Sulconazole Nitrate (Synonyms: RS 44872)

Sulconazole nitrate is an antifungal medication of the imidazole class.

After cutaneous application of radioactive solutions of Sulconazole nitrate in the hairless rat, the total absorption of the substance by the skin, estimated from the sum of the cumulative urinary and fecal excretions over 96 h, is 2.4% of the dose administered. The elimination reaches a maximum between 6 and 24 h and is virtually complete after 96 h. The excretion is almost equally distributed between the urine and the feces, which corresponds to an intense elimination via the biliary tract. The quantities present in the stratum corneum, epidermis and dermis at the end of the period of contact constituted another estimation of the total absorption of the substance which confirmed the previous estimation (3.6% of the dose). The measurement of the concentrations of Sulconazoleand its metabolites in the various layers of the skin reveals a high affinity of the substance for the stratum corneum, where it remains present in large quantities for more than 48 h. This affinity is due to the very intense lipophilia of the molecule. The concentrations in the other tissues are inversely proportional to the distance from the surface of the skin and are virtually nil in the circulating blood[3].

References:
[1]. Zaro BA, et al. Species variation in percutaneous absorption of sulconazole nitrate, a new anti-fungal agent. Proc West Pharmacol Soc. 1982;25:357-9.
[2]. Bielejewska A, et al. Effect of (+) or (-) camphorsulfonic acid additives to the mobile phase on enantioseparations of some basic drugs on a Chiralcel OD column. J Chromatogr A. 2005 Aug 12;1083(1-2):133-40.
[3]. Hercelin B, et al. Pharmacokinetics of cutaneous Sulconazole nitrate in the hairless rat: absorption, excretion, tissue concentrations. Eur J Drug Metab Pharmacokinet. 1993 Apr-Jun;18(2):149-54.