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Journal of chromatography. B, Biomedical sciences and applications1998; 704(1-2); 207-214; doi: 10.1016/s0378-4347(97)00461-1

Disposition of human drug preparations in the horse. VI. Tiaprofenic acid.

Abstract: Urinary and plasma concentrations of the nonsteroidal anti-inflammatory drug tiaprofenic acid were determined following oral and intramuscular administration of a dose of 1 g to five fasted horses. Quantitation was performed by high-performance liquid chromatography (HPLC). The limit of quantitation (LOQ) was 0.1 microg/ml and 0.5 microg/ml in 2 ml plasma and 1 ml urine, respectively. Assay precision and extraction recovery were between acceptable values. Tiaprofenic acid pharmacokinetics were described by non-compartment analysis of the data. Absorption was faster after oral administration as maximum plasma concentrations (oral: 6.0+/-3.3 microg/ml; intramuscular: 6.6+/-2.5 microg/ml) were obtained after 1 h (oral) compared to 1.6+/-0.4 h (intramuscular) post dosage. Plasma binding (66+/-3%) was lower than measured in other species. Tiaprofenic acid was detected in urine for at least 24 h. The percentage of the parent drug excreted in the first 12 h after oral and intramuscular administration was 38+/-6% and 34+/-5%, respectively.
Publication Date: 1998-03-28 PubMed ID: 9518152DOI: 10.1016/s0378-4347(97)00461-1Google Scholar: Lookup
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  • Comparative Study
  • Journal Article

Summary

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The study explores how horses metabolize the drug tiaprofenic acid, which is a nonsteroidal anti-inflammatory drug. Both oral and intramuscular administration methods were tested, revealing the drug’s presence in plasma and urine, and examined its absorption, plasma binding, and excretion pattern.

Methodology

  • The researchers administered a dose of 1 gram of tiaprofenic acid to five horses that hadn’t eaten. The administration was both oral (swallowed) and intramuscular (injected into the muscle).
  • The performance of the drug was evaluated through measurements of its concentrations in the urine and plasma (liquid part of the blood) of the horses.
  • High-performance liquid chromatography (HPLC), a technique in analytical chemistry, was used to separate, identify, and quantify each component in the mixtures. In this case, it was used to measure the amount of tiaprofenic acid.

Results

  • The tests revealed that the absorption of tiaprofenic acid was quicker when administered orally, attaining the maximum plasma concentrations in about an hour, compared to intramuscular administration which took around 1.6 hours.
  • The limit of quantitation (LOQ), which is the lowest amount of drug that could be reliably measured, was defined as 0.1 microgram/ml in plasma and 0.5 microgram/ml in urine.
  • The binding of the drug to plasma was 66%, which was lower than what was previously observed in other species. Such binding is usually an important factor influencing the drug’s distribution within the body.
  • The drug was detected in urine for at least 24 hours post administration which helps in determining the duration of the drug’s effect.
  • The study also found that after both types of administration, the percentage of the original drug that was excreted in the first half-day was around one-third of the given dose. This indicates its metabolism and elimination characteristics in horses.

The outcomes of this study could provide insight on optimizing the therapeutic use of tiaprofenic acid, particularly in horses. However, these results only apply to the specific parameters used in the study. Therefore, variations can be expected with different dose sizes, different forms of the drug or other animal species.

Cite This Article

APA
Delbeke FT, Baert K, De Backer P. (1998). Disposition of human drug preparations in the horse. VI. Tiaprofenic acid. J Chromatogr B Biomed Sci Appl, 704(1-2), 207-214. https://doi.org/10.1016/s0378-4347(97)00461-1

Publication

ISSN: 1387-2273
NlmUniqueID: 9714109
Country: Netherlands
Language: English
Volume: 704
Issue: 1-2
Pages: 207-214

Researcher Affiliations

Delbeke, F T
  • Vakgroep Farmacologie, Farmacie en Toxicologie, Faculteit Diergeneeskunde, Universiteit Gent, Merelbeke, Belgium.
Baert, K
    De Backer, P

      MeSH Terms

      • Absorption
      • Animals
      • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics
      • Chromatography, High Pressure Liquid / methods
      • Cold Temperature
      • Drug Stability
      • Female
      • Horses / metabolism
      • Humans
      • Hydrolysis
      • Kidney / metabolism
      • Light
      • Microchemistry
      • Propionates / administration & dosage
      • Propionates / blood
      • Propionates / pharmacokinetics
      • Sensitivity and Specificity

      Citations

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