Cocrystal habit engineering to improve drug dissolution and alter derived powder properties
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Journal ArticleDate:
2016Access:
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Serrano DR, O'Connell P, Paluch KJ, Walsh D, Healy AM, Cocrystal habit engineering to improve drug dissolution and alter derived powder properties, The Journal of pharmacy and pharmacology, 68, 5, 2016, 665-7Download Item:
Abstract:
Objectives: Cocrystallization of sulfadimidine (SDM) with suitable coformers, such as 4-aminosalicylic acid (4-ASA), combined with changes in the crystal habit can favourably alter its physicochemical properties. The aim of this work was to engineer SDM:4-ASA cocrystals with different habits in order to investigate the effect on dissolution, and the derived powder properties of flow and compaction.
Methods: Cocrystals were prepared in a 1:1 molar ratio by solvent evaporation using ethanol (habit I) or acetone (habit II), solvent evaporation followed by grinding (habit III) and spray-drying (habit IV).
Key findings: Powder X-ray diffraction showed Bragg peak position was the same in all the solid products. The peak intensity varied, indicating different preferred crystal orientation confirmed by SEM micrographs: large prismatic crystals (habit I), large plate-like crystals (habit II), small cube-like crystals (habit III) and microspheres (habit IV). The habit III exhibited the fasted dissolution rate; however, it underwent a polymorphic transition during dissolution. Habits I and IV exhibited the highest Carr’s compressibility index, indicating poor flowability. However, habits II and III demonstrated improved flow. Spray drying resulted in cocrystals with improved compaction properties.
Conclusions: Even for cocrystals with poor pharmaceutical characteristics, a habit can be engineered to alter the dissolution, flowability and compaction behavior.
Sponsor
Grant Number
Science Foundation Ireland (SFI)
12/RC/2275
Author's Homepage:
http://people.tcd.ie/healyamhttp://people.tcd.ie/peoconne
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PUBLISHED
Author: Healy, Anne-Marie; O'Connell, Peter
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Journal ArticleSeries/Report no:
The Journal of pharmacy and pharmacology68
5
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Full text availableSubject (TCD):
Nanoscience & Materials , DISSOLUTION RATES , DISSOLUTION TESTINGDOI:
http://dx.doi.org/10.1111/jphp.12476Metadata
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