Pharmacokinetics of Enrofloxacin and its Metabolite Ciprofloxacin in Goats given Enrofloxacin Alone and in Combination with Probenecid

Rao, G. Srinivasa; Ramesh, S.; Ahmad, A. H.; Tripathi, Hema; Sharma, Lalita; Malik, Jitendra K.

doi:10.1053/tvjl.2001.0594

Cited by 22 publications

(28 citation statements)

References 14 publications

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“…The maximum serum concentrations (C max ) were 2.45, 2.83 and 3.12 μg ml -1 being achieved at 1.41, 1.15 and 1.26 h (t max ) for Baytril, Mucotryl and Mucotryl without bromhexine, respectively. The C max obtained in the present study were higher than those reported by [15] in desert sheep and Nubian goats, 1.29 and 1.33 μg ml -1 , respectively, and higher than reported by [30] and [13] for goats and pigs 1.13, 1.17 μg ml -1 , respectively and higher than those reported in sheep following the same intramuscular dose of enrofloxacin [16] following intramuscular administration of enrofloxacin in a single dose of 2.5 mg kg -1 , and [7] reported 2.80 μg ml -1 in goats given the same im dose of the drug, which is similar to that obtained for Mucotryl, while higher than that obtained for Baytril and lower than that obtained for Mucotryl without bromhexine. The difference in the dose rate in these studies may contribute to the differences in the C max .…”

Section: Discussionmentioning

confidence: 70%

“…Fluoroquinolones exhibit bactericidal action by targeting the bacterial DNA topoisomerases II(gyrase) and IV which is responsible for supercoiling of DNA around RNA core to provide a suitable spatial arrangement of DNA within the bacterial cell [3,4]. Enrofloxacin is partly de-ethylated to ciprofloxacin in vivo, which is also pharmacologically active [5][6][7].…”

Section: Introductionmentioning

confidence: 99%

“…P.O. Box 12111, Giza, Egypt; Fax: 0020235725240 -0020235710305; E-mail: drelbanna3@yahoo.com poultry [11,12], pigs [13], rabbits [14], sheep [15 and 16], goats [7,15], horses [17,18] , cows [19], dogs [2,20], calves [1], and buffaloes [21].…”

Section: Introductionmentioning

confidence: 99%

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Comparative Bioequivalence Study of Three Formulations of Enrofloxacin in Sheep

El-Banna

Goudah²,

El-Zorba³

2011

DML

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A comparative pharmacokinetic study of three enrofloxacin injectable solutions was carried out in six healthy Barky rams after intramuscular injection according to a single dose, randomized, crossover experimental design. The three formulations were enrofloxacin 10% (Baytril(®)), enrofloxacin 10% plus bromhexine 1% (Mucotryl(®)) and enrofloxacin 10 % solution without bromhexine (Mucotryl without bromhexine). The three formulations were given a single intramuscular dose at a dose rate of 5 mg kg(-1) b.wt. The concentrations of the drug in the serum were measured using high-performance liquid chromatography (HPLC) with fluorescence detection. The results indicate that there were no significant differences between the distribution rate constant (k(ab)) and distribution half-life (t(1/2ab)), the maximum serum concentration (C(max)) and the time to peak concentration (T(max)) between Baytril and the other two formulations. There were significant differences between the elimination half life (t(1/2el)) and elimination rate constant (k(el)), for Baytril and enrofloxacin (the exact formulation of Mucotryl without bromhexine). Enrofloxacin was rapidly absorbed following IM administration of 5 mg kg(-1) b. wt. The peak serum concentrations (C(max)) were 2.83, 2.45 and 3.12 µg ml(-1) and were attained at (t(max)) 1.15, 1.41 and 1.26 hours when given Mucotryl, Baytril and enrofloxacin (the exact formulation of Mucotryl without bromhexine) to sheep, respectively. The injectable formulations investigated were bioequivalent after their intramuscular injection to sheep at recommended dose rate. As our results showed that, values of T(max), C(max) and AUC (Area under time curve concentration) determined for both Baytril, Mucotryl, and enrofloxacin (the exact formulation of Mucotryl without bromhexine ( reference ant test products) are within the acceptable range of 0.80-1.20, this means that the tested products product under investigation was bio-equivalent. These findings showed that the efficacy of the two test formulations was similar or possibly enhanced compared with Baytril based on the pharmacokinetic parameters obtained and due to concentration dependent activity of enrofloxacin.

