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KMID : 0648320080140020037
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Journal of The Korean Society of Hypertension
2008 Volume.14 No. 2 p.37 ~ p.42
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Effects of resveratrol, antioxidant, on the bioavailability of diltiazem in rats
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Choi Dong-Hyun
Jeong Joong-Wha
Koh Young-Youp
Chang Kyoung-Sig
Hong Soon-Pyo
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Abstract
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Background : The purpose of this study was to investigate the effect of resveratrol on the pharmacokinetics and
bioavailability of diltiazem in rats.
Methods : A single dose of diltiazem was administred to rats intravenously (5 mg/kg) or orally (15 mg/kg) without or with resveratrol (1, 5 and 15 mg/kg).
Results : Presence of resveratrol (5 and 15 mg/kg) significantly (p<0.05) increased the area under the plasma concentration-time curve (AUC) and peak concentration (Cmax) of oral administration of diltiazem compared to the control group. Consequently, the absolute bioavailability (AB%) of diltiazem in the presence of resveratrol (5 and 15 mg/kg) was 10.3-11.0%, which was enhanced significantly (p<0.05) compared with the oral control group (6.6%). The relative bioavailability (RB%) of diltiazem is increased from 1.16- to 1.68-fold. there was no significant changes in the terminal half-lives (t1/2) and the time to reach the peak concentration (Tmax) of diltiazem.
Conclusion : Orally administered resveratrol, as the P-gp and CYP3A inhibitors, may provide a therapeutic effects to improve bioavailability of diltiazem in the combination therapy.
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KEYWORD
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Diltiazem, Resveratrol, Bioavailability, Pharmacokinetics, CYP3A, P-glycoprotein
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