Document Detail


Investigation of solution and vapor phase mediated phase transformation in thiamine hydrochloride.
MedLine Citation:
PMID:  20575002     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Paroma Chakravarty; Ramprakash Govindarajan; Raj Suryanarayanan
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.    
Journal Detail:
Title:  Journal of pharmaceutical sciences     Volume:  99     ISSN:  1520-6017     ISO Abbreviation:  J Pharm Sci     Publication Date:  2010 Sep 
Date Detail:
Created Date:  2010-07-28     Completed Date:  2010-11-26     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  2985195R     Medline TA:  J Pharm Sci     Country:  United States    
Other Details:
Languages:  eng     Pagination:  3941-52     Citation Subset:  IM    
Affiliation:
Department of Pharmaceutics, University of Minnesota, Minneapolis, Minnesota 55455, USA.
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MeSH Terms
Descriptor/Qualifier:
Cellulose / chemistry
Phase Transition
Powder Diffraction
Solubility
Thiamine / chemistry*
Water / chemistry*
X-Ray Diffraction
Chemical
Reg. No./Substance:
0/microcrystalline cellulose; 59-43-8/Thiamine; 7732-18-5/Water; 9004-34-6/Cellulose

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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