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《Drug development and industrial pharmacy》2013,39(7):787-794
Purpose: The objective of this study was to investigate the absorption behavior of total flavones of Hippophae rhamnoides L. (TFH) (the sum of isorhamnetin and quercetin as the index component) in the rat intestine using in situ circulation method. Methods: The accumulated TFH absorption and related absorption parameters were calculated. Furthermore, the influences of Cremophor ELP and the P-glycoprotein inhibitor, verapamil, on the intestinal absorption of TFH were studied using the in situ circulation model. Results and Discussion: The results showed that the absorption of TFH increased linearly with its concentration, indicating that a passive diffusion process was dominated. There were no significant differences in the absorption of TFH in three small intestine segments of duodenum, jejunum, and ileum and at different concentrations of Cremophor ELP ranging from 0.25% to 1% (P > 0.05). With the presence of P-gp inhibitor, verapamil, in the circulation fluid, the accumulated absorption of TFH did not increase significantly (P > 0.05). Further studies on the solubility and permeability enhancement of TFH should be investigated to develop new TFH products with high bioavailability. 相似文献
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《Drug development and industrial pharmacy》2013,39(7):1037-1045
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. 相似文献
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