Hydrocortisone Acetate （CAS 50-03-3）

Hydrocortisone Acetate

Hydrocortisone Acetate (Hydrocortisone Acetate) Comprehensive Information

​Chemical Properties

1. ​Basic Parameters
   • ​Chemical Formula: C₂₃H₃₂O₆
   • ​Molecular Weight: 404.5
   • ​CAS Number: 50-03-3
   • ​EINECS Number: 200-004-4
   • ​Melting Point: 223°C (decomposition)
   • ​Solubility: Practically insoluble in water; slightly soluble in anhydrous ethanol and methylene chloride
   • ​Appearance: White powder
   • ​Stability: Stable under normal conditions but sensitive to light and moisture. Store at 0–6°C.
2. ​Structural Features
   A synthetic derivative of the natural steroid hormone cortisol, hydrocortisone acetate is an esterified form with enhanced stability. Its structure includes a 21-acetate group at the C21 position, improving its pharmacokinetic properties for topical or injectable use.

​Pharmacological Actions and Clinical Applications

1. ​Mechanism of Action
   • ​Anti-inflammatory & Immunosuppressive: Binds to glucocorticoid receptors, inhibiting the release of inflammatory mediators (e.g., prostaglandins, leukotrienes) and suppressing immune cell activity.
   • ​Replacement Therapy: Addresses adrenal insufficiency (e.g., Addison’s disease) by supplementing deficient cortisol.
2. ​Indications
   • ​Dermatological: Eczema, psoriasis, allergic dermatitis, and insect bites.
   • ​Ophthalmic: Allergic conjunctivitis (topical).
   • ​Systemic: Rheumatoid arthritis, asthma (short-term adjunct), and ulcerative colitis.
   • ​Local: Hemorrhoid-associated itching and swelling.
3. ​Dosage Forms and Administration
   • ​Topical: 1% cream or ointment applied 2–4 times daily.
   • ​Oral: Tablets (5/10/20 mg) for replacement therapy; dosage adjusted by body weight.
   • ​Injectable: Subcutaneous or intramuscular for acute inflammation or severe allergic reactions.

​Safety and Precautions

1. ​Adverse Effects
   • ​Local: Skin atrophy, telangiectasia, or secondary infections with prolonged use.
   • ​Systemic: Cushing’s syndrome (moon face, hypertension), HPA axis suppression.
2. ​Contraindications
   • Fungal or bacterial infections at application sites.
   • Pregnancy (risk-benefit assessment required); caution in lactating women.
3. ​Drug Interactions
   • Potentiated effects with CYP3A4 inhibitors (e.g., ketoconazole).
   • Avoid live vaccines during therapy due to immunosuppression.

​Manufacturing and Quality Control

1. ​Synthesis
   Prepared via acetylation of hydrocortisone under sterile conditions.
2. ​Analytical Standards
   • ​HPLC: C18 column with acetonitrile-water (38:62) mobile phase; detection at 254 nm for assay and impurity profiling.
   • ​Impurity Limits: Single impurity ≤1.0% of main peak area; total impurities ≤2.0%.

​Research and Market

1. ​Scientific Use
   • Inflammatory disease models (e.g., murine IgG modulation).
   • Studies on skin barrier repair mechanisms (e.g., PTEN/AKT/VEGF pathway inhibition).
2. ​Market Overview
   • ​Suppliers: ChemeGen, Bio Basic Inc., and others offer research-grade products (≥98% purity).
   • ​Price: ~0.50–0.60 per mg (100 mg vial).

​Regulatory and Storage

• ​Storage: Refrigerated (0–6°C) in light-resistant containers.
• ​Regulatory Status: Approved globally for veterinary and human use; classified as a prescription drug in most jurisdictions.

For detailed toxicological data or formulation protocols, consult specialized pharmacological references.