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Section: Discussionmentioning

confidence: 70%

Section: Introductionmentioning

confidence: 99%

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Comparative Bioequivalence Study of Three Formulations of Enrofloxacin in Sheep

El-Banna

Goudah²,

El-Zorba³

2011

DML

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“…About 40% of the radioactivity was recovered from the bile, which contained mainly the unchanged parent molecule. In various food animal species, the metabolism pathway of enrofloxacin has been well documented by many earlier investigators (Bergan et al, 1988;Tyczkowska et al, 1989;Anadon et al, 1995;Kaartinen et al, 1997;Rao et al, 2001;Sharma et al, 2003). This drug induces inhibition of cytochrome P450 isoenzymes (Vancutsem and Babish, 1996;Vaccaro et al, 2003).…”

Section: Discussionmentioning

confidence: 98%

“…Heinen (Heinen, 2002) reported that in dogs, enrofloxacin had more favorable pharmacokinetic/pharmacodynamic properties than other fluoroquinolones, such as difloxacin, marbofloxacin and orbifloxacin. Rao et al (2001) also reported favorable metabolic properties of the drug in goats. Martinez et al (2006) reviewed that the oral bioavailability of enrofloxacin was greater than 80% in most animal species.…”

Section: Introductionmentioning

confidence: 89%

Nonlinear toxicokinetics of enrofloxacin in rats

Shin

Cho

et al. 2010

Arch. Pharm. Res.

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The dose-dependent toxicokinetics of enrofloxacin were studied by administering various single subcutaneous doses (5, 10, 20, 40, 70, 100, 150, 200, 300 and 400 mg/kg) in male Sprague-Dawley rats. The blood samples were collected from the tail veins, and the plasma concentration of enrofloxacin was determined by an HPLC-fluorescence detection (FLD) method. The time-concentration profiles of enrofloxacin were well fitted by an one-compartmental model with first order elimination. The absorption half-lives (t₁(/)₂(abs)) ranged from 0.2-0.8 h, and the mean time to maximum plasma concentration (T(max)) ranged from 0.6-1.8 h. On the other hand, marked disproportionate increases of the area under the curve (AUC) and elimination half-lives (t₁(/)₂) were observed from the increase of the doses. This result indicates that the elimination of enrofloxacin has nonlinear pharmacokinetic properties with increasing doses. Therefore, we need to take into consideration the possible occurrence of side effects resulting from greater systemic exposure from high dose therapies.

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Determination of enrofloxacin and ciprofloxacin in milk using molecularly imprinted solid‐phase extraction

Yan

Tian

Row

2008

J of Separation Science

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A molecularly imprinted solid-phase extraction procedure was developed for the simultaneous identification of enrofloxacin and its active metabolite, ciprofloxacin, in milk samples. Water-compatible molecularly imprinted polymers synthesized in a water-methanol system show a high degree of cross-reactivity for enrofloxacin and ciprofloxacin in aqueous environments. The imprinted particles were applied as selective sorbents in a solid-phase extraction process focusing upon complex milk matrices, which allowed the matrix compounds present in milk samples to be removed effectively. The extracts were sufficiently clean for further chromatographic analysis, and no interference originating from the biological matrix was observed. The mean recoveries of enrofloxacin and ciprofloxacin from milk sample were 82.6-93.5% and 81.2-94.8%, respectively, with the RSD less than 7.5%. This method is simple and sensitive, and is therefore an alternative tool to the existing HPLC methods for analyzing residual enrofloxacin and ciprofloxacin in biological samples.

show abstract

Pharmacokinetics of Enrofloxacin and its Metabolite Ciprofloxacin in Goats given Enrofloxacin Alone and in Combination with Probenecid

Cited by 22 publications

References 14 publications

Comparative Bioequivalence Study of Three Formulations of Enrofloxacin in Sheep

Comparative Bioequivalence Study of Three Formulations of Enrofloxacin in Sheep

Nonlinear toxicokinetics of enrofloxacin in rats

Determination of enrofloxacin and ciprofloxacin in milk using molecularly imprinted solid‐phase extraction

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