Sertaconazole Research Articles

Effects of sertaconazole nitrate on T-cell activation, irritant dermatitis, and contact hypersensitivity

Effects of sertaconazole nitrate on T-cell activation, irritant dermatitis, and contact hypersensitivity

Memantine

Each month, subscribers to The Formulary Monograph Service receive five to six well-documented monographs on drugs that are newly released or are in late Phase III trials. The monographs are targeted to your Pharmacy and Therapeutics Committee. Subscribers also receive monthly one-page summary monographs on the agents that are useful for agendas and pharmacy/nursing in-services. A comprehensive target drug utilization evaluation (DUE) is also provided each month. With a subscription, the monographs are sent to you in print and CD ROM forms and are available online. Monographs can be customized to meet the needs of your facility. Subscribers to the The Formulary Monograph Service also receive access to a pharmacy bulletin board, The Formulary Information Exchange (The F.I.X.). All topics pertinent to clinical and hospital pharmacy are discussed on The F.I.X. Through the cooperation of The Formulary, Hospital Pharmacy publishes selected reviews in this column. If you would like information about The Formulary Monograph Service or The F.I.X., call The Formulary at 800-322-4349. The March 2004 monograph topics are cinacalcet hydrochloride, sertaconazole nitrate, etoricoxib, abetimus sodium, and rasagiline mesylate. The DUE is on atypical antipsychotics.

Effect of Cyclodextrins on the Solubility and Antimycotic Activity of Sertaconazole: Experimental and Computational Studies

This study investigated the effects of the complexation of sertaconazole nitrate with different cyclodextrin (CD) derivatives (α‐CD, β‐CD, γ‐CD, hydroxypropyl‐β‐CD, and hydroxypropyl‐γ‐CD) on the aqueous solubility and antimycotic activity of the drug. Phase solubility studies indicated that the solubility of sertaconazole in enzyme‐free simulated gastric‐ and enzyme‐free simulated enteric fluids was significantly increased in the presence of cyclodextrins. The observed order of solubility increasing effect was: γ‐CD > HPγ‐CD > HPβ‐CD > β‐CD > α‐CD. Solid‐state sertaconazole–cyclodextrin complexes were prepared by freeze drying, and characterized by X‐ray powder difractometry, differential scanning calorimetry (DSC), and infrared spectroscopy (FTIR). Freeze‐dried complexes showed markedly higher solubility than both physical mixtures and sertaconazole alone. The antimycotic activities of sertaconazole–cyclodextrin complexes in solution were evaluated by inhibition zone assays with Candida albicans. The activity ranking agrees with the solubility ranking observed for these complexes, with the γ‐CD–sertaconazole complex showing the strongest antimycotic activity. Finally, molecular modeling studies were carried out using the MM2 force field method, for complexes in vacuum and in water. This enable indentification of the preferred orientation of sertaconazole in the γ‐CD cavity and of the main structural features responsible for the enhancement of its solubility and antimycotic activity. © 2002 Wiley‐Liss, Inc. and the American Pharmaceutical Association J Pharm Sci 91:2408–2415, 2002

Sertaconazole: In-Vitro Antifungal Activity Against Vaginal and Other Superficial Yeast Isolates

The in vitro susceptibilities of 183 clinical yeast isolates to sertaconazole (STZ) were compared to their susceptibilities to clotrimazole (CTZ), econazole (ECZ), ketoconazole (KTZ), miconazole (MNZ), fluconazole (FLZ), itraconazole (ITZ), tioconazole (TCZ), amphotericin B (AMB) and flucytosine (5FC) by using a commercial agar diffusion method. Strains were isolated from vaginal and other superficial clinical samples (18 species of Candida and five strains belonging to other yeast genera). Only one strain (0.5%) was resistant to STZ out of 87.4% of susceptible strains (n=160). The percentage of susceptible strains was higher than those obtained with the other agents evaluated and the percentage of resistant strains was lower than for most of the other antifun-gals. The pattern of susceptibility of C. albicans to STZ, TCZ, ITZ and CLZ was similar and superior to the pattern of susceptibility of this species to MNZ, ECZ, FLZ, 5FC and KTZ. C. dubliniensis was more susceptible to STZ, MNZ, MNZ, FLZ, ITZ, CLZ than to TCZ, ECZ, 5FC, AMB or KTZ. Ten susceptible strains to STZ were resistant to FLZ and one strain was resistant to ITZ. The overall antifungal activity of STZ in vitro against a wide range of clinically important yeasts from vaginal and cutaneous samples indicates the therapeutic potential of this agent for the treatment of infections caused by these fungi. However, the activity of STZ and the clinical value of in vitro data need to be verified in human clinical trials.

Sertaconazole in the treatment of mycoses: from dermatology to gynecology

Sertaconazole is a pharmaceutical product in the form of a cream, gel, powder and solution for dermatological use and vaginal cream, tablets and ovules for gynecological use. It is marketed in 24 countries and registered in a further 22. The active ingredient is 2% sertaconazole nitrate. Sertaconazole nitrate is an azole antifungal agent, with notable antifungal activity. Its molecule has a highly lipophilic fragment. This is a review of the efficacy and safety of all pharmaceutical forms of sertaconazole in order to provide data on vaginal sertaconazole for marketing purposes.

Determination of sertaconazole nitrate, a new imidazole antifungal, by high-performance liquid chromatography.

A high-performance liquid chromatographic method is developed for the determination of bulk sertaconazole nitrate and related compounds (potential impurities and degradation products) as well as a sertaconazole nitrate cream formulation. A 10-microns Spherisorb CN column is used along with a mobile phase consisting of acetonitrile and aqueous 0.01 M sodium phosphate (37:63, v/v). The sertaconazole nitrate peak is monitored at a wavelength of 260 nm; the retention time being 19.3 min. The detector response for sertaconazole nitrate is linear over the concentration range from 64 to 96 micrograms ml-1. The method is found to be sufficiently selective for the reliable determination of related compounds, FI-7001, FI-7009 and FI-7011, as indicated by same-day and between-day relative standard deviations (RSD) for replicate assays of 1.72% (n = 9) and 2.17% (n = 24), respectively. The application of this method to a cream formulation of sertaconazole nitrate is found to give a mean percentage recovery of 99.4% with RSD of 1.14% (n = 9); none of the cream vehicle peaks are found to interfere with the determination of sertaconazole nitrate.