title: 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.
abstract: 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.
authors: Science and Technology Center, Shanghai University of Traditional Chinese Medicine, Shanghai, China.
authors: Guoying
authors: G
authors: Zhao
authors: Jingze
authors: J
authors: Duan
authors: Yan
authors: Y
authors: Xie
authors: Guobei
authors: G
authors: Lin
authors: Huilin
authors: H
authors: Luo
authors: Guowen
authors: G
authors: Li
authors: Xiurong
authors: X
authors: Yuan
mesh_terms: D000818:Animals; D002626:Chemistry, Pharmaceutical; D004655:Emulsions; D047309:Flavones / Q000737:chemistry* / Q000493:pharmacokinetics; D031281:Hippophae / Q000737:chemistry*; D007413:Intestinal Mucosa / Q000378:metabolism; D044949:Kaempferols / Q000737:chemistry* / Q000493:pharmacokinetics; D008297:Male; D010539:Permeability; D011794:Quercetin / Q000031:analogs & derivatives* / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility
chemical_list: D004655:Emulsions; D047309:Flavones; D044949:Kaempferols; C047368:3-methylquercetin; C006552:kaempferol; D011794:Quercetin