Effect of naringenin on the pharmacokinetics of metoprolol succinate in rats / Ravindra Babu Pingili, Sridhar Vemulapalli, Vijaya R. Dirisala, Surya Sandeep Mullapudi, Yamini Gullapalli, Naveen Babu Kilaru
Abstract The aim of the present study was to investigate the effect of naringenin (4,5,7-trihydroxy flavonone) on the pharmacokinetics of metoprolol, a substrate of Cytochrome P-450 3A4 (CYP3A4), CYP2C9, and CYP2D6 in rats. Male Wistar rats were treated orally with metoprolol (30 mg/kg) alone and in combination with naringenin (25, 50, and 100 mg/kg) once daily for 15 consecutive days. The plasma concentrations of metoprolol were determined using Reverse Phase-High Performance Liquid Chromatography (RP-HPLC) on the 1st day in single-dose pharmacokinetic (PK) study (SDS) and on the 15th day in multiple dosing PK studies (MDS). Compared to the metoprolol control group, the C max , AUC, and half-life ( T 1/2 ) of metoprolol increased in rats pre-treated with naringenin, while there was no significant change in T max . There is a significant decrease in clearance and volume of distribution. The present study results revealed that naringenin significantly enhanced the C max, AUC, MRT, t 1/2 , and decreased the clearance of metoprolol possibly through the inhibition of CYP enzymes involved in the metabolism of metoprolol.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2021 |
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| Erschienen: |
2021 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:51 |
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| Enthalten in: |
Xenobiotica - 51(2021), 8, Seite 926-932 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Pingili, Ravindra Babu [VerfasserIn] |
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| Links: |
FID Access [lizenzpflichtig] |
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| Themen: |
Bioavailability |
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| Umfang: |
1 Online-Ressource (7 p) |
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| doi: |
10.1080/00498254.2021.1942311 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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KFL011117982 |
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| 520 | |a Abstract The aim of the present study was to investigate the effect of naringenin (4,5,7-trihydroxy flavonone) on the pharmacokinetics of metoprolol, a substrate of Cytochrome P-450 3A4 (CYP3A4), CYP2C9, and CYP2D6 in rats. Male Wistar rats were treated orally with metoprolol (30 mg/kg) alone and in combination with naringenin (25, 50, and 100 mg/kg) once daily for 15 consecutive days. The plasma concentrations of metoprolol were determined using Reverse Phase-High Performance Liquid Chromatography (RP-HPLC) on the 1st day in single-dose pharmacokinetic (PK) study (SDS) and on the 15th day in multiple dosing PK studies (MDS). Compared to the metoprolol control group, the C max , AUC, and half-life ( T 1/2 ) of metoprolol increased in rats pre-treated with naringenin, while there was no significant change in T max . There is a significant decrease in clearance and volume of distribution. The present study results revealed that naringenin significantly enhanced the C max, AUC, MRT, t 1/2 , and decreased the clearance of metoprolol possibly through the inhibition of CYP enzymes involved in the metabolism of metoprolol | ||
| 653 | |a Metoprolol | ||
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