Journal article
Investigation of Solution and Vapor Phase Mediated Phase Transformation in Thiamine Hydrochloride
Journal of pharmaceutical sciences, Vol.99(9), pp.3941-3952
2010
DOI: 10.1002/jps.22240
PMID: 20575002
Abstract
Thiamine hydrochloride (THCl) can exist as an anhydrate (AH), a hemihydrate (HH) and as a nonstoichiometric hydrate (NSH) where the water content can range between 0 and approximately 1 mole of water per mole of THCl. We have investigated the NSH --> HH phase transformation, in the presence of microcrystalline cellulose (MCC), following (i) wet massing, (ii) fluid-bed granulation, and (iii) exposure to water vapor (40 degrees C/75% RH). Based on Raman spectroscopy (40 degrees C), wet massing of NSH alone caused near complete transformation to HH in <100 min. In the presence of MCC, the transformation rate was decelerated. During fluid-bed granulation, approximately 20% of NSH was transformed to HH and the deceleratory effect of MCC was much less pronounced. Exposure to water vapor, of both NSH-MCC powder blends and granules (prepared by fluid-bed) resulted in complete HH formation within 6 days. Presence of MCC in the powder blend did not affect HH formation kinetics, but facilitated phase transformation in the granules. NSH --> HH conversion appeared to follow two-dimensional nucleation and growth model in powder blends, whereas the granules showed either three-dimensional diffusion controlled or a first-order kinetics. In a wet mass, polyvinyl pyrrolidone, a widely used binder, was much more effective than MCC in inhibiting HH formation during wet massing.
Details
- Title: Subtitle
- Investigation of Solution and Vapor Phase Mediated Phase Transformation in Thiamine Hydrochloride
- Creators
- Paroma CHAKRAVARTY - Department of Pharmaceutics, University of Minnesota, Minneapolis, Minnesota 55455, United StatesRamprakash GOVINDARAJAN - Department of Pharmaceutics, University of Minnesota, Minneapolis, Minnesota 55455, United StatesRaj SURYANARAYANAN - Department of Pharmaceutics, University of Minnesota, Minneapolis, Minnesota 55455, United States
- Resource Type
- Journal article
- Publication Details
- Journal of pharmaceutical sciences, Vol.99(9), pp.3941-3952
- DOI
- 10.1002/jps.22240
- PMID
- 20575002
- NLM abbreviation
- J Pharm Sci
- ISSN
- 0022-3549
- eISSN
- 1520-6017
- Publisher
- Wiley; Washington, DC; Hoboken, NJ
- Language
- English
- Date published
- 2010
- Academic Unit
- Pharmaceutical Sciences and Experimental Therapeutics
- Record Identifier
- 9984065696102771
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