EFFECT OF SOLID DISPERSION METHOD ON THE SOLUBILITY OF NAPHTHIFIN HYDROCHLORIDE

Author:

Kosenkova S.I.1,Krasniuk (Jr.) I.I.1,Krasniuk I.I.1,Zubareva I.M.1,Belyatskaya А.V.1,Stepanova О.I.1

Affiliation:

1. I.M. Sechenov First Moscow State Medical University, Ministry of Health of the Russian Federation; 8 Trubetskaya St., Moscow, 119991, Russian Federation

Abstract

The wide-spread use of Naphthyphine hydrochloride is limited by its low solubility in water, which causes technological difficulties in the production of drugs based on it, and low bioavailability indicators. To increase solubility and increase the release of most active substances from a number of solid and soft dosage forms, the modern method of obtaining their solid dispersions can be used successfully. Objective. Study the effect of the solid dispersion method obtained using polyvinylpyrrolidone with a molar mass of 10000 g/mol (PVP-10000) on the solubility of Naphthyphine hydrochloride. Material and methods. A substance of Naphthyphine hydrochloride was used. PVP-10000 was used as a solid dispersion carrier. The solid dispersion of Nap hthyphinе hydrochloride with PVP-10000 was obtained with the help of the solvent removal method. Results. It has been found that the production of solid dispersions increases the solubility and the rate of dissolving of Naphthyphine hydrochloride. The solubility of Naphthyphine hydrochloride from solid dispersion is increased by 2.2 times compared to the original substance. The combination of physico-chemical analysis methods, such as UV spectroscopy and microcrystalloscopy, makes it highly likely to suggest that the observed increase in the solubility of Naphthyphine hydrochloride from the tested solid dispersions is due to the loss of the active substance's crystallinity and the transi-tion of the effective substance into the solid state in the PVP-10000 matrix, and is also due to solubilization under the action of the polymer, resulting in the formation of the colloidal solutions of Naphthythine hydochloride when dissolved in the water itself of the dispersion. Conclusion. Obtaining solid dispersions with PVP-10000 improves the water solubility of Naphthyphine hydrochloride. The authors plan to use the re-sults presented in the article in the further development of the composition and technology of rapidly soluble solid forms of Naphthypine hydrochloride tablets and granules, having accelerated (less than 5 minutes) the release of the active substance and increased bioavailability. This will help to ap-proach the treatment of fungal infections in a comprehensive way

Publisher

Russian Vrach, Publishing House Ltd.

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