Development of antifungal gel, composition and technology based on pomiferin metabolite isolated from fruits of Maclura aurantiaca growing in Kazakhstan

Abstract

The aim. The purpose of this study is to develop the optimal composition and rational gel technology under the conventional name "Kaz-P7" based on the antifungal pomiferin.
 Materials and methods. The object of the study is the substance pomiferin.
 Based on the physicochemical properties of the gel (poorly soluble in water) and technological properties structurant - Carbopol Ultrez 20 (swelling) chosen optimal solvent system: DMSO-PG-water (1:4:1) corresponding to the maximum solubility of drug and polymer provides swelling.
 Following the requirements of GF RK I, vol. 1, 2.2.8, 2.2.10 was determined by rotational viscometric method. Rheological properties of the sample are determined using rotational viscometer "Rheolab QC" (firm "Anton Paar", Austria) with coaxial cylinders CC27/S-SN29766 determined. The rheological parameters were studied at a temperature of 20 °C – 35 °C using the MLM U15c thermostat included in the rheostat.
 Results. Gel dosage forms provide better bioavailability of the drug substance. In addition, gels are a more modern dosage form, pleasant in terms of organoleptic characteristics.
 The technology of gel manufacturing consists of two parallel processes: preparation of the drug substance solution and its introduction into the base. From the point of view of biopharmacy, which studies the biological effect of drugs depending on their physical properties, dosage form and preparation technology, the greatest release of the drug substance occurs when it is introduced into the dosage form in dissolved form.
 Pomiferin administered in the dissolved state has the most therapeutic effect on the gel base. At the same time, active pharmaceutical ingredients (APIs) were dissolved in different solvents with gradual heating. The ratio of solvents DMSO-PG-water (1:4:1) at which the developed dosage form will be more structured, stable, and thixotropic gel is established.
 Conclusions. Fungal skin diseases are among the most frequently discussed problems in the literature. The relevance of this topic is determined by the high prevalence of pathogens, which account for 37-42 % of all skin diseases. It was experimentally established that for the complete neutralization of one gm of carbopol Ultraz 20 in the DMSO-PG-water solvent system (1:4:1), one gm of triethanolamine (pH 7.0) is consumed. The optimal diluent consisting of DMSO-PG- water in the ratio (1:4:1) was selected by physico-chemical analysis methods, and one gm of triethanolamine (pH 7.0) was selected as the neutralizing agent. The following composition was chosen as the optimal gel model: API-3.0, DMSO-3.0, PG-50.0, Carbopol Ultrez 20-1.0, and Triethanolamine-1.0. The optimal composition and technology of the gel codenamed "Kaz-P7" based on the substance obtained by pomiferin was developed