表没食子儿茶素没食子酸酯对大鼠体内尼卡地平药代动力学的影响。

Effects of oral epigallocatechin gallate on the pharmacokinetics of nicardipine in rats.

机构信息

BK 21 Project Team and College of Pharmacy, Chosun University, Gwangju, 501-759, Korea.

出版信息

Arch Pharm Res. 2009 Dec;32(12):1721-5. doi: 10.1007/s12272-009-2209-7. Epub 2010 Feb 17.

PMID:20162400

Abstract

Epigallocatechin gallate (EGCG), irreversibly inhibits cytochrome P450 (CYP) 3A subfamily and P-glycoprotein (P-gp) in vitro. This study investigated the effect of oral EGCG on the pharmacokinetics of intravenous and oral nicardipine in rats. Nicardipine was administered orally (12 mg/kg) or intravenously (4 mg/kg) with or without oral EGCG (0.5, 3 or 10 mg/kg) to rats. Compared to controls (without EGCG), the total areas under the plasma concentration-time curve (AUCs) of intravenous nicardipine were greater with oral EGCG. Compared to controls (without EGCG), the AUCs of oral nicardipine and the extent of absolute oral bioavailability (F) were also greater with oral EGCG. The above data suggest that oral EGCG inhibited both the hepatic CYP3A subfamily and intestinal P-gp.

摘要

没食子酸表没食子儿茶素酯（EGCG）在体外不可逆地抑制细胞色素 P450（CYP）3A 亚家族和 P 糖蛋白（P-gp）。本研究探讨了口服 EGCG 对大鼠静脉注射和口服尼卡地平药代动力学的影响。尼卡地平分别口服（12mg/kg）或静脉注射（4mg/kg），同时或不同时给予大鼠口服 EGCG（0.5、3 或 10mg/kg）。与对照组（无 EGCG）相比，口服 EGCG 使静脉注射尼卡地平的血浆浓度-时间曲线下总面积（AUCs）增加。与对照组（无 EGCG）相比，口服尼卡地平的 AUC 和绝对口服生物利用度（F）也随着口服 EGCG 的增加而增加。上述数据表明，口服 EGCG 抑制了肝 CYP3A 亚家族和肠道 P-gp。