Abstract
This study was performed to evaluate and compare the pharmacokinetic parameters between two dosage formulations of hesperidin and naringenin: mixture and tablet. Our objective was to determine that the flavonoid tablet does not significantly modify the pharmacokinetic parameters compared with the mixture. For this study, we administered 161 mg/kg of either mixture (Mix-160) or tablet composed of hesperidin and by intragastric administration. Blood microsamples were collected from tail vein up to 24 h. Serum flavonoid extraction was performed by solid phase extraction and analyzed by LC-MS/MS of triple quadrupole (QqQ). Serum concentration vs. time plot showed that data fitted for a first-order model. The pharmacokinetic parameters were calculated by a noncompartmental model. The results showed that the absorption constant is higher than the elimination constant. The first concentration was found at five minutes, and minimal concentration at 24 h after administration, suggesting a enterohepatic recirculation phenomena and regulation of liver cytochromes’ activity. We did not find meaningful differences between the pharmacokinetic parameters of both samples. We concluded that tablet form did not interfere with the bioavailability of hesperidin and naringenin, and it could be a suitable candidate for developing a drug product.
Highlights
Diabetes and hypertension are chronic degenerative diseases with a high prevalence worldwide
Results showed that previous evidence reported by Araujo-León et al [8] showed a precision lower than 10% and an excellent recovery of more than 90% in picograms concentration order. This was compared to our results with research with flavonoids with a similar chemical structure that were evaluated in rat serum samples analyzed by LC-MS/MS
Results of flavonoid quantification were expressed as mean ± standard deviation. Both presentations of naringenin/hesperidin (Mix-160 vs. tablet) did not show statistical differences (p > 0.05) of pharmacokinetic parameters in a first-order kinetic model of absorption and a noncompartmental model of elimination. Both flavonoids showed a latency time of zero which means that the initial absorption began immediately after intragastric gavage
Summary
Diabetes and hypertension are chronic degenerative diseases with a high prevalence worldwide. There has been a growing interest in the research of bioactive molecules with multitarget affinity for treating different health conditions at once [2]. This approach should reduce polypharmacy of current treatments [3]. Toxicological assays in animal models showed that both molecules are safe because they did not exert severe toxicological effects. This evidence suggests that they could be classified as low-risk molecular entities, useful substances for drug development. A mixture of naringenin/hesperidin could be a good candidate for developing a dosage form with antidiabetic and antihypertensive properties [5]
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
