Document Detail


Solid-state esterification of codeine phosphate by the acid constituent of effervescent tablets.
MedLine Citation:
PMID:  3585724     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Codeine phosphate in a paracetamol:codeine effervescent tablet was found to react at room temperature and 37 degrees C with the citric acid constituent to form citrate esters of codeine. The esterification was confirmed in a solid-state reaction at elevated temperature. The structures of the three possible monosubstituted esters (1-3) were elucidated from spectroscopic data (nuclear magnetic resonance and mass spectrometry) and by selective hydrolysis of the dimethyl esters to give symmetrical and asymmetrical dimethyl citrates. In the degradation reaction, formation of the symmetrically substituted citrate ester of codeine, 1, was found to predominate. Tartaric acid, which can be used in effervescent tablet formulations, was also found to give an ester with codeine phosphate in a similar nonsolvolytic reaction. A liquid chromatographic method was developed for the separation of the citrate esters of codeine.
Authors:
B Silver; E G Sundholm
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Journal of pharmaceutical sciences     Volume:  76     ISSN:  0022-3549     ISO Abbreviation:  J Pharm Sci     Publication Date:  1987 Jan 
Date Detail:
Created Date:  1987-07-01     Completed Date:  1987-07-01     Revised Date:  2008-11-21    
Medline Journal Info:
Nlm Unique ID:  2985195R     Medline TA:  J Pharm Sci     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  53-5     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Chemical Phenomena
Chemistry
Chromatography, High Pressure Liquid
Citrates
Citric Acid
Codeine / analysis*
Esters / chemical synthesis
Magnetic Resonance Spectroscopy
Mass Spectrometry
Tablets
Tartrates
Chemical
Reg. No./Substance:
0/Citrates; 0/Esters; 0/Tablets; 0/Tartrates; 526-83-0/tartaric acid; 76-57-3/Codeine; 77-92-9/Citric Acid

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


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