Journal of Chemical and Pharmaceutical Research (ISSN : 0975-7384)

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Original Articles: 2010 Vol: 2 Issue: 6

Synthesis and evaluation of some amino acid conjugates of NSAIDS


The purpose of present research work is to improve solubility behavior by amino acid conjugation and to overcome general side effects of NSAID. Conversion of drug to prodrug is a chemically modified inert drug precursor, which u pon biotransformation lead to activation and produce pharmacological action. Present prodrug approach stands for modification to overcome pharmaceutical barriers like solubility be havior. Though the amino acid conjugates comes under prodrug but it overcome the limitation of prodrug such as formation of unexpected metabolite and undesirable side effec ts. Tryptophan-Aceclofenac conjugate has maximum water solubility, while in methanol and chl oroform solubility of remaining synthesized compounds shows greater result than par ent compound. The partition coefficient of some the synthesized compound in octanol/water s ystem was found to be more than the parent drug. Present research work indicates that c onjugates synthesized with hydrophilic amino acid possess more water solubility. In future this approach can be applied to other NSAID having free carboxyl functional group as well as in vivo bioavailability study can be undertaken in animals and can be correlated in huma ns