Purpose: Hesperetin is a flavanone distributed in citrus fruits and herbs. It exhibits a wide range of pharmacological activities such as antioxidative, anti-inflammatory, antihypertension and anticarcinogenic effects. In this study, the pharmacokinetics of hesperetin was investigated in rats. Methods: Hesperetin was administered to rats via intravenous bolus (10 mg/kg) and oral route (50 mg/kg). The blood sample were withdrawn at predetermined time points post dosing. The plasma concentrations of hesperetin were assayed by HPLC method prior to and after hydrolysis with β-glucuronidase and sulfatase at 37℃ for 2 h. The pharmacokinetic parameters were calculated by using WINNONLIN. Results: After intravenous bolus, the concentrations of free form hesperetin sulfates and hesperetin glucuronides emerged instantaneously, whereas hesperetin was present below the profiles of its conjugated metabolites. In contrast, when hesperetin were orally administered, hesperetin sulfates and hesperetin glucuronides were found predominantly circulating in the bloodstream, whereas no hesperetin was detected except the blood sample within 15 min after dosing. Conclusions: The conjugated metabolites of hesperetin were predominantly present in the circulation whether hesperetin was given orally or intravenously. Therefore, pharmacologists should focus more on the activities of conjugated metabolites of hesperetin.
關聯:
2nd World congress of the board of Pharmaceutical sciences of FIP
