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A. A. Skuredina, T. Y. Kopnova, I. M. Le-Deygen, E. V. Kudryashova
Physico-chemical
properties of guest-host inclusion complexes of ciprofloxcin with β-cyclodextrin derivatives
Abstract
The effect of
the nature of the substituent in the β-cyclodextrin
derivative on the physicochemical properties of antibacterial drug
ciprofloxacin was investigated. It has been established that ciprofloxacin is
capable of forming "guest-host" inclusion complexes with β-cyclodextrin derivatives characterized by Kdis.
in the range of 10–3–10–4 M. The formation of the most
stable complex is observed for a ligand with a small polar uncharged
substituent, 2-hydroxypropyl, which also helps to increase the solubility of
ciprofloxacin up to 20 and 64% in buffer systems pH 4,0 and pH 7,4
respectively. It was found that the inclusion of ciprofloxacin in a complex
with Kdis. values of 10–3 M and lower leads to
slowdown of the release of the drug. The obtained physicochemical properties of
the complexes will contribute to the development of highly effective formulation
of the drug.
Key words: β-cyclodextrin, fluoroquinolones, inclusion complexes, IR
spectrocopy.
Copyright (C) Chemistry Dept., Moscow State University, 2002
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