Pharmacokinetics, urinary excretion and plasma protein binding of pralidoxime in goats

Rahal, Anu; Jk, Malik

doi:10.1016/j.smallrumres.2010.10.005

Cited by 2 publications

(1 citation statement)

References 15 publications

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“…Its effectiveness has been tested against a range of Eimeria strains in chickens and it has shown remarkable anticoccidial activity, especially against E. tenella. [6] Its potential use as a coccidiostat encouraged us to further study its pharmacokinetic and distribution characteristics, which are important for a new drug; [7][8][9] in this sense, it is essential to establish a reliable method for the quantification of NZL concentration in plasma.…”

Section: Introductionmentioning

confidence: 99%

A Bioisosteres’ Application as Internal Standard for Simultaneous Determination of Three Triazine Anticoccidial Chemicals by Uplc

Xue

Zhang

et al. 2014

Journal of Liquid Chromatography & Related Technologies

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& A new chemical entity, 2-(3-methyl-4-(4-nitrophenoxy) phenyl)-1, 2, 4-triazine-3, 5 (2H, 4H)-dione (NZL), possesses remarkable anticoccidial activity. Its nonclassical bioisosterism, whereas one of its analogues, triclabendazole sulfoxide (TCB-SO), was used as the internal standard (IS) for the determination of NZL in plasma. TCB-SO's physicochemical data were proved to be more similar to NZL than the analogues, namely diclazuril (DIC) and toltrazuril (TOL), which were commonly used in previous reports. By investigating the effect of mobile phase's pH on the retention of the four substances (i.e., NZL, DIC, TOL, and TCB-SO), simultaneous separation of these analytes could be achieved, demonstrating TCB-SO's application as IS for simultaneous quantification. The 5 mM acetic acid-ammonium acetate buffer (pH 4.5) was used as aqueous phase that successfully overcame the peak-overlapping (when ammonium acetate buffer at pH 6.5 was used) of analytes and peak-tailing (when 0.1% formic acid was used) of NZL. The low limit of quantification (LLOQ) of NZL was determined to be 0.08 lg mL À1 with a good linearity range of 0.08-50 lg mL À1 , fully meeting with the requirement for pharmacokinetic determination. This method has been successfully applied to study the protein binding rate in vitro and the pharmacokinetics of broilers.

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Section: Introductionmentioning

confidence: 99%

A Bioisosteres’ Application as Internal Standard for Simultaneous Determination of Three Triazine Anticoccidial Chemicals by Uplc

Xue

Zhang

et al. 2014

Journal of Liquid Chromatography & Related Technologies

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A physiologically based pharmacokinetic model for the oxime TMB-4: simulation of rodent and human data

et al. 2013

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Multiple oximes have been synthesized and evaluated for use as countermeasures against chemical warfare nerve agents. The current U.S. military and civilian oxime countermeasure, 2-[(hydroxyimino)methyl]-1-methylpyridin-1-ium chloride (2-PAM), is under consideration for replacement with a more effective acetylcholinesterase reactivator, 1,1'-methylenebis{4-hydroxyiminomethyl}pyridinium dimethanesulfonate (MMB-4). Kinetic data in the scientific literature for MMB-4 are limited; therefore, a physiologically based pharmacokinetic (PBPK) model was developed for a structurally related oxime, 1,1'-trimethylenebis{4-hydroximinomethyl}pyridinium dibromide. Based on a previous model structure for the organophosphate diisopropylfluorophosphate, the model includes key sites of acetylcholinesterase inhibition (brain and diaphragm), as well as fat, kidney, liver, rapidly perfused tissues and slowly perfused tissues. All tissue compartments are diffusion limited. Model parameters were collected from the literature, predicted using quantitative structure-property relationships or, when necessary, fit to available pharmacokinetic data from the literature. The model was parameterized using rat plasma, tissue and urine time course data from intramuscular administration, as well as human blood and urine data from intravenous and intramuscular administration; sensitivity analyses were performed. The PBPK model successfully simulates rat and human data sets and has been evaluated by predicting intravenous mouse and intramuscular human data not used in the development of the model. Monte Carlo analyses were performed to quantify human population kinetic variability in the human evaluation data set. The model identifies potential pharmacokinetic differences between rodents and humans, indicated by differences in model parameters between species. The PBPK model can be used to optimize the dosing regimen to improve oxime therapeutic efficacy in a human population.

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Pharmacokinetics, urinary excretion and plasma protein binding of pralidoxime in goats

Cited by 2 publications

References 15 publications

A Bioisosteres’ Application as Internal Standard for Simultaneous Determination of Three Triazine Anticoccidial Chemicals by Uplc

A Bioisosteres’ Application as Internal Standard for Simultaneous Determination of Three Triazine Anticoccidial Chemicals by Uplc

A physiologically based pharmacokinetic model for the oxime TMB-4: simulation of rodent and human data

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