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三种不同沙棘总黄酮制剂在比格犬口服给药后的药代动力学比较。

A comparison of the pharmacokinetics of three different preparations of total flavones of Hippophae rhamnoides in beagle dogs after oral administration.

作者信息

Duan Jingze, Dang Yang, Meng Houjun, Wang Huizhen, Ma Ping, Li Guowen, Wu Tao, Xie Yan

机构信息

Research Center for Health and Nutrition, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai, 201203, People's Republic of China.

Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, China.

出版信息

Eur J Drug Metab Pharmacokinet. 2016 Jun;41(3):239-49. doi: 10.1007/s13318-015-0254-9. Epub 2015 Jan 23.

DOI:10.1007/s13318-015-0254-9
PMID:25613316
Abstract

Pharmacokinetic properties of isorhamnetin, quercetin, and kaempferol in three different total flavones of Hippophae rhamnoides (TFH) preparations were compared after oral administration to beagle dogs by a UPLC-MS method. The pharmacokinetic results showed that C max of isorhamnetin and quercetin in TFH solid dispersion (TFH-SD) and TFH self-emulsifying (TFH-SE) preparations was significantly enhanced than that in TFH preparations (p < 0.05). The AUCs of isorhamnetin and quercetin in TFH-SD were 5.9- and 3.1-fold higher than that of TFH, while the AUCs of isorhamnetin and quercetin in TFH-SE were 3.4- and 2.4-fold higher than that of TFH. These findings suggested that the oral bioavailability of isorhamnetin and quercetin in beagle dogs can be significantly increased in TFH-SD and TFH-SE preparations compared to TFH preparations, which was helpful to explore the new forms for oral administration TFH and explain their in vivo processes.

摘要

采用超高效液相色谱-质谱联用(UPLC-MS)法,对比了比格犬口服沙棘总黄酮(TFH)三种不同制剂后,异鼠李素、槲皮素和山奈酚的药代动力学特性。药代动力学结果表明,TFH固体分散体(TFH-SD)和TFH自乳化制剂(TFH-SE)中异鼠李素和槲皮素的Cmax显著高于TFH制剂(p < 0.05)。TFH-SD中异鼠李素和槲皮素的AUC分别比TFH高5.9倍和3.1倍,而TFH-SE中异鼠李素和槲皮素的AUC分别比TFH高3.4倍和2.4倍。这些结果表明,与TFH制剂相比,TFH-SD和TFH-SE制剂中异鼠李素和槲皮素在比格犬体内的口服生物利用度显著提高,这有助于探索TFH口服给药的新剂型,并解释其体内过程。

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