Simultaneously improving tabletability and solubility of diclofenac by cocrystallization with picolinamide

Jan. 4, 2025, midnight - by Chenyu Wu , Zijian Wang , Xu Han , Xinyi Yu , Changquan Calvin Sun , Zhengzheng Zhou

Remove from favorites

Add to favorites

Diclofenac (DIC), a nonsteroidal anti-inflammatory drug, is characterized by poor tabletability and low water solubility. This study introduces a novel diclofenac-picolinamide cocrystal (DIC-PIC) aimed at improving both properties. The cocrystal was evaluated through various analytical techniques, including X-ray diffraction, thermal analysis, and spectroscopy. Compared to DIC, DIC-PIC exhibited significantly enhanced tabletability, attributed to increased plasticity and a larger bonding area between crystals. This was reflected in its lower in-die mean yield pressure (Py,i), measured at 59.5 ± 0.6 MPa, compared to 86.6 ± 1.4 MPa for DIC. The improved plasticity of DIC-PIC is consistent with the presence of a slip plane (001) in its crystal structure. Furthermore, DIC-PIC demonstrated a remarkable increase in thermodynamic solubility, being 112 times higher in water and 22 times higher in a pH 6.8 buffer solution. These advancements address two major challenges in developing DIC tablets, positioning DIC-PIC as a promising candidate for tablets with enhanced performance.

Read full article