Farmacocinética plasmática y urinaria de marbofloxacina intramuscular en caninos

Abstract

Plasma and urinary disposition of marbofloxacin was studied in canines (n = 6) after intramuscular administration of 2 mg/kg. At different times post-administration, blood samples were collected until 24 h, and urine samples, only from male dogs (n = 4) at 4; 8; 12, and 24 h. Liquid-liquid extraction of analyte with water, methanol, and centrifugation at 13500 rpm at 4 °C were performed. Separation and quantification were made using HPLC by reverse phase isocratic elution with a C18 column, fluorescence detector at 295 nm excitation and 490 nm emission, and a mobile phase consisting of water, acetonitrile, and triethylamine. Temporary plasma concentrations were analyzed with non-compartmental PK Solution 2.0 software. The results obtained indicate rapid absorption, as well as rapid and wide distribution. Cl and values of t½β and MRT indicate slow clearance and prolonged stay. The study evidenced plasma concentrations up to 24 h, which exceed the MIC of relevant pathogens. The AUC/MIC ratio indicates efficacy against microorganisms withMIC ≤ 0.15 μg/ml. Urinary levels of marbofloxacin are more significant than plasmatic levels. However, new studies are required to assess their use with the tested dose and route of application.

Plasma and urinary disposition of marbofloxacin was studied in canines (n = 6) after intramuscular administration of 2 mg/kg. At different times post-administration, blood samples were collected until 24 h, and urine samples, only from male dogs (n = 4) at 48 12, and 24 h. Liquid-liquid extraction of analyte with water, methanol, and centrifugation at 13500 rpm at 4 °C were performed. Separation and quantification were made using HPLC by reverse phase isocratic elution with a C18 column, fluorescence detector at 295 nm excitation and 490 nm emission, and a mobile phase consisting of water, acetonitrile, and triethylamine. Temporary plasma concentrations were analyzed with non-compartmental PK Solution 2.0 software. The results obtained indicate rapid absorption, as well as rapid and wide distribution. Cl and values of t½β and MRT indicate slow clearance and prolonged stay. The study evidenced plasma concentrations up to 24 h, which exceed the MIC of relevant pathogens. The AUC/MIC ratio indicates efficacy against microorganisms with MIC ≤ 0.15 μg/ml. Urinary levels of marbofloxacin are more significant than plasmatic levels. However, new studies are required to assess their use with the tested dose and route of application.

Se estudou a disposição plasmática e urinária de marbofloxacina em caninos (n = 6) após a aplicação intramuscular de 2 mg/kg. Em diferentes tempos pós-administração se tomaram amostras de sangue hasta as 24 h, e de urina somente nos caninos machos (n = 4) a as 48 12 e 24 h. Se realizou uma extração líquido-líquido do analito com água, metanol e centrifugado a 13500 r. p. m. a 4 °C. A separação e quantificação se realizou por HPLC mediante a eluição isocrática em fase reversa, utilizando coluna C-18, detector de fluorescência a 295 nm de excitação e 490 nm de emissão e fase móvel composta por água, acetonitrilo e trietilamina. As concentrações plasmáticas temporárias se analisaram com o software não compartimental PK Solution 2.0. Os resultados conseguidos indicam pronta absorção, rápida e ampla distribuição. O Cl e os valores conseguidos de t½β e TMR indicam lenta depuração e prolongada permanência. O ensaio determinou concentrações plasmáticas perduráveis hasta 24 h, e que excedem a CMI de patógenos relevantes. O cociente ABC/ CMI indica eficácia frente a micro-organismos com CMI ≤ 15 μg/ml. Os níveis urinários de marbofloxacina são mais significativos que os plasmáticos. Não obstante, se requerem novos estudos que avalizem seu uso com a dose e via de aplicação ensaiada.