Abstract

SYNTHESIS, CHARACTERIZATION AND RELEASE STUDIES OF MUTUAL PRODRUGS OF NORFLOXACIN AND TRIMETHOPRIM WITH ASPIRIN FOR COLON RELEASE

Arshi Hussain*, Pradeep Parashar, Anil Kumar Shrivastava

ABSTRACT

Non-steroidal anti-inflammatory drugs (NSAIDs) and Antibiotics are commonly used for the treatment of Intestinal bowel diseases (IBD) such as ulcerative colitis, crohn’s disease etc. Prodrug designing is one of the several approach used to treat such colonic diseases. However, mutual prodrug concept also can be exploited for this purpose. In view of this context, mutual amide prodrugs of norfloxacin with aspirin (AN) and trimethoprim with aspirin (AT) were synthesized by coupling method. Their physico-chemical characterizations were carried out by analytical and spectral methods. In vitro release study of the synthesized derivatives was done in different simulated fluids to identify the expected hydrolysis of these mutual prodrugs in gastrointestinal tract. It was revealed that these compounds were chemically stable in simulated gastrointestinal fluid and an appreciable release of drugs was observed in simulated colonic fluid with 74.29 % from AN and 79.21 % from AT, although, simulated intestinal fluid reported a little release of drugs. So, the purpose of targeting the drugs to colon for treating infection as well as inflammation may be achieved.

Keywords: IBD, Mutual prodrugs, Norfloxacin, Trimethoprim, Aspirin, colon-targeting.