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The importance of metabolism in drug design. Galeno Research Unit, R. It is widely recognized that pharmacokinetic optimization needs to be addressed early in drug discovery to reduce the high failure rate in bringing drugs to market. Poor absorption, too short duration of action due to high elimination rate, or the presence of active metabolites are examples of properties that can potentially lead to unsuccessful clinical programmes. Here I describe a brief overview of advantages and molecular strategies for improving metabolic and pharmacokinetic properties applied to the discovery of fluconazol, b -blockers, ritonavir and ezetimibe and to the development of the prodrugs enalapril and bambuterol. Keywords: drug metabolism; drug design; structure-metabolism relationship.

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The importance of metabolism in drug design. Galeno Research Unit, R. It is widely recognized that pharmacokinetic optimization needs to be addressed early in drug discovery to reduce the high failure rate in bringing drugs to market. Poor absorption, too short duration of action due to high elimination rate, or the presence of active metabolites are examples of properties that can potentially lead to unsuccessful clinical programmes.

Here I describe a brief overview of advantages and molecular strategies for improving metabolic and pharmacokinetic properties applied to the discovery of fluconazol, b -blockers, ritonavir and ezetimibe and to the development of the prodrugs enalapril and bambuterol.

Keywords: drug metabolism; drug design; structure-metabolism relationship. Como veremos adiante, diversas vantagens surgem destas abordagens. Quando administrados por via oral, entretanto, estes compostos ex. A descoberta dos b -bloqueadores. A descoberta do ritonavir. A descoberta da ezetimiba. Abdel-Rahman, S. Smith, D. Drug Metab. Masimirembwa, C. Prentis, R. Chaikin, P. Korolkovas, A. Guanabara: Rio de Janeiro, , cap. Albert, A. Barreiro, E. Artmed: Porto Alegre, , cap.

Low, L. Lin, J. Nassar, A. Today , 9 , Testa, B. Bundgaard, H. Richardson, K. Humphrey, M. Lyman, C. Agents Chemother. Bomont, H. Manoury, P. Riddell, J.

Benfield, P. Johnson, R. Em ref. Hoffman, B. Bodor, N. Smith, F. Kempf, D. Raffanti, S. Clader, J. Waller, D. Chin, C. Nova , 22 , Ferreira, E. Drug Deliv. Patchett, A. Kubo, S. Ranadive, S. Tegner, K. Svensson, L. Persson, G. Manuila, L. Wermuth, C. Penildon, S. Em Farmacologia ; Penildon, S. Solomons, G. Hardman, J. All the contents of this journal, except where otherwise noted, is licensed under a Creative Commons Attribution License.

Services on Demand Journal. Secretaria Executiva Av. How to cite this article.

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Biofarmacéutica

Como prueba de control de calidad rutinaria para ciertos tipos de productos medicinales p. Para apoyar exenciones para otros requisitos de bioequivalencia. Para productos medicinales poco solubles en agua p. Las CMV. La prueba in vitro sirve como herramienta para distinguir entre productos medicinales aceptables e inaceptables. Por lo general, los valores de f1 de hasta 15 y los valores de f2 mayores de 50 aseguran la igualdad o equivalencia de las dos curvas y, por lo tanto, del rendimiento de los productos de prueba posteriores al cambio y referencia anteriores al cambio. Se sugieren los siguientes pasos:.

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