Co-Crystals of Active Pharmaceutical Ingredients - Acetazolamide

Autor: Karina Mondragón-Vásquez, Jenniffer I. Arenas-García, Herbert Höpfl, Hugo Morales-Rojas, Dea Herrera-Ruiz
Rok vydání: 2010
Předmět:
Zdroj: Crystal Growth & Design. 10:3732-3742
ISSN: 1528-7505
1528-7483
Popis: A total of 20 co-crystal formers have been combined with acetazolamide (ACZ) via solvent drop grinding in acetone, acetonitrile, and water. The screening experiments provided co-crystals with 4-hydroxybenzoic acid (4HBA) and nicotinamide (NA) (ACZ-4HBA and ACZ-NA-H2O), which were identified by X-ray powder diffraction (XRPD) and further characterized by IR spectroscopy and differential scanning calorimetry-thermogravimetric analysis (DSC-TGA). Both co-crystals could be prepared also by neat grinding (NG) and reaction crystallization (RC). Single-crystal X-ray diffraction analyses allowed for an examination of the dominant hydrogen bonding patterns in the co-crystals, showing that 4HBA binds to the thiadiazole acetamide fragment of ACZ via C(N)NH···HOOC and O−H···N interactions, while NA is linked through N−H···N and N−H···O contacts. In ACZ-NA-H2O, the components are connected further by crystal lattice water molecules through N−H···Ow and Ow−H···N hydrogen bonds. Phase stability assays in water at physio...
Databáze: OpenAIRE