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2017, N4, pp. 66-83

K.V. Sukhoverkov, I.M. Le-Deygen, .. Egorov, E.V. Kudryashova

Physico-chemical Properties of Moxifloxacin Inclusion Complex with Hydroxypropyl-β-cyclodextrin Synthesized by RESS Method

A new method to synthesize guesthost inclusion complex of moxifloxacin (MF) with 2-hydroxypropyl-β-cyclodextrin (HPCD) based on the supercritical fluid technologies in RESS (Rapid Expansion of Supercritical Solutions) regime was suggested for further development of new drug formulations with improved bioavailability. Using the RESS method, the MF-HPCD complex was obtained as 24 micron particles, which are optimal for both oral and inhalation forms of the drug based on MF. According to the scanning electron microscopy data, the morphology of MF-HPCD particles obtained via RESS processing is different from both initial components and from MF-HPCD complex obtained by lyophilization from aqueous solution. According to the X-ray diffraction data, the crystallinity of MF drops from 95 to 2030% upon the formation of the complex with HPCD. The IR spectroscopic and equilibrium dialysis data demonstrated that RESS provides higher efficiency of the drug substance inclusion in the complex with HPCD compared to traditional methods such as lyophilization or solid-phase components mixing.

Key words: moxifloxacin, 2-hydroxypropyl-β-cyclodextrin (HPCD), guesthost inclusion complex, supercritical fluids (SCF), Rapid Expansion of Supercritical Solutions (RESS), FTIR spectroscopy, drug release kinetics

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