Ofloxacin/beta-cyclodextrin complexation

Citation
Ls. Koester et al., Ofloxacin/beta-cyclodextrin complexation, DRUG DEV IN, 27(6), 2001, pp. 533-540
Citations number
17
Categorie Soggetti
Pharmacology & Toxicology
Journal title
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
ISSN journal
03639045 → ACNP
Volume
27
Issue
6
Year of publication
2001
Pages
533 - 540
Database
ISI
SICI code
0363-9045(2001)27:6<533:OC>2.0.ZU;2-7
Abstract
ofloxacin (OFX) is a fluorquinolone characterized by photochemical instabil ity. With the goal to improve its photostability in aqueous solutions, the complexation of ofloxacin with beta -cyclodextrin was investigated. The com plexes showed a water solubility enhancement of approximately 2.6 times; ne vertheless, the photodegradation of ofloxacin was not reduced. The complexe s obtained were characterized by thermal and H-1 nuclear magnetic resonance (NMR) analysis, which revealed an interaction between ofloxacin and beta - cyclodextrin. The last analysis indicated that only partial inclusion of th e N-methylpiperazinyl moiety occurred, which can explain the fact that phot ostabilization was not improved. This partial inclusion phenomenon could be explained also by computer-aided molecular modeling.