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通过正常大鼠和患病大鼠大黄提取物的比较药代动力学阐明大黄蒽醌对便秘的协同作用机制。

The synergism mechanism of Rhubarb Anthraquinones on constipation elucidated by comparative pharmacokinetics of Rhubarb extract between normal and diseased rats.

作者信息

Gong Xiao-Hong, Li Yan, Zhang Ruo-Qi, Xie Xiao-Fang, Peng Cheng, Li Yun-Xia

机构信息

The Ministry of Education Key Laboratory of Standardization of Chinese Herbal Medicine, State Key Laboratory Breeding Base of Systematic Research, Development and Utilization of Chinese Medicine Resources, Pharmacy College, Chengdu University of Traditional Chinese Medicine, Chengdu, 610075, People's Republic of China.

出版信息

Eur J Drug Metab Pharmacokinet. 2015 Dec;40(4):379-88. doi: 10.1007/s13318-014-0216-7. Epub 2014 Jul 5.

DOI:10.1007/s13318-014-0216-7
PMID:24996641
Abstract

In the study, it was hypothesized that Rhubarb Anthraquinones synergistically enhanced the purgative effect on constipation rat from the direct and indirect pathway at the same time. A validated HPLC method was successfully applied to elucidate the synergism mechanism from pharmacokinetics aspect after oral administration of Rhubarb extract with a dose of 0.25 g to normal and constipation rats. Comparison of the pharmacokinetic data of normal and constipation rats showed that there were significant differences (p < 0.05) in the main pharmacokinetic parameters. The C max and AUC of emodin in constipation rats were about ten times that of normal rats, while the t 1/2 was remarkably decreased (p < 0.05). However, a significant decrease (p < 0.05) in AUC value for aloe-emodin and rhein was observed in model group compared with normal group. The results may be attributed to the direct action of aloe-emodin and rhein on intestinal cell membranes and the indirect action of emodin on bowel movement through the adjustment by nervous system.

摘要

在该研究中,假设大黄蒽醌可同时从直接和间接途径协同增强对便秘大鼠的通便作用。在给正常大鼠和便秘大鼠口服0.25 g大黄提取物后,一种经过验证的高效液相色谱法成功用于从药代动力学方面阐明协同作用机制。正常大鼠和便秘大鼠药代动力学数据的比较表明,主要药代动力学参数存在显著差异(p < 0.05)。便秘大鼠中大黄素的Cmax和AUC约为正常大鼠的10倍,而t1/2显著降低(p < 0.05)。然而,与正常组相比,模型组中芦荟大黄素和大黄酸的AUC值显著降低(p < 0.05)。结果可能归因于芦荟大黄素和大黄酸对肠细胞膜的直接作用以及大黄素通过神经系统调节对肠道运动的间接作用。

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