Crystal Structures and Phase Behavior of Sulfadiazine and a Method for the Preparation of Aggregates with Good Performance

The solvate and the solvent‐free form of sulfadiazine (SD) were investigated. SD was found to exist in one solvent‐free form and the N‐methylpyrrolidone (NMP) solvate form. The NMP solvate was shown to be a channel‐type compound. The intrinsic properties of the solvents were used to evaluate the eff...

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Bibliographic Details
Published in:Chemical engineering & technology 2018-03, Vol.41 (3), p.532-540
Main Authors: Wu, Songgu, Du, Shichao, Chen, Mingyang, Li, Kangli, Jia, Lina, Zhang, Dejiang, Macaringue, Estevao G. J., Hou, Baohong, Gong, Junbo
Format: Article
Language:English
Subjects:
Aggregate
Aggregates
Crystal structure
Crystallization
Dissolution rate
Free form
Penetration
Phase transformation
Phase transitions
Solvate
Sulfadiazine
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Summary:The solvate and the solvent‐free form of sulfadiazine (SD) were investigated. SD was found to exist in one solvent‐free form and the N‐methylpyrrolidone (NMP) solvate form. The NMP solvate was shown to be a channel‐type compound. The intrinsic properties of the solvents were used to evaluate the effects of solubility on the phase transformation of SD and the NMP solvate. The SD phase could transform to the NMP solvate by NMP‐mediated phase transformation, which was governed by crystallization of the NMP solvate. The crystalline NMP solvate could transform to the solvent‐free solid state through solid‐solid transformation upon heating or water penetration‐mediated phase transformation. The rate of this water penetration‐mediated phase transformation of the NMP solvate to SD was unusually fast. It can be used to obtain SD aggregates of well‐defined shape and good powder properties. Sulfadiazine (SD) exists in one solvent‐free form and the N‐methylpyrrolidone (NMP) solvate form, with the NMP solvate being a channel‐type compound. The SD phase can transform to the NMP solvate by NMP‐mediated phase transformation. Water penetration‐mediated phase transformation of the NMP solvate to SD can be used to obtain SD aggregates of well‐defined shape and good powder properties.
ISSN:0930-7516
1521-4125
DOI:10.1002/ceat.201700053