Synthesis, characterization, release kinetics, pharmacological screening and in-silico adme prediction of mutual prodrugs of aceclofenac

Velingkar, Yadav
2014 Journal of Chemical and Pharmaceutical Research   unpublished
Mutual Prodrugs of some non-steroidal anti-inflammatory agent NSAID i.e. Aceclofenac with Salicylamide, Thymol and Glucosamine, were synthesized with the aim of improving the therapeutic index through prevention of gastrointestinal implications and to check the efficiency of release of the parent drug in presence of spacer as well as without spacer. These mutual prodrugs were synthesized by direct condensation method using dicyclohexylcarbodiimide as a coupling agent and alanine as spacer. The
more » ... ine as spacer. The title compounds were characterized by spectral techniques and the release of the parent drug from mutual prodrug was studied in two different non-enzymatic buffer solutions at pH 1.2, pH 7.4 and in 80% human plasma. All mutual prodrugs exihibited encouraging hydrolysis profile in 80% human plasma. Biological activity of title compounds was studied by carrageenan-induced rat paw edema method. From the results obtained, it was concluded that these compounds possess the Anti-inflammatory action.