Pharmaceutical cocrystals and poorly soluble drugs

R Thakuria, A Delori, W Jones, MP Lipert, L Roy… - International journal of …, 2013 - Elsevier
In recent years cocrystal formation has emerged as a viable strategy towards improving the
solubility and bioavailability of poorly soluble drugs. In this review the success of numerous …

Pharmaceutical cocrystals: formulation approaches to develop robust drug products

NK Duggirala, SM LaCasse, MJ Zaworotko… - Crystal Growth & …, 2019 - ACS Publications
Phase transformation of an active pharmaceutical ingredient in the solid state can influence
the physicochemical properties and consequently drug product performance. The neat …

Co-crystal phase diagram determination by the solution addition method

V Svoboda, R Venkatramanan, M Jaap… - Crystal Growth & …, 2022 - ACS Publications
Multicomponent crystals such as co-crystals, salts, and solid solutions can be used to modify
physical properties of active pharmaceutical ingredients. Phase diagrams of such …

Case studies in the application of a workflow-based crystallization design for optimized impurity rejection in pharmaceutical development

P Agrawal, SH Rawal, VR Reddy… - … Process Research & …, 2023 - ACS Publications
Crystallization is an important unit operation in pharmaceutical drug substance
manufacturing for the isolation of organic products. Impurity control is a recurring critical …

Mitigating drug stability challenges through cocrystallization

J Haneef, M Amir, NA Sheikh, R Chadha - AAPS PharmSciTech, 2023 - Springer
Drug stability plays a significant role in the pharmaceutical industry from early-phase drug
discovery to product registration as well as the entire life cycle of a product. Various …

Impact of pharmaceutical cocrystals: the effects on drug pharmacokinetics

N Shan, ML Perry, DR Weyna… - Expert opinion on drug …, 2014 - Taylor & Francis
Introduction: Pharmaceutical cocrystallization has emerged in the past decade as a new
strategy to enhance the clinical performance of orally administered drugs. A pharmaceutical …

Design space for polymorphic co-crystallization: incorporating process model uncertainty and operational variability

ZQ Yu, PS Chow, RBH Tan - Crystal growth & design, 2014 - ACS Publications
A methodology has been developed to determine the design space of caffeine–glutaric acid
co-crystallization for process development and scale-up. Polymorphic purity is chosen as a …

Cocrystallization as a tool to stabilize liquid active ingredients

A Bacchi, PP Mazzeo - Crystallography Reviews, 2021 - Taylor & Francis
Cocrystallization is an extensively used method in Crystal Engineering for tuning the
properties of target compounds by pairing them with ad-hoc selected molecular partners (ie …

High-throughput 96-well solvent mediated sonic blending synthesis and on-plate solid/solution stability characterization of pharmaceutical cocrystals

V Luu, J Jona, MK Stanton, ML Peterson… - International journal of …, 2013 - Elsevier
A 96-well high-throughput cocrystal screening workflow has been developed consisting of
solvent-mediated sonic blending synthesis and on-plate solid/solution stability …

Mitigating cocrystal physical stability liabilities in preclinical formulations

S Bhardwaj, M Lipert, A Bak - Journal of Pharmaceutical Sciences, 2017 - Elsevier
Poor aqueous solubility of a majority of new small molecule chemical entities is a significant
challenge in drug discovery since considerably high exposures are often required to enable …