提高中药疏水性抗肝炎有效成分花锚口山酮总苷溶出度  

Improving dissolution of antihepatitis-effective-ingredients total xanth-one glucosides of Halenia elliptica

作　　者：王业清[1] 史可丽[1] 廖志新[1] 纪兰菊[2] 孙洪发[2] 

机构地区：[1]东南大学化学化工学院,南京211189 [2]中国科学院西北高原生物研究所,西宁810001

出　　处：《东南大学学报（自然科学版）》2011年第4期809-814,共6页Journal of Southeast University：Natural Science Edition

基　　金：国家自然科学基金资助项目(30770233);青海省重点攻关资助项目(2008-G-136)

摘　　要：针对某些中药有效成分因水溶性差而引起药物生物利用度低的问题,选取具有抗肝炎活性的花锚总苷为研究对象,运用熔融法或溶剂法分别制备了4种不同载体组成的花锚总苷固体分散体,通过HPLC方法测定溶出度.研究结果表明,聚乙二醇4000、聚乙二醇6000、泊洛沙姆188、聚乙烯基吡咯烷酮k30均能与花锚总苷制备固体分散体,相对于花锚总苷,固体分散体的溶出度都有明显提高,且随着载体比例的增加而增加,其中聚乙二醇6000-花锚总苷固体分散体(药载比6∶1)将溶出度从花锚总苷的18.3%提高到92%.采用扫描电子显微镜对花锚总苷、各固体分散体及样品载体物理混合物的微观形态进行了观察,结果表明,花锚总苷与载体以有助于增强溶解性的低共溶物形式存在于固体分散体中.Against the low bioavailability of the effective ingredients in many chinese herb medicines,solid dispersions（SDs） of 4 different carriers with antihepatitis total glucosides of halenia elliptica D.Don（ATH） were prepared by melt or solvent method,and the dissolution rate was determined by HPLC（high pressure liquid chromatography）.According to the results,PEG4000,PEG6000,Poloxamer188 and PVPk30 can be used to prepare SD with ATH.Compared with ATH,the dissolution rate of SDs is increased obviously,and the dissolution rate become higher with the increase of carrier ratio.The dissolution rate of PEG6000-ATH SD may increase up to 92%（carrier drug ratio 6∶1）,in contrast it is only 18.3% in ATH.Microscopical morphology of ATH,SDs and physical mixture samples was analyzed by scanning electron microscope（SEM）,the results indicate that the drug and carriers exist as eutectic which is conducive to a high dissolution rate in the SDs.

关 键 词：中药有效成分 花锚总苷 固体分散体 溶出度 扫描电子显微镜 

分 类 号：R969.1[医药卫生—药理学]