Micronization of tolbutamide using rapid expansion of supercritical solution with solid co-solvent (RESS-SC) process

Micronization of tolbutamide using rapid expansion of supercritical solution with solid... Micronization of a sulfonylurea antidiabetic agent, tolbutamide, using rapid expansion of supercritical solution with solid co-solvent (RESS-SC) process was investigated in this study. Menthol was selected as the solid co-solvent in the RESS-SC process owing to its high vapor pressure and ease of removal by sublimation. The tolbutamide particles were micronized successfully from its original mean size of 89.4 μm to the smallest mean size of 2.1 μm through the RESS-SC process. The use of solid co-solvent in this process enhanced the saturated solubility of tolbutamide in supercritical carbon dioxide and inhibited the particle growth during pressure expansion after the nozzle. In addition, polymorph conversion from form I to form II after the RESS-SC process was confirmed by XRD and DSC analyses. Measurements of the dissolution rate profiles before and after the RESS-SC process were also investigated. It is shown that the micronized tolbutamide by the RESS-SC process had novelty in dissolution behavior compared to that of the original compound. Its dissolution rate was enhanced by 8.8 times after the RESS-SC process. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Research on Chemical Intermediates Springer Journals

Micronization of tolbutamide using rapid expansion of supercritical solution with solid co-solvent (RESS-SC) process

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Publisher
Springer Netherlands
Copyright
Copyright © 2011 by Springer Science+Business Media B.V.
Subject
Chemistry; Inorganic Chemistry ; Catalysis; Physical Chemistry
ISSN
0922-6168
eISSN
1568-5675
D.O.I.
10.1007/s11164-011-0262-6
Publisher site
See Article on Publisher Site

Abstract

Micronization of a sulfonylurea antidiabetic agent, tolbutamide, using rapid expansion of supercritical solution with solid co-solvent (RESS-SC) process was investigated in this study. Menthol was selected as the solid co-solvent in the RESS-SC process owing to its high vapor pressure and ease of removal by sublimation. The tolbutamide particles were micronized successfully from its original mean size of 89.4 μm to the smallest mean size of 2.1 μm through the RESS-SC process. The use of solid co-solvent in this process enhanced the saturated solubility of tolbutamide in supercritical carbon dioxide and inhibited the particle growth during pressure expansion after the nozzle. In addition, polymorph conversion from form I to form II after the RESS-SC process was confirmed by XRD and DSC analyses. Measurements of the dissolution rate profiles before and after the RESS-SC process were also investigated. It is shown that the micronized tolbutamide by the RESS-SC process had novelty in dissolution behavior compared to that of the original compound. Its dissolution rate was enhanced by 8.8 times after the RESS-SC process.

Journal

Research on Chemical IntermediatesSpringer Journals

Published: Feb 4, 2011

References

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