Effects of various absorption enhancers on the intestinal absorption of water soluble drugs by in vitro Ussing chamber method: correlation with an in situ absorption experiment.
The effect of absorption enhancers on the small and large intestinal absorption of drug in rats was examined using an in vitro modified Ussing chamber method, and the results were compared with those from an in situ absorption experiment. Phenol red was chosen as a model drug, while the absorption enhancers used were sodium glycocholate (Na-GC), sodium taurocholate (Na-TC), sodium deoxycholate (Na-DC), EDTA, sodium salicylate (Na-Sal), sodium caprate (Na-Cap), diethyl maleate (DEM) and N-lauryl-beta-D-maltopyranoside (LM), all used at a concentration of 20 mM. This modified Ussing chamber method showed that Na-DC, EDTA and LM were the most effective absorption enhancers in the large intestine. A good correlation exists between the area under the curve (AUC) (in situ loop model) and the cumulative amount of phenol red absorbed (in vitro modified Ussing chamber method). These results indicated that the in vitro modified Ussing chamber method can be used to evaluate the effects of various absorption enhancers in the intestine.
Sugiyama
T
T
Department of Biopharmaceutics, Kyoto Pharmaceutical University, Japan.
Yamamoto
A
A
Kawabe
Y
Y
Uchiyama
T
T
Quan
Y S
YS
Muranishi
S
S
D000818:Animals; D019540:Area Under Curve; D004357:Drug Synergism; D007408:Intestinal Absorption / Q000187:drug effects*; D008297:Male; D010637:Phenolsulfonphthalein / Q000737:chemistry / Q000493:pharmacokinetics*; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility
D010637:Phenolsulfonphthalein