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Australian veterinary journal1998; 75(12); 897-901; doi: 10.1111/j.1751-0813.1997.tb11261.x

Uptake of drugs from topically applied anti-inflammatory preparations applied to racing animals.

Abstract: To determine whether a drug detected in the blood or urine of a racing animal could have penetrated through the skin from a topically applied preparation. Methods: Blood and urine of dogs and horses were analysed after topical administration of three common nonsteroidal anti-inflammatory preparations. Methods: Dimethylsulphoxide was analysed using a gas chromatograph with a flame photometric detector. Phenylbutazone, its metabolites and lignocaine were analysed using a gas chromatograph with a mass selective detector. Results: Dimethylsulphoxide, phenylbutazone and lignocaine were detected in dog urine after multiple applications of the preparations. The maximum concentration of dimethylsulphoxide in dog urine correlated with the concentration of dimethylsulphoxide in the preparation. Phenylbutazone penetrated the skin more effectively from the cream than from the solution or gel preparations. This penetration was independent of the concentration of dimethylsulphoxide. Conclusions: The superior penetration of phenylbutazone from the cream can be explained by it being present as a neutral molecule in an hydrophobic medium. It is proposed that phenylbutazone penetrates the skin of greyhounds most effectively by a hydrophobic lipid route which is likely to be different from the path by which dimethylsulphoxide penetrates the skin.
Publication Date: 1998-02-20 PubMed ID: 9469226DOI: 10.1111/j.1751-0813.1997.tb11261.xGoogle Scholar: Lookup
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  • Journal Article
  • Research Support
  • Non-U.S. Gov't

Summary

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The research investigates whether drugs in topically applied anti-inflammatory preparations could enter the bloodstream of racing animals. It found that some substances from these products did indeed appear in the urine of dogs and horses after application, with different preparations affecting the rate of absorption.

Research Methodology

  • The study used dogs and horses as subjects and applied three common nonsteroidal anti-inflammatory preparations topically.
  • The substances tested were dimethylsulphoxide, phenylbutazone, its metabolites, and lignocaine. These were monitored in the blood and urine of the animals.
  • A gas chromatograph with a flame photometric detector was used to analyse the presence of dimethylsulphoxide.
  • A gas chromatograph with a mass selective detector was used to analyse phenylbutazone, its metabolites, and lignocaine.

Research Findings

  • Dimethylsulphoxide, phenylbutazone, and lignocaine were identified in the urine of dogs following multiple applications of the anti-inflammatory preparations.
  • The amount of dimethylsulphoxide found in dog urine was proportionate to the amount present in the preparation applied.
  • Phenylbutazone penetrated the skin more effectively from a cream-based preparation than from a solution or gel. This absorption wasn’t impacted by the concentration of dimethylsulphoxide.

Conclusions

  • The study concluded that the superior skin penetration of phenylbutazone from cream preparations could be due to its presence as a neutral molecule in a hydrophobic medium.
  • The researchers suggest that phenylbutazone penetrates the skin of dogs most effectively via a hydrophobic lipid route. This mechanism is likely distinct from the pathway used by dimethylsulphoxide to penetrate the skin.

By understanding the pathways and mechanisms of topical drug absorption, better monitoring and regulation strategies could be set up for the use of such preparations in racing animals. This could help prevent the misuse of performance-enhancing substances.

Cite This Article

APA
Thomas AD, Bowater IC, Vine JH, McLean JG. (1998). Uptake of drugs from topically applied anti-inflammatory preparations applied to racing animals. Aust Vet J, 75(12), 897-901. https://doi.org/10.1111/j.1751-0813.1997.tb11261.x

Publication

ISSN: 0005-0423
NlmUniqueID: 0370616
Country: England
Language: English
Volume: 75
Issue: 12
Pages: 897-901

Researcher Affiliations

Thomas, A D
  • School of Engineering and Science, Swinburne University of Technology, Hawthorn, Victoria.
Bowater, I C
    Vine, J H
      McLean, J G

        MeSH Terms

        • Administration, Topical
        • Animals
        • Anti-Inflammatory Agents / administration & dosage
        • Anti-Inflammatory Agents / analysis
        • Anti-Inflammatory Agents / pharmacokinetics
        • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
        • Anti-Inflammatory Agents, Non-Steroidal / analysis
        • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics
        • Chromatography, Gas / methods
        • Chromatography, Gas / veterinary
        • Dimethyl Sulfoxide / administration & dosage
        • Dimethyl Sulfoxide / analysis
        • Dimethyl Sulfoxide / pharmacokinetics
        • Dogs / metabolism
        • Dogs / physiology
        • Doping in Sports
        • Horses / metabolism
        • Horses / physiology
        • Lidocaine / administration & dosage
        • Lidocaine / analysis
        • Lidocaine / pharmacokinetics
        • Phenylbutazone / administration & dosage
        • Phenylbutazone / analysis
        • Phenylbutazone / pharmacokinetics

        Citations

        This article has been cited 2 times.
        1. Stahl J, Kietzmann M. The effects of chemical and physical penetration enhancers on the percutaneous permeation of lidocaine through equine skin. BMC Vet Res 2014 Jun 20;10:138.
          doi: 10.1186/1746-6148-10-138pubmed: 24950611google scholar: lookup
        2. Kayasuga-Kariya Y, Iwanaga S, Fujisawa A, Lin LS, Suzuki S, Chung UI, Sasaki N, Shimohata N, Mochizuki M. Dermal cell damage induced by topical application of non-steroidal anti-inflammatory drugs is suppressed by trehalose co-lyophilization in ex vivo analysis. J Vet Med Sci 2013 Dec 30;75(12):1619-22.
          doi: 10.1292/jvms.12-0502pubmed: 23884023google scholar: lookup