[HTML][HTML] Trends in oral small-molecule drug discovery and product development based on product launches before and after the Rule of Five

S Stegemann, C Moreton, S Svanbäck, K Box… - Drug Discovery …, 2023 - Elsevier
Highlights•Orally delivered drug products gradually continue to exceed the Rule-of-five on
Molecular Weight and clogP.•New predictive descriptors and tools, advanced chemistry and …

[HTML][HTML] Advancing algorithmic drug product development: Recommendations for machine learning approaches in drug formulation

JD Murray, JJ Lange, H Bennett-Lenane… - European Journal of …, 2023 - Elsevier
Artificial intelligence is a rapidly expanding area of research, with the disruptive potential to
transform traditional approaches in the pharmaceutical industry, from drug discovery and …

[HTML][HTML] Leveraging the use of in vitro and computational methods to support the development of enabling oral drug products: An InPharma commentary

C Reppas, M Kuentz, A Bauer-Brandl, S Carlert… - European Journal of …, 2023 - Elsevier
Due to the strong tendency towards poorly soluble drugs in modern development pipelines,
enabling drug formulations such as amorphous solid dispersions, cyclodextrins, co-crystals …

[HTML][HTML] Microdialysis and nanofiltration allow to distinguish molecularly dissolved from colloid-associated drug concentrations during biomimetic dissolution testing of …

FL Holzem, JP Schaffland, M Brandl… - European Journal of …, 2022 - Elsevier
Many new drug entities are poorly water-soluble and thus require solubility-enhancing
formulations to ensure sufficient bioavailability. On the other hand, it is more and more …

Hydroxypropyl cellulose for drug precipitation inhibition: from the potential of molecular interactions to performance considering microrheology

A Niederquell, E Stoyanov, M Kuentz - Molecular Pharmaceutics, 2022 - ACS Publications
There has been recent interest in using hydroxypropyl cellulose (HPC) for supersaturating
drug formulations. This study investigated the potential for molecular HPC interactions with …

Artificial neural networks to predict the apparent degree of supersaturation in supersaturated lipid-based formulations: a pilot study

H Bennett-Lenane, JP O'Shea, JD Murray, AR Ilie… - Pharmaceutics, 2021 - mdpi.com
In response to the increasing application of machine learning (ML) across many facets of
pharmaceutical development, this pilot study investigated if ML, using artificial neural …

Application of biorelevant in vitro assays for the assessment and optimization of ASD-based formulations for pediatric patients

J Niessen, ÁL Mármol, R Ismail, JT Schiele… - European Journal of …, 2023 - Elsevier
Amorphous solid dispersions (ASD) have been a successful formulation strategy to
overcome the poor aqueous solubility of many novel drugs, but the development of pediatric …

Developing clinically relevant dissolution specifications (CRDSs) for oral drug products: virtual webinar series

M McAllister, T Flanagan, S Cole, A Abend… - 2022 - mdpi.com
A webinar series that was organised by the Academy of Pharmaceutical Sciences
Biopharmaceutics focus group in 2021 focused on the challenges of developing clinically …

Comparative Analysis of Chemical Descriptors by Machine Learning Reveals Atomistic Insights into Solute–Lipid Interactions

JJ Lange, A Anelli, J Alsenz, M Kuentz… - Molecular …, 2024 - ACS Publications
This study explores the research area of drug solubility in lipid excipients, an area
persistently complex despite recent advancements in understanding and predicting …

Mucin-protected Caco-2 assay to study drug permeation in the presence of complex biorelevant media

D Ye, Á López Mármol, V Lenz, P Muschong… - Pharmaceutics, 2022 - mdpi.com
The poor solubility and permeability of compounds beyond Lipinski's Rule of Five (bRo5)
are major challenges for cell-based permeability assays. Due to their incompatibility with …