TY - JOUR
T1 - Intestinal Absorption of (–)-Carbovir in the Rat
AU - Soria, Inmaculada
AU - Zimmerman, Cheryl L.
PY - 1994/2
Y1 - 1994/2
N2 - (–)-Carbovir (CBV) is a carbocyclic nucleoside analogue with in vitro activity against the human immunodeficiency virus. The sites and mechanism of absorption of (–)-CBV from the rat small intestine were studied in the anesthetized male Sprague–Dawley rat. (–)-CBV was perfused through either duodenal, jejunal, or ileal segments at three concentration levels ranging from 1 to 500 µg/mL. The fraction remaining to be absorbed at steady-state and the absorptive clearance were calculated for each experiment. The effect of solvent drag on the absorptive clearance was also investigated. Two-way ANOVA for the absorptive clearance per unit length was not significant for either (–)-CBV concentration or site of perfusion. The fraction remaining to be absorbed at steady-state was found to be 0.804 ± 0.091 (n = 30). A strong correlation was found between the absorptive clearance and the net water absorptive flux. The mechanism of (–)-CBV absorption across the rat small intestine apparently consists of both passive diffusion and convection.
AB - (–)-Carbovir (CBV) is a carbocyclic nucleoside analogue with in vitro activity against the human immunodeficiency virus. The sites and mechanism of absorption of (–)-CBV from the rat small intestine were studied in the anesthetized male Sprague–Dawley rat. (–)-CBV was perfused through either duodenal, jejunal, or ileal segments at three concentration levels ranging from 1 to 500 µg/mL. The fraction remaining to be absorbed at steady-state and the absorptive clearance were calculated for each experiment. The effect of solvent drag on the absorptive clearance was also investigated. Two-way ANOVA for the absorptive clearance per unit length was not significant for either (–)-CBV concentration or site of perfusion. The fraction remaining to be absorbed at steady-state was found to be 0.804 ± 0.091 (n = 30). A strong correlation was found between the absorptive clearance and the net water absorptive flux. The mechanism of (–)-CBV absorption across the rat small intestine apparently consists of both passive diffusion and convection.
KW - (–)-carbovir
KW - absorptive clearance
KW - intestinal absorption
KW - solvent drag
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U2 - 10.1023/A:1018911609410
DO - 10.1023/A:1018911609410
M3 - Article
C2 - 8165186
AN - SCOPUS:0028350163
SN - 0724-8741
VL - 11
SP - 267
EP - 271
JO - Pharmaceutical Research: An Official Journal of the American Association of Pharmaceutical Scientists
JF - Pharmaceutical Research: An Official Journal of the American Association of Pharmaceutical Scientists
IS - 2
ER -
