Curcio, Annalisa and Sasso, Oscar and Melisi, Daniela and Nieddu, Maria and La Rana, Giovanna and Russo, Roberto Cosimo and Gavini, Elisabetta and Boatto, Gianpiero and Abignente, Enrico and Calignano, Antonio and Rimoli, Maria Grazia (2009) Galactosyl prodrug of ketorolac: synthesis, stability, and pharmacological and pharmacokinetic evaluations. Journal of Medicinal Chemistry, Vol. 52 (12), p. 3794-3800. eISSN 1520-4804. Article.
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Although ketorolac is one of the most potent anti-inflammatory and analgesic drugs, its use has been strongly limited owing to the high incidence of adverse effects reported, particularly in the gastrointestinal tract. Using the prodrug approach, which allows the reduction of toxicological features of the parent drug without altering its pharmacological properties, we synthesized an orally administrable prodrug of ketorolac by means of its reversible conjugation to d-galactose (ketogal). In a single dose study, its pharmacokinetic profile was compared with that of ketorolac. Moreover, we found that this prodrug was able to maintain the anti-inflammatory and the analgesic activity of the drug without giving rise to gastric ulcer formation. Thus, these results indicate that ketogal is a highly effective and valid therapeutic alternative to ketorolac itself.
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