Ofloxacin/beta-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 beta-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 beta-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.
Koester
L S
LS
Curso de Pós-graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Porto Alegre, Brasil.
Guterres
S S
SS
Le Roch
M
M
Eifler-Lima
V L
VL
Zuanazzi
J A
JA
Bassani
V L
VL
D000890:Anti-Infective Agents / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D002851:Chromatography, High Pressure Liquid; D003196:Computer Graphics; D003505:Cyclodextrins / Q000737:chemistry*; D004355:Drug Stability; D007700:Kinetics; D008027:Light; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D015242:Ofloxacin / Q000737:chemistry*; D012995:Solubility; D014466:Ultraviolet Rays; D047392:beta-Cyclodextrins
D000890:Anti-Infective Agents; D003505:Cyclodextrins; D047392:beta-Cyclodextrins; D015242:Ofloxacin; C031215:betadex