Effect of Resveratrol on the Pharmacokinetics of Carbamazepine in Healthy XXXX Volunteers.

@entity1 @entity5842
UNASSIGNED: The purpose of the present study was to assess the effect of resveratrol ( @entity5842 ) pretreatment on CYP3A4 enzyme activity and pharmacokinetics of carbamazepine (CBZ) in healthy @entity1 volunteers. The open-label, two period, sequential study was conducted in 12 healthy @entity1 volunteers. A single dose of @entity5842 500   mg was administered once daily for 10   days during treatment phase. A single dose of CBZ 200   mg was administered during control and after treatment phases under fasting conditions. The blood samples were collected after CBZ dosing at predetermined time intervals and analyzed by LC-MS/MS. In comparison with the control, @entity5842 pretreatment significantly enhanced maximum plasma concentration (Cmax ), area under the curve (AUC), and half life (t1/2 ) and significantly decreased apparent oral clearance (CL/F) and apparent volume of distribution (Vd/F), while there was no significant change observed in time to reach maximum concentration (tmax ) and elimination rate constant (kel ) of CBZ. Furthermore, @entity5842 pretreatment significantly decreased metabolite to parent (CBZE/CBZ) ratios of Cmax and AUC and significantly increased CBZE/CBZ ratios of CL/F and Vd/F, indicating the reduced formation of CBZE to CBZ. The results suggest that the altered CYP3A4 enzyme activity and pharmacokinetics of CBZ might be attributed to @entity5842 -mediated inhibition of CYP3A4 enzyme. Thus, there is a potential pharmacokinetic interaction between @entity5842 and CBZ including other CYP3A4 substrates. Copyright    2015 John Wiley _ Sons, Ltd.
