Separation of therapeutic effects from toxicity is a valuable goal in the drug development process. Prodrug design is a part of the general drug discovery process, in which a unique combination of therapeutically active substances is observed to have desirable pharmacological effects. In human therapy prodrug designing has given successful results in overcoming undesirable properties like absorption, nonspecificity, and poor bioavailability and GIT toxicity. Prodrug design is opening new doors in the challenging field of drug discovery, revolutionizing the art of Drug development.In this dissertation work, Synthesis of amide prodrugs of Niflumic acid and Ketoprofen with Glucosamine was achieved in good yields by a simple technique.Here prodrug approach has been successfully applied in attaining the goal of minimized gastrointestinal toxicity without loss of desired anti-inflammatory activities of the drug.