کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
600078 | 1454295 | 2013 | 6 صفحه PDF | دانلود رایگان |
• Three microemulsion systems were applied as solvents for polymorph screening of APIs.
• A new crystal form of diflunisal monohydrate was discovered.
• The diflunisal monohydrate was prepared from a microemulsion system.
• The diflunisal crystals were characterized by DSC, XRD and SEM.
• The dissolution rate of diflunisal hydrate is much higher than that of anhydrous one.
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.
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Journal: Colloids and Surfaces B: Biointerfaces - Volume 109, 1 September 2013, Pages 68–73