Aceclofenac and Diclofenac Sodium Conjugates with Amino Acids to Overcome Acidity

Shuchi Jain; Amreen Khan; Paridhi Jain

Abstract

This research work was based on a conjugate approach with some non-steroidal anti-inflammatory drugs (NSAIDs) to overcome the side effects like gastric irritation, solubility behavior, and some other effects of NSAIDs. Almost all the NSAIDs have undesirable reactions as well as they cause some types of major adverse reactions. Here the prodrugs conjugates are the approaches that increase the lipophilicity of the drug and decrease the solubility in water by decreasing the concentration gradient, by this absorption of the drug is controlled. We have synthesized some conjugated derivatives and all the derivatives were confirmed by TLC, solubility, partition coefficient, UV, and IR spectroscopy. This approach is used to increase the lipophilicity of those drugs which cause lower water solubility. These types of conjugates are prepared by a conventional method using N,N-dicyclo-hexyl carbodiimide, and this method is characterized by melting point, TLC, and UV and NMR spectroscopy methods. In this method, we found that aceclofenac conjugates have maximum water solubility and having less side effects. The partition coefficient seems to be more than that parent compound. So that the present work shows that the conjugates with amino acids were more water soluble and had stability in the given pH profile and in that pH, it shows an increased rate of hydrolysis. The results of the current study reveal that the amino acid-conjugated derivatives that were produced have increased water solubility. This method can be used in the future to reduce the side effects of additional NSAIDs and improve their solubility in water. In the future, this study must be concluded the mechanism of action and efficiency study of compounds on different animals.

Abstract

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