Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
|
pubmed:dateCreated |
1999-2-4
|
pubmed:abstractText |
As a new colon-specific prodrug of 5-aminosalicylic acid (5-ASA), 5-aminosalicyl-glycine (5-ASA-Gly) was prepared by a simple synthetic route in good yield. Apparent partition coefficients of 5-ASA-Gly were lower than those of 5-ASA, which determined in CHCl3/pH 6.8 buffer or n-octanol/pH 6.8 buffer system. Stability of 5-ASA-Gly by peptidases was investigated by incubation of 5-ASA-Gly with the homogenates of tissue and contents of stomach, proximal small intestine or distal small intestine of rats at 37 degrees C. 5-ASA was not detected, indicating that the prodrug was stable in the upper intestine. The amount of 5-ASA liberated from incubation of the prodrug in cecal or colonic contents of rats was about 65% or 27% in 8 hrs, respectively, which indicated that the prodrug activation took place more readily in the rat cecum whose bacterial counts are high like human colon. Results from in vitro experiments suggested 5-ASA-Gly as a promising candidate of a colon-specific prodrug of 5-ASA.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Aminosalicylic Acids,
http://linkedlifedata.com/resource/pubmed/chemical/Buffers,
http://linkedlifedata.com/resource/pubmed/chemical/Hippurates,
http://linkedlifedata.com/resource/pubmed/chemical/Mesalamine,
http://linkedlifedata.com/resource/pubmed/chemical/Prodrugs
|
pubmed:status |
MEDLINE
|
pubmed:month |
Apr
|
pubmed:issn |
0253-6269
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:volume |
21
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
174-8
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
pubmed-meshheading:9875427-Aminosalicylic Acids,
pubmed-meshheading:9875427-Animals,
pubmed-meshheading:9875427-Buffers,
pubmed-meshheading:9875427-Calibration,
pubmed-meshheading:9875427-Cecum,
pubmed-meshheading:9875427-Chromatography, High Pressure Liquid,
pubmed-meshheading:9875427-Colon,
pubmed-meshheading:9875427-Hippurates,
pubmed-meshheading:9875427-Male,
pubmed-meshheading:9875427-Mesalamine,
pubmed-meshheading:9875427-Prodrugs,
pubmed-meshheading:9875427-Rats,
pubmed-meshheading:9875427-Rats, Sprague-Dawley,
pubmed-meshheading:9875427-Spectrophotometry, Ultraviolet,
pubmed-meshheading:9875427-Stomach
|
pubmed:year |
1998
|
pubmed:articleTitle |
Synthesis and evaluation of 5-aminosalicyl-glycine as a potential colon-specific prodrug of 5-aminosalicylic acid.
|
pubmed:affiliation |
College of Pharmacy, Pusan National University, Korea.
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|