Strategies to address low drug solubility in discovery and development

HD Williams, NL Trevaskis, SA Charman… - Pharmacological …, 2013 - Elsevier
Drugs with low water solubility are predisposed to low and variable oral bioavailability and,
therefore, to variability in clinical response. Despite significant efforts to “design in” …

Pharmaceutical aspects of salt and cocrystal forms of APIs and characterization challenges

PC Vioglio, MR Chierotti, R Gobetto - Advanced Drug Delivery Reviews, 2017 - Elsevier
In recent years many efforts have been devoted to the screening and the study of new solid-
state forms of old active pharmaceutical ingredients (APIs) with salification or co …

Advanced crystallisation methods for small organic molecules

JP Metherall, RC Carroll, SJ Coles, MJ Hall… - Chemical Society …, 2023 - pubs.rsc.org
Molecular materials based on small organic molecules often require advanced structural
analysis, beyond the capability of spectroscopic techniques, to fully characterise them. In …

Early pharmaceutical profiling to predict oral drug absorption: current status and unmet needs

CAS Bergström, R Holm, SA Jørgensen… - European Journal of …, 2014 - Elsevier
Preformulation measurements are used to estimate the fraction absorbed in vivo for orally
administered compounds and thereby allow an early evaluation of the need for enabling …

Co‐crystal Prediction by Artificial Neural Networks

JJ Devogelaer, H Meekes, P Tinnemans… - Angewandte Chemie …, 2020 - Wiley Online Library
A significant amount of attention has been given to the design and synthesis of co‐crystals
by both industry and academia because of its potential to change a molecule's …

'Pro et contra'ionic liquid drugs–Challenges and opportunities for pharmaceutical translation

A Balk, U Holzgrabe, L Meinel - European Journal of Pharmaceutics and …, 2015 - Elsevier
Ionic liquids (ILs) are organic salts with a melting point below 100° C. Active pharmaceutical
ingredients (APIs) are transformed into ILs by combining them with typically large yet …

Current trends and advancements in crystallization and single-crystal structural analysis of small molecules

Y Xiao, C Wu, L Zhou, P Commins, L Li… - Coordination Chemistry …, 2024 - Elsevier
The advancement of single-crystal structural analysis has emerged as a pivotal technology
surpassing spectroscopic methods in revealing the intricate structural details of organic …

Advanced methodologies for pharmaceutical salt synthesis

MS Hossain Mithu, S Economidou, V Trivedi… - Crystal Growth & …, 2021 - ACS Publications
Pharmaceutical salt formation is the most preferred and effective method to enhance the
physicochemical properties of an active pharmaceutical ingredient (API) such as solubility …

Efficient throughput method for hygroscopicity classification of active and inactive pharmaceutical ingredients by water vapor sorption analysis

V Murikipudi, P Gupta, V Sihorkar - … development and technology, 2013 - Taylor & Francis
The conventional method of hygroscopicity determination proposed by Callahan and co-
workers utilizes more sample and time, may not be precise in all the cases, and is a …

Modulation of biopharmaceutical properties of acidic drugs using cationic counterions: A critical analysis of FDA-approved pharmaceutical salts

SS Bharate - International Journal of Pharmaceutics, 2021 - Elsevier
Salification has a successful track record in modulating the biopharmaceutical properties of
drugs. This is evident from the significant share (40%) of pharmaceutical salts in FDA …