Ofloxacin β-Cyclodextrin Complexation

Ofloxacin (OFX) is a fluorquinolone characterized by photochemical instability. With the goal to improve its photostability in aqueous solutions, the complexation of ofloxacin with β-cyclodextrin was investigated. The complexes showed a water solubility enhancement of approximately 2.6 times; nevert...

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Veröffentlicht in:Drug development and industrial pharmacy 2001-01, Vol.27 (6), p.533-540
Hauptverfasser: Koester, L. S., Guterres, S. S., Le Roch, M., Eifler-Lima, V. L., Zuanazzi, J. A., Bassani, V. L.
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Sprache:eng
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Zusammenfassung:Ofloxacin (OFX) is a fluorquinolone characterized by photochemical instability. With the goal to improve its photostability in aqueous solutions, the complexation of ofloxacin with β-cyclodextrin was investigated. The complexes showed a water solubility enhancement of approximately 2.6 times; nevertheless, the photodegradation of ofloxacin was not reduced. The complexes obtained were characterized by thermal and 1H nuclear magnetic resonance (NMR) analysis, which revealed an interaction between ofloxacin and β-cyclodextrin. The last analysis indicated that only partial inclusion of the N-methylpiperazinyl moiety occurred, which can explain the fact that photostabilization was not improved. This partial inclusion phenomenon could be explained also by computer-aided molecular modeling.
ISSN:0363-9045
1520-5762
DOI:10.1081/DDC-100105178