Synthesis and Evaluation of Glyceride Prodrugs of Naproxen

Vivekkumar K. Redasani, Sanjay B. Bari

H. R. Patel Institute of Pharmaceutical Education and Research, Shirpur, India.
R. C. Patel Institute of Pharmaceutical Education and Research, Shirpur, India.

DOI: 10.4236/ojmc.2013.33011                

Abstract

The glyceride ester derivatives 6a and 6b were prepared by reacting 1,2,3-trihydroxy propane 1,3-dipalmitate/stearate with (S)-naproxen as potential prodrugs. The synthesis was achieved successfully with the aid of N,N’-dicyclohexyl- carbodiimide. These prodrugs were evaluated for anti inflammatory, analgesic and gastroprotective activity. It was found that prodrugs 6a and 6b showed less irritation to gastric mucosa as indicated by ulcer index. The synthesized glyceride esters were found to possess good pharmacological profile as shown by results of anti inflammatory and analgesic activity. The aqueous studies were performed in order to ensure the release of prodrugs. Both prodrugs were found to stable at acidic pH while undergoes hydrolysis at pH 7.4. These findings suggest that the glyceride prodrugs 6a and 6b might be used as potential biolabile derivatives.

Keywords

Naproxen; Glyceride Prodrugs; Anti-Inflammatory; Analgesic; Gastroprotective; Hydrolysis Kinetics

Conflicts of Interest

The authors declare no conflicts of interest.

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