1999 Volume 14 Issue supplement Pages 122-123
It has been reported that orally active cephalosporin antibiotics are absorbed from the small intestine via the oligopeptide transporter (PepTl). In the present study, methods have been established to predict oral absorption of cephalosporins using the in vitro data obtained with rat intestinal brush border membrane vesicles (BBMV) or Caco-2 cells. Uptake into BBMV or Caco-2 cells via PepTl was estimated by subtracting the uptake at 4°C from that at 25 or 37°C, which was well correlated with the extent of oral absorption (F) according to the intestinal absorption model reported by Amidon at al. The present method gave fairly good prediction of oral absorption of cephalosporins (Tablel, Figs. 1 and 2).
