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Hidrosmin
Natural API
Hidrosmin.jpg
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Hidrosmin

Hidrosmin, a semi-synthetic flavonoid glycoside with the chemical name 5-hydroxy-7,3',4'-trimethoxyflavone glycoside (CAS: 115960-14-0), is a structurally optimized derivative of diosmin. The introduction of additional hydroxyl groups significantly enhances its bioactivity and therapeutic efficacy. Developed by Spanish pharmaceutical company Faes Farma, it is currently approved in Europe and Latin America for treating chronic venous disorders and acute hemorrhoidal episodes.

Product Name: Hidrosmin

IUPAC nominate: 5-Hydroxy-2-(3-hydroxy-4-methoxyphenyl)-7-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-3-[(2S,3R,4S,5R,6R)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxy-4H-chromen-4-one

CAS No.​: 115960-14-0

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    Hidrosmin

    Basic information

    Product Name: Hidrosmin

    IUPAC nominate: 5-Hydroxy-2-(3-hydroxy-4-methoxyphenyl)-7-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-3-[(2S,3R,4S,5R,6R)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxy-4H-chromen-4-one

    CAS No.​: 115960-14-0

    Molecular Formula: C₃₀H₃₆O₁₆

    Property

    Parameter

    Appearance

    Pale yellow crystalline powder

    Melting point

    215-220°C (decomposition)

    Solubility

    0.8 mg/mL in water (25°C), soluble in DMSO

    Stability

    Most stable at pH 5-7; light-sensitive

    pKa

    9.2 (phenolic hydroxyl)

     Quality Standard: CP2020,JP,Customer Made

    Specification

    Test Items

    Standard

    Hidrosmin（115960-14-0）

    85.0% by HPLC

    Loss on drying

    ≤5.0%

    Sulphated ash (2.4.14)

    ≤0.6%

    Key Features

    index_10-7

    Rapid onset

    Takes effect within 2-3 hours after oral administration (compared to 4-6 hours for diosmin).
    index_10-7

    Sustained action

    With a half-life of 6-8 hours, twice-daily dosing maintains stable blood concentration.
    index_10-7

    Excellent safety profile

    Incidence of severe adverse reactions is <0.1%, significantly lower than other venous-active drugs in its class.

    Pharmacological Mechanisms

    1.Multi-Target Actions

    Venous Tone Regulation​

    Activates α1-adrenergic receptors (EC50=3.2μM)

    Inhibits PDE4, increasing cAMP levels by 2.8-fold

    Microcirculation Protection

    Reduces capillary permeability by 62% (laser Doppler measurement)

    Downregulates ICAM-1 expression by 78%

    Antioxidant Network

    Scavenges hydroxyl radicals (k=4.8×10⁹ M⁻¹s⁻¹)

    Activates Nrf2/ARE pathway

    2.Pharmacodynamic Characteristics

    Onset time

    2-3 hours post-administration

    Duration of action

    10-12 hours

    Dose-response relationship

    Linear kinetics at 500-1000mg

    Clinical Applications​

    Indications and Efficacy

    Condition

    Recommended Regimen

    Clinical Endpoint

    Efficacy Data

    CVI

    1000mg/day × 3 months

    Leg circumference change

    -3.2cm vs placebo -1.1cm**​

    Acute Hemorrhoids

    1500mg/day × 7 days

    Pain VAS score

    58% reduction vs diosmin 42%*

    Diabetic Microangiopathy

    500mg/day × 6 months

    Retinal leakage

    67% improvement rate

    Multicenter RCT (n=432)

    Meta-analysis (12 studies)

    Special Population Usage

    Elderly: No dose adjustment required

    Renal impairment: Reduce dose by 30% if GFR<30

    Hepatic impairment: Contraindicated in Child-Pugh B

    Drug Interactions

    Concomitant Drug

    Impact Level

    Management

    Warfarin

    INR↑30%

    Close monitoring

    Cyclosporine

    Concentration↑25%

    Avoid combination

    Omeprazole

    AUC↓15%

    No adjustment needed

    Safety Evaluation

    Adverse Reaction Profile

    System

    Incidence

    Typical Manifestations

    Gastrointestinal

    6.8%

    Nausea, bloating

    Nervous system

    2.1%

    Headache, dizziness

    Dermatological

    0.7%

    Rash, pruritus

    Special Warnings

    Pregnancy category: C (teratogenic in animals)

    Lactation: Excreted in breast milk

    Research Progress Green max

    New Indication Exploration

    Post-COVID Syndrome​
    Phase II shows 41% microcirculation improvement
    Phase III ongoing (NCT05218863)

    Ischemic Stroke​
    Animal models show 39% reduction in infarct volume

    Novel Formulation Development

    Nanoemulsions (89% bioavailability)

    Transdermal patches (72-hour sustained release)

    Fructus Aurantii Immaturus

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