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Molecules 2018, 23(9), 2174; https://doi.org/10.3390/molecules23092174

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

1
Giellepi S.p.A. Health Science, via B. Cellini 37, 20851 Lissone (MB), Italy
2
Bioagile Therapeutics Pvt. Ltd., Bangalore 560094, India
3
Dipartimento di Farmacia, Università di Salerno, via Giovanni Paolo II 132, 84084 Fisciano (SA), Italy
*
Author to whom correspondence should be addressed.
Received: 26 July 2018 / Revised: 24 August 2018 / Accepted: 25 August 2018 / Published: 29 August 2018
(This article belongs to the Special Issue The Potential Use of Herbal Medicinal Products in Chronic Disorders)
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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. The relative bioavailability was 9.4 greater for the tested formulation than in micronized diosmin. In conclusion, our data indicate that µSmin® Plus was rapidly and well absorbed into systemic circulation and may therefore be ideally suitable to deliver diosmin in human interventional trials. View Full-Text
Keywords: µSmin® Plus; diosmin; diosmetin; pharmacokinetics; chronic venous insufficiency (CVI) µSmin® Plus; diosmin; diosmetin; pharmacokinetics; chronic venous insufficiency (CVI)
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Russo, R.; Chandradhara, D.; De Tommasi, N. Comparative Bioavailability of Two Diosmin Formulations after Oral Administration to Healthy Volunteers. Molecules 2018, 23, 2174.

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