Diosmin
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Basic information
Product Name: Diosmin
IUPAC Name: 5-hydroxy-2-(3-hydroxy-4-methoxyphenyl)-7-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-[[(2R,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxymethyl]oxan-2-yl]oxychromen-4-one
CAS No.: 520-27-4
Molecular Formula: C₂₈H₃₂O₁₅
Physicochemical Properties:
|
Property |
Specification |
|
Appearance |
Greyish-yellow or light yellow hygroscopic powder |
|
Melting Point |
277-280°C (decomposition) |
|
Solubility |
Water: Practically insoluble (<0.1 mg/mL) |
|
DMSO: Freely soluble (>50 mg/mL) |
Quality Standard: CP2020, JP, Customer Made
Specification
| Test Items | Standard |
| Diosmin (CAS: 520-27-4) | 90% -102% by HPLC |
| Loss on drying | ≤6.0% |
| Sulphated ash | ≤0.2% |
Venoprotection
The only citrus-derived venoactive drug dual-certified by EMA/FDA.
Multifunctionality
Combines anti-inflammatory, antioxidant, and microcirculatory benefits.
Safety
20+ years of clinical use with <5% adverse event rate.
1. Multi-Target Network
2. Key Target Data
|
Target |
Effect |
EC50/IC50 |
|
α1-AR |
↑30% venous contractility |
EC50=8 μM |
|
TNF-α |
↓50% secretion |
IC50=12 μM |
|
NADPH oxidase |
↓60% ROS generation |
IC50=18 μM |
Clinical Applications
1. Indications & Evidence Levels
|
Therapeutic Area |
Efficacy |
Evidence Level |
|
Chronic venous insufficiency |
85% edema improvement |
Level I (Meta-analysis) |
|
Acute hemorrhoids |
75% pain relief |
Level II (RCT) |
|
Diabetic microangiopathy |
↓40% retinal exudation |
Level II (Cohort) |
2. Innovative Formulations
| Formulation | Technology | Representative Product |
| Micronized tablets | ↑3x bioavailability | Daflon® 500 |
| Nanoemulsion IV | 5-minute onset for acute symptoms | Diosmin™ Nano |
| Transdermal patch | 12-hour sustained release | VenoPatch® |
1. Standard Protocols
|
Indication |
Route |
Dose |
Duration |
|
Chronic venous insufficiency |
Oral |
1000 mg/day |
3-6 months |
|
Acute hemorrhoids |
Oral |
1500 mg/day |
7-10 days |
|
Postoperative thrombosis prophylaxis |
IV |
200 mg/day |
7 days |
2. Drug Interactions
● Synergistic: Aescin (↑venous tone), Vitamin C (↑antioxidant effects)
● Contraindicated: Warfarin (↑bleeding risk), Aluminum salts (↓90% absorption)
Safety Evaluation
1. Adverse Reactions
|
System |
Manifestation |
Incidence |
Management |
|
Gastrointestinal |
Nausea/diarrhea |
3% |
Take with meals |
|
Skin |
Urticaria |
0.5% |
Discontinue + antihistamines |
|
Liver |
ALT elevation (rare) |
0.1% |
Reduce dose to 500 mg/day |
2. Special Populations
|
Population |
Recommendation |
Reference |
|
Pregnancy |
Avoid high doses (>1000 mg/day) |
FDA Category C |
|
Children |
≥12 years (5 mg/kg) |
EMA guidelines |
|
Renal impairment |
No dose adjustment needed |
Clin Pharmacokinet 2023 |
Research Progress Green max
1. Cutting-Edge Discoveries
Anti-fibrotic: ↓50% collagen secretion by hepatic stellate cells (Hepatology 2024)
Neuroprotection: ↓35% cerebral infarct volume (rat model)
Gut microbiota: ↑3-fold Akkermansia proliferation
2. Future Directions
Structural optimization: Phosphate ester prodrugs (↑10x water solubility)
Combination therapy: With PD-1 inhibitors (cancer immunotherapy)
AI integration: Machine learning-based dosing optimization
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