Comparative Study on Pharmacokinetics of Four Long-Acting Injectable Formulations of Enrofloxacin in Pigs

Ahmad, Salah Uddin; Sun, Jichao; Cheng, Fang; Li, Bing; Arbab, Safia; Zhou, Xuefei; Zhang, Jiyu

doi:10.3389/fvets.2020.604628

Cited by 6 publications

(5 citation statements)

References 60 publications

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“…In the case of animal species, when it is necessary to use the prescribing cascade principle, extrapolation from human doses is used due to the lack of knowledge of the pharmacokinetic parameters and, therefore, the most appropriate dosing regimens, which may cause problems in treated animals. In this context, in veterinary medicine, the special conditions for the treatment of animals make long-acting formulations powerful tools for use in animals affected by diabetes (and other medical conditions) [ 10 – 12 ].…”

Section: Introductionmentioning

confidence: 99%

An in vivo pharmacokinetic study of metformin microparticles as an oral sustained release formulation in rabbits

et al. 2021

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Background Metformin hydrochloride is a biguanide derivative that has been widely used to treat type 2 diabetes in humans. In veterinary medicine, metformin has shown increasing potential for diabetes treatment in different species, such as equids, dogs, cats and rabbits. It is highly hydrophilic, with incomplete gastrointestinal absorption and very large variability in absolute bioavailability between species, ranging from 4% in equids to 60% in humans. Metformin also shows a short half-life of approximately 2 h in dogs, cats, horses and humans. The objectives of this study were to evaluate a poly (lactic acid) (PLA) metformin microparticle formulation to test in rabbits and conduct a pharmacokinetics study of intravenous (SIV) and oral solution (SPO) metformin administration and oral PLA microparticle (SPLA) administration to rabbits to evaluate the improvement in the metformin pharmacokinetics profile. Results Metformin-loaded PLA microparticles were characterized by a spherical shape and high encapsulation efficiency. The results from Fourier transform infrared (FTIR) spectroscopy suggested the presence of interactions between metformin and PLA. X-Ray diffraction (XRD) analysis corroborated the results from the differential scanning calorimetry (DSC) studies, showing that metformin is present in an amorphous state within the microparticles. Physicochemical characterization suggested that PLA and metformin hydrochloride interacted within the microparticles via hydrogen bonding interactions. The pharmacokinetic study in rabbits showed sustained-release characteristics from the prepared microparticles with a delay in the time needed to reach the maximum concentration (Tmax), decreased Cmax and bioavailability, and increased mean residence time (MRT) and half-life compared to the pure drug solution. Conclusions Metformin-loaded PLA microparticles showed optimal and beneficial properties in terms of their physicochemical characteristics, making them suitable for use in an in vivo pharmacokinetic study. The pharmacokinetic parameters of the metformin microparticles from the in vivo study showed a shorter Tmax, longer MRT and half-life, decreased Cmax and the prolonged/sustained release expected for metformin. However, the unexpected decrease in bioavailability of metformin from the microparticles with respect to the oral solution should be evaluated for microparticle and dose design in future works, especially before being tested in other animal species in veterinary medicine.

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Section: Introductionmentioning

confidence: 99%

An in vivo pharmacokinetic study of metformin microparticles as an oral sustained release formulation in rabbits

et al. 2021

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“…59 The conversion of enrofloxacin to ciprofloxacin varies in different species of mammal from 59% in dairy cows to 51.5% in pigs. 60 This rate of conversion has important implications for determining the appropriate dose to administer to achieve the desired antimicrobial effect from this therapeutic. For the pharmacokinetics of enrofloxacin in birds, chickens have been studied extensively and a comprehensive population analysis by Guo et al report that after IV administration 30% of enrofloxacin was metabolized to ciprofloxacin in chickens.…”

Section: ■ Discussionmentioning

confidence: 99%

“…In a study in dogs, it was found that 40.44 ± 10.08% of an enrofloxacin-administered IV was metabolized to ciprofloxacin and a similar conversion was found following oral administration (40.17 ± 8.33%) . The conversion of enrofloxacin to ciprofloxacin varies in different species of mammal from 59% in dairy cows to 51.5% in pigs . This rate of conversion has important implications for determining the appropriate dose to administer to achieve the desired antimicrobial effect from this therapeutic.…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetics in Penguins Compared to Other Avian Species: A Review of Enrofloxacin and Voriconazole

