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氟伐他汀与地尔硫䓬在大鼠体内的药代动力学相互作用。

Pharmacokinetic interaction between fluvastatin and diltiazem in rats.

作者信息

Choi Jun-Shik, Piao Yong-Ji, Han Hyo-Kyung

机构信息

College of Pharmacy, Chosun University, 375 Seosuk-dong, Dong-Gu, Gwangju, Korea.

出版信息

Biopharm Drug Dispos. 2006 Dec;27(9):437-41. doi: 10.1002/bdd.521.

Abstract

The present study aimed to investigate the effect of fluvastatin on the pharmacokinetics of diltiazem in rats. Pharmacokinetic parameters of diltiazem were determined in rats following an oral administration of diltiazem (15 mg/kg) in the presence and absence of fluvastatin (0.6 and 2.0 mg/kg). Compared with the control given diltiazem alone, the C(max) and AUC of diltiazem increased by 30-70% in rats with the concurrent use of fluvastatin, while there was no significant change in T(max) and the plasma half-life (T(1/2)) of diltiazem. Consequently, absolute and relative bioavailability values of diltiazem in the presence of fluvastatin were significantly higher (p<0.05) than those from the control group, implying that fluvastatin could reduce the presystemic extraction of diltiazem. In conclusion, the concurrent use of fluvastatin significantly enhanced the oral exposure of diltiazem in rats.

摘要

本研究旨在探讨氟伐他汀对大鼠体内地尔硫䓬药代动力学的影响。在有和没有氟伐他汀(0.6和2.0mg/kg)存在的情况下,给大鼠口服地尔硫䓬(15mg/kg)后测定地尔硫䓬的药代动力学参数。与单独给予地尔硫䓬的对照组相比,同时使用氟伐他汀的大鼠地尔硫䓬的C(max)和AUC增加了30-70%,而地尔硫䓬的T(max)和血浆半衰期(T(1/2))没有显著变化。因此,存在氟伐他汀时地尔硫䓬的绝对和相对生物利用度值显著高于(p<0.05)对照组,这意味着氟伐他汀可以减少地尔硫䓬的首过消除。总之,同时使用氟伐他汀显著提高了大鼠体内地尔硫䓬的口服暴露量。

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