Gong Zipeng, Chen Ying, Zhang Ruijie, Wang Yinghan, Guo Yan, Yang Qing, Zhang Haixian, Dong Yu, Weng Xiaogang, Gao Shuangrong, Zhu Xiaoxin
Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, No.16, Dongzhimen Nei Nanxiao Road, Dongcheng District, Beijing 100700, China.
Institute of Ethnic Medicine, Southwest University, Chengdu 610041, China.
Int J Mol Sci. 2014 Jan 2;15(1):456-67. doi: 10.3390/ijms15010456.
In the present study, post inflammation irritable bowel syndrome (PI-IBS) rats were firstly established by intracolonic instillation of acetic acid with restraint stress. Then the pharmacokinetics of berberine in the rat plasma were compared after oral administration of berberine hydrochloride (25 mg/kg) to normal rats and PI-IBS rats. Quantification of berberine in the rat plasma was achieved by using a sensitive and rapid UPLC-MS/MS method. Plasma samples were collected at 15 different points in time and the pharmacokinetic parameters were analyzed by WinNonlin software. Compared with the normal group, area under the plasma concentration vs. time curve from zero to last sampling time (AUC0-t) and total body clearance (CL/F) in the model group significantly increased or decreased, (2039.49 ± 492.24 vs. 2763.43 ± 203.14; 4999.34 ± 1198.79 vs. 3270.57 ± 58.32) respectively. The results indicated that the pharmacokinetic process of berberine could be altered in PI-IBS pathological conditions.
在本研究中，首先通过结肠内注入乙酸并施加束缚应激建立炎症后肠易激综合征（PI-IBS）大鼠模型。然后，将盐酸小檗碱（25mg/kg）分别口服给予正常大鼠和PI-IBS大鼠，比较二者血浆中小檗碱的药代动力学。采用灵敏快速的超高效液相色谱-串联质谱（UPLC-MS/MS）法对大鼠血浆中的小檗碱进行定量分析。在15个不同时间点采集血浆样本，并使用WinNonlin软件分析药代动力学参数。与正常组相比，模型组从零至最后采样时间的血浆浓度-时间曲线下面积（AUC0-t）和总体清除率（CL/F）分别显著升高或降低（分别为2039.49±492.24对2763.43±203.14；4999.34±1198.79对3270.57±58.32）。结果表明，在PI-IBS病理状态下，小檗碱的药代动力学过程可能会发生改变。
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