Inflammatory Bowel Disease Preventative Development

The long-term objective of this project is to commercially develop a target-specific chemopreventatinflammatory bowel diseases that works by releasing the therapeutic agents directly in the lower intsite of the disease. It is noted that ulcerative colitis and Crohn's disease are the most severe infno truly effective preventative measures are available. It is indicated that the substance to be synchemical conjugate of the bile acid ursodeoxycholic acid (UDCA) and the nonsteroidal anti-inflammatodrug (NSAID) 5-amino- salicylic acid (5-ASA). The principal investigator reports that animal and humUDCA and anti-inflammatory/anti-infective 5- ASA have shown that each has the potential to reduce thinflammation and that thus UDCA-5ASA is expected to be effective in preventing inflammatory bowel disuperior to the individual substances since the preventative agents are not released in active formintestine and the colon. It is indicated that here, UDCA-5ASA will be activated by enzymes producedmicroflora to release UDCA and 5-ASA in high localized concentration. It is suggested that this targthe delivery of therapeutically effective and smaller doses of the drug to the target site, thus redspecific goal of this application is to synthesize quantities of UDCA-5ASA for subsequent in vivo Phtests of the effectiveness and safety of the compound. It is noted that methods for the synthesis ofbe tailored for the efficient production of batches of UDCA-5ASA to produce the required 1.5 kg. Thestates that to ascertain bioavailability and targeted release of UDCA and 5-ASA, the compound and powill be subjected to conditions simulating the stomach, small intestine and lower intestine to assurmodified until it reaches its target site, the lower intestine, where it is hydrolyzed by bacterial5-ASA.