Effect of Berberine on the Pharmacokinetics of Substrates of CYP3A and P-gp

doi:10.1002/ptr.2808

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	Effect of Berberine on the Pharmacokinetics of Substrates of CYP3A and P-gp
	Qiu, W; Jiang, XH; Liu, CX; Ju, Y; Jin, JX; Jiang, XH (reprint author), Sichuan Univ, W China Sch Pharm, Dept Clin Pharm, 17,Sect 3,Renmin S Rd, Chengdu 610041, Peoples R China.
刊名	PHYTOTHERAPY RESEARCH
	2009-11
卷号	23 期号:11 页码:1553-1558
关键词	berberine P-glycoprotein CYP3A carbamazepine digoxin cyclosporine A
ISSN号	0951-418X
DOI	10.1002/ptr.2808
文献子类	Article
英文摘要	The in vivo effects of berberine (BBR), the widely used bioactive herbal ingredient from many traditional Chinese medicinal herbs, on the pharmacokinetics of carbamazepine (CBZ, a substrate of CYP3A) and its metabolite carbamazepine 10,11-epoxide (ECBZ), digoxin (DIG, a substrate of P-gp) and cyclosporine A (CsA, a dual substrate of CYP3A and P-gp) were evaluated in rats. After a 2-week pretreatment with BBR, the pharmacokinetic parameters of i.g. administered CBZ and ECBZ were not significantly altered. The pharmacokinetics of i.v. administered DIG was not modified by single and 2-week pretreatments with BBR, but a dose-dependent increase in AUC and C(max) Was observed in the i.g. administered DIG parameters in rats. The AUCs of DIG with BBR (30 mg/kg, 100 mg/kg) were 133%, 170% (single) and 123%, 169% (2-week) of control, respectively. The AUC and C(max) of i.g. administered CsA with a 2-week pretreatment with BBR increased by 62% and 43% (BBR 30 mg/kg, p < 0.05), 96% and 60% (BBR 100 mg/kg, p < 0.01), compared with the control. In conclusion, berberine produced a dose-dependent increased bioavailability of digoxin and cyclosporine A by inhibition of intestinal P-gp. No significant changes in CYP3A activity by berberine were observed. Copyright (C) 2009 John Wiley & Sons, Ltd.
学科主题	Pharmacology & Pharmacy
出版地	CHICHESTER
语种	英语
WOS记录号	WOS:000271782500009
内容类型	期刊论文
源URL	[http://ir.lzu.edu.cn/handle/262010/126007]
专题	第二临床医学院_期刊论文
通讯作者	Jiang, XH (reprint author), Sichuan Univ, W China Sch Pharm, Dept Clin Pharm, 17,Sect 3,Renmin S Rd, Chengdu 610041, Peoples R China.
推荐引用方式 GB/T 7714	Qiu, W,Jiang, XH,Liu, CX,et al. Effect of Berberine on the Pharmacokinetics of Substrates of CYP3A and P-gp[J]. PHYTOTHERAPY RESEARCH,2009,23(11):1553-1558.
APA	Qiu, W,Jiang, XH,Liu, CX,Ju, Y,Jin, JX,&Jiang, XH .(2009).Effect of Berberine on the Pharmacokinetics of Substrates of CYP3A and P-gp.PHYTOTHERAPY RESEARCH,23(11),1553-1558.
MLA	Qiu, W,et al."Effect of Berberine on the Pharmacokinetics of Substrates of CYP3A and P-gp".PHYTOTHERAPY RESEARCH 23.11(2009):1553-1558.