Use of Cannulated Everted Intestinal Sac for Serial Sampling as a Drug Absorbability (Permeability) Screen

Pharmacokinetic Profiles of Clonazepam in Dog and Humans and of Flunitrazepam in Dog

“…The permeability characteristics of clonazepam across the everted rat intestinal sac are consistent with good absorbability (16). The pKa of 1.5 corresponds to the removal of the proton of the protonated nitrogen in the 4-position of the molecule, and the pKa of 10.5 corresponds to the deprotonation of the nitrogen in the 1-position.…”

“…The permeability of the drug across the lumen of the everted rat intestinal sac (16) was consistent with good absorbability. The aqueous solubility decreases with an increase in pH, being 850 pg/ml at pH 1 and 11 pg/ml at pH 5.3.…”

Modeling of Intestinal Drug Absorption: Roles of Transporters and Metabolic Enzymes (For the Gillette Review Series)

“…Gene expression systems (Smit et al, 1998b;Cvetkovic et al, 1999;Gotoh et al, 2000;Shitara et al, 2002) provide direct information on the involvement of individual transporters or enzymes. Then there are the intestinal membrane segments/preparations (Wilson and Treanor, 1975;Hopfer et al, 1976;Lasker and Rickert, 1978;Johnson et al, 2001), cells (Koster and Noordhoek, 1983;Traber et al, 1991), everted sacs (Munck, 1965;Barr and Riegelman, 1970;Kaplan and Cotler, 1972), and the Ussing chamber (Fiddian-Green and Silen, 1975;Rogers et al, 1987;Lampen et al, 1995). For flux measurements, a donor compartment is used for drug administration and a receiving compartment is used for sampling.…”

Organ‐on‐a‐Chip Technology for Reproducing Multiorgan Physiology

“…For example, the intestinal membrane segments/preparation can be used to study the transport and metabolism of drugs . Cannulated everted sacs have been used to measure the absorption permeability of drugs . The Ussing chamber can be used to study the transport of molecules across the intestinal membrane, which separates the chamber into a donor and acceptor compartments .…”