落新妇苷无定型纳米混悬剂的制备及其体外评价  

Preparation of astilbin amorphous nanosuspension and its in vitro evaluation

作　　者：汪小涵[1,2] 钟芮娜 申宝德[2] 沈成英[2] 刘肖[1,2] 戴博 袁海龙[2] WANG Xiao-han;ZHONG Rui-na;SHEN Bao-de;SHEN Cheng-ying;LIU Xiao;DAI Bo;YUAN Hai-long(College of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China;Department of Pharmacy, Air Force General Hospital, PLA, Beijing 100142, China)

机构地区：[1]成都中医药大学药学院,四川成都611137 [2]中国人民解放军空军总医院药学部,北京100142

出　　处：《中国中药杂志》2018年第8期1626-1632,共7页China Journal of Chinese Materia Medica

基　　金：国家自然科学基金项目(81573696);军队后勤科研重点项目(BKJ16J011)

摘　　要：采用单因素试验优化沉淀法制备落新妇苷纳米混悬剂的处方及工艺参数,对所得纳米混悬剂进行理化性质表征,并评价其体外累积释放度。结果显示,以PVP K30为稳定剂制备的落新妇苷纳米混悬剂平均粒径为（149±3）nm,多分散度指数（PDI）为0.137±0.014,稳定性指数（SI）为0.940±0.012。扫描电镜显示所得纳米混悬剂中落新妇苷呈圆球状,大小较均匀。X射线衍射图谱和差式扫描量热法均表明落新妇苷制备成纳米混悬剂后,以无定型状态存在。体外释放结果表明落新妇苷纳米混悬剂的溶出速率和溶解度显著高于物理混合物及原料药。该方法工艺简单、操作方便,能成功制备均匀稳定的纳米混悬剂,改善其溶解性,为解决落新妇苷应用局限提供了实验基础。Astilbil nanosuspension（ AT-NS） was prepared by an antisolvent precipitation method. The formula and process of ATNS were optimized by the single factor experiment. AT-NS was prepared under the optimal conditions,and its morphology and crystallinity were characterized. In vitro release of AT-NS was also determined. The particle size of AT-NS stabilized by PVP K30 was（ 149 ± 3） nm,and the polydispersity index（ PDI） and stability index（ SI） were 0. 137 ± 0. 014 and 0. 940 ± 0. 012,respectively.The results of SEM showed that AT-NS was spherical. Both XRD and DSC showed that AT was amorphous in nanosuspension. In the in vitro release test,AT-NS showed a significantly increased dissolution. This simple low-cost approach could prepare AT-NS successfully. AT-NS could significantly improve the dissolution of AT and provide the reference to break the limitation on the clinical application of AT.

关 键 词：落新妇苷 沉淀法 无定型纳米混悬剂 体外释放 

分 类 号：R283.6[医药卫生—中药学]