Troxerutin
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Basic information
Product Name: Troxerutin
IUPAC Name: 3′,4′,7-Tris[O-(2-hydroxyethyl)]quercetin-3-O-rutinoside
CAS No.: 7085-55-4
Molecular Formula: C₁₅H₁₀O₅
Physicochemical Properties:
Parameter |
Value/Description |
Appearance |
Pale yellow to white powder |
Melting Point |
195-198°C (decomposition) |
Solubility |
>300 mg/mL in water (25°C), superior to rutin (15 mg/mL) |
logP |
-1.2 (strong hydrophilicity) |
Optical Rotation |
[α]²⁵D = +12° (c=1, methanol) |
Quality Standard: CP2020,JP,Customer Made
Specification
Test Items |
Standard |
Troxerutin (CAS: 7085-55-4) |
EP10.0 |
Loss on drying |
≤5.0% |
Sulphated ash |
≤0.4% |
Structural Optimization
Multi-Target Action
Clinical Status
1. Molecular Target Network
2. Pharmacokinetics
Absorption
Oral bioavailability 45-50% (vs. 5-10% for rutin).
Distribution
Primarily in vascular-rich tissues (liver, spleen, lungs).
Metabolism
Hydrolyzed to quercetin and hydroxyethyl quercetin by gut microbiota.
Excretion
60% urinary excretion (<10% as parent compound).
Clinical Applications
Indications & Efficacy
Condition |
Regimen |
Evidence |
Chronic Venous Insufficiency |
300 mg tid ×4 weeks |
Leg circumference↓2.8 cm* |
Acute Hemorrhoids |
500 mg bid ×7 days |
75% pain relief |
Diabetic Retinopathy |
200 mg tid ×6 months |
Microaneurysms↓40% |
*Meta-analysis (18 RCTs, n=2500)
Special Populations
Renal Impairment: Reduce dose by 30% if GFR 30-60 mL/min.
Elderly: No dose adjustment (monitor blood pressure).
Dosage and Administration
Formulations
Tablets: 300 mg (oral)
Injection: 100 mg/2 mL (IV infusion)
Suppositories: 500 mg (rectal)
Dosing Guidelines
Use |
Dose |
Duration |
Varicose Veins |
300 mg tid |
≥2 months |
Postoperative Edema |
100 mg IV bid |
3-5 days |
Microcirculation Disorders |
200 mg tid |
Long-term |
Safety Evaluation
1.Adverse Reactions
System |
Incidence |
Management |
Gastrointestinal |
3-5% |
Take with food |
Headache |
1-2% |
Reduce dose |
Hypersensitivity |
<0.5% |
Discontinue |
2.Contraindications & Interactions
Absolute CI:
Active gastrointestinal bleeding.
Hypersensitivity to hydroxyethyl starch (excipient in injections).
Cautions:Anticoagulants (e.g., warfarin): May prolong PT/INR.
Research Progress Green max
Novel Formulations
Nanoliposomes: Bioavailability↑to 75% (animal studies).
Sustained-release Microspheres: Single injection maintains efficacy for 7 days.
New Indications
Ischemic Stroke: Reduces infarct volume (35%↓ in animal models).
COVID-19 Coagulopathy: Improves D-dimer levels (Phase II trials).
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