Majority of the agents which are non-selective COX-1 and COX-2 inhibitors, shares the undesirable effect to gastric and intestinal mucosa, resulting in erosion, ulcers and represent the major adverse reactions to the use of NSAIDs. The belief behind this book is to bring in one new method for upgrading solubility behavior by amino acid conjugation and thereby overcome general side effects of NSAID. Prodrug is a chemically modified inert drug precursor, which upon biotransformation lead to activation and produce pharmacological action. In this book prodrug approach stands for modification to overcome pharmaceutical barriers like solubility behavior. Even if the amino acid conjugates formerly classified under prodrug but it defeat the limitation of them such as formation of unforeseen metabolite and disagreeable side effects. Some conjugate has maximum water solubility than parent compound. The partition coefficient of the synthesized compound was found to be more than the parent drug. It indicates that conjugates synthesized with hydrophilic amino acid possess more water solubility. In future this approach can be applied to other NSAIDs having free carboxyl functional group.