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  • Title: Synthesis, kinetic studies and pharmacological evaluation of mutual azo prodrugs of 5-aminosalicylic acid for colon-specific drug delivery in inflammatory bowel disease.
    Author: Dhaneshwar SS, Gairola N, Kandpal M, Vadnerkar G, Bhatt L, Rathi B, Kadam SS.
    Journal: Eur J Med Chem; 2009 Oct; 44(10):3922-9. PubMed ID: 19442419.
    Abstract:
    Colon-specific mutual azo prodrugs of 5-aminosalicylic acid with essential amino acids were synthesized for the management of inflammatory bowel disease. The structures were confirmed by elemental and spectral analyses. 85-88% release of 5-aminosalicylic acid was achieved in rat fecal matter with half-lives ranging from 140 to 160 min, following first order kinetics. The prodrugs exhibited comparable ameliorating effect as that of sulfasalazine on trinitrobenzenesulfonic acid-induced experimental colitis in rats with a better safety profile.
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