Synthesis, kinetic studies and pharmacological evaluation of mutual azo prodrugs of 5-aminosalicylic acid for colon-specific drug delivery in inflammatory bowel disease

被引:41
作者
Dhaneshwar, Suneela S. [1 ]
Gairola, Neha [1 ]
Kandpal, Mini [1 ]
Vadnerkar, Gaurav [1 ]
Bhatt, Lokesh [2 ]
Rathi, Badal [2 ]
Kadam, S. S. [1 ]
机构
[1] Bharati Vidyapeeth Univ, Poona Coll Pharm, Dept Pharmaceut Chem, Pune 411038, Maharashtra, India
[2] Bharati Vidyapeeth Univ, Poona Coll Pharm, Dept Pharmacol, Pune 411038, Maharashtra, India
关键词
Mutual azo prodrug; 5-Aminosalicylic acid; Amino acids; Inflammatory bowel disease; ULCERATIVE-COLITIS; RECTAL DELIVERY; METAANALYSIS; OLSALAZINE; DICLOFENAC; THERAPY; MODELS; AGENTS; RATS;
D O I
10.1016/j.ejmech.2009.04.018
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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. (C) 2009 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码:3922 / 3929
页数:8
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