Protonation equilibrium and lipophilicity of moxifloxacin

This study was performed to characterise the protonation equilibrium at the molecular level and pH-dependent lipophilicity of moxifloxacin. After determining macro- and micro-constants, distribution features of four microspecies in aqueous phase were assessed. The apparent partition coefficient vers...

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Bibliographic Details
Published in:Journal of pharmaceutical and biomedical analysis 2005-02, Vol.37 (2), p.389-393
Main Authors: Langlois, Marie-Hélène, Montagut, Martine, Dubost, Jean-Pierre, Grellet, Jean, Saux, Marie-Claude
Format: Article
Language:English
Subjects:
1-Octanol
Analysis
Analytical, structural and metabolic biochemistry
Aza Compounds - chemistry
Biological and medical sciences
Buffers
Fluoroquinolones
Fundamental and applied biological sciences. Psychology
General pharmacology
Hydrogen-Ion Concentration
Lipids - chemistry
Macroconstants
Medical sciences
Microconstants
Models, Chemical
Moxifloxacin
Octanol/buffer partition coefficients
Pharmacology. Drug treatments
Protons
Quinolines - chemistry
Solutions
Spectrophotometry, Ultraviolet
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Summary:This study was performed to characterise the protonation equilibrium at the molecular level and pH-dependent lipophilicity of moxifloxacin. After determining macro- and micro-constants, distribution features of four microspecies in aqueous phase were assessed. The apparent partition coefficient versus pH profile of moxifloxacin showed a parabolic curve in n-octanol/buffer system which reached near pI. The true partition coefficient was calculated from the log P app and microconstants values.
ISSN:0731-7085
1873-264X
DOI:10.1016/j.jpba.2004.10.022