枇杷叶三萜酸固体分散体的制备及体外溶出研究  

Preparation of Solid Dispersion of Triterpenoid Acids from Eriobotrya japonica Leaf and Study on Their Dissolution in vitro

作　　者：石慧慧[1] 蔡雪萍[1,2] 鞠建明[1,2] 张振海[1] 华俊磊[1,2] 吕寒[3] 李维林[3] 

机构地区：[1]中国中医科学院江苏分院/江苏省中医药研究院,江苏南京210028 [2]南京中医药大学药学院,江苏南京210046 [3]江苏省中科院植物研究所,江苏南京210014

出　　处：《中药材》2014年第8期1467-1470,共4页Journal of Chinese Medicinal Materials

基　　金：江苏省产学研前瞻性联合研究项目(BY2009144)

摘　　要：目的:制备枇杷叶三萜酸(EJA)固体分散体,以提高其体外溶出度。方法:以枇杷叶三萜酸中溶解度最低的熊果酸、齐墩果酸的体外溶出度为代表性指标,通过单因素试验考察不同载体材料及药载比对EJA固体分散体中药物溶出的影响;以差示扫描量热法(DSC)和X-射线衍射法(X-RD)对固体分散体进行表征。结果:制备EJA固体分散体载体为泊洛沙姆188(P188),药载比为1∶5;DSC和X-RD分析试验表明药物以无定形状态存在于固体分散体中,且药物溶出速率比原药及其物理混合物都显著提高。结论:将EJA制备成固体分散体能显著增加三萜酸的体外溶出,为将其进一步制备成固体剂型提供了实验依据。To prepare the solid dispersion of Eriobotrya japonica leaf triterpenoid acids（EJA） in order to enhance their dissolution characteristics in vitro. Methods：Taking ursolic acid and oleanolic acid in vitro dissolution as an indicator,the influence of factors including different water-soluble carriers（PEG 6000,PVPk30 and P188）and the drug /carrier weight ratio for the preparation of solid dispersion were examined using single factor experiment. Differential scanning calorimetry（ DSC） and X-ray diffraction（ X-RD） were used to describe the characterization of solid dispersion. Results：P188 was used as appropriate carrier for the preparation of solid dispersion and the drug /carrier weight ratio was 1∶ 5. The X-RD and DSC showed EJA existed in the solid dispersion as the way of amorphous. The dissolution rate of EJA solid dispersion was significantly higher than physical mixture and EJA. Conclusion：The solid dispersion prepared with P188 can significantly increase the solubility and dissolution of EJA in vitro. This study provides the scientific evidence for further preparation of solid dispersion tablet.

关 键 词：枇杷叶三萜酸 固体分散体 溶出度 泊洛沙姆188 

分 类 号：R283.6[医药卫生—中药学]