2014 · 12 citations · 12 references
PharmacyMedicinal ChemistryPharmaceuticsDissolution TestingPharmaceutical FormulationSolid-state ChemistryCrystal ChemistryCrystal EngineeringCrystallization ProcessesDrug SolubilitySolubility EnhancementSolubility OptimizationCrystallizationDrug Crystal FormPharmaceutical CocrystallizationPharmaceutical CrystalsPhysicochemical PropertiesPowder Diffraction AnalysisPowder X-ray DiffractionSolution Crystallization
Objective: Cocrystals have been increasingly recognized as an attractive alternative for solid forms of drug products. In this work nicotinamide (NCT) was employed to form the cocrystal with the active pharmaceutical ingredient prulifloxacin (PF). Methods: The PF-NCT cocrystal was prepared by employing slow evaporation and solution crystallization methodology from acetone as a solvent. The PF-NCT cocrystal was characterized by powder X-ray diffraction (PXRD), infrared (IR) spectroscopy, raman spectroscopy, I H NMR spectroscopy and differential scanning calorimetry (DSC). The PF-NCT cocrystal was then subsequently evaluated for pharmaceutical relevant properties such as aqueous solubility and hygroscopicity. Results: Synthesis of cocrystal of prulifloxacin with nicotinamide were successfully carried out by solvent evaporation and solution crystallization methods using acetone solvent. The results from Powder X-ray diffraction, DSC, IR, Raman spectroscopic analysis revealed the formation of cocrystal of prulifloxacin and nicotinamide. Conclusion: The PF-NCT cocrystal is moderately hygroscopic and exhibit enhanced solubility than the pure drug. This study confirms cocrystallization offers a valuable way to improve the physicochemical properties of the API.
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Pharmaceutical Cocrystals and Their Physicochemical Properties
N. Schultheiss, Ann Newman · Crystal Growth & Design · 2009 · 1.5K citations · Full text
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