Diosmin and vascular health: the well-established venotonic mechanism (and the technology that takes it further)

Chronic venous insufficiency is the second most prevalent pathology in the world, yet its most common symptoms (pain, swelling, heaviness in the legs) are still often treated as a minor inconvenience. In the blog article Your circulation support, we already explained why Diosmin is one of the citrus flavonoids with the longest track record in vascular health. On this occasion, we review exactly what it does at the vascular level, what published evidence supports it, and why the way it is administered, not just the molecule, determines how much of that potential actually reaches the body.

From sweet orange to a vasoprotective ingredient

Diosmin is a flavone that we obtain from Hesperidin, naturally present in Citrus sinensis (sweet orange). At Bordas, we extract, purify, and process it under our own quality control from origin to final product.

Its pharmaceutical application has been well established for decades due to its venotonic and vasoprotective properties, indicated in the treatment of disorders stemming from chronic venous insufficiency (varicose veins, oedema, haemorrhoids). It is one of the best-documented uses across our entire catalogue of active ingredients.

What Diosmin does in the vascular system

Cardiotonic¹: In patients undergoing coronary artery bypass surgery, pretreatment with micronised purified flavonoid fraction showed documented beneficial effects in a human clinical study.

Antithrombotic²: Molecular binding studies show antiplatelet activity of Diosmin and related flavonoids.

Enhancer of lymphatic drainage³: Clinical reviews on venoactive compounds place micronised purified flavonoid fraction among the most backed options for the treatment of chronic venous disease.

Anti-inflammatory⁴ and antioxidant⁵: In vitro studies describe how Diosmin modulates inflammatory pathways in macrophages and protects endothelial cells against oxidative stress (mechanistic evidence, not patient trials).

The combined result: it improves vascular tone and the resistance of small blood vessels, helps prevent the rupture of capillary walls, and improves blood circulation and microcirculation.

Reference dose in pharmaceutical application: 500 mg twice daily, usually in combination with Hesperidin in a 9:1 ratio.

Why the molecule is not enough: the role of micronisation

Non-micronised Diosmin has a relatively large particle size (100% below 100 μm). Our micronised Diosmin, the foundation of our Micronised Purified Flavonoid Fraction (MPFF) technology, substantially reduces that size: 100% below 45 μm, 90% below 5 μm, and 50% below 2 μm.

Review our article.

Reviews on MPFF in chronic venous disease⁶ document that this particle reduction translates into faster absorption and greater bioavailability compared to the non-micronised form, allowing for more precise dosing, dose reduction without compromising the therapeutic effect, and improved stability of the finished product.

Our MPFF combines 90% Diosmin with 10% complementary flavonoids (diosmetin, hesperidin, linarin, isorhoifolin)⁶.

Would you like to see more about the differences between Diosmin and micronised Diosmin? Take a look here.

What this means for formulators

For pharmaceuticals, Bordas’ Diosmin, with or without micronisation, comes backed by complete regulatory documentation: GMP, CEP, and customisable ASMF, thus supporting its positioning in vascular health.

We are a leading European manufacturer of Diosmin and Micronised Purified Flavonoid Fraction (MPFF) for the following reasons:

  • Regulatory trust: High-quality system, strict compliance with GMP, and full traceability. We protect regulatory records and marketing authorisations.
  • Security of supply: Manufacturing in Europe and consistent deliveries. Your production does not stop.
  • Competitive price: Optimised cost structure. Yes, we are competitive and we also comply with the regulations.
  • Technical flexibility: We adapt the API specifications to different requirements: impurity profile, moisture content, and customisation of the ASMF (Active Substance Master File).

Zero risk of Nitrosamines in Bordas Diosmin

At Bordas, we have an in-house study evaluating the risk of Nitrosamines in our Diosmin.

Nitrosamines are chemical compounds that can form in medicines and food. They are of special regulatory interest because they are genotoxic (they can alter DNA) and carcinogenic.

Although the Diosmin molecule does not generate nitrosamines on its own, the extraction method of other manufacturers could leave traces of “chemical species” (precursors) that could indeed form them. Bordas’ study seeks to demonstrate that its manufacturing process eliminates this risk.

Our objective with this study is to guarantee the suitability of our Diosmin in the pharmaceutical industry; therefore, in our study we did not limit ourselves to measuring the final product, we forced the creation of impurities to see if it were possible.

We did so in three phases:

Phase A (Validation): First, we established the ideal conditions to create nitrosamines from a known amine (DMA) to ensure that our detection method worked correctly.

Phase B ( Challenge): We subjected three industrial batches of our Bordas Diosmin to “highly nitrosating” conditions: a highly acidic medium (pH 1), high temperatures (90°C), and a 20% excess of nitrites over a hypothetical contamination situation.

Phase C ( Control): To leave no room for doubt, we intentionally spiked a sample of Diosmin with an amine (DMA) and subjected it to the same process. This serves to demonstrate that, had there been previous impurities, the analysis would have detected them.

The result was key.

On the one hand, we obtained total purity across all three Bordas industrial batches. The results for the 9 nitrosamines were negative or below the limit of quantitation (< 1 ppb).

Furthermore, we guaranteed the effectiveness of the test, as the positive control (spiked sample) detected high levels of NDMA (>100 g/kg), which confirms that our procedure at Bordas is extremely rigorous and capable of detecting any anomaly.

 

Diosmin does not need to be presented as a discovery, as its vasoprotective and venotonic function has been established and documented for years. What is evolving is how much of that potential is harnessed, that is where our MPFF technology comes in; with controlled particle size below 5 μm, it enables greater bioavailability and more efficient dosing.

Would you like the full technical data for our Diosmin? Get in touch with our team.

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