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Pharmacokinetics and plasma concentrations of acetylsalicylic acid after intravenous, rectal, and intragastric administration to horses.

Abstract: Six healthy adult horses (5 mares and 1 stallion) were given a single dose of acetylsalicylic acid (ASA), 20 mg/kg of body weight, by intravenous (IV), rectal, and intragastric (IG) routes. Serial blood samples were collected via jugular venipuncture over a 36-h period, and plasma ASA and salicylic acid (SA) concentrations were determined by high-performance liquid chromatography. After IV administration, the mean elimination rate constant of ASA (+/- the standard error of the mean) was 1.32 +/- 0.09 h(-1), the mean elimination half-life was 0.53 +/- 0.04 h, the area under the plasma concentration-versus-time curve (AUC) was 2555 +/- 98 microg x min/mL, the plasma clearance was 472 +/- 18.9 mL/h/kg, and the volume of distribution at steady state was 0.22 +/- 0.01 L/kg. After rectal administration, the plasma concentration of ASA peaked at 5.05 +/- 0.80 microg/mL at 0.33 h, then decreased to undetectable levels by 4 h; the plasma concentration of SA peaked at 17.39 +/- 5.46 microg/mL at 2 h, then decreased to 1.92 +/- 0.25 microg/mL by 36 h. After rectal administration, the AUC for ASA was 439.4 +/- 94.55 microg x min/mL and the bioavailability was 0.17 +/- 0.037. After IG administration, the plasma concentration of ASA peaked at 1.26 +/- 0.10 microg/mL at 0.67 h, then declined to 0.37 +/- 0.37 microg/mL by 36 h; the plasma concentration of SA peaked at 23.90 +/- 4.94 microg/mL at 4 h and decreased to 0.85 +/- 0.31 microg/mL by 36 h. After IG administration, the AUC for ASA was 146.70 +/- 24.90 microg x min/mL and the bioavailability was 0.059 +/- 0.013. Administration of a single rectal dose of ASA of 20 mg/kg to horses results in higher peak plasma ASA concentrations and greater bioavailability than the same dose given IG. Plasma ASA concentrations after rectal administration should be sufficient to inhibit platelet thromboxane production, and doses lower than those suggested for IG administration may be adequate.
Publication Date: 2003-11-19 PubMed ID: 14620867PubMed Central: PMC280715
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  • Journal Article

Summary

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The study investigates the effects and plasma concentrations of acetylsalicylic acid (ASA), commonly known as aspirin, administered via different routes to horses. Key findings indicate that the rectal administration of ASA results in higher bioavailability and peak plasma concentration as compared to stomach administration.

Research Methodology

  • Six healthy adult horses were chosen for the study, 5 mares and one stallion.
  • The horses were given a single dose of 20mg/kg body weight of ASA in three different ways: intravenous (through a vein), rectal (via the rectum), and intragastric (via the stomach).
  • The study spanned over a period of 36 hours during which regular blood samples were collected through jugular venipuncture (blood extracted from the jugular vein).
  • The researchers used high-performance liquid chromatography to measure the plasma ASA and salicylic acid (SA) concentrations.

Research Findings

  • IV administration of ASA had a mean elimination rate constant of 1.32 +/- 0.09 h(-1), the mean elimination half-life of 0.53 +/- 0.04 hours, and the area under the plasma concentration-versus-time curve (AUC) was 2555 +/- 98 microg x min/mL. The plasma clearance was found to be 472 +/- 18.9 mL/h/kg, and the volume of distribution at steady state was 0.22 +/- 0.01 L/kg.
  • After rectal administration, the peak plasma concentration of ASA was 5.05 +/- 0.80 microg/mL at 0.33 hours and it decreased to undetectable levels by the 4th hour.
  • The peak plasma concentration of SA was 17.39 +/- 5.46 microg/mL at 2 hours, and it decreased to 1.92 +/- 0.25 microg/mL by 36 hours. The AUC for ASA was 439.4 +/- 94.55 microg x min/mL and the bioavailability was 0.17 +/- 0.037.
  • With IG administration, the max plasma concentration of ASA peaked at 1.26 +/- 0.10 microg/mL at 0.67 hours and declined to 0.37 +/- 0.37 microg/mL by 36 hours. The peak plasma concentration of SA was 23.90 +/- 4.94 microg/mL at 4 hours and reduced to 0.85 +/- 0.31 microg/mL by 36 hours. The AUC for ASA was 146.70 +/- 24.90 microg x min/mL and the bioavailability was 0.059 +/- 0.013.

Research Conclusions

  • Based on the findings, the rectal administration of ASA showed a higher peak plasma ASA concentration and greater bioavailability than IG administration.
  • The study suggests that the administration of a single rectal dose of ASA of 20mg/kg to horses could lead to plateau plasma ASA levels adequate to inhibit platelet thromboxane production (an important factor in blood clotting). Further, the research suggests that lower doses than those suggested for IG administration may be adequate when administered rectally.

Cite This Article

APA
Broome TA, Brown MP, Gronwall RR, Casey MF, Meritt KA. (2003). Pharmacokinetics and plasma concentrations of acetylsalicylic acid after intravenous, rectal, and intragastric administration to horses. Can J Vet Res, 67(4), 297-302.

Publication

ISSN: 0830-9000
NlmUniqueID: 8607793
Country: Canada
Language: English
Volume: 67
Issue: 4
Pages: 297-302

Researcher Affiliations

Broome, Ted A
  • Department of Large Animal Clinical Sciences, College of Veterinary Medicine, University of Florida, Gainesville, Florida 32610-0136, USA.
Brown, Murray P
    Gronwall, Ronald R
      Casey, Matthew F
        Meritt, Kelly A

          MeSH Terms

          • Absorption
          • Administration, Rectal
          • Animals
          • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
          • Anti-Inflammatory Agents, Non-Steroidal / blood
          • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics
          • Area Under Curve
          • Aspirin / administration & dosage
          • Aspirin / blood
          • Aspirin / pharmacokinetics
          • Biological Availability
          • Chromatography, High Pressure Liquid / methods
          • Chromatography, High Pressure Liquid / veterinary
          • Cross-Over Studies
          • Female
          • Horses / blood
          • Horses / metabolism
          • Infusions, Intravenous / veterinary
          • Infusions, Parenteral / veterinary
          • Male

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          Citations

          This article has been cited 5 times.