흰쥐에 경구및정맥투여시 에피가로카테친이 니모디핀의 생체이용률에 미치는 영향 (Effects of Epigallocatechin Gallate on the Bioavailability of Nimodipine after Oral and Intravenous Administration in Rats)

서지정보

· 발행기관 : 대한약학회
· 수록지 정보 : 약 학 회 지 / 55권 / 4호 / 332 ~ 337페이지
· 저자명 : 최동현, 이종기, 최준식

초록

The purpose of this study was to investigate the effect of epigallocatechin gallate (EGCG) on the pharmacokinetics of nimodipine in rats. Pharmacokinetic parameters of nimodipine were determined in rats after oral and iv administration of nimodipine with or without EGCG and also the effect of EGCG on the cytochrome P450 (CYP) 3A4 and P-glycoprotein (P-gp) activity were evaluated. EGCG inhibited CYP3A4 and P-gp activity. EGCG significantly increased the area under the plasma concentration-time curve (AUC) and peak plasma concentration (C_max) of nimodipine. The absolute bioavailability (AB%) and relative bioavailability (RB%) of nimodipine by EGCG were increased by 16% and by 48%, respectively,compared to the control. In contrast, EGCG did not affect the intravenous pharmacokinetics of nimodipine. Based on these results, the increased bioavailability of nimodipine might be due to inhibition of CYP3A4 in the small intestine and/or in the liver and inhibition of P-gp in the small intestine by EGCG.

영어초록

The purpose of this study was to investigate the effect of epigallocatechin gallate (EGCG) on the pharmacokinetics of nimodipine in rats. Pharmacokinetic parameters of nimodipine were determined in rats after oral and iv administration of nimodipine with or without EGCG and also the effect of EGCG on the cytochrome P450 (CYP) 3A4 and P-glycoprotein (P-gp) activity were evaluated. EGCG inhibited CYP3A4 and P-gp activity. EGCG significantly increased the area under the plasma concentration-time curve (AUC) and peak plasma concentration (C_max) of nimodipine. The absolute bioavailability (AB%) and relative bioavailability (RB%) of nimodipine by EGCG were increased by 16% and by 48%, respectively,compared to the control. In contrast, EGCG did not affect the intravenous pharmacokinetics of nimodipine. Based on these results, the increased bioavailability of nimodipine might be due to inhibition of CYP3A4 in the small intestine and/or in the liver and inhibition of P-gp in the small intestine by EGCG.

참고자료

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