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Effects of solvents and crystallization conditions on the polymorphic behaviors and dissolution rates of valsartan
journal contribution
posted on 2012-07-01, 00:00 authored by T T-D Tran, Phuong TranPhuong Tran, J-B Park, B-J LeeFor the quality evaluation of raw materials, the influence of various types of solvents on the polymorphic crystallization behaviors and dissolution rates of two sources of valsartan (VAL) from China and India was investigated. Samples were prepared by recrystallization from water or organic solvents, such as acetonitrile, acetone and ethanol, using methods with and without heating. Recrystallization behaviors were characterized by differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD). Scanning electron microscopy (SEM) was also used to observe the morphology of samples. The dissolution rate of recrystallized samples in water was evaluated and compared to the original VAL sample. There were significant differences in morphology, crystal structure and dissolution rate among the samples recrystallized using organic solvents. VAL was transformed into another polymorphic form by the solvents and recrystallization conditions. These physical properties of VAL also differed between the two sources of VAL. Thus, the physicochemical differences of raw materials should be carefully considered in early dosage formulation approaches.
History
Journal
Archives of pharmacal researchVolume
35Issue
7Pagination
1223 - 1230Publisher
SpringerLocation
Berlin, GermanyPublisher DOI
ISSN
0253-6269Language
engPublication classification
C1.1 Refereed article in a scholarly journal; C Journal articleCopyright notice
[2012, Springer]Usage metrics
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No categories selectedKeywords
AcetoneAcetonitrilesAngiotensin II Type 1 Receptor BlockersCalorimetry, Differential ScanningChemistry, PharmaceuticalCrystallizationCrystallography, X-RayEthanolHot TemperatureKineticsMicroscopy, Electron, ScanningPowder DiffractionPowdersSolubilitySolventsTechnology, PharmaceuticalTetrazolesValineValsartanWaterScience & TechnologyLife Sciences & BiomedicineChemistry, MedicinalPharmacology & PharmacyCrystallization conditionStructural behaviorSolvent typePolymorphismDissolution rateCRYSTAL MODIFICATIONGROWTHIMPROVEMENTTECHNOLOGYSTABILITY
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