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Home / Equine Research Bank / Equine Vet J / Pharmacokinetics and oral bioavailability of cannabidiol in ...
Equine veterinary journal2023; 55(6); 1094-1103; doi: 10.1111/evj.13923

Pharmacokinetics and oral bioavailability of cannabidiol in horses after intravenous and oral administration with oil and micellar formulations.

Abstract: Intravenous pharmacokinetics and oral bioavailability of cannabidiol (CBD) with different formulations have not been investigated in horses and may represent a starting point for clinical studies. Objective: To describe pharmacokinetics after intravenous and oral administrations with oil and micellar formulations and simulate different treatments. Methods: Single intravenous experiment and two-way randomised oral experiments, Latin-square design. Methods: Eight healthy horses received intravenous CBD at 1.00 mg/kg dose, oral CBD in sesame oil and in micellar formulation, both at 10.00 mg/kg. Concentrations were measured using LC-MS/MS and fitted by nonlinear mixed effect modelling. Parameters obtained were used to simulate single and multiple treatments at steady state. Results: Intravenous and oral concentrations were simultaneously fitted using a three-compartment model. Final estimates indicate that CBD has a volume of distribution of 36 L/kg associated with a systemic clearance of 1.46 L/h/kg and half-lives ranged between 24 and 34 h. Oral bioavailability was close to 14% for both oral administrations. Simulated dose regimen of CBD every 12 and 24 h predicted similar percentages to reach effective plasma concentration with both oral formulation at 10.00 mg/kg. Conclusions: A small horse population was used (8 horses per trial). Conclusions: Oral bioavailability was low at the doses studied but fell within the range described for horse and other species. CBD had a high steady-state volume of distribution, a high clearance and long half-lives. No adverse reactions were detected at any dose or route. The micellar formulation showed a faster absorption and higher concentration peak, while the oil formulation presented lower levels, but more maintained over time. Simulations predicted that both could be useful in multiple oral dose treatments. These results indicated that CBD could be of interest, but further studies are needed to evaluate its clinical use in horses.
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Publication Date: 2023-01-16 PubMed ID: 36624043DOI: 10.1111/evj.13923Google 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.

The research studied the oral bioavailability and intravenous pharmacokinetics of cannabidiol (CBD) in horses using oil and micellar formulations. The findings reveal that CBD absorption and oral availability may be low but sustainable in horses and may be useful in various oral dose treatments, although more research is necessary to confirm its safety and efficiency.

Research Methods

  • The study was conducted on eight healthy horses using single intravenous experiments and two-way randomized oral experiments, designed through a Latin-square pattern.
  • The horses received an intravenous dose of CBD at 1.00 mg/kg, oral CBD in sesame oil, and in micellar formulation, both at 10.00 mg/kg.
  • CBD concentrations were measured using LC-MS/MS (a technique used for identifying and quantifying components in a sample) and fitted by nonlinear mixed effect modelling to analyze the data and statistically model the effect of CBD.

Results

  • The research applied a three-compartment model to fit both intravenous and oral concentrations of CBD. This model takes into account the complexities of drug distribution and excretion within the body, particularly for this compound.
  • The study found that CBD has a high volume of distribution (36 L/kg) associated with a systemic clearance of 1.46 L/h/kg and half-lives ranged between 24 and 34 h. The volume of distribution and clearance values illustrate how the body processes CBD.
  • Oral bioavailability was close to 14% for both oral administrations, which means about 14% of the CBD was available to have an active effect. Oral bioavailability was low at the doses studied but fell within the range described for horses and other species.
  • Simulated dose regimen of CBD every 12 and 24 hours predicted similar percentages to reach effective plasma concentration with both oral formulation at 10.00 mg/kg.
  • No adverse reactions were detected at any dose or route. The micellar formulation showed a faster absorption and higher concentration peak, while the oil formulation presented lower levels, but was more maintained over time.

Conclusion

  • Based on the research with a small horse population (8 horses per trial), CBD showed potential as a treatment methodology via both oil and micellar formulation. However, the general bioavailability of these methods were low, but the slow and sustained absorption could provide clinical benefits.
  • The micellar formulation had a faster absorption and peak in concentration while the oil formulation took more time but maintained lower levels over time.
  • Though promising, further studies with larger sample sizes are needed to evaluate its clinical use in horses and to ascertain long-term safety and efficiency.

Cite This Article

APA
Sánchez de Medina A, Serrano-Rodríguez JM, Díez de Castro E, García-Valverde MT, Saitua A, Becero M, Muñoz A, Ferreiro-Vera C, Sánchez de Medina V. (2023). Pharmacokinetics and oral bioavailability of cannabidiol in horses after intravenous and oral administration with oil and micellar formulations. Equine Vet J, 55(6), 1094-1103. https://doi.org/10.1111/evj.13923

Publication

Equine veterinary journal
ISSN: 2042-3306
NlmUniqueID: 0173320
Country: United States
Language: English
Volume: 55
Issue: 6
Pages: 1094-1103

Researcher Affiliations

Sánchez de Medina, Antonia
  • Veterinary Clinical Hospital, University of Cordoba, Córdoba, Spain.
  • Department of Animal Medicine and Surgery, Veterinary Faculty, University of Cordoba, Córdoba, Spain.
Serrano-Rodríguez, Juan Manuel
  • Department of Nursing, Pharmacology and Physiotherapy, Veterinary Faculty, University of Córdoba, Córdoba, Spain.
Díez de Castro, Elisa
  • Veterinary Clinical Hospital, University of Cordoba, Córdoba, Spain.
  • Department of Animal Medicine and Surgery, Veterinary Faculty, University of Cordoba, Córdoba, Spain.
García-Valverde, María Teresa
  • Phytoplant Research S.L.U., Córdoba, Spain.
Saitua, Aritz
  • Veterinary Clinical Hospital, University of Cordoba, Córdoba, Spain.
Becero, Mireia
  • Veterinary Clinical Hospital, University of Cordoba, Córdoba, Spain.
Muñoz, Ana
  • Department of Animal Medicine and Surgery, Veterinary Faculty, University of Cordoba, Córdoba, Spain.
  • Equine Sport Medicine Center CEMEDE, Department of Animal Medicine and Surgery, Veterinary Faculty, University of Córdoba, Córdoba, Spain.
Ferreiro-Vera, Carlos
  • Phytoplant Research S.L.U., Córdoba, Spain.
Sánchez de Medina, Verónica
  • Phytoplant Research S.L.U., Córdoba, Spain.

MeSH Terms

  • Horses
  • Animals
  • Cannabidiol / pharmacokinetics
  • Biological Availability
  • Chromatography, Liquid / veterinary
  • Tandem Mass Spectrometry / veterinary
  • Administration, Oral

Grant Funding

  • 12020087 / Phytoplant Research S.L.U.
  • Institut Hospital del Mar d'Investigacions Mèdiques

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This article has been cited 14 times.
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