Dose dependency in the gastrointestinal absorption of cefatrizine: correlation between in vivo and in situ

Biological & Pharmaceutical Bulletin
K MatsudaJ Watanabe

Abstract

We evaluated the dose-dependent (saturable) gastrointestinal absorption of cefatrizine, an aminocephalosporin transported by peptide carriers, in rats by a physiological mechanism-based approach to clarify its absorption characteristics and to examine the in vitro (in situ)-in vivo correlation in intestinal transport. With an increase in oral dose (mumol/5 ml/kg) from 5 (low) to 50 (high), the intestinal absorption rate constant (ka), which was estimated by analysis of gastrointestinal disposition, decreased markedly, from 0.301 to 0.056 min-1. This decrease was ascribable to the saturability of intestinal membrane transport, of which the concentration dependency in the perfused intestine was similar in extent to the dose dependency in ka. However, the apparent absorption rate constant (ka'), which was estimated by analysis of plasma concentrations after oral administration, decreased only modestly from 0.037 to 0.023 min-1. This was associated with the result that, at the low dose, ka' was far smaller than ka and comparable with k(g) (gastric emptying rate constant), suggesting gastric emptying-limited absorption. At the high dose, where intestinal cefatrizine absorption was less efficient, ka' was closer to ka than k(g). It w...Continue Reading

Citations

Mar 22, 2005·International Journal of Pharmaceutics·Kouki ObataYosinori Aso
Feb 24, 2001·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·N NishimuraK Iwamoto
Feb 1, 2005·Drug Metabolism and Pharmacokinetics·Takahiro IwaoJun Watanabe

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