Related Experiment Video
Updated: May 17, 2026

Electric Cell-Substrate Sensing for Real-Time Evaluation of Metal-Organic Framework Toxicological Profiles
Published on: May 26, 2023
Amorphous solid dispersion successfully improved oral exposure of ADX71943 in support of toxicology studies
Mohamad H Ayad1, Beatrice Bonnet, Jacques Quinton
1Addex Pharmaceuticals, Plan-les-Ouates, Switzerland. haithamayad@hotmail.com
Abstract:
ADX71943 is a potent and selective GABA(b) receptor positive allosteric modulator (PAM) which exhibits poor aqueous solubility at all physiologically relevant pHs. The aim of this study was to identify an adequate formulation to improve the solubility of ADX71943 to achieve a sufficiently high plasma exposure after oral administration to support the toxicology program. Considering the overall physicochemical properties and the low solubility of ADX71943 in a variety of solvents, solid dispersion, and particle size reduction have been successfully chosen as potential strategies to improve its oral bioavailability. Both technologies have proven useful in improving the in vitro dissolution profile and as a result of the solubility enhancement, higher bioavailability was obtained in vivo. As the solid dispersion gave better bioavailability (30-fold compared with the neat active pharmaceutical ingredient (API)), this formulation was selected for the toxicology study. Changing the crystalline form of ADX71943 into amorphous state by preparing a solid dispersion has greatly improved its oral bioavailability and has allowed achieving the required plasma concentration needed in toxicology studies.
Related Concept Videos
Drug Delivery Systems: Different Types
Toxicity Testing in Animals
Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence
Oral Drug Delivery Systems: Introduction
Bioavailability Enhancement: Drug Stability Enhancement and GI Retention
Dosage Regimen: Multiple Oral Dosage
