Effects of solid dispersion and self-emulsifying formulations on the solubility, dissolution, permeability and pharmacokinetics of isorhamnetin, quercetin and kaempferol in total flavones of Hippophae rhamnoides L.

被引:40
|
作者
Zhao, Guoying [1 ]
Duan, Jingze [2 ]
Xie, Yan [1 ]
Lin, Guobei [1 ]
Luo, Huilin [1 ]
Li, Guowen [2 ]
Yuan, Xiurong [1 ]
机构
[1] Shanghai Univ Tradit Chinese Med, Ctr Sci & Technol, Shanghai 201203, Peoples R China
[2] Shanghai Univ Tradit Chinese Med, Inst Chinese Mat Med, Shanghai 201203, Peoples R China
关键词
Total flavones of Hippophae rhamnoides L; solid dispersion; self-emulsifying; solubility; dissolution rate; pharmacokinetics; DRUG-DELIVERY SYSTEMS; IN-VITRO; INTESTINAL PERMEABILITY; PROCESS OPTIMIZATION; SEED RESIDUES; ABSORPTION; BIOAVAILABILITY; VIVO; EXTRACT;
D O I
10.3109/03639045.2012.699066
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The aim of this study was to investigate the effects of solid dispersions (SD) and self-emulsifying (SE) formulations on the solubility and absorption properties of active components in total flavones of Hippophae rhamnoides L. (TFH). The solubility, dissolution rate, permeability and pharmacokinetics of isorhamnetin, quercetin and kaempferol in TFH SD/SE formulations and TFH were compared. The results showed that the solubility and dissolution rate of isorhamnetin, quercetin and kaempferol in SD/SE formulations were significantly enhanced compared to those in TFH, however, their intestinal permeability was comparable. The bioavailability of isorhamnetin, quercetin and kaempferol in rats remarkably increased after oral administration of TFH SD formulations compared to TFH, but there was no significant increase after oral administration of TFH SE formulations. The results of this study indicated the SD formulations on the improvement of pharmacokinetic properties of isorhamnetin, quercetin and kaempferol in TFH were much better than those of SE formulations. The improvement of pharmacokinetic properties of isorhamnetin, quercetin and kaempferol in TFH by SD formulations was probably ascribed to the enhancement of the solubility and dissolution of the three components, but was not relevant to the intestinal permeability. Therefore, as for herb extracts containing multiple components, especially for their major components with poor water solubility, solid dispersion formulations might have the better potential to enhance their bioavailability.
引用
收藏
页码:1037 / 1045
页数:9
相关论文
共 2 条
  • [1] Phytic acid enhances the oral absorption of isorhamnetin, quercetin, and kaempferol in total flavones of Hippophae rhamnoides L.
    Xie, Yan
    Luo, Huilin
    Duan, Jingze
    Hong, Chao
    Ma, Ping
    Li, Guowen
    Zhang, Tong
    Wu, Tao
    Ji, Guang
    FITOTERAPIA, 2014, 93 : 216 - 225
  • [2] Pharmacokinetic properties of isorhamnetin, kaempferol and quercetin after oral gavage of total flavones of Hippophae rhamnoides L. in rats using a UPLC-MS method
    Li, Guowen
    Zeng, Xiaoli
    Xie, Yan
    Cai, Zhenzhen
    Moore, Jeffrey C.
    Yuan, Xiurong
    Cheng, Zhihong
    Ji, Guang
    FITOTERAPIA, 2012, 83 (01) : 182 - 191