Predicting the human jejunal permeability and fraction absorbed of fluoroquinolones based on a biophysical model

Biomed Mater Eng. 2014;24(6):3849-54. doi: 10.3233/BME-141215.

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.

Keywords: Caco-2; fluoroquinolones; fraction absorbed; human intestine; permeability.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / pharmacokinetics*
  • Biological Availability
  • Caco-2 Cells
  • Computer Simulation
  • Fluoroquinolones / pharmacokinetics*
  • Humans
  • Intestinal Absorption / physiology*
  • Metabolic Clearance Rate
  • Models, Biological*
  • Permeability

Substances

  • Anti-Bacterial Agents
  • Fluoroquinolones