Surface Activity Profiling (SAP): A potential means of predicting intestinal membrane permeability

[Display omitted] Early characterization of new drug substances intended for oral application includes not only physicochemical properties and stability but also the ability of the substance to permeate through the intestinal mucosa. In this work, a rapid screening method, surface activity profiling...

Full description

Saved in:
Bibliographic Details
Published in:European journal of pharmaceutics and biopharmaceutics 2019-09, Vol.142, p.291-299
Main Authors: Rosenberger, J., Schmid, K., Schäfer, K.J., Dressman, J.
Format: Article
Language:English
Subjects:
Oral drug absorption
PAMPA
Permeability
Surface activity analysis
Tensiometer
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:[Display omitted] Early characterization of new drug substances intended for oral application includes not only physicochemical properties and stability but also the ability of the substance to permeate through the intestinal mucosa. In this work, a rapid screening method, surface activity profiling (SAP), is proposed as an alternative to animal studies and screening in cell cultures. Measurements are made with a multichannel tensiometer and require only 50 µl of stock solution for the complete permeability analysis. Correlation of SAP results with human absorption was demonstrated for marketed drugs and with absorption in rats for development compounds of Boehringer Ingelheim. Cross-laboratory results for marketed drugs showed excellent agreement. For early stage investigations of lead compounds, where only small amounts of the compound are available, the SAP method appears to be an effective and fast tool to accurately predict fa, provided the compound is amphiphilic.
ISSN:0939-6411
1873-3441
DOI:10.1016/j.ejpb.2019.06.024