Comparative Pharmacokinetics of Commercially Available Cannabidiol Isolate, Broad-Spectrum, and Full-Spectrum Products

• Published in: European journal of drug metabolism and pharmacokinetics Vol. 48; no. 4; pp. 427 - 435
• Main Authors: Berthold, Erin C., Kamble, Shyam H., Kanumuri, Siva Rama Raju, Kuntz, Michelle A., Senetra, Alexandria S., Chiang, Yi-Hua, McMahon, Lance R., McCurdy, Christopher R., Sharma, Abhisheak
• Format: Journal Article
• Language: English
• Published: Cham Springer International Publishing 01-07-2023
• Subjects: Biomedical and Life Sciences; Biomedicine; Human Physiology; Medical Biochemistry; Original Research Article; Pharmaceutical Sciences/Technology; Pharmacology/Toxicology; Pharmacy
• ISSN: 0378-7966; 2107-0180
• DOI: 10.1007/s13318-023-00839-3

Background and Objectives
A wide variety of products containing cannabidiol (CBD) are available on the commercial market. One of the most common products, CBD oil, is administered to self-treat a variety of conditions. These oils are available as CBD isolate, broad-spectrum [all terpenes and minor cannabinoids except Δ-9-tetrahydrocannabinol (THC)], or full-spectrum (all terpenes and minor cannabinoids with THC < 0.3% dried weight) products. A systematic pharmacokinetic study was performed to determine whether there are differences in the pharmacokinetic parameters and systemic exposure of CBD after oral dosing as an isolate, broad-spectrum, or full-spectrum product.
Methods
Male and female Sprague Dawley rats were treated with a single, equivalent oral dose of CBD delivered as isolate, broad-spectrum, or full-spectrum product. An additional study using an in-house preparation of CBD isolate plus 0.2% THC was performed. A permeability assay was also conducted to investigate whether the presence of THC alters the intestinal permeability of CBD.
Results
There was an increase in the oral bioavailability of CBD (12% and 21% in male and female rats, respectively) when administered as a full-spectrum product compared with the isolate and broad-spectrum products. There was no difference in the bioavailability of CBD between the commercially available full-spectrum formulation (3.1% CBD; containing 0.2% THC plus terpenes and other minor cannabinoids) versus the in-house preparation of CBD full-spectrum (CBD isolate 3.2% plus 0.2% THC isolate). In vitro permeability assays demonstrated that the presence of THC increases permeability of CBD while also decreasing efflux through the gut wall.
Conclusions
The presence of 0.2% THC increased the oral bioavailability of CBD in male and female rats, indicating that full-spectrum products may produce increased effectiveness of CBD due to a greater exposure available systemically.