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Intestinal Absorption of (–)-Carbovir in the Rat

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Abstract

(–)-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.

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Authors and Affiliations

  1. Department of Pharmaceutics, University of Minnesota, Minneapolis, Minnesota, 55455

    Inmaculada Soria & Cheryl L. Zimmerman

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  1. Inmaculada Soria
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  2. Cheryl L. Zimmerman
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Soria, I., Zimmerman, C.L. Intestinal Absorption of (–)-Carbovir in the Rat. Pharm Res 11, 267–271 (1994). https://doi.org/10.1023/A:1018911609410

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