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Towards medicinal mechanochemistry: evolution of milling from pharmaceutical solid form screening to the synthesis of active pharmaceutical ingredients (APIs)
09 Jun 2023 | Contributor(s):: Tan, D, Loots, L, Friscic, T
This overview highlights the emergent area of mechanochemical reactions for making active pharmaceutical ingredients (APIs), and covers the latest advances in the recently established area of mechanochemical screening and synthesis of pharmaceutical solid forms, specifically polymorphs,...
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Toward Continuous Crystallization of Urea-Barbituric Acid: A Polymorphic Co-Crystal System
09 Jun 2023 | Contributor(s):: Powell, KA, Bartolini, GWittering, KE, Saleemi, AN, Wilson, CC, Rielly, CD, Nagy, ZK
Pharmaceutical co-crystals are multicomponent molecular systems typically formed through hydrogen bonding of a co-former molecule with the active pharmaceutical ingredient (API). Just as many single component molecular structures can exhibit polymorphism due to the geometry of hydrogen bond...
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Microfluidic droplet liquid reactors for active pharmaceutical ingredient crystallization by diffusion controlled solvent extraction
09 Jun 2023 | Contributor(s):: Tona, RM, McDonald, TAOAkhavein, N, Larkin, JD, Lai, D
A novel method for crystallization utilizing solvent/antisolvent extraction in microfluidic droplet liquid reactors has been developed for rapid and low-cost screening of crystal polymorphism (i. e. molecular crystallographic arrangement or internal structure) and habit (i.e. crystallographic...
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Highly Selective, Kinetically Driven Polymorphic Selection in Microfluidic Emulsion-Based Crystallization and Formulation
09 Jun 2023 | Contributor(s):: Leon, RAL, Badruddoza, AMZheng, L, Yeap, EWQ, Toldy, AI, Wong, KY, Hatton, TA, Khan, SA
We present a simple, potentially generalizable method to create highly monodisperse spherical microparticles (SMs) of similar to 200 mu m size containing active pharmaceutical ingredient (API) crystals and a macromolecular excipient, with unprecedented, highly specific, and selective control over...
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From form to function: Crystallization of active pharmaceutical ingredients
09 Jun 2023 | Contributor(s):: Variankaval, Narayan, Cote, Aaron S., Doherty, Michael F.
In this perspective, we describe the state-of-the-art in API crystal product and process design, highlight barriers that currently prevent the production of better, cheaper crystalline products, and give our best estimate of where the field is going and should go during the next decade.