Abstract

IMPROVEMENT OF PHYSICHOCHEMICAL PROPERTIES OF ACECLOFENAC BY DEVELOPING NOVEL AMINOACID CONJUAGATES

Naeemurrahman M.*¹, Ashish. N. Phuge²

ABSTRACT

The purpose of present research work is to improve physicochemical properties of aceclofeanc by amino acid conjugation and to overcome general side effects of NSAID’S. Conversion of drug to prodrug is a chemically modified inert drug precursor, which upon biotransformation leads to activation and produce pharmacological effects. Present research work stands for modification to overcome pharmaceutical barriers like solubility, poor lipophilicity etc. Though the amino acid conjugates comes under prodrug but it overcomes the limitation of prodrug such as formation of unexpected metabolite and undesirable side effects. Serine-Aceclofenac conjugate has maximum water solubility, while in methanol and chloroform solubility of remaining synthesized conjugates shows greater result than parent conjugate. The partition coefficients of some of the synthesized conjugates in octanol/water system was found to be more than the parent drug .present research work indicates the conjugates synthesized with hydrophilic amino acid possess more water solubility .In future this approach can be applied to other NSAID’S having free carboxyl group as well as in vivo bioavailability study can be undertaken in animals and can be correlate in humans.

Keywords: Aceclofenac, amino acids, bioavailability, conjugates, prodrug, synthesis.