Effect of solid dispersion method on the solubility of naphthifin hydrochloride
- Authors: Kosenkova S.I.1, Krasniuk I.I.1, Krasniuk I.I.1, Zubareva I.M.1, Belyatskaya A.V.1, Stepanova O.I.1
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Affiliations:
- I. M. Sechenov First Moscow State Medical University, Ministry of Health of the Russian Federation
- Issue: Vol 27, No 9 (2024)
- Pages: 19-25
- Section: Pharmaceutical chemistry
- URL: https://journals.eco-vector.com/1560-9596/article/view/636211
- DOI: https://doi.org/10.29296/25877313-2024-09-03
- ID: 636211
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Abstract
Introduction. Naphthyphine hydrochloride is an antifungal and antibacterial drug; a representative of the chemical group of allylamins. The widespread 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 Naphthyphinе 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 transition 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 results 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 approach the treatment of fungal infections in a comprehensive way.
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About the authors
S. I. Kosenkova
I. M. Sechenov First Moscow State Medical University, Ministry of Health of the Russian Federation
Author for correspondence.
Email: sv-omega@yandex.ru
ORCID iD: 0000-0001-9337-5917
Ph. D. (Pharm.), Lecturer, Department of Pharmaceutical Technology, A. P. Nelyubin Institute of Pharmacy sv-omega@yandex.ru
Russian Federation, 8 Trubetskaya St., Moscow, 119991I. I. Krasniuk
I. M. Sechenov First Moscow State Medical University, Ministry of Health of the Russian Federation
Email: krasnyuk.79@mail.ru
ORCID iD: 0000-0001-8557-8829
Dr. Sc. (Pharm.), Professor, Head of Department of Analytical, Physical and Colloidal Chemistry, A. P. Nelyubin Institute of Pharmacy
Russian Federation, 8 Trubetskaya St., Moscow, 119991
I. I. Krasniuk
I. M. Sechenov First Moscow State Medical University, Ministry of Health of the Russian Federation
Email: krasnyuki@mail.ru
ORCID iD: 0000-0002-7242-2988
доктор фармацевтических наук, профессор, зав. кафедрой, фармацевтической технологии, Институт фармации имени А. П. Нелюбина
Russian Federation, 8 Trubetskaya St., Moscow, 119991I. M. Zubareva
I. M. Sechenov First Moscow State Medical University, Ministry of Health of the Russian Federation
Email: irina.kashlikova@mail.ru
ORCID iD: 0000-0002-0367-214X
Ph. D. (Pharm.), Associate Professor, Department of Pharmaceutical Technology, A. P. Nelyubin Institute of Pharmacy
Russian Federation, 8 Trubetskaya St., Moscow, 119991A. V. Belyatskaya
I. M. Sechenov First Moscow State Medical University, Ministry of Health of the Russian Federation
Email: av.beliatskaya@mail.ru
ORCID iD: 0000-0002-8214-4483
Ph. D. (Pharm.), Associate Professor, Department of Pharmaceutical Technology, A. P. Nelyubin Institute of Pharmacy
Russian Federation, 8 Trubetskaya St., Moscow, 119991O. I. Stepanova
I. M. Sechenov First Moscow State Medical University, Ministry of Health of the Russian Federation
Email: o.i.nikulina@mail.ru
ORCID iD: 0000-0002-9885-3727
Ph. D. (Pharm.), Associate Professor, Department of Pharmacology, A. P. Nelyubin Institute of Pharmacy
Russian Federation, 8 Trubetskaya St., Moscow, 119991References
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