caa a22 4500 477128505 CHVBK 20180405111657.0 cr unu---uuuuu 170330e19971101xx s 000 0 eng 10.1023/A:1012134503107 doi (NATIONALLICENCE)springer-10.1023/A:1012134503107 Influence of Dosage Form on the Gastroenteropathy of Flurbiprofen in the Rat: Evidence of Shift in the Toxicity Site [Elektronische Daten] [Neal Davies, Fakhreddin Jamali] Purpose. Gastroduodenal and intestinal permeability were compared after single doses of sustained release and regular release flurbiprofen in the rat to assess possible site-specific formulation-dependent toxicity. Methods. Pharmacokinetics was assessed and gastrointestinal permeability was evaluated using sucrose and 51Cr-EDTA as gastroduodenal and intestinal permeability probes, respectively. Results. The two formulations demonstrated equal areas under the flurbiprofen concentration-time curve. The sustained release formulation peaked 2−3 h slower with 57−74% lower concentrations than regular release formulation. In comparison, the regular release powder induced greater gastroduodenal permeability while sustained release granules induced greater intestinal permeability. When S-flurbiprofen concentrations were plotted versus intestinal permeability, a linear relationship and an anti-clockwise hysteresis were obtained for regular and sustained release formulations, respectively. Conclusions. Sustained release formulations of flurbiprofen demonstrate reduced gastroduodenal permeability but shift the site of this side-effect to the more distal intestine. Plenum Publishing Corporation, 1997 non-steroidal antiinflammatory drugs nationallicence gastroduodenal nationallicence intestinal permeability nationallicence flurbiprofen nationallicence Davies Neal Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, T6G 2N8, Edmonton, Alberta, Canada aut Jamali Fakhreddin Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, T6G 2N8, Edmonton, Alberta, Canada aut Pharmaceutical Research Kluwer Academic Publishers-Plenum Publishers 14/11(1997-11-01), 1597-1600 0724-8741 14:11<1597 1997 14 11095 https://doi.org/10.1023/A:1012134503107 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1023/A:1012134503107 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Davies Neal Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, T6G 2N8, Edmonton, Alberta, Canada aut NATIONALLICENCE 700 1- Jamali Fakhreddin Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, T6G 2N8, Edmonton, Alberta, Canada aut NATIONALLICENCE 773 0- Pharmaceutical Research Kluwer Academic Publishers-Plenum Publishers 14/11(1997-11-01), 1597-1600 0724-8741 14:11<1597 1997 14 11095 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer