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Diosmin | CAS No: 520-27-4 | GMP-certified suppliers
A medication that supports venous and capillary function to help manage chronic venous disorders and hemorrhoidal symptoms for appropriate use in vascular‑health product lines.
Therapeutic categories
Primary indications
- Diosmin is used over-the-counter alone or with ingredients such as [hesperidin] and [diosmetin] to support vein and capillary function
Product Snapshot
- Oral and topical small‑molecule flavonoid supplied in multiple solid and semi‑solid formulations
- Used in products intended to support venous and microvascular function
- Marketed in the US with mixed status including approved and investigational listings
Clinical Overview
Pharmacologically, diosmin modulates microcirculatory function by improving lymphatic drainage and enhancing venous tone and elasticity. These effects contribute to reduced edema and improved venous return. Diosmin also exhibits antioxidant activity, scavenging reactive oxygen species and reducing oxidative stress biomarkers. Clinical studies have reported decreases in inflammatory mediators such as TNF‑alpha, IL‑6, FGF2, and VEGF isoforms during therapy, accompanied by reductions in leg circumference in patients with venous insufficiency.
The mechanism of action is not fully defined. Proposed pathways include interactions with the aryl hydrocarbon receptor, though the relevance to venous physiology remains unclear. Experimental findings also suggest modulatory effects on noradrenaline metabolism in varicose vein tissue. Diosmin has been associated with improved glucose metabolism in certain metabolic conditions, although the clinical significance of this observation requires further study.
ADME parameters are not comprehensively characterized, and available data are limited. Diosmin undergoes metabolic conversion to its aglycone forms, but detailed pharmacokinetic profiles vary across studies.
Safety experience indicates a favorable tolerability profile, with most reported adverse effects mild and gastrointestinal in nature. Diosmin is classified within several pharmacologic groups, including vasoprotectives, flavonoids, and inhibitors of multiple cytochrome P450 isoenzymes and transporters, highlighting the need to consider potential drug interaction risks in multi‑therapy settings.
For API procurement, sourcing should prioritize authenticated botanical or synthetic origins, control of flavonoid composition, and verification of contaminants and residual solvents, with adherence to pharmacopeial specifications where applicable.
Identification & chemistry
| Generic name | Diosmin |
|---|---|
| Molecule type | Small molecule |
| CAS | 520-27-4 |
| UNII | 7QM776WJ5N |
| DrugBank ID | DB08995 |
Pharmacology
| Summary | Diosmin is a venoactive flavonoid thought to support vascular structure and microcirculatory function, although its precise molecular mechanism remains unclear. It may interact with the aryl hydrocarbon receptor and influence processes such as venous tone, lymphatic drainage, and oxidative stress. Additional observations include effects on inflammatory and metabolic markers, but the clinical relevance of these findings is not fully established. |
|---|---|
| Mechanism of action | Diosmin helps to maintain circulatory system structure and function, particularly vein strength and competence.The molecular mechanism of action of diosmin has not been established.Several resources indicate that diosmin binds to the aryl hydrocarbon receptor, however clinical relevance to vascular function is unknown.One study demonstrates that oral diosmin exerts effects on the in vitro metabolism of noradrenaline by varicose veins, potentially benefitting vascular health. |
| Pharmacodynamics | Diosmin is a venoactive drug supporting circulatory health through various actions on blood vessels; it supports lymphatic drainage and improves microcirculation while increasing venous tone and elasticity. For these reasons, diosmin is frequently taken by individuals with chronic venous disease to support vascular health and has been demonstrated to improve quality of life.In addition to the above effects, diosmin exerts antioxidant activity and scavenges oxygen free radicals, reducing levels of oxidative stress normally detected through biomarkers such as prostaglandins isoprostane precursors. In one clinical study, mean content of TNF alpha, VEGF-C, VEGF-A IL-6, in addition to FGF2 were decreased by after the therapy with diosmin; findings were statistically significant. Additionally, a decrease in edema and mean leg circumference of patients taking diosmin for three months was observed in a clinical study.Diosmin has been demonstrated to enhance the metabolism of glucose in diabetic disorders. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Aryl hydrocarbon receptor | Humans | agonist |
