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Journal of veterinary pharmacology and therapeutics2020; 43(4); 364-368; doi: 10.1111/jvp.12852

Pharmacokinetics of three formulations of vitacoxib in horses.

Abstract: The pharmacokinetic properties of three formulations of vitacoxib were investigated in horses. To describe plasma concentrations and characterize the pharmacokinetics, 6 healthy adult Chinese Mongolian horses were administered a single dose of 0.1 mg/kg bodyweight intravenous (i.v.), oral paste, or oral tablet vitacoxib in a 3-way, randomized, parallel design. Blood samples were collected prior to and at various times up to 72 hr postadministration. Plasma vitacoxib concentrations were quantified using UPLC-MS/MS, and pharmacokinetic parameters were calculated using noncompartmental analysis. No complications resulting from the vitacoxib administration were noted on subsequent administrations, and all procedures were tolerated well by the horses throughout the study. The elimination half-life (T1/2λz ) was 4.24 ± 1.98 hr (i.v.), 8.77 ± 0.91 hr (oral paste), and 8.12 ± 4.24 hr (oral tablet), respectively. Maximum plasma concentration (Cmax ) was 28.61 ± 9.29 ng/ml (oral paste) and 19.64 ± 9.26 ng/ml (oral tablet), respectively. Area under the concentration-versus-time curve (AUClast ) was 336 ± 229 ng hr/ml (i.v.), 221 ± 94 ng hr/ml (oral paste), and 203 ± 139 ng hr/ml, respectively. The results showed statistically significant differences between the 2 oral vitacoxib groups in Tmax value. T1/2λz (hr), AUClast (ng hr/ml), and MRT (hr) were significantly different between i.v. and oral groups. The longer half-life observed following oral administration was consistent with the flip-flop phenomenon.
© 2020 John Wiley & Sons Ltd.
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Publication Date: 2020-03-11 PubMed ID: 32162352DOI: 10.1111/jvp.12852Google Scholar: Lookup
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  • Journal Article
  • Randomized Controlled Trial
  • Veterinary

Summary

This research summary has been generated with artificial intelligence and may contain errors and omissions. Refer to the original study to confirm details provided. Submit correction.

This study investigates how three forms of vitacoxib, a pain and inflammation reducer, are processed and spread in the body (pharmacokinetics) of horses. Through testing on six horses, the research found significant differences in the duration of drug action based on the method of administration.

Investigation Plan and Methods

  • The study involved six healthy adult Chinese Mongolian horses which were administered a single dose of 0.1 mg/kg bodyweight of vitacoxib through intravenous transfusion, oral paste, or oral tablet in a three-way, randomized method. This method aimed to help understand the different impacts of drug delivery systems on the same drug.
  • Blood samples were collected from the horses before and at various points up to 72 hours after drug administration. The vitacoxib concentrations in the collected plasma were quantified using Ultra Performance Liquid Chromatography-Mass Spectrometry/Mass Spectrometry (UPLC-MS/MS) which is a technique used for identifying and quantifying substances in a sample.
  • The pharmacokinetic parameters of vitacoxib were calculated using noncompartmental analysis, which is a simpler and quicker method for predicting a drug’s disposition in the body.

Results and Findings

  • The results showed no issues arising from the administration of vitacoxib in any of the three methods. All procedures were well-tolerated by the horses during the study. This is an important finding as it suggests that vitacoxib can be safely and reliably administered to horses in different ways without inducing averse effects.
  • The elimination half-life (T), the time taken for the concentration of vitacoxib in the body to decrease by half, was found to vary significantly across the different methods of administration: 4.24 hours for intravenous, 8.77 hours for oral paste, and 8.12 hours for oral tablet.
  • The peak concentration of vitacoxib in the horses’ blood (C) was found to be 28.61 ng/ml for the oral paste and 19.64 ng/ml for the oral tablet. The values highlighted here represent the maximum concentration reached in the bloodstream, indicating how quickly and to what extent the drug becomes available to work in the body.
  • The study also reported observations related to the area under the concentration-versus-time curve (AUC), an important pharmacokinetic parameter that measures the total drug exposure over time. Different AUC values were also observed across the three delivery methods: 336 ng/hr/ml for intravenous, 221 ng/hr/ml for oral paste, and 203 ng/hr/ml for the oral tablet.
  • The differences in these parameters confirm a flip-flop phenomenon, a pharmacokinetic concept which refers to cases where the rate of absorption of an orally administered drug is slower than the rate of elimination. This justifies the longer half-life observed with oral administration methods.

