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Título : Pharmacokinetics of a cephalone (CQ-M-EPCA) in rats after oral, intraduodenal and intravenous administration
Creador: Pérez Guillé B
Nivel de acceso: Open access
Palabras clave : Agentes antibacterianos - Administración y dosificación
Cromatografía Líquida de Alta Presión
Duodeno - Metabolismo
Anti-Bacterial Agents - Administration & dosage
Chromatography, High Pressure Liquid
Duodenum - Metabolism
Farmacocinética
Cefalona
CQ-M-EPCA
Rata
Pharmacokinetics
Cephalone
CQ-M-EPCA
Rat
Descripción : As part of the development of a new series of antibacterial agents derived from coupling a β-lactamic precursor with a fluoroquinolone and named cephalones, the pharmacokinetics of one derivate: CQ-M-EPCA in rats after intravenous, intragastric and intraduodenal routes, was carried out. After the IV injection of 20 mg/kg or 40 mg/kg of this cephalone, plasma concentrations at the time zero (Cp0) were 3.1 and 11.26 μg/ml, respectively. Plasma concentrations decreased rapidly to almost disappear in both instances. Forty-five minutes later, a surge in concentrations, in the 40 mg/kg group, with a maximal plasma concentration (Cpmax) of 2.97 μg/ml was observed. An elimination half-life (T(1/2)el) of 2.36 ± 0.33 h. was calculated. The drug was undetected by the ninth hour. Intragastric administration of the drug resulted in Cpmax of 3.78 ± 0.26 μg/ml with a time to reach Cpmax (Tmax) of 25 min and T(1/2)el = 3.22 h. Same variables after intraduodenal administration were Cpmax 4.71 μg/ml; Tmax 1 h, and T (1/2)el 3.41 h. Outstandingly high bioavailabilities after intragastric and intraduodenal administration (169 and 246%, respectively), together with the shape of the concentration versus time profiles after IV administration suggest that the drug undergoes a complex redistribution phenomenon, while showing high tissue diffusion with an apparent volume of distribution of 3.33 l/kg. © 2004 Elsevier B.V. All rights reserved.
Colaborador(es) u otros Autores: Sumano LH
Villegas-Alvarez F
Soriano-Rosales R
González-Zamora JF
Jiménez-Bravo-Luna M
Carmona-Mancilla A
Ocampo CL.
Fecha de publicación : 2004
Tipo de publicación: Artículo
Formato: pdf
Identificador del Recurso : 10.1016/j.ijpharm.2004.06.001
Fuente: International Journal of Pharmaceutics 282(42767):87-94
URI : http://repositorio.pediatria.gob.mx:8180/handle/20.500.12103/2685
Idioma: eng
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