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

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 44卷 / 10期

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

页码：3922 / 3929

页数：8

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