Towards the Development of Novel Diclofenac Multicomponent Pharmaceutical Solids

Abstract

Multicomponent pharmaceutical materials offer new opportunities to address drug physicochemical issues and to obtain improved drug formulation, especially on oral administration drugs. This work reports three new multicomponent pharmaceutical crystals of the non-steroidal anti-inflammatory drug diclofenac and the nucleobases adenine, cytosine, and isocytosine. They have been synthesized by mechanochemical methods and been characterized in-depth in solid-state by powder and single crystal X-ray diffraction, as well as other techniques such as thermal analyses and infrared spectroscopy. Stability and solubility tests were also performed on these materials. This work aimed to evaluate the physicochemical properties of these solid forms, which revealed thermal stability improvement. Dissociation of the new phases was observed in water, though. This fact is consistent with the reported observed layered structures and BFDH morphology calculations.

Increased Dissolution Rate of Aceclofenac by Formation of Multicomponent Crystals With L-Glutamine

“…1) shows that the physical mixture and MCC have one sharp endothermic peak, which means ACF and LGLN fuse simultaneously. Several small endothermic peaks above the sample's melting point indicate the sample's degradation in the physical mixture and MCC thermograms [26][27][28]. One endothermic peak with a melting point lower than its pure component was also detected in the DSC data of ACF and caffeine eutectic mixtures [30].…”

Development Strategies of Polymorphs and Solvates for Enhancing Powder Properties: A Case Study of Thiothiamine

“…The development of new solid forms is essential to overcoming challenges in the production of crystalline materials or active pharmaceutical ingredients, such as poor powder properties, stability issues, and low bioavailability. − Different solid forms, such as polymorphs, cocrystals, and solvates, often exhibit distinct properties that can enhance product properties and improve downstream performance. − Solvate formation is a common phenomenon in the process of solution crystallization, with approximately one-third of organic molecules being able to form solvates, making it a subject of significant research interest. − …”

Multicomponent Pharmaceutical Solids

“…The last contribution of this Special Issue is devoted to multicomponent formulations of the non-steroidal anti-inflammatory drug Diclofenac, using nucleobases as coformers due to their versatility to build multiple H-bonding patterns [10]. Careful structure-property analysis reveals that the large surface exposure of two of the novel cocrystals favors their dissociation in aqueous media.…”