Assessment of Key Pharmacokinetic Variables of Bioequivalent and Non-bioequivalent Enrofloxacin Preparations under Various Water Management Conditions

López, Héctor Sumano; Cortés-Cuevas, Arturo; Rosario, C.; Gutiérrez, Lilia

doi:10.2141/jpsa.009092

Cited by 5 publications

(4 citation statements)

References 22 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…maximum serum concentration (C MAX ) should reach at least 10-12 times the value of the minimal inhibitory concentration (MIC) (C MAX > 10-12 MIC), and the area under the serum concentration vs. time curve (AUC 0-24 )/MIC should be equal to or higher than 125 (AUC/MIC ≥ 125) (10). These ratios are not always accomplished for enrofloxacin due to many factors, such as defective maneuvers to deliver the correct dose (11,12), the lack of bioequivalence of many pharmaceutical preparations (4)(5)(6)(7), and the presence of resistant bacteria to this antimicrobial agent.…”

Section: Introduction Enrofloxacinmentioning

confidence: 99%

Serum pharmacokinetics and tissue concentrations of a newrecrystallized enrofloxacin hydrochloride-dihydrate in hamsters

Carrascosa¹,

Peã'a²,

Gutiérrez³

et al. 2015

Turk J Vet Anim Sci

Self Cite

View full text Add to dashboard Cite

Pharmacokinetics (PK), pharmacodynamics (PD), and PK/PD ratios of a new solvate of enrofloxacin (enrofloxacin hydrochloride-dihydrate; enro-C), were studied in hamsters. Enrofloxacin from Baytril® 5% (enro R) served as the reference preparation. Two groups of 60 Syrian golden hamsters were intramuscularly injected individually with 10 mg/kg of enro R or with enro-C. Tissue and serum samples were obtained for 72 h; enrofloxacin concentrations were determined by HPLC with UV detection. Ninety percent minimum inhibitory concentrations (MIC 90 ) were determined for strains of methicillin-resistant Staphylococcus aureus, Leptospira interrogans, and Escherichia coli. All PK variables were statistically different between groups (P < 0.01). C MAX of enrofloxacin for enro-C was 17.3 µg/mL and it was 2.6 µg/mL for enro R . AUC was considerably higher for enro-C (459.2 µg/mL h vs. 19.9 µg/mL h). There were no statistically significant differences in MIC 90 values between enro R and enro-C. Tissue concentrations of enro-C in all cases were higher and remained above the MIC for longer periods than those of enro R . Relevant PK/PD ratios for enrofloxacin (AUC/MIC ≥ 125 and C MAX > MIC = 10-12) are consequently superior for enro-C. Given the outstanding PK/PD ratios of enro-C, this new moiety is proposed as a possible solution when high tissue concentrations of enrofloxacin are necessary.

show abstract

Section: Introduction Enrofloxacinmentioning

confidence: 99%

Serum pharmacokinetics and tissue concentrations of a newrecrystallized enrofloxacin hydrochloride-dihydrate in hamsters

Carrascosa¹,

Peã'a²,

Gutiérrez³

et al. 2015

Turk J Vet Anim Sci

Self Cite

View full text Add to dashboard Cite

show abstract

“…The correct use of this antibacterial drug requires the achievement of specific pharmacokinetic/pharmacodynamic (PK/PD) ratios to optimize clinical efficacy; that is, the maximum serum concentration (Cmax) should reach 10–12 times the value of the minimal inhibitory concentration ( MIC ) (Cmax > 10–12 MIC ), and the area under the serum concentration vs. time curve ( AUC 0‐24 )/ MIC should be equal or higher than 125 ( AUC / MIC ≥ 125) (Wright et al ., ). These ratios are not always accomplished due to many factors, such as defective maneuvers to deliver the correct dose in broiler chickens (Randall et al ., ; Sumano et al ., ) and due to lack of bioequivalence (Sumano et al ., , , ).…”

Section: Introductionmentioning

confidence: 99%

Physicochemical characterization and pharmacokinetics in broiler chickens of a new recrystallized enrofloxacin hydrochloride dihydrate

