Isoconazole Nitrate API | Antifungal API Manufacturer in India

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Isoconazole Nitrate API

Isoconazole Nitrate is a synthetic imidazole antifungal agent used for the treatment of superficial fungal infections of the skin. It exhibits broad-spectrum antifungal activity against various dermatophytes, yeasts and other susceptible fungi.

Isoconazole Nitrate acts primarily by inhibiting the fungal enzyme lanosterol 14α-demethylase, interfering with ergosterol biosynthesis and disrupting the fungal cell membrane.

Isoconazole Nitrate API Manufacturer in India

Isoconazole Nitrate is a specialized azole antifungal pharmaceutical API manufactured through controlled chemical synthesis, purification and crystallization processes.

Quality evaluation focuses on identity, assay, related substances, residual solvents, water content, inorganic impurities, particle characteristics and stability.

Chemical Information

CAS Number: 24168-96-5
Molecular Formula: C18H14Cl4N2O · HNO3
Molecular Weight: 479.14 g/mol
Drug Class: Antifungal Agent
Pharmacological Class: Imidazole Antifungal
Therapeutic Class: Antifungal
Therapeutic Area: Dermatology / Infectious Diseases

Mechanism of Action

Isoconazole inhibits lanosterol 14α-demethylase, a cytochrome P450-dependent enzyme involved in the biosynthesis of ergosterol.

Ergosterol is an essential component of fungal cell membranes. Inhibition of its production results in:

  • Reduced ergosterol synthesis
  • Alteration of fungal membrane structure
  • Increased membrane permeability
  • Impaired fungal growth
  • Ultimately, inhibition or destruction of susceptible fungal organisms

Antifungal Activity

Isoconazole Nitrate demonstrates activity against a variety of organisms responsible for superficial fungal infections, including susceptible:

  • Dermatophytes
  • Yeasts
  • Yeast-like fungi
  • Other susceptible fungal organisms

Its spectrum and clinical effectiveness depend on the organism and infection being treated.

Pharmaceutical Applications

Isoconazole Nitrate is primarily relevant to the treatment of superficial fungal infections of the skin, including infections associated with dermatophytes and yeasts.

It may be incorporated into topical pharmaceutical formulations such as:

  • Creams
  • Topical preparations
  • Other dermatological dosage forms

Specific indications depend on the approved formulation and regulatory market.

Manufacturing Process

Typical API manufacturing may involve:

  1. Controlled chemical synthesis
  2. Formation of the isoconazole intermediate
  3. Purification
  4. Salt formation with nitric acid
  5. Crystallization
  6. Filtration
  7. Drying
  8. Milling where required
  9. Final analytical testing
  10. Packaging under controlled conditions

Quality and Analytical Testing

Isoconazole Nitrate API quality evaluation may include:

  • Identification by IR
  • Identification by HPLC
  • Assay
  • Related substances
  • Organic impurities
  • Residual solvents
  • Water content
  • Nitrate content
  • Inorganic impurities
  • Residue on ignition
  • Heavy metals / elemental impurities
  • Particle-size distribution where required
  • Polymorphic characterization
  • Stability testing

Storage

Isoconazole Nitrate should be stored in a tightly closed container under controlled pharmaceutical storage conditions, protected from excessive heat, moisture and direct light. Final storage conditions should be established from validated stability data.

Pharmaceutical Research and Development

Isoconazole Nitrate is relevant to research involving:

  • Azole antifungals
  • Imidazole antifungal agents
  • Fungal membrane biology
  • Ergosterol biosynthesis
  • Dermatological formulations
  • Topical antifungal development
  • Superficial fungal infections
  • Antifungal susceptibility

Isoconazole Nitrate API Summary

Isoconazole Nitrate is a synthetic imidazole antifungal API with CAS Number 24168-96-5, molecular formula C18H14Cl4N2O·HNO3, and molecular weight 479.14 g/mol. It inhibits fungal ergosterol biosynthesis by targeting lanosterol 14α-demethylase and is primarily used in topical treatment of superficial fungal infections.

Detailed Specifications

Parameter Specification
Appearance White to off-white crystalline powder
Identification IR & HPLC compliant
Assay (HPLC) 98.0% – 102.0%
Loss on Drying NMT 1.0%
Residue on Ignition NMT 0.5%
Individual Impurity NMT 0.5%
Total Impurities ≤ 1.5%
Water Content NMT 1.0%
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