Sulconazole Nitrate API is the nitrate salt of sulconazole, a synthetic imidazole antifungal active pharmaceutical ingredient. It is used in topical pharmaceutical formulations for the treatment of fungal skin infections. Sulconazole Nitrate has the chemical formula C₁₈H₁₅Cl₃N₂S·HNO₃, molecular weight 460.76 g/mol, and CAS Number 61318-91-0.
Sulconazole belongs to the imidazole class of antifungal compounds and acts by interfering with fungal sterol biosynthesis. The resulting disruption of fungal cell membrane formation contributes to its antifungal activity. Current U.S. labeling describes Sulconazole Nitrate as a broad-spectrum antifungal and antiyeast agent for topical use.
Sulconazole Nitrate is a white to off-white crystalline powder with a molecular weight of approximately 460.77 g/mol. It is freely soluble in pyridine, slightly soluble in ethanol, acetone and chloroform, and very slightly soluble in water. The current drug label reports a melting point of approximately 130°C.
The compound is supplied as the nitrate salt of racemic sulconazole. USP identifies the API as (±)-1-[2,4-dichloro-β-[(p-chlorobenzyl)thio]phenethyl]imidazole mononitrate.
Sulconazole Nitrate is primarily used in topical antifungal formulations. It has activity against common pathogenic dermatophytes, including Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum and Microsporum canis, and also demonstrates activity against organisms associated with pityriasis versicolor and certain Candida species.
Commercial topical formulations include 1.0% cream and 1.0% solution, corresponding to 10 mg/g or 10 mg/mL Sulconazole Nitrate respectively.
Sulconazole inhibits fungal cytochrome P450-dependent sterol C14-alpha-demethylation, interfering with ergosterol biosynthesis. Reduction of ergosterol disrupts fungal cell membrane integrity and inhibits fungal growth.
Sulconazole Nitrate has a USP monograph with defined requirements for identity, assay, organic impurities, residue on ignition and loss on drying. The USP assay uses liquid chromatography with UV detection at 230 nm.
The USP specification requires an assay of 98.0–102.0% on the dried basis. Organic impurities are controlled through a chromatographic procedure, including Sulconazole Related Compound A and unspecified impurities.
Sulconazole sulfoxide has been identified as an important oxidative degradation product and was specifically investigated to support modernization of the USP analytical procedure.
Swapnroop Drugs and Pharmaceuticals provides pharmaceutical API manufacturing capabilities supported by controlled processing, analytical testing and quality documentation.
Sulconazole Nitrate can be evaluated against applicable USP and customer-specific requirements, with analytical controls covering assay, related substances, loss on drying and residue on ignition.
Sulconazole Nitrate should be stored in well-closed containers and protected from light, consistent with the USP additional requirements.
Suitable moisture- and light-protective packaging should be used to maintain the quality and stability of the API during storage and transportation.
Depending on applicable commercial and regulatory requirements, documentation may include:
Sulconazole Nitrate has established USP analytical requirements for assay and related substances. Swapnroop focuses on controlled pharmaceutical API manufacturing, analytical quality evaluation and documentation support for pharmaceutical-grade requirements.
| 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 0.1% |
| Individual Impurity | NMT 0.10% |
| Total Impurities | NMT 2.0% |
| Melting Point | About 130°C |