Intestinal absorption of a series of 6-fluoquinolone derivatives: a comparative study.
The intestinal absorption rate constants of the five 6-fluoquinolones (norfloxacin, ciprofloxacin, pefloxacin, CNV 8802 and CNV 8804), have been estimated in the rat (n = 5) by means of an "in situ" intestinal perfusion method. Remaining 6-fluoquinol one concentrations in the perfusion liquid at fixed time (15, 30, 45, 60, 75, 90 and 120 minutes) were determined using a HPLC procedure with UV detection. Absorptions rate constants were estimated according to first order kinetics. A simple non-linear correlation between Ka and log K' on the one hand and a multiple linear correlation between Ka and the structural theoretical parameters: molar volume, dipolar moment and the charge associated to nitrogen 18 on the other, were performed. Only a correlation between Ka values as dependent variable versus dipolar moment and molecular volume values has been obtained, but this correlation is not statistically significant (p = 0.1808) and not accurate enough to have predictive value.
Escribano
E
E
Department of Pharmacy, University of Barcelona, Spain.
Freixas
J
J
Colom
H
H
Lauroba
J
J
Calpena
A C
AC
Domenech
J
J
D042462:4-Quinolones; D000818:Animals; D000890:Anti-Infective Agents / Q000493:pharmacokinetics*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002851:Chromatography, High Pressure Liquid; D005260:Female; D007408:Intestinal Absorption; D010477:Perfusion; D051381:Rats; D011919:Rats, Inbred Strains; D012044:Regression Analysis; D013056:Spectrophotometry, Ultraviolet
D042462:4-Quinolones; D000890:Anti-Infective Agents