| Synthesis and properties of N,N'-bis(5-aminosalicyl)-L-cystine as a colon-specific deliverer of 5-aminosalicylic acid and cystine. | |
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MedLine Citation:
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PMID: 18197522 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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N,N(')-bis(5-aminosalicyl)-L-cystine (5-ASA-Cys) was prepared by a simple synthetic route. 5-ASA-Cys was not degraded in pH 1.2 and 6.8 buffer solutions, and in the homogenates of the upper intestine. In marked contrast, 5-ASA-Cys was deconjugated extensively to liberate 5-ASA in the cecal contents. Upon oral administration of 5-ASA-Cys to rats, the plasma concentration of 5-ASA-Cys was extremely low and the urinary recovery of 5-ASA-Cys was approximately 10% of the dose. These results suggest that 5-ASA-Cys administered orally is delivered efficiently to the large intestine followed by deconjugation to liberate 5-ASA and cystine. |
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Authors:
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Heejung Kim; Duksoo Kim; Daekyu Choi; Hyunchu Jeon; Jungoh Han; Yunjin Jung; Hyesik Kong; Young Mi Kim |
Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Drug delivery Volume: 15 ISSN: 1071-7544 ISO Abbreviation: Drug Deliv Publication Date: 2008 Jan |
Date Detail:
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Created Date: 2008-01-16 Completed Date: 2008-05-19 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9417471 Medline TA: Drug Deliv Country: United States |
Other Details:
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Languages: eng Pagination: 37-42 Citation Subset: IM |
Affiliation:
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Laboratory of Biomedicinal, College of Pharmacy, Pusan National University, Busan, Korea. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Administration, Oral Aminosalicylic Acids / administration & dosage, chemical synthesis, pharmacokinetics* Animals Anti-Inflammatory Agents / administration & dosage, chemical synthesis, pharmacokinetics* Biotransformation Cecum / metabolism Colon / metabolism* Cystine / administration & dosage, analogs & derivatives*, chemical synthesis, pharmacokinetics Drug Stability Gastrointestinal Agents / administration & dosage, chemical synthesis, pharmacokinetics* Hippurates / pharmacokinetics Hydrogen-Ion Concentration Intestinal Absorption* Intestine, Small / metabolism Male Prodrugs / administration & dosage, chemical synthesis*, metabolism Rats Rats, Sprague-Dawley Stomach / metabolism |
| Chemical | |
Reg. No./Substance:
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0/5-aminosalicyl-glycine; 0/Aminosalicylic Acids; 0/Anti-Inflammatory Agents; 0/Gastrointestinal Agents; 0/Hippurates; 0/N,N'-bis(5-aminosalicyl)cystine; 0/Prodrugs; 56-89-3/Cystine |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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