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Journal of veterinary pharmacology and therapeutics2022; 45(3); 273-282; doi: 10.1111/jvp.13057

Pharmacokinetics of glaucine after intravenous and oral administrations and detection of systemic aporphine alkaloids after ingestion of tulip poplar shavings in horses.

Abstract: Glaucine, an aporphine alkaloid with anti-tussive, anti-inflammatory, and anti-nociceptive properties, has been identified in post-race samples from racehorses. To investigate pharmacokinetics of glaucine in horses, a three-way crossover study of intravenous and oral glaucine (0.1 mg/kg) and orally administered tulip poplar shavings (50 g shavings = 0.001 mg/kg glaucine) was performed in six horses. A two-compartment model best described IV administration with alpha ( ) and beta ( ) half-life lives of 0.3 (0.1-0.7) and 3.1 (2.4-7.8) h, respectively. The area under the curve ( ) was 45.4 (34.7-52.3) h*ng/ml, and the volume of distribution of the central (Vd ) and peripheral (Vd ) compartments was 2.7 (1.3-4.6) and 4.9 (4.3-8.2) L/kg, respectively. A one compartment model best described the oral administration of glaucine with absorption ( ) and elimination ( ) half-lives of 0.09 (0.05-0.15) and 0.7 (0.6-0.8) h, respectively. The area under the curve ( ) was 15.1 (8.0-19.5) h·ng/ml. Bioavailability following oral administration was 17%-48%. Following ingestion of shavings, glaucine and liriodenine were detectable in plasma for up to 16 and 48 h, respectively. Glaucine was quantifiable briefly in the urine from two horses. Liriodenine was quantifiable in urine for 12-20 h in four horses and for 48 h in two horses. The presence of liriodenine indicates ingestion of tulip poplar tree parts, however, does not rule out co-administration of purified glaucine in horses.
© 2022 John Wiley & Sons Ltd.
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Publication Date: 2022-04-08 PubMed ID: 35394081DOI: 10.1111/jvp.13057Google Scholar: Lookup
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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 research article is about a study conducted on horses to understand the pharmacokinetics of glaucine, a drug found in post-race samples from racehorses, when administered via intravenous and oral routes.

Understanding the Pharmacokinetics of Glaucine

The researchers in this study aimed to understand the movement of glaucine in the body of horses. Glaucine is known to have anti-cough, anti-inflammatory, and anti-pain properties. This alkaloid had been identified in samples taken after horse races.

  • The study was conducted as a three-way crossover study, involving intravenous and oral administration of glaucine, and orally provided tulip poplar shavings.
  • To represent realistic conditions, both the oral and intravenous doses of glaucine used were 0.1 mg/kg. The shavings administered were equivalent to 0.001 mg/kg of glaucine.

Findings Post Intravenous Administration

  • It was found that the best way to describe the movement of the compound after intravenous administration was a two-compartment model.
  • They found two half-lives for the compound (0.3 hours and 3.1 hours), indicating the rate at which the compound reduced to half its concentration in the horse’s body.
  • The area under the curve (AUC), indicating the total body exposure to the drug, was calculated as 45.4 h*ng/ml.
  • The volume of distribution revealed that the central compartment volume (2.7 L/kg) was smaller than the peripheral compartment volume (4.9 L/kg).

Findings Post Oral Administration

  • After oral administration of glaucine, it was best described by a one-compartment model.
  • The absorption and elimination half-lives were found to be relatively quick, at 0.09 hours and 0.7 hours respectively.
  • The area under the curve (AUC) was lower at 15.1 h*ng/ml.
  • The bioavailability of the compound, indicating the percentage of administered drug that reaches systemic circulation, was between 17% and 48%.

Detection of Aporphine Alkaloids After Ingestion of Tulip Poplar Shavings

  • Glaucine and liriodenine were detected in the plasma of horses for up to 16 and 48 hours respectively after ingesting tulip poplar shavings.
  • Glaucine was briefly quantifiable in the urine of two horses.
  • Liriodenine, another aporphine alkaloid, was quantifiable in the urine for between 12 and 20 hours in four horses, and for 48 hours in two horses. This suggests that the presence of liriodenine indicates intake of tulip poplar tree parts by the horses. However, it does not exclude the possibility of co-administration of purified glaucine in horses.

Cite This Article

APA
Haughan JE, Missanelli JR, You Y, Stefanovski D, Soma LR, Robinson MA. (2022). Pharmacokinetics of glaucine after intravenous and oral administrations and detection of systemic aporphine alkaloids after ingestion of tulip poplar shavings in horses. J Vet Pharmacol Ther, 45(3), 273-282. https://doi.org/10.1111/jvp.13057

Publication

Journal of veterinary pharmacology and therapeutics
ISSN: 1365-2885
NlmUniqueID: 7910920
Country: England
Language: English
Volume: 45
Issue: 3
Pages: 273-282

Researcher Affiliations

Haughan, Joanne E
  • Department of Clinical Studies - New Bolton Center, School of Veterinary Medicine, University of Pennsylvania, Kennett Square, Pennsylvania, USA.
Missanelli, Jaclyn R
  • Department of Clinical Studies - New Bolton Center, School of Veterinary Medicine, University of Pennsylvania, Kennett Square, Pennsylvania, USA.
  • PA Equine Toxicology & Research Laboratory, West Chester, Pennsylvania, USA.
You, Youwen
  • Department of Clinical Studies - New Bolton Center, School of Veterinary Medicine, University of Pennsylvania, Kennett Square, Pennsylvania, USA.
  • PA Equine Toxicology & Research Laboratory, West Chester, Pennsylvania, USA.
Stefanovski, Darko
  • Department of Clinical Studies - New Bolton Center, School of Veterinary Medicine, University of Pennsylvania, Kennett Square, Pennsylvania, USA.
Soma, Lawrence R
  • Department of Clinical Studies - New Bolton Center, School of Veterinary Medicine, University of Pennsylvania, Kennett Square, Pennsylvania, USA.
Robinson, Mary A
  • Department of Clinical Studies - New Bolton Center, School of Veterinary Medicine, University of Pennsylvania, Kennett Square, Pennsylvania, USA.
  • PA Equine Toxicology & Research Laboratory, West Chester, Pennsylvania, USA.

MeSH Terms

  • Administration, Oral
  • Animals
  • Anti-Inflammatory Agents / pharmacokinetics
  • Aporphines
  • Area Under Curve
  • Cross-Over Studies
  • Eating
  • Half-Life
  • Horses
  • Injections, Intravenous / veterinary
  • Tulipa

Grant Funding

  • Pennsylvania Department of Agriculture State Horse Racing Commission

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Citations

This article has been cited 1 times.
  1. Chen HY, Li C, Shao CY, Wu YJ, Wan HT, He Y. An auxiliary strategy of partial least squares regression in pharmacokinetic/pharmacodynamic studies: A case of application of guhong injection in myocardial ischemia/reperfusion rats. J Food Drug Anal 2024 Mar 15;32(1):79-102.
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