RT Journal Article
T1 Novel Polymorphic Cocrystals of the Non-Steroidal Anti-Inflammatory Drug Niflumic Acid: Expanding the Pharmaceutical Landscape
A1 Acebedo-Martinez, Francisco Javier
A1 Alarcon-Payer, Carolina
A1 Frontera, Antonio
A1 Barbas, Rafael
A1 Prohens, Rafel
A1 Di Crisci, Milena
A1 Dominguez-Martin, Alicia
A1 Gomez-Morales, Jaime
A1 Choquesillo-Lazarte, Duane
K1 cocrystal polymorphism
K1 niflumic acid
K1 caffeine
K1 NSAIDs
K1 mechanochemical synthesis
K1 Hydrogen-bond patterns
K1 Crystals
K1 Caffeine
K1 Mechanochemistry
K1 Clathrate
K1 Features
K1 Release
K1 Program
K1 Salt
AB Any time the pharmaceutical industry develops a new drug, potential polymorphic events must be thoroughly described, because in a crystalline pharmaceutical solid, different arrangements of the same active pharmaceutical ingredient can yield to very different physicochemical properties that might be crucial for its efficacy, such as dissolution, solubility, or stability. Polymorphism in cocrystal formulation cannot be neglected, either. In this work, two different cocrystal polymorphs of the non-steroidal anti-inflammatory drug niflumic acid and caffeine are reported. They have been synthesized by mechanochemical methods and thoroughly characterized in solid-state by powder and single crystal X-ray diffraction respectively, as well as other techniques such as thermal analyses, infrared spectroscopy and computational methods. Both theoretical and experimental results are in agreement, confirming a conformational polymorphism. The polymorph NIF-CAF Form I exhibits improved solubility and dissolution rate compared to NIF-CAF Form II, although Form II is significantly more stable than Form I. The conditions needed to obtain these polymorphs and their transition have been carefully characterized, revealing an intricate system.
PB Mdpi
YR 2021
FD 2021-12-01
LK https://hdl.handle.net/10668/26327
UL https://hdl.handle.net/10668/26327
LA en
DS RISalud
RD Apr 11, 2025