Farmacocinética y biodisponibilidad de ceftiofur sódico en caprinos

Authors

  • Carlos Errecalde
  • Guillermo Prieto
  • Carlos Lüders
  • Hugo García

DOI:

https://doi.org/10.17533/udea.rccp.324084

Keywords:

ceftiofur, cephalosporins, goats, Pasteurella spp, pharmacokinetics

Abstract

Resumen

Se determinaron parámetros farmacocinéticos de ceftiofur sódico con dosis única de 2.2 mg/kg por vía intravenosa e intramuscular, en un diseño cruzado de tratamiento en hembras caprinas adultas no gestantes (n= 6). Las concentraciones plasmáticas en función del tiempo se determinaron por el método microbiológico de difusión en agar utilizando medio Mueller-Hinton y Providencia alcalifaciens, cuyo límite de cuantificación se estableció en 0.039 μg/ml. Los datos de concentración plasmática de ceftiofur en función del tiempo se analizaron por el modelo farmacocinético no compartimental utilizando el sofware PK Solution 2.0. Los parámetros obtenidos para la vía intravenosa fueron: vida media de eliminación (t1/2 B) = 1.63 ± 0.04 horas, clearance total (Cltot) = 3.3 ± 1.1 ml/kg/min, volumen de distribución  (Vdss) = 0.38 ± 0.19 L/kg, área bajo la curva (ABC) = 716.5 ± 225.5 μg/min/ml. Estos valores no difieren significativamente de los obtenidos del ensayo intramuscular (p < 0.05) y son similares a los informados en otras especies animales con ceftiofur. En el ensayo intramuscular se obtuvo una concentración máxima (Cmáx) de 3.6 ± 0.5 μg/ml, con un tiempo máximo (tmáx) de 0.53 ± 0.31 horas y elevada biodisponibilidad  (97.6 ± 0.1%). Los resultados indican que la aplicación intramuscular provee rápida absorción y óptima biodisponibilidad, generando niveles plasmáticos que exceden la concentración inhibitoria mínima (CIM) de patógenos respiratorios sensibles durante 12 horas. Considerando estos resultados y la  CIM90 (≤ 0.06 μg/ml) frente a bacterias como Pasteurella haemolitica y P. multocida, se propone como tratamiento de este tipo de cuadros infecciosos en caprinos, una dosis de mantenimiento de 1.3 mg/kg cada 12 horas por vía intramuscular, cuyo predictor de eficacia (t > CIM) se calculó en 77.8 %.

Summary

Pharmacokinetic parameters of ceftiofur sodium were determined with a unique dose of 2.2 mg/kg either by the intravenous on the intramuscular routes, in a crossed design treatment in non pregnant adult female goats (n= 6). Variations in plasmatic concentrations over time were determined by the microbiological assay in Mueller-Hinton agar, with Providencia alcalifaciens as indicator. The limit of quantification was set in 0.039 mg/ml. The plasmatic concentrations of Ceftiofur were determined by the non compartimental pharmacokinetic model using sofware PK Solution 2.0. The parameters obtained when the intravenous route was used were: average elimination time (t1/2 B) = 1.63 ± 0.04 hours, total clearance (Cltot) = 3.3 ± 1.1 ml/kg/min, volume of distribution (Vdss) = 0.38 ± 0.19 L/Kg, area under the curve (ABC) = 716.5 ± 225.5 mg/min/ml. These values did not differ significantly from those obtained by the intramuscular test (P < 0.05) and are similar to those informed in other animal species for the same drug. When the intramuscular route was used, the maximum concentration (Cmáx) of 3.6 ± 0.5 mg/ml was obtained at a maximum time (tmáx) of 0.53 ± 0.31 min, and the bioavailability was high (97.6 ± 0.1%). The results indicate that the intramuscular application provides fast absorption and optimal bioavailability, generating plasmatic levels that exceed the MIC90 for sensitive respiratory pathogens for a period of 12 hours. Considering these results and a MIC (≤ 0.06 mg/ml) for bacteria like Pasteurella haemolitica and P. multocida, the treatment of this type of infections in goats, requires 1.3 mg/Kg every 12 hours by intramuscular route, to obtain a predictive effectiveness (t > MIC) of 77.8%.

 

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Published

2016-07-22

How to Cite

Errecalde, C., Prieto, G., Lüders, C., & García, H. (2016). Farmacocinética y biodisponibilidad de ceftiofur sódico en caprinos. Revista Colombiana De Ciencias Pecuarias, 19(3), 6. https://doi.org/10.17533/udea.rccp.324084

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Original research articles