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Drug-drug Interactions between Ketoconazole and Berberine in Rats: Pharmacokinetic Effects Benefit Pharmacodynamic Synergism

  作者 Zhou, YM; He, P; Liu, AM; Zhang, LX; Liu, YD; Dai, RK  
  选自 期刊  Phytotherapy Research;  卷期  2012年26-5;  页码  772-777  
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[摘要]Ketoconazole (KTZ), a clinical antifungal agent, is a known inhibitor of CYP3A and permeability glycoprotein (P-gp). Berberine (BBR), a natural plant-derived product used for gastroenteritis, is a substrate of P-gp. Recently, a synergistic antifungal effect of KTZ combined with BBR has been revealed. In this study, we performed both in vivo and in vitro experiments to explore whether pharmacokinetic interactions between KTZ and BBR would benefit their phamacodynamic synergism. After oral co-administration of 10?mg/kg KTZ with 60?mg/kg BBR, the average area under the curve (AUC) and the maximum concentration (Cmax) for KTZ increased to 215% and 449% (p?

 
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