흰쥐에서 나린진이 로살탄의 생체이용율에 미치는 영향

• 영문명: Effect of Naringin on the Bioavailability of Losartan in Rats
• 발행기관: 대한약학회
• 저자명: 이종기(Chong Ki Lee) 최준식(Jun Shik Choi)
• 간행물 정보: 『약학회지』제53권 제5호 (2009년), 259~264쪽, 전체 6쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 2009.10.31

영문 초록

The present study was to investigate the effect of naringin, a flavonoid, on the pharmacokinetics of losartan in rats. Pharmacokinetic parameters of losartan in rats were determined after an oral administration of losartan (9 mg/kg) in the presence or absence of naringin (0.5, 2.5 and 10 mg/kg). The pharmacokinetic parameters of losartan were significantly altered by the presence of naringin compared with the control group (given losartan alone). Presence of naringin significantly (p<0.05, 2.5 mg/kg; p<0.01, 10 mg/kg) increased the area under the plasma concentration뻯ime curve (AUC) of losartan by 43.7~63.0% and peak plasma concentration (Cmax) of losartan by 31.7~45.5%. Consequently, the absolute bioavailability (AB) of losartan in the presence of naringin was 43.8~62.9%, which was enhanced significantly (p<0.05, p<0.01) compared to that in the oral control group (22.4%). The relative bioavailability (R.B.) of losartan increased by 1.44-to 1.63-fold in the presence of naringin. However, there was no significant change in the peak plasma concentration (Tmax) and terminal half-life (t1/2) of losartan in the presence of naringin. In conclusion, the presence of naringin significantly enhanced the oral bioavailability of losartan, implying that presence of naringin might be mainly effective to inhibit the cytochrome P450 (CYP)3A-mediated metabolism, resulting in reducing gastrointestinal and hepatic first-pass metabilism and Pglycoprotein (P-gp)-mediated efflux of losartan in small intestine. Concurrent use of naringin or naringin-containing dietary supplement with losartan should require close monitoring for potential drug interactions.

키워드

losartan bioavailability naringin pharmacokinetics CYP3A4 p-gp rat