Quantitative determination of two polymorphic forms of imatinib mesylate in a drug substance and tablet formulation by X-ray powder diffraction, differential scanning calorimetry and attenuated total reflectance Fourier transform infrared spectroscopy

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

“…The exothermic events in the sequence correspond to the degradation process. These results are consistent with the literature data [14].…”

“…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).…”

“…IMA exists as a polymorph with two principal forms, α and β, and also in amorphous form. Form β is the most stable, while α form is the most metastable [12,13,14]. Imatinib mesylate examined in this work was synthetized using new method in a continuous-flow microwave reactor according to the patented procedure [15].…”

Pluronic F127 as a suitable carrier for preparing the imatinib base solid dispersions and its potential in development of a modified release dosage forms

“…In aqueous media, imatinib base is characterized by poor solubility (0.01 mg mL -1 ) [1]. However, the mesylate salt of imatinib, which exists as a polymorph with two principal forms, [2,3] is very soluble in media at pH values B5.5, but in neutral and alkaline aqueous buffers is poorly soluble or insoluble [4]. Therefore, imatinib mesylate belongs to Class 2 of Biopharmaceutical Classification System (BCS) with a solubility of 1 mg mL -1 determined at pH 7.4 [4].…”

Generic formulations of imatinib for treatment of Philadelphia chromosome–positive leukemia in pediatric patients

“…Theoretically, polymorphic conversions may occur during the manufacturing process of an imatinib tablet, which includes granulation, compression, coating, and drying. However, studies have found that the α‐crystal form is stable and not converted to the β‐crystal form during a defined manufacturing process and stability period . Initial studies suggested that the β‐crystal form is superior with regard to efficacy and pharmacologic properties (eg, bioavailability influenced by water solubility, absorption); however, subsequent studies in adults showed no difference between the α‐ and β‐crystal forms that significantly influence the performance of GI .…”