[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 …
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 …
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
Due to the strong tendency towards poorly soluble drugs in modern development pipelines,
enabling drug formulations such as amorphous solid dispersions, cyclodextrins, co-crystals …
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 …
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 …
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
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 …
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 …
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 …
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
This study explores the research area of drug solubility in lipid excipients, an area
persistently complex despite recent advancements in understanding and predicting …
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 …
are major challenges for cell-based permeability assays. Due to their incompatibility with …