Producing amorphous solid dispersions via co-precipitation and spray drying: impact to physicochemical and biopharmaceutical properties

AKP Mann, L Schenck, A Koynov… - Journal of …, 2018 - Elsevier
Many small-molecule active pharmaceutical ingredients (APIs) exhibit low aqueous
solubility and benefit from generation of amorphous dispersions of the API and polymer to …

Processing impact on in vitro and in vivo performance of solid dispersions—a comparison between hot-melt extrusion and spray drying

Y Li, AKP Mann, D Zhang, Z Yang - Pharmaceutics, 2021 - mdpi.com
Presently, a large number of drug molecules in development are BCS class II or IV
compounds with poor aqueous solubility. Various novel solubilization techniques have been …

Building a better particle: Leveraging physicochemical understanding of amorphous solid dispersions and a hierarchical particle approach for improved delivery at …

L Schenck, AKP Mann, Z Liu, M Milewski… - International journal of …, 2019 - Elsevier
Amorphous solid dispersions are a promising option for managing compounds with poor
aqueous solubility. However, for compounds with high melting points, thermal stability …

In Vitro and In Vivo Behaviors of KinetiSol and Spray-Dried Amorphous Solid Dispersions of a Weakly Basic Drug and Ionic Polymer†

SV Jermain, MB Lowinger, DJ Ellenberger… - Molecular …, 2020 - ACS Publications
Oral delivery of poorly water-soluble, weakly basic drugs may be problematic based on the
drugs' intrinsic properties. Many drugs in this subset have overcome barriers to delivery …

Coprecipitated amorphous dispersions as drug substance: opportunities and challenges

NA Strotman, L Schenck - Organic Process Research & …, 2021 - ACS Publications
The toolbox of methods for generating amorphous solid dispersions, which are often critical
to achieving high kinetic solubility and bioavailability of drug molecules, continues to grow …

Influence of particle size and drug load on amorphous solid dispersions containing pH-dependent soluble polymers and the weak base ketoconazole

M Monschke, K Kayser, KG Wagner - AAPS PharmSciTech, 2021 - Springer
Among the great number of poorly soluble drugs in pharmaceutical development, most of
them are weak bases. Typically, they readily dissolve in an acidic environment but are prone …

Development of fast-dissolving amorphous solid dispersion of itraconazole by melt extrusion of its mixture with weak organic carboxylic acid and polymer

T Parikh, ATM Serajuddin - Pharmaceutical research, 2018 - Springer
Purpose The purpose of this study was to explore the feasibility of developing amorphous
solid dispersion (ASD) by inducing acid-base interaction at an elevated temperature using …

Combining co-amorphous-based spray drying with inert carriers to achieve improved bioavailability and excellent downstream manufacturability

Y Zhang, Y Gao, X Du, R Guan, Z He, H Liu - Pharmaceutics, 2020 - mdpi.com
It is crucial to improve poorly water-soluble orally administered drugs through both
preclinical and therapeutic drug discovery. A co-amorphous formulation consisting of two …

Development of Ternary Amorphous Solid Dispersions Manufactured by Hot-Melt Extrusion and Spray-Drying─Comparison of In Vitro and In Vivo Performance

E Trenkenschuh, SM Blattner, D Hirsh… - Molecular …, 2024 - ACS Publications
Producing amorphous solid dispersions (ASDs) by hot-melt extrusion (HME) is favorable
from an economic and ecological perspective but also limited to thermostable active …

Solvent-free direct formulation of poorly-soluble drugs to amorphous solid dispersion via melt-absorption

SC Shen, WK Ng, J Hu, K Letchmanan, J Ng… - Advanced Powder …, 2017 - Elsevier
To improve the dissolution properties of poorly water soluble active pharmaceutical
ingredients (APIs), a solvent-free melt-absorption process was applied to directly load the …