Study of Antifungal Activity of Experimental Soft Dosage Form Based on the Hydrazone Derivative of Getarylamide 4-phenyl-2-hydroxy-4-oxo-2-butenoic acid

Abstract

Introduction. Recently, there has been a significant increase in fungal infections. The most common is vulvovaginal candidiasis, affecting millions of women worldwide. Resistance is formed to existing antifungal drugs, and they are not devoid of side effects. Previously, we have shown high antimicrobial activity of derivatives of 4-R-2-hydroxy-4-oxo-2-butenic acids. The creation of soft dosage forms based on them and the study of antifungal action is promising.Aim. To develop experimental soft dosage forms based on one of the most active derivatives of 4-R-2-hydroxy-4-oxo-2-butenic acids and to evaluate the effect of the ointment composition of the ointment composition on the severity of antifungal action.Materials and methods. As a pharmacologically active component, a hydrazone derivative of 4-phenyl-2-hydroxy-4-oxo-2-butenoic acid synthesized by us was used, which has pronounced antifungal activity. 8 experimental soft dosage forms based on hydrophobic and hydrophilic character have been developed. The active substance in a concentration of 1 % was introduced by standard technological methods according to the rules for the manufacture of dermatological ointments. To determine the antifungal activity of the ointments obtained, a three-nesting variant of the agar diffusion method was used. Comparison preparations are 2 % cream "Pimafucin" and 1 % cream "Clotrimazole".Results and discussion. All the studied experimental soft dosage forms showed antifungal effects of varying degrees of severity. The greatest pharmacological effect was found in ointment compositions based on hydrophilic components of sodium-carboxymethylcellulose and polyethylene oxides. Their antifungal effect is comparable or exceeds the effect of comparison drugs.Conclusion. 8 experimental soft dosage forms based on a derivative of 4-phenyl-2-hydroxy-4-oxo-2-butenic acid have been developed. Their antifungal activity has been studied. Two most active samples of experimental ointments were selected for further in-depth study.

Keywords

• derivatives of 4-r-2-hydroxy-4-oxo-2-butenic acids
• antifungal activity
• soft dosage form