Сверхкритические флюиды. Теория и практика
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2015, N4, pp. 52-66

E.V. Kudryashova, I.M. Deygen, K.V. Sukhoverkov, L.Yu. Filatova, N.L. Klyahcko, A.M. Vorobei, O.I. Pokrovskiy, K.B. Ustinovich, O.O. Parenago, E.N. Antonov, A.G. Dunaev, L.I. Krotova, V.K. Popov, А.М. Egorov

Micronization of Levofloxacin by Supercritical Antisolvent Precipitation

Micronization of levofloxacin (LF) — antibacterial drug of fluoroquinolons group — using Supercritical Antisolvent Preci pitation method (SAS) is studied. Depending on the type of solvent used in the SAS process, particles of different size (1-10 microns) and morphology (from thin plates to elongated parallelepipeds) can be obtained. Characterization of micronized LF forms by FTIR, Raman and circular dichroism spectroscopies showed that micronization doesn’t cause any changes in chemical structure of LF or its racemization. Micronization has a significant effect on the rate of LF dissolution in model media, which depends on the type of the solvent used in the SAS process. At pH = 4, the LF samples micronized using chlorohydrocarbons exhibit the highest dissolution rate. At pH = 7.5 the dissolution rate of micronized LF samples is 15-30 % higher compared to the original one, that can be associated with the degree of crystallinity / amorphousness, as well as with the morphology of microparticles formed during the SAS micronization.

Key words: levofloxacin, SCF-micronization, supercritical antisolvent preci pitation (SAS), FTIR and Raman spectroscopy, CD spectroscopy, solubility

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