Desolvation Energy: The Major Determinate of Absorption in a Model Peptide Series
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Authors
Karls, Michael S.
Issue Date
1990
Type
Thesis
Language
en_US
Keywords
Alternative Title
Abstract
The delivery of tetrapeptidic and higher oligopeptidic drugs is
problematic due to degradation of the peptides in the gastrointestinal
tract and low absorption through the intestinal mucosa.
To address the absorption problem, these studies utilized two series
of digestion-resistant peptides to determine whether molecular
weight, lipophilicity, or the number of theoretical hydrogen bonding
sites most influenced absorption. In previous in vitro human colon
adenocarcinomona cell and in situ rabbit perfusion model system
studies, absorption of these peptides was found to be most
influenced by the number of hydrogen bonding sites. This paper
describes in vivo rat studies which were undertaken to supplement
these earlier studies. The results support the earlier findings that
the predominant factor influencing absorption for these peptides is
the number of theoretical hydrogen bonding sites, the major
determinant of desolvation energy. Molecular weight also plays a
secondary role in the this absorption.
Description
vii, 35 p.
Citation
Publisher
Kalamazoo College
License
U.S. copyright laws protect this material. Commercial use or distribution of this material is not permitted without prior written permission of the copyright holder.