Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
9014884 | Pharmacological Research | 2005 | 6 Pages |
Abstract
The present study aims to investigate the effect of morin, a flavonoid, on the pharmacokinetics of diltiazem and its active metabolite, desacetyldiltiazem, in rats. Pharmacokinetic parameters of diltiazem and desacetyldiltiazem were determined in rats after an oral administration of diltiazem (15 mg kgâ1) to rats in the presence and absence of morin (1.5, 7.5 and 15 mg kgâ1). Compared to the control given diltiazem alone, the Cmax and AUC of diltiazem increased by 30-120% in the rats co-administered with a 1.5 or 7.5 mg kgâ1 of morin, while there was no significant change in Tmax and terminal plasma half-life (T1/2) of diltiazem in the presence of morin. Consequently, absolute and relative bioavailability values of diltiazem in the rats co-administered with morin were significantly higher (p < 0.05) than those from the control group. Metabolite-parent AUC ratio in the presence of morin (7.5 mg kgâ1) decreased by 30% compared to the control group, implying that coadministration of morin could be effective to inhibit the CYP3A4-mediated metabolism of diltiazem. In conclusion, the presence of morin significantly enhanced the oral exposure of diltiazem, suggesting that concurrent use of morin or morin-containing dietary supplement with diltiazem should require close monitoring for potential drug interactions.
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Authors
Jun-Shik Choi, Hyo-Kyung Han,