Mutual impact of phase separation/crystallization and water sorption in amorphous solid dispersions

C Luebbert, M Wessner, G Sadowski - Molecular Pharmaceutics, 2018 - ACS Publications
The molecular integration of poorly water soluble active pharmaceutical ingredients (APIs) in
a suitable polymeric matrix is a possible approach to enhance the dissolution behavior and …

Combining crystalline and polymeric excipients in API solid dispersions–Opportunity or risk?

H Veith, F Wiechert, C Luebbert, G Sadowski - European Journal of …, 2021 - Elsevier
Amorphous solid dispersions (ASDs) are often metastable against crystallization of the
active pharmaceutical ingredient (API) and thus might undergo unwanted changes during …

Moisture-induced amorphous phase separation of amorphous solid dispersions: molecular mechanism, microstructure, and its impact on dissolution performance

H Chen, Y Pui, C Liu, Z Chen, CC Su… - Journal of …, 2018 - Elsevier
Amorphous phase separation (APS) is commonly observed in amorphous solid dispersions
(ASD) when exposed to moisture. The objective of this study was to investigate:(1) the phase …

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 …

Understanding the tendency of amorphous solid dispersions to undergo amorphous–amorphous phase separation in the presence of absorbed moisture

ACF Rumondor, H Wikström, B Van Eerdenbrugh… - Aaps Pharmscitech, 2011 - Springer
Abstract Formulation of an amorphous solid dispersion (ASD) is one of the methods
commonly considered to increase the bioavailability of a poorly water-soluble small …

Choosing appropriate solvents for ASD preparation

C Luebbert, D Real, G Sadowski - Molecular pharmaceutics, 2018 - ACS Publications
Amorphous solid dispersions (ASDs) are often used for formulating poorly water-soluble
active pharmaceutical ingredients (APIs). In an ASD, the amorphous API is embedded in a …

Crystallization risk assessment of amorphous solid dispersions by physical shelf-life modeling: a practical approach

B Liu, F Theil, K Lehmkemper, D Gessner… - Molecular …, 2021 - ACS Publications
Amorphous solid dispersions (ASDs) of a poorly water-soluble active pharmaceutical
ingredient (API) in a polymer matrix can enhance the water solubility and therefore generally …

Water sorption in rubbery and glassy polymers, nifedipine, and their ASDs

B Gronniger, E Fritschka, I Fahrig, A Danzer… - Molecular …, 2023 - ACS Publications
Polymers like poly (vinylpyrrolidone-co-vinyl acetate)(PVPVA) or hydroxypropyl
methylcellulose acetate succinate (HPMCAS) are commonly used as a matrix for amorphous …

The shelf life of ASDs: 1. Measuring the crystallization kinetics at humid conditions

F Wolbert, K Nikoleit, M Steinbrink… - Molecular …, 2022 - ACS Publications
Amorphous solid dispersions (ASDs), where an active pharmaceutical ingredient (API) is
dissolved in a polymer, are a favored formulation technique to achieve sufficient …

Investigating phase separation in amorphous solid dispersions via Raman mapping

C Luebbert, C Klanke, G Sadowski - International journal of pharmaceutics, 2018 - Elsevier
The bioavailability of poorly-water-soluble active pharmaceutical ingredients (APIs) can be
significantly improved by so-called amorphous solid dispersions (ASDs). However, the long …