2016, №3

сс. 71-86

Micronization of Moxifloxacin by Supercritical Antisolvent Precipitation

2016, №3

сс. 71-86

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E.V. Kudryashova, K.V. Sukhoverkov, I.M. Deygen, A.M. Vorobei, O.I. Pokrovskiy, O.O. Parenago, D.E. Presnov, A.M. Egorov

Key words: moxifloxacin, SCF-micronization, supercritical antisolvent preci pitation (SAS), FTIR, circular dichroism spectroscopy, rate of dissolution

For the development of new dosage forms of moxifloxacin (MF) (antibacterial
medication of fluoroquinolons group) Supercritical Antisolvent Preci pitation method
(SAS) is applied. SAS provides with the formation of particles of sizes ranged from
0.6 to 8 microns and of various morphologies (from thin polygonal plates to oblong
parallelepi peds). Studies of micronized samples using FTIR and circular dichroism
spectroscopies showed that micronization does not cause any changes in chemical
structure of MF or its racemization. Micronization of MF has a significant effect on
the rate of its dissolution in physiological solution at рН = 7.5: the dissolution rate of
micronized MF is 20—30% higher compared to the original MF; it is determined by
the sample particle size, morphology and degree of crystallinity/amorphousness. The
obtained data will be used to develop new formulations of MF for the treatment of
drug-resistant forms of tuberculosis.

doi:10.1134/S1990793117070120