Gutiérrez¹,

Miranda-Calderón²,

García-Gutiérrez

et al. 2014

Vet Pharm & Therapeutics

View full text Add to dashboard Cite

Enrofloxacin, a key antimicrobial agent in commercial avian medicine, has limited bioavailability (60%). This prompted its chemical manipulation to yield a new solvate-recrystallized enrofloxacin hydrochloride dihydrate entity (enroC ). Its chemical structure was characterized by means of mass spectroscopy, Fourier transformed infrared spectroscopy, X-ray powder diffraction, and thermal analysis. Comparative oral pharmacokinetics (PK) of reference enrofloxacin (enroR ) and enroC in broiler chickens after oral administration revealed noticeable improvements in key parameters and PK/PD ratios. Maximum serum concentration values were 2.61 ± 0.21 and 5.9 ± 0.42 μg/mL for enroR and enroC , respectively; mean residence time was increased from 5.50 ± 0.26 h to 6.20 ± 0.71 h and the relative bioavailability of enroC was 336%. Considering Cmax /MIC and AUC/MIC ratios and the MIC values for a wild-type Escherichia coli O78/H12 (0.25 μg/mL), optimal ratios will only be achieved by enroC (Cmax /MIC = 23.6 and AUC/MIC = 197.7 for enroC ; vs. Cmax /MIC = 10.4 and AUC/MIC = 78.1 for enroR ). Furthermore, enroC may provide in most cases mutant prevention concentrations (Cmax /MIC ≥ 16). Ready solubility of powder enroC in drinking water at concentrations regularly used (0.01%) to provide an additional advantage of enroC in the field. Further development of enroC is warranted before it can be recommended for clinical use in veterinary medicine.

show abstract

“…In addition there may be variable wastage depending on the type and management of drinkers (140,263). Failure to ensure these factors are optimised can lead to ineffective drug delivery, as observed in a study of enrofloxacin in chickens (250,251). Because of the number of factors influencing water intake, it is usually recommended that current water intake is actually measured and used in calculations on dilution rates.…”

Section: Water Medicationmentioning

confidence: 99%

“…There are few cases published in the veterinary literature, although one report observed a preponderance of fake and/or expired drugs in Nigeria (61) and participants in a WHO consultation suggested that expired products were being relabelled and sold (289). In countries where there is no regulatory requirement to demonstrate bioequivalence, some generic versions of pioneer products have been shown to be of variable quality and to have pharmacokinetic profiles unlikely to be associated with effective antimicrobial activity (250,252).…”

Section: Product Qualitymentioning

confidence: 99%

Use of antimicrobial agents in livestock

Page¹,

Gautier²

2012

Rev. Sci. Tech. OIE

185

169

View full text Add to dashboard Cite

Antimicrobial agents, especially antibacterial agents, are used throughout the world, across a diverse array of extensive and intensive livestock production systems, to protect the health and welfare of livestock and to improve their performance. While some agents that are used in livestock belong to classes that have no counterpart in human medicine, this is not the case for the most widely used agents: the tetracyclines, penicillins, macrolides and sulphonamides. Many bacterial diseases of livestock cause devastating losses of animal life and productivity. As a result, their keepers can lose their livelihoods and see a dramatic reduction in income, so there is often a great sense of urgency to treat affected animals early. However, there are a large number of bacterial pathogens that cause disease and it is frequently difficult to reach a conclusive diagnosis prior to instituting treatment. There are many ways in which existing uses of antimicrobial agents can be improved, amongst the most important are increased utilisation of veterinary professional services, the introduction of enhanced infection control measures, improved point-of-care diagnostic tests, and the application of physiologically based population pharmacokinetic-pharmacodynamic modelling.

show abstract

Assessment of Key Pharmacokinetic Variables of Bioequivalent and Non-bioequivalent Enrofloxacin Preparations under Various Water Management Conditions

Cited by 5 publications

References 22 publications

Serum pharmacokinetics and tissue concentrations of a newrecrystallized enrofloxacin hydrochloride-dihydrate in hamsters

Serum pharmacokinetics and tissue concentrations of a newrecrystallized enrofloxacin hydrochloride-dihydrate in hamsters

Physicochemical characterization and pharmacokinetics in broiler chickens of a new recrystallized enrofloxacin hydrochloride dihydrate

Use of antimicrobial agents in livestock

Contact Info

Product

Resources

About