Cite This Article

APA
Wang J, Qiu J, Xiao H, Gong X, Sun P, Li J, Zhang S, Cao X. (2020). Pharmacokinetics of three formulations of vitacoxib in horses. J Vet Pharmacol Ther, 43(4), 364-368. https://doi.org/10.1111/jvp.12852

Publication

Journal of veterinary pharmacology and therapeutics
ISSN: 1365-2885
NlmUniqueID: 7910920
Country: England
Language: English
Volume: 43
Issue: 4
Pages: 364-368

Researcher Affiliations

Wang, Jianzhong
  • Department of Veterinary Pharmacology and Toxicology, College of Veterinary Medicine, China Agricultural University, Beijing, China.
  • Laboratory of Quality & Safety Risk Assessment for Animal Products on Chemical Hazards (Beijing), Ministry of Agriculture and Rural affairs, Beijing, China.
  • Biomedical Sciences, SMART Pharmacology at Iowa State University College of Veterinary Medicine, Ames, IA, USA.
Qiu, Jicheng
  • Department of Veterinary Pharmacology and Toxicology, College of Veterinary Medicine, China Agricultural University, Beijing, China.
  • Laboratory of Quality & Safety Risk Assessment for Animal Products on Chemical Hazards (Beijing), Ministry of Agriculture and Rural affairs, Beijing, China.
Xiao, Hongzhi
  • Department of Veterinary Pharmacology and Toxicology, College of Veterinary Medicine, China Agricultural University, Beijing, China.
  • Laboratory of Quality & Safety Risk Assessment for Animal Products on Chemical Hazards (Beijing), Ministry of Agriculture and Rural affairs, Beijing, China.
Gong, Xiaohui
  • Department of Veterinary Pharmacology and Toxicology, College of Veterinary Medicine, China Agricultural University, Beijing, China.
  • Laboratory of Quality & Safety Risk Assessment for Animal Products on Chemical Hazards (Beijing), Ministry of Agriculture and Rural affairs, Beijing, China.
Sun, Pan
  • Department of Veterinary Pharmacology and Toxicology, College of Veterinary Medicine, China Agricultural University, Beijing, China.
  • Laboratory of Quality & Safety Risk Assessment for Animal Products on Chemical Hazards (Beijing), Ministry of Agriculture and Rural affairs, Beijing, China.
Li, Jing
  • Beijing Orbiepharm Co. Ltd., Beijing, China.
Zhang, Suxia
  • Department of Veterinary Pharmacology and Toxicology, College of Veterinary Medicine, China Agricultural University, Beijing, China.
  • Laboratory of Quality & Safety Risk Assessment for Animal Products on Chemical Hazards (Beijing), Ministry of Agriculture and Rural affairs, Beijing, China.
Cao, Xingyuan
  • Department of Veterinary Pharmacology and Toxicology, College of Veterinary Medicine, China Agricultural University, Beijing, China.
  • Laboratory of Quality & Safety Risk Assessment for Animal Products on Chemical Hazards (Beijing), Ministry of Agriculture and Rural affairs, Beijing, China.
  • Key Laboratory of Detection for Veterinary Drug Residue and Illegal Additive, Ministry of Agriculture and Rural affairs, Beijing, China.

MeSH Terms

  • Administration, Oral
  • Animals
  • Area Under Curve
  • Biological Availability
  • Cross-Over Studies
  • Female
  • Half-Life
  • Horses / blood
  • Horses / metabolism
  • Imidazoles / administration & dosage
  • Imidazoles / chemistry
  • Imidazoles / pharmacokinetics
  • Injections, Intravenous / veterinary
  • Male
  • Sulfones / administration & dosage
  • Sulfones / chemistry
  • Sulfones / pharmacokinetics

Grant Funding

  • 31672599 / National Natural Science Foundation of China
  • 2016YFD0501309-1 / National Science & Technology Pillar Program during the Thirteenth Five-Year Plan Period

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This article includes 20 references
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Citations

This article has been cited 2 times.
  1. Flood J, Stewart AJ. Non-Steroidal Anti-Inflammatory Drugs and Associated Toxicities in Horses. Animals (Basel) 2022 Oct 26;12(21).
    doi: 10.3390/ani12212939pubmed: 36359062google scholar: lookup
  2. Wang J, Schneider BK, Xiao H, Qiu J, Gong X, Seo YJ, Li J, Mochel JP, Cao X. Non-Linear Mixed-Effects Pharmacokinetic Modeling of the Novel COX-2 Selective Inhibitor Vitacoxib in Cats. Front Vet Sci 2020;7:554033.
    doi: 10.3389/fvets.2020.554033pubmed: 33102567google scholar: lookup
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