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

Issue title: Frontiers in Biomedical Engineering and Biotechnology – Proceedings of the 3rd International Conference on Biomedical Engineering and Biotechnology, 25–28 September 2014, Beijing, China

Article type: Research Article

Authors: Wang, Chenyin | Avdeef, Alex | Zhang, Wen | Tam, Kin Y.;

Affiliations: Faculty of Health Sciences, University of Macau, Macau, China | ADME Research, 1732 First Avenue, #102, New York, NY 10128, USA

Note: [] Corresponding author: Kin Y. Tam, Faculty of Health Sciences, University of Macau, Macau, China. Tel.: +853 8822 4988; Fax: +853 8822 2314; E-mail: [email protected].

Keywords: permeability, fraction absorbed, fluoroquinolones, human intestine, Caco-2

DOI: 10.3233/BME-141215

Journal: Bio-Medical Materials and Engineering, vol. 24, no. 6, pp. 3849-3854, 2014

Published: 2014
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Abstract

The purpose of this study is to predict human jejunal permeability (Peff) and fraction absorbed in human (%Fa) for a group of antibacterial fluoroquinolones (FQs), by using a biophysical model based on measured Caco-2 permeability. The predicted Peff (in 10−4cm·s−1 units) ranged from 0.7 (norfloxacin) to 4.5 (pefloxacin). The calculated %Fa for norfloxacin = 51% (lit. 35%) and for ciprofloxacin = 76% (lit. 81%). Most of the FQs showed calculated %Fa>90%, and are expected to be well-absorbed. Estimates of Peff 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.

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