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Chem Biol Drug Des ; 87(6): 878-84, 2016 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-26715009

RESUMEN

This study investigates anti-inflammatory activity with improved pharmacokinetic and non-ulcerogenic properties of various novel synthesized prodrugs of ketoprofen in experimental animals. Prodrugs 3a, 3f and 3k were found to possess significant anti-inflammatory activity with almost non-ulcerogenic potential than standard drug ketoprofen (1) in both normal and inflammation-induced rats. The experimental findings elicited higher AUC and plasma concentration at 1 and 2 h indicating improved oral bioavailability as compared to parent drug ketoprofen. These prodrugs are found to have no gastric ulceration with retained anti-inflammatory activity. Therefore, present experimental findings demonstrated significant improvement of various pharmacokinetic properties with non-ulcerogenic potential of ester prodrugs of ketoprofen.


Asunto(s)
Cetoprofeno , Profármacos , Administración Oral , Animales , Evaluación Preclínica de Medicamentos , Cetoprofeno/efectos adversos , Cetoprofeno/síntesis química , Cetoprofeno/química , Cetoprofeno/farmacocinética , Ratones , Profármacos/efectos adversos , Profármacos/síntesis química , Profármacos/química , Profármacos/farmacocinética , Ratas , Sigmodontinae , Úlcera Gástrica/sangre , Úlcera Gástrica/inducido químicamente
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