Pharmaceutical Cocrystals for Drug Delivery DOI
Ashwini Nangia

Burger's Medicinal Chemistry and Drug Discovery, Journal Year: 2025, Volume and Issue: unknown, P. 1 - 62

Published: May 26, 2025

Abstract Pharmaceutical cocrystals offer the ability to tune solubility, permeability, tableting, and bioavailability of a solid, oral drug formulation without changing chemical structure molecule. Crystal engineering pharmaceutical salts via supramolecular heterosynthons with acceptable generally recognized as safe (GRAS) coformers provides platform technology for improving efficacy optimal delivery. With almost 90% drugs in Biopharmaceutics Classification System (BCS) class II IV suffering from low‐solubility and/or low‐permeability challenges, have provided an opportune intervention populating pipeline over past decade. From prototype cocrystal itraconazole‐succinic acid first salt‐cocrystal complex Entresto containing valsartan‐sacubitril, this review covers origins subject early 2000s peak growth curve model systems between 2005 2015, successful lab‐to‐market translation witnessed The combined application machine learning neural network tools is bringing speed accuracy research exercise designing drug–coformer therapeutic properties. This article snapshot summary latest trends leading discovery, development, continuous manufacturing.

Language: Английский

Direct Nucleation of Caffeine and Benzoic Acid Cocrystals by Using Periodic Taylor Vortex Flow DOI
Zunhua Li, Gérard Coquerel, Bum Jun Park

et al.

Crystal Growth & Design, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 7, 2025

Since 1961, researchers have highlighted that it was impossible to achieve direct nucleation of caffeine/benzoic acid (CAF/BA) cocrystals. To address this challenge, we explored periodic Taylor vortex flow (PTVF) for CAF/BA Our findings robustly indicated the PTVF directly promotes pure cocrystals without any other crystals, even at a low rotation speed 100 rpm in Couette-Taylor (CT) crystallizer. Conversely, when using random turbulent eddy (RTEF) mixing tank crystallizer, produced β-form caffeine crystals. Then, these crystals were slowly shifted via solution-mediated recrystallization. This result demonstrated different patterns caused distinct crystallization pathways. Consequently, can be employed produce high-purity drug with enhanced solubility and bioavailability, thereby improving efficacy safety drugs.

Language: Английский

Citations

0
Pharmaceutical Cocrystals for Drug Delivery DOI
Ashwini Nangia

Burger's Medicinal Chemistry and Drug Discovery, Journal Year: 2025, Volume and Issue: unknown, P. 1 - 62

Published: May 26, 2025

Abstract Pharmaceutical cocrystals offer the ability to tune solubility, permeability, tableting, and bioavailability of a solid, oral drug formulation without changing chemical structure molecule. Crystal engineering pharmaceutical salts via supramolecular heterosynthons with acceptable generally recognized as safe (GRAS) coformers provides platform technology for improving efficacy optimal delivery. With almost 90% drugs in Biopharmaceutics Classification System (BCS) class II IV suffering from low‐solubility and/or low‐permeability challenges, have provided an opportune intervention populating pipeline over past decade. From prototype cocrystal itraconazole‐succinic acid first salt‐cocrystal complex Entresto containing valsartan‐sacubitril, this review covers origins subject early 2000s peak growth curve model systems between 2005 2015, successful lab‐to‐market translation witnessed The combined application machine learning neural network tools is bringing speed accuracy research exercise designing drug–coformer therapeutic properties. This article snapshot summary latest trends leading discovery, development, continuous manufacturing.

Language: Английский

Citations

0