Synthesis, kinetic studies and pharmacological evaluation of mutual azo prodrugs of 5-aminosalicylic acid for colon-specific drug delivery in inflammatory bowel disease.
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.
Dhaneshwar
Suneela S
SS
Department of Pharmaceutical Chemistry, Bharati Vidyapeeth University, Poona College of Pharmacy, Pune 411038, Maharashtra, India. suneeladhaneshwar@rediffmail.com
Gairola
Neha
N
Kandpal
Mini
M
Vadnerkar
Gaurav
G
Bhatt
Lokesh
L
Rathi
Badal
B
Kadam
S S
SS
D000636:Aminosalicylic Acids / Q000138:chemical synthesis* / Q000627:therapeutic use*; D000818:Animals; D001168:Arthritis / Q000139:chemically induced / Q000188:drug therapy; D003092:Colitis / Q000139:chemically induced / Q000188:drug therapy; D003106:Colon / Q000187:drug effects / Q000473:pathology; D005260:Female; D015212:Inflammatory Bowel Diseases / Q000139:chemically induced / Q000188:drug therapy*; D008297:Male; D009195:Peroxidase / Q000378:metabolism; D011355:Prodrugs / Q000138:chemical synthesis* / Q000627:therapeutic use*; D051381:Rats; D017208:Rats, Wistar; D014456:Ulcer / Q000188:drug therapy / Q000473:pathology
D000636:Aminosalicylic Acids; D011355:Prodrugs; D009195:Peroxidase