Colloids and Surfaces B: Biointerfaces 2013-09-01

A new hydrate form of diflunisal precipitated from a microemulsion system

Hsuan-Lei Sung, Yueh-Lin Fan, Kimberly Yeh, Yen-Fu Chen, Li-Jen Chen

文献索引：Colloids Surf. B Biointerfaces 109 , 68-73, (2013)

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摘要

Three microemulsion systems were applied as solvents for polymorph screening of seven active pharmaceutical ingredients (APIs): carbamazepine, piroxicam, sulfaguanidine, nitrofurantoin, theophylline, quercetin, and diflunisal. All the recrystallized compounds were examined by using powder X-ray diffractometry, differential scanning calorimetry, elemental analysis, Karl Fischer titration and dissolution rate. A new crystal form of diflunisal hydrate was discovered by the cooling method of recrystallization in a water-in-oil microemulsion system, composed of water, alkane and dioctyl sodium sulfosuccinate. The new hydrate form of diflunisal was characterized and confirmed to be a stoichiometry of diflunisal:water of 1:1. The other two microemulsion systems were able to convert the anhydrous diflunisal Form I to Form III. The dissolution rate of diflunisal hydrate is unexpectedly much higher than that of anhydrous ones (Forms I and III). All the other six APIs (carbamazepine, piroxicam, sulfaguanidine, nitrofurantoin, theophylline and quercetin) recrystallized from the microemulsion systems were all converted into hydrate form.Copyright © 2013 Elsevier B.V. All rights reserved.