Development of an Experimental Dosage Form for Topical Use With Antifungal Action

Abstract

Currently, mycoses are one of the urgent health problems. According to WHO, up to 1/3 of the world's population suffers from fungal pathologies. Currently, fungal infections are becoming increasingly difficult to treat, which is associated both with the identification of new species of fungi that were previously considered non-pathogenic, and with the development of resistance of pathogens to available medicines. The problem of mycoses is becoming more urgent due to the variety of pathways of transmission of pathogens and their high resistance in the external environment, changes in the immune response of the human body. Therefore, it is so important to expand the range and constantly improve the compositions and forms of antifungal agents. The substance of the silver salt pyrazole-3-carboxamide (SSP) synthesized in PGFA showed antifungal activity, which allowed it to be included in the experimental mild dosage form. The purpose of this study is to develop an experimental mild dosage form based on the silver salt of pyrazole–3-carboxamide for topical use in candidiasis dermatomycosis and to evaluate its antifungal activity. Materials and methods. The pharmacologically active component is the pharmaceutical substance of the silver salt N-{4-[(1,3-thiazole-2-yl)sulfamoyl]phenyl}-1-phenyl-5-(4-ethoxyphenyl)pyrazole-3-carboxamide. The antifungal activity of the compound was studied by double serial dilutions in a liquid nutrient medium in relation to reference strains of fungi of the genus Candida: Candida albicans NCTC 885-653, Candida krusei RCPGU-1472/310, Candida glabrata RCPGU-1485/47. To determine the antifungal activity of an experimental mild dosage form in relation to a typical strain of fungi of the genus Candida, a three-nesting variant of the agar diffusion method was used. Statistical processing of the results of chemical studies was carried out according to generally accepted methods using standard EXCEL computer programs. Results and discussion. As a result of the conducted research, the composition of an experimental mild dosage form based on the silver salt of pyrazole-3-carboxamide has been substantiated and developed. A technology for the manufacture of ointment has been developed to ensure the quality of the dosage form, its therapeutic activity and stability. Conclusion. Based on technological and microbiological studies, an experimental mild dosage form based on the silver salt of pyrazole-3-carboxamide has been developed with the aim of further introduction into medical practice for the local treatment of dermatomycosis after appropriate studies.