Diosmin and its application in the treatment of venous insufficiency

Introduction to the treatment of chronic venous insufficiency

For patients with chronic venous insufficiency (CVI), causal treatment is not available, and the therapy of this disease therefore relies primarily on conservative approaches, such as the use of compression bandages, elastic stockings, or intermittent pneumatic compression. In addition to physical therapy, venotropic drugs are used to enhance the tone of the venous wall, support lymphatic drainage from the limbs, and have anti-eczema and anti-inflammatory effects. These are usually substances of plant origin, such as troxerutin, rutoside, tribenoside, escin, or diosmin. Treatment of CVI is a long-term matter involving angiologists, dermatologists, and surgeons.

Diosmin in the treatment of CVI

Diosmin is part of many medicinal products and is commonly used, for example, in the treatment of CVI. It is a mixture of flavonoids, with an accepted specifically defined content of impurities (hesperidin, isorhoifolin, linarin, hesperidin diosmetin, 6-iododiosmin, and acetoisovanillin). Diosmin is derived through dehydrogenation from hesperidin, which is isolated from orange peels. The key properties of diosmin include antioxidant, anti-aggregation, and venotonic effects.

Pharmacokinetics

According to pharmacokinetic studies, diosmin is transformed by intestinal flora into the aglycone diosmetin. Its absorption and distribution occur throughout the body, with a plasma half-life of 26–43 hours. Diosmetin degrades mainly into phenolic acids and is eliminated through urine. Unabsorbed diosmin and diosmetin are excreted in feces.

Pharmacodynamics

Diosmin demonstrably has a positive impact on microcirculation, lymphatic drainage, capillary filtration, as well as the fragility and permeability of the venous wall. Diosmin improves its tone, suppresses inflammation, and protects against microcirculatory damage.

Enhancing the effect of diosmin

The absorption of diosmin, whose therapeutic effects depend on achieving the desired plasma level after oral administration, is influenced by several factors. These include solubility, ionization, molecular size, intestinal transit time specific to the patient, comorbidities, co-medication, and stomach pH. For diosmin, its modification into an appropriate dosage form to support absorption is crucial.

One way to improve absorption is through the process of micronization. This technique reduces particle size and increases their solubility to achieve greater absorption. Micronization can occur in grinding mills or fluid energy mills and is currently the most suitable technological process to ensure easier absorption of diosmin after oral administration. Besides diosmin, micronization is also used for other substances, such as griseofulvin or progesterone.

Conclusion

Medicinal products containing diosmin have been commonly used in the treatment of chronic venous insufficiency for decades; however, they also play a role in the treatment of hemorrhoids. Thanks to its beneficial effects on the venous wall, diosmin still holds an irreplaceable place in the comprehensive therapy of this venous disease even after many years since its introduction into CVI treatment. Moreover, through micronization, better absorption of diosmin is achieved, and medicinal products containing micronized diosmin are among the most effective.

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Source: Slíva J. Diosmin – still an important modality in the treatment of venous insufficiency. Internal Medicine 2019; 65 (7–8): 524–526.