ADME / PK
| Absorption | Diosmin is rapidly absorbed in the gastrointestinal tract.After a 900 mg single oral dose in a study using liquid chromatography with tandem mass spectrometry (LC-MS/MS) method, Cmax was 4.2±3.8 <sup>ng·mL-1</sup>, Tmax was 18.7±9.9 hours, and AUC0~96 was 185.4±166.2 <sup>ng·mL-1</sup> in healthy volunteers.Another pharmacokinetic study of 5 adults revealed a Cmax of 417±94.1 ng/dL. |
|---|---|
| Half-life | Diosmin half-life ranges from 26 to 43 hours.One study using a liquid chromatography with tandem mass spectrometry (LC-MS/MS) method after a single 900 mg dose of diosmin demonstrated a half-life of 60.2±85.7 hours in healthy volunteers. |
| Protein binding | Diosmin binds to serum albumin. |
| Metabolism | Degradation products of diosmin such as alkyl-phenolic acids confirm a metabolic pattern similar to that of other flavonoids. |
| Route of elimination | Pharmacokinetic data show absence of urinary elimination for diosmin and its aglycone diosmetin. Minor metabolites are found to be eliminated in the urine as glucuronic acid conjugates. |
| Volume of distribution | A pharmacokinetic study of 5 adults revealed a volume of distribution of 62.1±7.9 L. |
Formulation & handling
- Oral formulations require solubility enhancement or dispersion-based approaches due to low logP and modest aqueous solubility for this high‑molecular‑weight flavonoid glycoside.
- Solid-state stability is generally good, but hygroscopicity and potential for poor wettability should be considered during granulation and suspension preparation.
- Topical forms rely on appropriate solvent or surfactant systems to improve dermal penetration given the compound’s hydrophilicity and bulky glycoside structure.
Regulatory status
| Lifecycle | Patent‑expiry details were not provided, so the lifecycle stage can only be characterized by market presence. With the API marketed in the US, its lifecycle reflects the maturity level typical for products established in a single, well‑regulated market, with competitiveness determined largely by remaining patent or exclusivity protections once known. |
|---|
| Markets | US |
|---|
Supply Chain
| Supply chain summary | Diosmin is supplied by multiple manufacturers, with no active exclusivity from an originator company and long‑expired patents supporting broad generic production. In the US market, branded formulations such as Vasculera and combination hemorrhoidal products indicate established commercial presence, while similar products are available in other regions. The mature patent landscape suggests existing global generic competition and a stable, widely distributed API supply. |
|---|
Safety
| Toxicity | The LD50 of diosmin is >3g/kg in animal studies, with an LD50 of great than 3000 mg/kg in rats.No cases of overdose have been reported, however, an overdose is likely to result in gastrointestinal effects such as nausea, dyspepsia, vomiting, and diarrhea. |
|---|
- Acute toxicity is low in animals, with reported oral LD50 values ›3000 mg/kg in rats
- Handling does not typically require high‑hazard controls at standard scales
- Overexposure may provoke gastrointestinal irritation (nausea, dyspepsia, vomiting, diarrhea)
Diosmin is a type of Phlebotonics
Phlebotonics is a subcategory of pharmaceutical Active Pharmaceutical Ingredients (APIs) that are specifically designed to address venous disorders and promote healthy blood circulation. These APIs are used in the formulation of medications aimed at treating conditions such as chronic venous insufficiency, varicose veins, and hemorrhoids.
Phlebotonics work by strengthening the walls of blood vessels and improving their elasticity. They also help reduce inflammation and edema, which can be common symptoms of venous disorders. By enhancing venous tone and reducing blood stasis, phlebotonics help alleviate pain, swelling, and discomfort associated with these conditions.
