Microdialysis as a tool to determine free kidney levels of voriconazole in rodents: A model to study the technique feasibility for a moderately lipophilic drug

Araújo, Bibiana Verlindo de; Silva, C.F.; Haas, Sandra Elisa; Costa, Teresa Dalla

doi:10.1016/j.jpba.2008.02.025

Cited by 23 publications

(26 citation statements)

References 16 publications

(39 reference statements)

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“…The recoveries at higher FCZ concentrations (50, 100, and 500 g/ml) were also investigated. The relative recovery of FCZ (n ϭ 3) was determined by dialysis and retrodialysis using a 1-g/ml solution described previously (3,23).…”

Section: Methodsmentioning

confidence: 99%

Comparison of Fluconazole Renal Penetration Levels in Healthy and Candida albicans-Infected Wistar Rats

Azeredo

Araújo

Haas

et al. 2012

Antimicrob Agents Chemother

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The aims of this study were to evaluate free levels of fluconazole (FCZ) in the kidneys of healthy and Candida albicansinfected Wistar rats using microdialysis and to establish the relationship between free renal and total plasma levels under both conditions. Microdialysis recovery rates were determined in vitro by dialysis, and retrodialysis recovery rates were determined in vivo by retrodialysis. The recovery rate was around 50%, independent of the method, drug concentration, or condition (in vitro or in vivo) used. FCZ kidney penetration in healthy and infected rats was investigated after the administration of 10 mg/kg of body weight intravenously (i.v.) or 50 mg/kg orally (n ‫؍‬ 6/group) and blood and microdialysate sample harvesting at predetermined time points up to 24 and 18 h, respectively. There were no statistical differences between the area under the free concentration-time curve (AUC 0 -ؕ ) values in plasma and in tissue for either healthy or infected groups for the same dose regimen investigated. The antifungal tissue penetrations were similar for both doses and under all conditions investigated (ranging from 0.77 to 0.84). The unbound fraction of FCZ was concentration independent (86.0% ؎ 2.0%), allowing the prediction of free renal levels using pharmacokinetic parameters obtained from total plasma fitting. The results showed that free renal and free plasma levels are similar in healthy and systemically C. albicansinfected rats. Therefore, free plasma levels are a good surrogate to estimate free FCZ renal concentrations in systemic candidiasis and can be used to optimize dosing regimens for this drug.

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Section: Methodsmentioning

confidence: 99%

Comparison of Fluconazole Renal Penetration Levels in Healthy and Candida albicans-Infected Wistar Rats

Azeredo

Araújo

Haas

et al. 2012

Antimicrob Agents Chemother

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show abstract

“…Esta condição faz com que o equilíbrio entre os meios, interno e externo da sonda, nunca sejam atingidos (ARAUJO et al, 2008). As substâncias difundidas pelo tubo de entrada são coletadas na outra extremidade da sonda, para posterior análise.…”

Section: Microdiáliseunclassified

“…Estas concentrações coletadas no dialisado, no entanto, não são iguais às concentrações livres no tecido, devido à condição sink estabelecida. Dessa forma, a concentração no dialisado representa apenas uma parcela da concentração livre no tecido (ARAUJO, 2008). Para determinar a fração livre tecidual é necessário antes calcular a recuperação relativa (RR), que pode ser medida em testes de retrodiálise (perda) ou diálise (ganho).…”

Section: Microdiáliseunclassified

“…Após estabilização da sonda, a recuperação foi determinada por retrodiálise in vivo, que permitiu a conversão das concentrações dos dialisados em concentrações livres no tecido (ARAUJO et al, 2008). Em seguida, a sonda e o tecido renal foram perfusados com salina por 30 min.…”

Section: Modelo Experimental In Vivounclassified

“…Em busca de quantificar a ligação do composto galoilquínico na sonda de microdiálise, realizou-se o experimento proposto por Araujo et al (2008). Assim, diferentes concentrações de galoilquínico (25, 50, 100, 200 e 400 Ƞg/mL) foram testadas conforme descrito no item 3.11.1.…”

Section: Avaliação Da Ligação De Galoilquínico a Sonda De Microdiáliseunclassified

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Avaliação farmacocinética do extrato bruto e de metabólitos secundários das folhas de Copaifera langsdorffii Desf.

Costa¹

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Microdialysis in the Hepatobiliary System: Monitoring Drug Metabolism, Hepatobiliary Excretion, and Enterohepatic Circulation

Wu¹,

Tsai²

2011

Applications of Microdialysis in Pharmaceutical Science

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Microdialysis as a tool to determine free kidney levels of voriconazole in rodents: A model to study the technique feasibility for a moderately lipophilic drug

Cited by 23 publications

References 16 publications

Comparison of Fluconazole Renal Penetration Levels in Healthy and Candida albicans-Infected Wistar Rats

Comparison of Fluconazole Renal Penetration Levels in Healthy and Candida albicans-Infected Wistar Rats

Avaliação farmacocinética do extrato bruto e de metabólitos secundários das folhas de Copaifera langsdorffii Desf.

Microdialysis in the Hepatobiliary System: Monitoring Drug Metabolism, Hepatobiliary Excretion, and Enterohepatic Circulation

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