Characterization of recrystallized itraconazole prepared by cooling and anti-solvent crystallization

The objective of the present study was to alter the crystal habit of itraconazole (ITZ) by cooling and anti-solvent crystallization and characterize its properties. ITZ was recrystallized in different solvents and the effects of each solvent on morphology of crystals, dissolution behavior and solid...

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Main Authors: Pornsak Sriamornsak, Kanokporn Burapapadh
Format: Article
Language:English
Published: Elsevier 2015-06-01
Series:Asian Journal of Pharmaceutical Sciences
Subjects:
Online Access:http://www.sciencedirect.com/science/article/pii/S1818087615000148
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author Pornsak Sriamornsak
Kanokporn Burapapadh
author_facet Pornsak Sriamornsak
Kanokporn Burapapadh
author_sort Pornsak Sriamornsak
collection DOAJ
description The objective of the present study was to alter the crystal habit of itraconazole (ITZ) by cooling and anti-solvent crystallization and characterize its properties. ITZ was recrystallized in different solvents and the effects of each solvent on morphology of crystals, dissolution behavior and solid state of recrystallized drug particles were investigated. The results revealed that ITZ crystals recrystallized by cooling and anti-solvent crystallization showed the different crystal habits from the untreated ITZ. Using cooling crystallization tended to provide needle-shaped crystals while the crystals obtained from anti-solvent crystallization showed more flaky, plate shape. This indicated the importance of preparation method on nucleation and crystal growth. No change in drug polymorphism was observed, according to determination of thermal property and crystalline state by differential scanning calorimetry and powder X-ray diffractometry, respectively. The recrystallized ITZ showed higher drug dissolution than untreated ITZ and the highest drug dissolution was observed from the samples recrystallized in the presence of PEG 200, which provided the small plate-shaped crystals with tremendously increased in surface area. However, the increasing of drug dissolution is relatively small, therefore, further development may be required.
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spelling doaj.art-8c86ae25bb7342f3b55f4e235e6b18be2022-12-22T01:06:16ZengElsevierAsian Journal of Pharmaceutical Sciences1818-08762015-06-0110323023810.1016/j.ajps.2015.01.003Characterization of recrystallized itraconazole prepared by cooling and anti-solvent crystallizationPornsak Sriamornsak0Kanokporn Burapapadh1Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, ThailandDepartment of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, ThailandThe objective of the present study was to alter the crystal habit of itraconazole (ITZ) by cooling and anti-solvent crystallization and characterize its properties. ITZ was recrystallized in different solvents and the effects of each solvent on morphology of crystals, dissolution behavior and solid state of recrystallized drug particles were investigated. The results revealed that ITZ crystals recrystallized by cooling and anti-solvent crystallization showed the different crystal habits from the untreated ITZ. Using cooling crystallization tended to provide needle-shaped crystals while the crystals obtained from anti-solvent crystallization showed more flaky, plate shape. This indicated the importance of preparation method on nucleation and crystal growth. No change in drug polymorphism was observed, according to determination of thermal property and crystalline state by differential scanning calorimetry and powder X-ray diffractometry, respectively. The recrystallized ITZ showed higher drug dissolution than untreated ITZ and the highest drug dissolution was observed from the samples recrystallized in the presence of PEG 200, which provided the small plate-shaped crystals with tremendously increased in surface area. However, the increasing of drug dissolution is relatively small, therefore, further development may be required.http://www.sciencedirect.com/science/article/pii/S1818087615000148ItraconazolePoorly water-soluble drugCooling crystallizationAnti-solvent crystallization
spellingShingle Pornsak Sriamornsak
Kanokporn Burapapadh
Characterization of recrystallized itraconazole prepared by cooling and anti-solvent crystallization
Asian Journal of Pharmaceutical Sciences
Itraconazole
Poorly water-soluble drug
Cooling crystallization
Anti-solvent crystallization
title Characterization of recrystallized itraconazole prepared by cooling and anti-solvent crystallization
title_full Characterization of recrystallized itraconazole prepared by cooling and anti-solvent crystallization
title_fullStr Characterization of recrystallized itraconazole prepared by cooling and anti-solvent crystallization
title_full_unstemmed Characterization of recrystallized itraconazole prepared by cooling and anti-solvent crystallization
title_short Characterization of recrystallized itraconazole prepared by cooling and anti-solvent crystallization
title_sort characterization of recrystallized itraconazole prepared by cooling and anti solvent crystallization
topic Itraconazole
Poorly water-soluble drug
Cooling crystallization
Anti-solvent crystallization
url http://www.sciencedirect.com/science/article/pii/S1818087615000148
work_keys_str_mv AT pornsaksriamornsak characterizationofrecrystallizeditraconazolepreparedbycoolingandantisolventcrystallization
AT kanokpornburapapadh characterizationofrecrystallizeditraconazolepreparedbycoolingandantisolventcrystallization