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Updated: Feb 6, 2026
11:11
Canine Intestinal Organoids in a Dual-Chamber Permeable Support System
Published on: March 2, 2022
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pH-permeability profiles for drug substances: Experimental detection, comparison with human intestinal absorption and
1Institute of Chemistry, University of Tartu, Ravila 14A, Tartu 50411, Estonia.
Summary
pH significantly impacts human intestinal drug absorption. This study developed quantitative structure-activity relationships (QSARs) to predict pH-dependent drug permeability, improving early drug discovery models.
Area of Science:
- Pharmacokinetics
- Computational Chemistry
- Drug Discovery
Background:
- Intestinal absorption prediction often overlooks pH effects.
- Accurate modeling is crucial for drug candidate selection.
Purpose of the Study:
- To investigate the influence of pH on drug intestinal absorption.
- To develop predictive quantitative structure-activity relationships (QSARs) for pH-dependent permeability.
Main Methods:
- Parallel Artificial Membrane Permeability Assay (PAMPA) at various pH values (3, 5, 7.4, 9).
- Development and validation of regression and classification QSAR models.
- Analysis of molecular descriptors for mechanistic insights.
Main Results:
- Experimental data confirmed pH significantly affects intestinal absorption efficiency.
- Developed QSAR models accurately predicted pH-permeability profiles.
- Models showed good agreement with experimental and external validation data.
Conclusions:
- pH-dependent permeability is critical for accurate drug absorption prediction.
- Developed QSAR models enhance early-stage drug discovery by predicting intestinal absorption.
- Validated models are available in the QsarDB repository for broader use.
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