Comparative Bioavailability of Two Diosmin Formulations after Oral Administration to Healthy Volunteers

Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry
Rosario RussoNunziatina De Tommasi

Abstract

Diosmin is a flavonoid commonly found in citrus fruits, largely used as adjuvant treatment for circulatory disorders, including chronic venous insufficiency (CVI) and hemorrhoids. Following oral administration, diosmin is not directly absorbed but must first be hydrolyzed into its aglycone, diosmetin, which is then absorbed into the systemic circulation. The aim of the current cross-over clinical study was to assess the pharmacokinetic profile of µSmin® Plus, a micronized diosmin flavonoid complex standardized in diosmin and formulated with a buffering agent (tested formulation). The study compared this to unformulated micronized diosmin (reference), in 16 healthy volunteers. Plasma samples were analyzed by HPLC-MS and plasma diosmetin concentration was measured after deconjugation with β-glucuronidase. For the tested formulation area under the curve (AUC0-t), and maximum plasma and time concentration (Cmax; tmax) were found to be 298.4 ± 163.7, 50.3 ± 22.6 and 2.2 ± 2.9, respectively. AUC0-t and Cmax of the reference were 31.9 ± 100.4 and 2.4 ± 1.9, respectively. The tested formulation showed higher plasmatic concentrations of diosmetin in comparison to those obtained after the administration of unformulated micronized diosmin...Continue Reading

Associated Clinical Trials

References

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Citations

Feb 28, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Cristina ZaragozáMelchor Álvarez-Mon
Aug 23, 2019·Critical Reviews in Toxicology·Tian YangYing-Yong Zhao
Dec 11, 2020·Phytomedicine : International Journal of Phytotherapy and Phytopharmacology·Jangho LeeChang Hwa Jung
Dec 19, 2020·Comprehensive Reviews in Food Science and Food Safety·Ana-Maria Chiorcea-PaquimAna Maria Oliveira-Brett
Apr 4, 2021·Micromachines·Iulia Gabriela DavidAdela Magdalena Ciobanu
Jul 7, 2021·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Cristina ZaragozáMelchor Álvarez-Mon
Jul 25, 2021·International Journal of Molecular Sciences·Ramona Oana Gunache Roșca, Constantin Apetrei
Aug 28, 2021·Cancers·Raghad Khalid Al-IshaqDietrich Büsselberg

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