Comparison of Pharmacological Properties of Micronized Diosmin and Hesperidin in the Treatment of Chronic Venous Insufficiency and Hemorrhoids
Diosmin and hesperidin belong to the group of bioflavonoids, which currently find wide application in the treatment of chronic venous insufficiency and hemorrhoidal disease. Both flavonoids have been described to have a similar, but still not fully understood mechanism of action. Nevertheless, diosmin significantly differs from hesperidin, especially in pharmacokinetic parameters, which makes it the main carrier of the effect of venotonics.
Introduction
Diosmin and hesperidin are bioflavonoids extracted from citrus fruits. Numerous studies have demonstrated their positive effect on circulatory disorders such as chronic venous insufficiency and hemorrhoidal disease. The mechanism of action of diosmin and hesperidin is similar. Hesperidin exhibits antioxidant and anti-inflammatory effects with a molecular basis that is not yet fully elucidated. According to recent findings, an effect is hypothesized through the transcription factor group NF-κB.
The pharmacological properties of diosmin have been better explored. Diosmin also shows strong anti-inflammatory and antioxidant effects, reduces the levels of TNF-α, VEGF-C, VEGF-A, and IL-6, which are important substances in the pathophysiology of edema. The antioxidant effect has been shown in experimental studies to influence the increase in vitamin C levels in plasma and tissues. The anti-inflammatory effects of diosmin are complex, and according to recent findings, it also acts via the transcription factors NF-κB and the MAPK signaling cascade.
Difference in Pharmacological Properties
Natural diosmin is manufactured for pharmaceutical purposes by extracting hesperidin from citrus fruits, after which hesperidin is dehydrogenated to diosmin. Thus, pure diosmin is not used in medicinal products, but diosmin with a certain proportion of a mixture of flavonoids, defined as impurities according to the European Pharmacopoeia. Upon oral administration, both substances are converted in the intestines into active metabolites, diosmetin and hesperetin.
They differ significantly in pharmacokinetic properties. The biological half-life of diosmetin is 26–43 hours, while that of hesperetin is only 3 hours. The bioavailability of hesperetin is also lower compared to diosmetin, being below 25%. For diosmetin it has been determined to be < 57%, with the micronized form of diosmin contributing to increased bioavailability, facilitating easier absorption.
Conclusion
The results of studies suggest that the mechanism of action of hesperidin and diosmin, as related substances, is similar. However, the fundamental difference lies in the pharmacological properties of both substances, with diosmin having a much longer biological half-life and better bioavailability compared to hesperidin, making diosmin the primary active ingredient in currently used venotonics.
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