Imatinib mesylate cocrystals: synthesis, screening, and preliminary characterization

Abstract

Drug-drug cocrystals of imatinib mesylate with several cocrystal formers, i.e. 5-chlorouracil, 5-fluorouracil, hydroxyurea, 5-fluorocytosine, N-acetylcytosine, chlorogenic acid, dacarbazine, curcumin, creatine, orotic acid, L-cysteine, glutathione, and caffeic acid, were prepared from mixtures by cogrinding or solvent cocrystallization. The samples prepared were analyzed by FTIR, DSC, and XRPD. Formation of cocrystals with different stoichiometry was observed. Novel cocrystals of imatinib mesylate with 5-fluorouracil or hydroxyurea were identified, characterized, and selected by the solid form screening approach. These cocrystals were non-hygroscopic and chemically and physically stable to thermal stress under the testing conditions.

Thermal stability and decompositions kinetics under non-isothermal conditions of imatinib mesylate α form

“…3. The obtained results correspond very well to α form, and are consistent with the literature data [14,[17][18][19]. FTIR showed characteristic bands at 3.256 cm -1 (N-H stretching vibration), 1.657 cm -1 (C=O band), 1.570, 1.525, and 1.444 cm -1 (aromatic C=C, C=N stretching vibration), 1.158 cm -1 (C-N stretching vibration), 1.036 cm -1 (C-O stretching vibration), and 807 cm -1 (aromatic C-H deformations out of plane).…”

Preparation and Solid-State Characterization of Dapsone Drug–Drug Co-Crystals

“…Drug–drug co-crystals fulfill the criteria for patent eligibility: novelty, utility, and nonobviousness . Consequently, there has been a growing interest in the study of drug–drug co-crystals reflected in the increasing number of publications and patent applications in recent years. − …”

Hydroxyurea-Loaded Albumin Nanoparticles: Preparation, Characterization, and In Vitro Studies

“…For hydroxyurea, a characteristic endothermic peak was observed at 145 °C with a change in enthalpy (Figure 4b), which was not accompanied by a mass loss, and characterized the HU phase transition (a value close to the melting point). Further, an exothermic peak was observed at a temperature of 168 °C, there was a mass loss of up to 53% in the range of 150–180 °C, which might correspond to the decomposition temperature of the drug [27,28]. HSA-NPs exhibited an endothermic peak at 96 °C (Figure 4c), which probably corresponded to the period of their melting.…”