Woods,

Hughes-Medlicott,

McDowell

2023

Mol. Pharmaceutics

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Australasia is home to unique and endangered avian species. Drug administration to this group of animal patients for prophylaxis and treatment is challenging from a number of different perspectives. A key limitation for optimal drug dosing in birds is the lack of published pharmacokinetic studies to guide dose requirements. The aim of this review was to systematically investigate published literature on pharmacokinetics in penguin species and compare that with the pharmacokinetics of other avian species with a focus on two drugs: enrofloxacin and voriconazole. The review was conducted following PRISMA guidelines. A systematic literature search was performed in Pubmed, Embase, Scopus, and Web of Science databases. A key finding is that penguin pharmacokinetics differs from other avian species, with weight-adjusted AUC and C max values higher than most other avian species (e.g., for enrofloxacin, the AUC in the African penguin is 85.7 μg h/mL, which is more than double the other bird species). Doses for some avian species may be successfully extrapolated from other avian species; however, it appears important to consider factors other than just body weight (e.g., clearance mechanism and drug physicochemical characteristics). Consequently, there is an important need for robust pharmacokinetic data in wildlife species to ensure optimal therapy for this special group of patients. As part of this review, we identify key aspects that should be considered when estimating dose in species for which there is limited pharmacokinetic information available.

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“…Co-resistance against multiple drug classes makes the problem of AMR in bacteria even more complex, as use of one class of antimicrobials can provide positive selection pressure to maintain resistance against other antimicrobial classes ( Holmes et al, 2016 ). Fluoroquinolones are also considered as critically important antimicrobials in human medicine ( World Health Organization., 2019 ) and are also used in food animals in some countries for treatment purposes ( Römer et al, 2017 ; Ahmad et al, 2021 ). Co-resistance to fluoroquinolones and 3GCs can hence be considered both a human and animal health threat.…”

Section: Discussionmentioning

confidence: 99%

Global Distribution of Extended Spectrum Cephalosporin and Carbapenem Resistance and Associated Resistance Markers in Escherichia coli of Swine Origin – A Systematic Review and Meta-Analysis

et al. 2022

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Third generation cephalosporins and carbapenems are considered critically important antimicrobials in human medicine. Food animals such as swine can act as reservoirs of antimicrobial resistance (AMR) genes/bacteria resistant to these antimicrobial classes, and potential dissemination of AMR genes or resistant bacteria from pigs to humans is an ongoing public health threat. The objectives of this systematic review and meta-analysis were to: (1) estimate global proportion and animal-level prevalence of swine E. coli phenotypically resistant to third generation cephalosporins (3GCs) and carbapenems at a country level; and (2) measure abundances and global distribution of the genetic mechanisms that confer resistance to these antimicrobial classes in these E. coli isolates. Articles from four databases (CAB Abstracts, PubMed/MEDLINE, PubAg, and Web of Science) were screened to extract relevant data. Overall, proportion of E. coli resistant to 3GCs was lower in Australia, Europe, and North America compared to Asian countries. Globally, <5% of all E. coli were carbapenem-resistant. Fecal carriage rates (animal-level prevalence) were consistently manifold higher as compared to pooled proportion of resistance in E. coli isolates. blaCTX–M were the most common 3GC resistance genes globally, with the exception of North America where blaCMY were the predominant 3GC resistance genes. There was not a single dominant blaCTX–M gene subtype globally and several blaCTX–M subtypes were dominant depending on the continent. A wide variety of carbapenem-resistance genes (blaNDM–, VIM–, IMP–, OXA–48, andKPC–) were identified to be circulating in pig populations globally, albeit at very-low frequencies. However, great statistical heterogeneity and a critical lack of metadata hinders the true estimation of prevalence of phenotypic and genotypic resistance to these antimicrobials. Comparatively frequent occurrence of 3GC resistance and emergence of carbapenem resistance in certain countries underline the urgent need for improved AMR surveillance in swine production systems in these countries.

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Comparative Study on Pharmacokinetics of Four Long-Acting Injectable Formulations of Enrofloxacin in Pigs

Cited by 6 publications

References 60 publications

An in vivo pharmacokinetic study of metformin microparticles as an oral sustained release formulation in rabbits

An in vivo pharmacokinetic study of metformin microparticles as an oral sustained release formulation in rabbits

Pharmacokinetics in Penguins Compared to Other Avian Species: A Review of Enrofloxacin and Voriconazole

Global Distribution of Extended Spectrum Cephalosporin and Carbapenem Resistance and Associated Resistance Markers in Escherichia coli of Swine Origin – A Systematic Review and Meta-Analysis

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