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Model-Based Analysis of Cannabidiol Dose-Exposure Relationship and Bioavailability
Sin Yin Lim1, Satish Sharan2, Sukyung Woo2
1Department of Pharmacy, Clinical and Administrative Sciences, University of Oklahoma Health- Sciences Center College of Pharmacy, Oklahoma City, Oklahoma.
Pharmacotherapy
|February 15, 2020
Summary
Cannabidiol (CBD) absorption varies significantly by dosage form and food intake. Bioavailability decreases with higher doses, especially for oral solutions, impacting effective dosing strategies.
Area of Science:
- Pharmacokinetics and Pharmacodynamics
- Cannabinoid Research
- Drug Absorption and Bioavailability
Background:
- Significant variability exists in the pharmacokinetics of cannabidiol (CBD).
- Limited data is available regarding CBD's systemic bioavailability.
- Understanding dose-exposure relationships is crucial for optimizing CBD therapy.
Purpose of the Study:
- To establish the dose-exposure relationship for CBD.
- To evaluate the impact of different dosage forms (oral solution, capsule, oromucosal spray/drop) on CBD absorption.
- To assess the influence of food intake and varying doses on CBD bioavailability.
Main Methods:
- A population-based meta-analysis of 15 clinical studies involving healthy volunteers.
- Extraction of CBD plasma concentration-time profiles for single doses ranging from 5 to 6000 mg.
- Application of nonlinear mixed-effects modeling with a three-compartment model, utilizing Weibull or zero-order absorption models to analyze dose, dosage form, and food effects.
Main Results:
- CBD exposure increased less than proportionally with doses ≥750 mg for oral solutions, with bioavailability decreasing at higher doses (6.5% at 3000 mg).
- Bioavailability was similar for oral capsules (5.6%) and fed-state oromucosal spray/drops (6.2%), but significantly lower in the fasted state (0.9%).
- The Weibull model best described oral solution, capsule, and fed-state oromucosal spray/drop absorption, with time to maximum concentration varying by formulation and feeding status.
Conclusions:
- The study quantifies the effects of dose, dosage form, and feeding status on CBD pharmacokinetics.
- These factors significantly influence CBD absorption and bioavailability.
- Consideration of these variables is essential for effective CBD dose optimization in clinical practice.
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