Amorphous solid dispersions: Utilization and challenges in preclinical drug development within AstraZeneca

AB Anane-Adjei, E Jacobs, SC Nash, S Askin… - International Journal of …, 2022 - Elsevier
The poor aqueous solubility of many active pharmaceutical ingredients (APIs) dominates
much of the early drug development portfolio and poses a major challenge in …

Analytical and computational methods for the determination of drug-polymer solubility and miscibility

SD Thakore, J Akhtar, R Jain, A Paudel… - Molecular …, 2021 - ACS Publications
In the pharmaceutical industry, poorly water-soluble drugs require enabling technologies to
increase apparent solubility in the biological environment. Amorphous solid dispersion …

[HTML][HTML] Solvent influence on the phase behavior and glass transition of Amorphous Solid Dispersions

S Dohrn, C Luebbert, K Lehmkemper… - European Journal of …, 2021 - Elsevier
Understanding the long-term stability of amorphous solid dispersions (ASDs) is important for
their successful approval for market. ASD stability does not only depend on the interplay …

Parametrization of PC-SAFT EoS for solvents reviewed for use in pharmaceutical process design: VLE, LLE, VLLE, and SLE study

J Yousefi Seyf, M Asgari - Industrial & Engineering Chemistry …, 2022 - ACS Publications
The perturbed chain-statistical associating fluid theory equation of state (PC-SAFT EoS) is
one of the state-of-the-art thermodynamic models used in the phase equilibrium calculation …

[HTML][HTML] Thermodynamic modeling of the amorphous solid dispersion-water interfacial layer and its impact on the release mechanism

S Dohrn, SO Kyeremateng, E Bochmann, E Sobich… - Pharmaceutics, 2023 - mdpi.com
During the dissolution of amorphous solid dispersion (ASD) formulations, the gel layer that
forms at the ASD/water interface strongly dictates the release of the active pharmaceutical …

[HTML][HTML] Predicting process design spaces for spray drying amorphous solid dispersions

S Dohrn, P Rawal, C Luebbert, K Lehmkemper… - International Journal of …, 2021 - Elsevier
Amorphous solid dispersions (ASDs) are commonly manufactured using spray-drying
processes. The product quality can be decisively influenced by the choice of process …

Phase behavior of pharmaceutically relevant polymer/solvent mixtures

S Dohrn, C Luebbert, K Lehmkemper… - International Journal of …, 2020 - Elsevier
In the pharmaceutical industry, polymers are used as excipients for formulating poorly water-
soluble active pharmaceutical ingredients (APIs) in so-called “amorphous solid …

Machine estimation of drug melting properties and influence on solubility prediction

N Wyttenbach, A Niederquell… - Molecular pharmaceutics, 2020 - ACS Publications
There has been much recent interest in machine learning (ML) and molecular quantitative
structure property relationships (QSPR). The present research evaluated modern ML-based …

The underestimated contribution of the solvent to the phase behavior of highly drug loaded amorphous solid dispersions

S Dedroog, E Boel, C Kindts, B Appeltans… - International Journal of …, 2021 - Elsevier
In spite of the fact that spray drying is widely applied for the formulation of amorphous solid
dispersions (ASDs), the influence of the solvent on the physical properties of the ASDs is still …

Thermodynamic modeling of solvent-impact on phase separation in amorphous solid dispersions during drying

S Dohrn, P Reimer, C Luebbert… - Molecular …, 2020 - ACS Publications
Understanding and prevention of unwanted changes of a pharmaceutical formulation during
the production process is part of the critical requirements for the successful approval of a …