Prodrug design of NSAIDs: synthesis and pharmacological profiles of amide prodrugs of etodolac with amino acids
Novel amide prodrugs of etodolac with various amino acids were synthesized and the structures were confirmed by elemental and spectral analyses. In vitro hydrolytic studies in various simulated fluids confirmed the hydrolysis of prodrugs in colon. The prodrugs showed an improved anti-inflammatory...
Guardado en:
| Autores principales: | , , , |
|---|---|
| Formato: | Articulo |
| Lenguaje: | Inglés |
| Publicado: |
2011
|
| Materias: | |
| Acceso en línea: | http://sedici.unlp.edu.ar/handle/10915/8103 http://www.latamjpharm.org/resumenes/30/1/LAJOP_30_1_1_11.pdf |
| Aporte de: |
| Sumario: | Novel amide prodrugs of etodolac with various amino acids were synthesized and the structures
were confirmed by elemental and spectral analyses. In vitro hydrolytic studies in various simulated
fluids confirmed the hydrolysis of prodrugs in colon. The prodrugs showed an improved anti-inflammatory
activity of 74.4 %, 79.3 %, 73.4 % and 74.5 % when compared to 42.5 % of etodolac. Further the mean
ulcer index of 10.1, 8.7, 6.8 and 7.3 were observed for the prodrugs while a score of 22.6 for etodolac. The
histopathological studies showed less ulceration in the gastric region when treated with prodrugs, thereby
proving the prodrugs to be better in action as compared to etodolac and are advantageous in having less
gastrointestinal side effects. |
|---|