Using a laser monitoring observation technique, we determined the solubilities of paroxetine hydrochloride
hemihydrate in N,N-dimethylformamide, methyl isobutyl ketone, tetrahydrofuran, ethyl acetate, methanol,
ethanol, 1-propanol, 1-butanol, and 2-butanol by the synthetic method from 286 K to 363 K. Results of
these measurements were correlated by an empirical equation.
Apatinib (APA) belongs to the targeted antineoplastic family of drugs by inhibiting the vascular endothelial cell growth factor receptor (VEGFR-2) of tyrosine kinase. APA encounters poor aqueous solubility problems, and its therapeutic dosage form, apatinib mesylate (ATM), is unstable and dissociates completely to APA in aqueous solution. Here, we synthesized and evaluated three new cocrystals of APA with adipic acid (APA + ADA), sebacic acid (APA + SEA), and D/L-mandelic acid (APA + D/L-MA), and four new salts with succinic acid (APA + SUA-H 2 O), salicylic acid (APA + SA), 1-hydroxy-2-naphthoic acid (APA + HNA), and saccharin (APA + SAC). All the solid forms were characterized by powder X-ray diffraction, infrared spectroscopy, differential scanning calorimetry, and dynamic vapor sorption. The molecular components and structures were confirmed by single crystal Xray diffraction. APA + SEA is able to overcome the instability problem and has improved solubility compared with ATM. Hence, APA + SEA has the potential to be a superior candidate for this important drug.
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