Enhanced oral bioavailability of felodipine by naringenin in Wistar rats and inhibition of P-glycoprotein in everted rat gut sacs in vitro

Abstract The aim of this study was to investigate the effect of naringenin on the pharmacokinetics (PK) of felodipine in rats and membrane permeability across rat everted gut sacs in vitro. Rats were simultaneously co-administered with felodipine 10 mg/kg, p.o. and naringenin (25, 50 and 100 mg/kg,...

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Published in:Drug development and industrial pharmacy 2014-10, Vol.40 (10), p.1371-1377
Main Authors: Surya Sandeep, M., Sridhar, V., Puneeth, Y., Ravindra Babu, P., Naveen Babu, K.
Format: Article
Language:English
Subjects:
Animals
Antihypertensive Agents - pharmacokinetics
Area Under Curve
ATP-Binding Cassette, Sub-Family B, Member 1 - antagonists & inhibitors
ATP-Binding Cassette, Sub-Family B, Member 1 - metabolism
Biological Availability
Calcium channel blockers
CYP3A4
Cytochrome P-450 CYP3A - drug effects
Cytochrome P-450 CYP3A - metabolism
Cytochrome P-450 CYP3A Inhibitors - pharmacology
Dose-Response Relationship, Drug
Drug Interactions
everted gut sacs
Felodipine - pharmacokinetics
first-pass metabolism
Flavanones - administration & dosage
Flavanones - pharmacology
hypertension
Male
naringenin
P-glycoprotein
Permeability
poor bioavailability
Rats
Rats, Wistar
Ritonavir - pharmacology
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Summary:Abstract The aim of this study was to investigate the effect of naringenin on the pharmacokinetics (PK) of felodipine in rats and membrane permeability across rat everted gut sacs in vitro. Rats were simultaneously co-administered with felodipine 10 mg/kg, p.o. and naringenin (25, 50 and 100 mg/kg, p.o.) for 15 consecutive days. Rats of the control groups received the corresponding volume of vehicle. Blood samples were withdrawn from retro-orbital plexus on first day in single dose PK study (SDS) and on 15th day in multiple dosing PK study (MDS). The PK parameters were calculated using Thermo kinetica. The co-administration of naringenin significantly elevated the Cmax and increased the AUCtotal of felodipine in dose-dependent manner. The Cmax of felodipine was increased from 173.25 ± 14.65 to 275.61 ± 44.62 and 223.26 ± 26.35 to 561.32 ± 62.53 ng/mL in SDS and MDS, respectively, at the dose of naringenin 100 mg/kg. The AUCtotal of felodipine was significantly (p 
ISSN:0363-9045
1520-5762
DOI:10.3109/03639045.2013.819885