介质研磨法制品相比,沉淀-高压均质法制品的溶出更完全。To improve the solubility and dissolution of the total flavones of Epimedium(1),three kinds of nanosuspensions(1-NSps)were respectively prepared by miniaturized media milling method and precipitation-high pressure homogenization method with sodium dodecyl sulfate(SDS)and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer(Soluplus).The characterization results showed that the particle sizes of the three 1-NSps were all below 200 nm and the products were all physically stable at 4℃.Moreover,the molecular structure of each compound was not changed after preparation of 1-NSps.The peak height and crystallinity of some crystalline compounds in 1 was weakened in the nanosuspension stabilized by Soluplus,but they existed in amorphous forms in the nanosuspension stabilized by SDS.The saturated solubilities of icariin and icarisideⅡin the three 1-NSps were related to the stabilizer species.Compared with the raw 1,the dissolution rate and degree of total flavonoids in the three 1-NSps were significantly increased,and their dissolution rates in water at 180 min were 75.77%,76.26%and 84.36%,respectively.The dissolution amount from the product obtained by precipitation-high-pressure homogenization method was more complete than those from the products prepared by miniaturized media milling method.

关 键 词：淫羊藿总黄酮 纳米混悬剂 微型化介质研磨法 沉淀-高压均质法 饱和溶解度 溶出度 

分 类 号：R944.9[医药卫生—药剂学]