The metabolic inhibition model which predicts the intestinal absorbability and Metabolizability of drug: Theory and experimentReport as inadecuate




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Biological Procedures Online

, Volume 1, Issue 1, pp 32–39

DOI: 10.1251-bpo8

Cite this article as: Mizuma, T. & Awazu, S. Biol Proced Online 1998 1: 32. doi:10.1251-bpo8

Abstract

The intestinal absorption of analgesic peptides leucine enkephalin and kyotorphin and modified peptides in rat were studied. Although these peptides were not absorbed, the absorbability absorption clearance of these peptides were increased in the presence of peptidase inhibitors. In order to kinetically analyze these phenomena, we proposed the metabolic inhibition model, which incorporated the metabolic clearance metabolizability with the absorption clearance. Metabolic activity was determined with intestinal homogenates. The higher the metabolic clearance was, the lower was the absorption clearance. The relationships between the absorption clearance and the metabolic clearance of the experimental data as well as of the theoretical values were hyperbolic. This model predicted the maximum absorption clearances of cellobiose-coupled leucine enkephalin 0.654 µl-min-cm and kyotorphin 0.247 µl-min-cm. Details of the experimental methods are described.

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Author: Takashi Mizuma - Shoji Awazu

Source: https://link.springer.com/







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