title: Predicting the human jejunal permeability and fraction absorbed of fluoroquinolones based on a biophysical model.
abstract: The purpose of this study is to predict human jejunal permeability (P(eff)) and fraction absorbed in human (%F(a)) for a group of antibacterial fluoroquinolones (FQs), by using a biophysical model based on measured Caco-2 permeability. The predicted P(eff) (in 10(-4) cm · s(-1) units) ranged from 0.7 (norfloxacin) to 4.5 (pefloxacin). The calculated %F(a) for norfloxacin = 51% (lit. 35%) and for ciprofloxacin = 76% (lit. 81%). Most of the FQs showed calculated %F(a)>90%, and are expected to be well-absorbed. Estimates of P(eff) can be predicted by the biophysical model. From these values, the human absorption may be calculated. Where absorption comparisons were possible, the agreement was acceptably good.
authors.affiliation: Faculty of Health Sciences, University of Macau, Macau, China.
authors.forename: Chenyin
authors.initials: C
authors.lastname: Wang
authors.affiliation: ADME Research, 1732 First Avenue, #102, New York, NY 10128, USA.
authors.forename: Alex
authors.initials: A
authors.lastname: Avdeef
authors.affiliation: Faculty of Health Sciences, University of Macau, Macau, China.
authors.forename: Wen
authors.initials: W
authors.lastname: Zhang
authors.affiliation: Faculty of Health Sciences, University of Macau, Macau, China.
authors.forename: Kin Y
authors.initials: KY
authors.lastname: Tam
mesh_terms: D000900:Anti-Bacterial Agents / Q000493:pharmacokinetics*; D001682:Biological Availability; D018938:Caco-2 Cells; D003198:Computer Simulation; D024841:Fluoroquinolones / Q000493:pharmacokinetics*; D006801:Humans; D007408:Intestinal Absorption / Q000502:physiology*; D008657:Metabolic Clearance Rate; D008954:Models, Biological; D010539:Permeability
chemical_list: D000900:Anti-Bacterial Agents; D024841:Fluoroquinolones
keywords: Caco-2; fluoroquinolones; fraction absorbed; human intestine; permeability