Role of hesperidin and fresh orange juice in altering the bioavailability of beta-blocker, metoprolol tartrate. An in vivo model

Abstract

1. The aim of my study was to find the effect of co-administrating orange juice and hesperidin on the bioavailability of metoprolol tartrate in rabbits.

2. Metoprolol tartrate (10 mg/kg) was given orally to rabbits with hesperidin (10 mg/kg) and with orange juice (6 mL/kg) separately.

3. The plasma concentrations of metoprolol tartrate were determined using reverse phase-high performance liquid chromatography at 1.5, 1, 2, 4, and 6 h, and the pharmacokinetic parameters were studied.

4. In comparison to the control group, the AUC of metoprolol tartrate was increased significantly by 68.32% with hesperidin while orange juice substantially reduced the AUC by 37.08%. However, no significant change was observed in T_max, K_el, and V_d in both groups. The relative bioavailability of metoprolol tartrate with hesperidin was 168.3% as compared to orange juice, that is, 62.9%.

5. The present study revealed that the concurrent intake of hesperidin with metoprolol tartrate increased its bioavailability while orange juice administration suppressed its bioavailability. The change in bioavailability of metoprolol tartrate might be due to alterations in the activity of cytochrome P450 enzymes involved in the metabolism of metoprolol tartrate. However, the exact mechanism is still not known. These interactions may be of clinical significance.

Keywords:

• Metoprolol tartrate
• hesperidin
• HPLC
• pharmacokinetics
• bioavailability

Disclosure statement

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of the paper.