The key active ingredients found in phlebotonics include substances like diosmin, hesperidin, rutosides, and troxerutin. These compounds exhibit venotonic properties, meaning they have a positive impact on venous tone and function. Phlebotonics are typically available in various dosage forms such as tablets, capsules, creams, and gels for convenient administration.
Medical professionals often recommend phlebotonics as an adjunctive treatment along with lifestyle modifications such as regular exercise, elevation of the legs, and compression therapy. These medications are generally well-tolerated and have a favorable safety profile.
In conclusion, phlebotonics are a specialized class of pharmaceutical APIs that play a crucial role in managing venous disorders. By improving venous tone, reducing inflammation, and enhancing blood circulation, these medications provide symptomatic relief and improve the overall quality of life for individuals with venous insufficiency, varicose veins, and hemorrhoids.
Diosmin (Phlebotonics), classified under Others
The others category refers to pharmaceutical APIs that do not fall under specific classifications such as antibiotics, antivirals, analgesics, or cardiovascular drugs. These APIs are diverse in nature and serve various therapeutic purposes, making them a crucial component of pharmaceutical formulations.
Pharmaceutical companies develop APIs in the others category to address specific medical conditions or target novel biological pathways. This category includes APIs used in oncology, neurology, immunology, and other specialized areas of medicine. The APIs in this category are often designed to interact with specific molecular targets or receptors, providing targeted therapeutic effects.
The development of APIs in the others category requires extensive research and testing to ensure their efficacy, safety, and compliance with regulatory standards. Pharmaceutical manufacturers employ advanced techniques such as chemical synthesis, biotechnology, and genetic engineering to produce these APIs.
Due to the broad range of applications and therapeutic uses, APIs in the others category contribute significantly to the advancement of medical treatments. Pharmaceutical companies constantly strive to innovate and discover new APIs within this category to address unmet medical needs and improve patient outcomes.
In conclusion, the others category of pharmaceutical APIs encompasses a diverse range of active ingredients used in drug formulation. These APIs play a crucial role in developing innovative therapies across various therapeutic areas, contributing to advancements in healthcare and patient well-being.
Diosmin API manufacturers & distributors
Compare qualified Diosmin API suppliers worldwide. We currently have 14 companies offering Diosmin API, with manufacturing taking place in 6 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Aurora Industry Co., Ltd | Distributor | China | China | BSE/TSE, CEP, CoA, FDA, GMP, ISO9001, MSDS, USDMF, WC | 250 products |
| Chengdu Okay | Producer | China | China | CEP, CoA, GMP | 2 products |
| Chengdu Runde | Producer | China | China | CEP, CoA, GMP | 1 products |
| Chengdu Shuxi | Producer | China | China | CEP, CoA, GMP | 1 products |
| Chr. Olesen Group | Distributor | Denmark | China | CEP, CoA, USDMF | 252 products |
| Faes Farma | Producer | Spain | Spain | CEP, CoA, GMP | 2 products |
| Hunan Yuantong | Producer | China | China | CEP, CoA, GMP, WC | 1 products |
| Isochem | Producer | France | France | CEP, CoA, FDA, GMP, USDMF | 12 products |
| KRKA | Producer | Slovenia | Slovenia | CoA, GMP | 81 products |
| PMC Isochem | Producer | France | Unknown | CEP, CoA, GMP | 7 products |
| Senova Technology Co., Lt... | Producer | China | China | BSE/TSE, CoA, ISO9001, MSDS | 157 products |
| Sichuan New Hawk Bio | Producer | China | China | CEP, CoA | 1 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CEP, CoA, GMP, ISO9001, MSDS, USDMF, WC | 762 products |
| Triquim | Producer | Argentina | Argentina | CoA, GMP, ISO9001 | 16 products |
When sending a request, specify which Diosmin API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Diosmin API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
Frequently asked questions about Diosmin API
Sourcing
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Technical
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Regulatory
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