Email this article Micronization of levofloxacin by supercritical antisolvent precipitation
- Authors: Kudryashova E.V.1, Popov V.K.2, Krotova L.I.2, Dunaev A.G.2, Antonov E.N.2, Parenago O.O.1,3, Ustinovich K.B.1,3, Pokrovskiy O.I.3, Vorobei A.M.1,3, Klyachko N.L.1, Filatova L.Y.1, Sukhoverkov K.V.1, Deygen I.M.1, Egorov A.M.1,4
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Affiliations:
- Department of Chemistry
- Institute of Laser and Information Technologies
- Kurnakov Institute of General and Inorganic Chemistry
- Russian Medical Academy of Postgraduate Education
- Issue: Vol 10, No 8 (2016)
- Pages: 1201-1210
- Section: Article
- URL: https://journal-vniispk.ru/1990-7931/article/view/198730
- DOI: https://doi.org/10.1134/S1990793116080054
- ID: 198730
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Abstract
The process of micronization of levofloxacin (LF, an antibacterial agent of the fluoroquinolone group) by the supercritical antisolvent precipitation technique (SAS) was investigated. It was shown that LF particles of different sizes (from 1 to 10 μm) and of various morphologies (from thin plates to elongated parallelepipeds) can be produced depending on the type of solvent used for conducting micronization. Investigation of the micronized LF preparations using the methods of IR-Fourier spectroscopy, Raman scattering, and circular dichroism showed that the LF micronization caused neither changes in its chemical structure nor racemization. Micronization of LF significantly affects the rate of its dissolution in model systems exhibiting effects dependent on the type of the solvent used for micronization. For example, the highest rate of dissolution at pH 4 was observed for LF preparations micronized with the help of chlorohydrocarbons. It was shown that the rate of dissolution of all micronized LF preparations was higher by 15–30% in comparison with the initial LF, which likely was related to the changes in the degree of crystallinity/amorphousness, as well as of morphologies of microparticles formed in the SAS process.
About the authors
E. V. Kudryashova
Department of Chemistry
Author for correspondence.
Email: Helena_Koudriachova@hotmail.com
Russian Federation, Moscow
V. K. Popov
Institute of Laser and Information Technologies
Email: Helena_Koudriachova@hotmail.com
Russian Federation, Troitsk, Moscow
L. I. Krotova
Institute of Laser and Information Technologies
Email: Helena_Koudriachova@hotmail.com
Russian Federation, Troitsk, Moscow
A. G. Dunaev
Institute of Laser and Information Technologies
Email: Helena_Koudriachova@hotmail.com
Russian Federation, Troitsk, Moscow
E. N. Antonov
Institute of Laser and Information Technologies
Email: Helena_Koudriachova@hotmail.com
Russian Federation, Troitsk, Moscow
O. O. Parenago
Department of Chemistry; Kurnakov Institute of General and Inorganic Chemistry
Email: Helena_Koudriachova@hotmail.com
Russian Federation, Moscow; Moscow
K. B. Ustinovich
Department of Chemistry; Kurnakov Institute of General and Inorganic Chemistry
Email: Helena_Koudriachova@hotmail.com
Russian Federation, Moscow; Moscow
O. I. Pokrovskiy
Kurnakov Institute of General and Inorganic Chemistry
Email: Helena_Koudriachova@hotmail.com
Russian Federation, Moscow
A. M. Vorobei
Department of Chemistry; Kurnakov Institute of General and Inorganic Chemistry
Email: Helena_Koudriachova@hotmail.com
Russian Federation, Moscow; Moscow
N. L. Klyachko
Department of Chemistry
Email: Helena_Koudriachova@hotmail.com
Russian Federation, Moscow
L. Yu. Filatova
Department of Chemistry
Email: Helena_Koudriachova@hotmail.com
Russian Federation, Moscow
K. V. Sukhoverkov
Department of Chemistry
Email: Helena_Koudriachova@hotmail.com
Russian Federation, Moscow
I. M. Deygen
Department of Chemistry
Email: Helena_Koudriachova@hotmail.com
Russian Federation, Moscow
A. M. Egorov
Department of Chemistry; Russian Medical Academy of Postgraduate Education
Email: Helena_Koudriachova@hotmail.com
Russian Federation, Moscow; Moscow
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