A Pharmacokinetic Study of Mix-160 by LC-MS/MS: Oral Bioavailability of a Dosage Form of Citroflavonoids Mixture

• Published in: Molecules (Basel, Switzerland) Switzerland), 2022-01, Vol.27 (2), p.391
• Main Authors: Araujo-León, Jesús Alfredo, Ortiz-Andrade, Rolffy, Hernández-Baltazar, Efrén, Hernández-Núñez, Emanuel, Rivera-Leyva, Julio César, Yáñez-Pérez, Víctor, Vazquez-Garcia, Priscila, Cicero-Sarmiento, Carla Georgina, Sánchez-Salgado, Juan Carlos, Segura-Campos, Maira Rubí
• Format: Article
• Language: English
• Subjects: Administration, Oral; Animals; Antihypertensives; Bioavailability; Biological Availability; Chromatography; Chromatography, Liquid - methods; Diabetes; Dosage; Drug dosages; Equilibrium; Flavanones - administration & dosage; Flavanones - blood; Flavanones - pharmacokinetics; Flavonoids; Flavonoids - administration & dosage; Flavonoids - blood; Flavonoids - pharmacokinetics; Formulations; Hesperidin; Hesperidin - administration & dosage; Hesperidin - blood; Hesperidin - pharmacokinetics; Hypertension; LC-MS/MS; Liquid Chromatography-Mass Spectrometry; Male; Metabolism; Metabolites; Naringenin; Oral administration; Parameter modification; Pharmacokinetics; Pharmacology; Quadrupoles; Rats; Solid phases; Tablets; Tandem Mass Spectrometry - methods
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules27020391

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.