Document Detail


Synthesis and properties of dextran-5-aminosalicylic acid ester as a potential colon-specific prodrug of 5-aminosalicylic acid.
MedLine Citation:
PMID:  9875428     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Dextran-5-aminosalicylic acid ester (dextran-5-ASA) was synthesized as a colon-specific prodrug of 5-aminosalicylic acid (5-ASA) which is active against inflammatory bowel diseases. Chemical stability of dextran-5-ASA in the bath of pH 1.2 or 6.8 was investigated at 37 degrees C for 6 hrs, and 5-ASA was not released on such conditions. Depolymerization (%) of dextran-5-ASA by dextranase with the degree of substitution (DS) of 18, 23, or 30 was 92, 62 or 45 in 8 hrs respectively, but was not affected by the MW of dextran (9,000, 40,600, 80,200 or 580,000). Distribution of 5-ASA in dextran, determined by gel filtration chromatography, appeared to be relatively uniform. Incubation of dextran-5-ASA (DS 18) in cecal contents of rats released 20% (28 g) and 35% (49 g) of 5-ASA in 8 hrs and 24 hrs, respectively, but no 5-ASA was liberated from small intestinal contents.
Authors:
Y J Jung; J S Lee; H H Kim; Y T Kim; Y M Kim
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Archives of pharmacal research     Volume:  21     ISSN:  0253-6269     ISO Abbreviation:  Arch. Pharm. Res.     Publication Date:  1998 Apr 
Date Detail:
Created Date:  1999-02-04     Completed Date:  1999-02-04     Revised Date:  2003-11-14    
Medline Journal Info:
Nlm Unique ID:  8000036     Medline TA:  Arch Pharm Res     Country:  KOREA    
Other Details:
Languages:  eng     Pagination:  179-86     Citation Subset:  IM    
Affiliation:
College of Pharmacy, Pusan National University, Korea.
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MeSH Terms
Descriptor/Qualifier:
Aminosalicylic Acids / chemical synthesis*,  pharmacokinetics
Animals
Buffers
Calibration
Cecum / metabolism
Chromatography, High Pressure Liquid
Colon / metabolism*
Dextrans / chemical synthesis*,  pharmacokinetics
Male
Mesalamine / chemical synthesis*,  pharmacokinetics
Prodrugs / chemical synthesis*,  pharmacokinetics
Rats
Rats, Sprague-Dawley
Spectrophotometry, Ultraviolet
Stomach / metabolism
Chemical
Reg. No./Substance:
0/Aminosalicylic Acids; 0/Buffers; 0/Prodrugs; 0/dextran-5-aminosalicylic acid; 89-57-6/Mesalamine; 9004-54-0/Dextrans

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