Document Detail

Synthesis and properties of polysaccharide prodrugs of 5-aminosalicylic acid as potential colon-specific delivery systems.
MedLine Citation:
PMID:  15567313     Owner:  NLM     Status:  MEDLINE    
The drug release of the polymer prodrugs of 5-aminosalicylic acid (5-ASA) was not only dependent on the property of the polymers but also dependent on the solubility of the prodrugs. We prepared several polysaccharide prodrugs of 5-ASA to examine the effect of solubility of prodrugs on the release characteristics of 5-ASA in the gastrointestinal contents of rats. The amide prodrug, chitosan-5-ASA (ChT-5-ASA), did not release the 5-ASA in the cecal and colonic contents. The ester prodrugs, hydroxypropyl cellulose-5-ASA (HPC-5-ASA), being poor solubility in 0.05mol/l acetic acid solution also did not release the 5-ASA in any of gastrointestinal contents of rats. Whereas the 5-ASA release from cyclodextrins-5-ASA (CyDs-5-ASA) in cecal and colonic contents was significantly higher than that in stomach and small intestine contents. And furthermore, with the decrease in the degree of substitution, the solubility of CyD-5-ASA increased, and the release of 5-ASA in the gastrointestinal contents was also higher at the same time interval of incubation. When the ratio of cyclodextrin (CyD) and 5-formylaminosalicylic acid (5-fASA), a precursor of 5-ASA prodrugs, was 1:10, CyD-5-ASA was very slightly soluble, and no release of 5-ASA was observed within 48h in gastrointestinal contents. The present results suggested that the ester prodrugs of 5-ASA with certain solubility could release 5-ASA in the cecal and colonic contents of rat.
Meijuan Zou; Hirokazu Okamoto; Gang Cheng; Xiuhua Hao; Jin Sun; Fude Cui; Kazumi Danjo
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft für Pharmazeutische Verfahrenstechnik e.V     Volume:  59     ISSN:  0939-6411     ISO Abbreviation:  Eur J Pharm Biopharm     Publication Date:  2005 Jan 
Date Detail:
Created Date:  2004-11-29     Completed Date:  2005-04-19     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9109778     Medline TA:  Eur J Pharm Biopharm     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  155-60     Citation Subset:  IM    
School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, China.
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MeSH Terms
Colon / drug effects,  metabolism*
Drug Delivery Systems / methods*
Mesalamine / administration & dosage,  chemical synthesis*,  pharmacokinetics
Polysaccharides / administration & dosage,  chemical synthesis*,  pharmacokinetics
Prodrugs / administration & dosage,  chemical synthesis*,  pharmacokinetics
Rats, Sprague-Dawley
Reg. No./Substance:
0/Polysaccharides; 0/Prodrugs; 89-57-6/Mesalamine

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