Development of Effervescent Granules with Solid Dispersion of Furazolidone

Introduction.In the treatment of infectious and inflammatory diseases, active substances (AI) are in demand, characterized by low resistance of microorganisms, high specificity of the mechanism of action and a wide spectrum of antimicrobial activity. Furazolidone (FZ) is an active substance that meets these criteria, but the fact that it is practically insoluble in water significantly limits its use. To increase the solubility and dissolution rate of active substances with low solubility in water, the method of solid dispersions (SD) allows. Previous studies indicate an increase in the solubility and dissolution rate of FZ in water from TD with polyvinylpyrrolidone-24000 (PVP-24000) in a ratio with AI > 6: 1 by weight. As a result, it becomes possible to introduce TD FZ into the composition of instant effervescent dosage forms, for example, Target. Development of the composition and technology for obtaining effervescent granules based on solid dispersions of FZ for obtaining a solution for external use. Materials and methods. FZ substance, polyvinylpyrrolidone-24000 ± 2000 (PVP-24000 ± 2000), tartaric acid, malic acid, anhydrous sodium carbonate, ethyl alcohol 96%, purified water. The granulates were obtained by fluidized bed granulation. The analysis of the obtained granules was carried out according to the following indicators: Description, granule size, weight loss upon drying, disintegration, dosing uniformity according to GPM.1.4.1.0004.15 "Granules". Also carried out a qualitative and quantitative determination of DI, analyzed the pH of an aqueous solution of granules. In order to study the stability and shelf life, the samples of granules were stored in accordance with OFS.1.10009.15 "Stability and shelf life of medicines".Results and discussion. The composition and technology of FZ effervescent granules for obtaining a solution for external use have been developed. The granules were obtained by separate granulation of the main (containing TD DV) and acidic components, followed by mixing in proportions that provide a solution of FZ with a concentration of 0.004% in water at room temperature. The quality of the resulting compositions was assessed, the shelf life (2 years) and storage conditions (in a dry place protected from light at a temperature of 25 °C) of the developed granule compositions were determined. Conclusion. As a result of technological and chemical-pharmaceutical studies using the TD method, a new dosage form of FZ has been developed - effervescent granules, which makes it possible to obtain an aqueous solution with an AI concentration of 0.004% in less than 5 minutes without heating. Based on the results of the work, an application was filed with Rospatent No. 2021105988 dated March 10, 2021 "Instantly soluble dosage form of furazolidone and a method for its preparation.". © Elagina A. O., Beliatskaya A. V., Krasnyuk (Jr.) I. I., Krasnyuk I. I., Stepanova O. I., Vorob'yov A. N., Fateeva T. V., 2022.