Comparison of Five Oral Cannabidiol Preparations in Adult Humans: Pharmacokinetics, Body Composition, and Heart Rate Variability

Abstract

Data supporting the physiological effects of cannabidiol (CBD) ingestion in humans are conflicting. Differences between CBD preparations and bioavailability may contribute to these discrepancies. Further, an influence of body composition on CBD bioavailability is feasible, but currently undocumented. The aims of this study were to: (1) compare the pharmacokinetics of five oral CBD preparations over 4 h; (2) examine the relationship between body composition and CBD pharmacokinetics; and, (3) explore the influence of CBD on heart rate variability. In total, five preparations of CBD, standardized to 30 mg, were orally administered to 15 healthy men and women (21–62 years) in a randomized, crossover design. Prior to and 60 min following CBD ingestion, heart rate variability was determined. Body composition was assessed using dual energy X-ray absorptiometry. Peak circulating CBD concentration, time to peak concentration, and area under the curve was superior in a preparation comprising 5% CBD concentration liquid. Fat free mass was a significant predictor (R2 = 0.365, p = 0.017) of time to peak concentration for this preparation. Several heart rate variability parameters, including peak frequency of the high frequency band, were favorably, but modestly modified following CBD ingestion. These data confirm an influence of CBD preparation and body composition on CBD bioavailability, and suggest that acute CBD ingestion may have a modest influence on autonomic regulation of heart rate.

Pharmacokinetic Investigation of Commercially Available Edible Marijuana Products in Humans: Potential Influence of Body Composition and Influence on Glucose Control

“…Previously, it has been reported that parameters of oral CBD pharmacokinetics, including T max , were associated with anthropometric variables, including fat-free mass and body mass index [ 11 ]. A number of explanations were proposed, such as the positive relationship between fat-free mass and blood volume [ 32 , 33 ], representing a greater reservoir in which to dilute circulating metabolites; greater perfusion of metabolically active tissues, thereby leading to enhanced clearance of circulating metabolites; and the lipophilic nature of CBD.…”

“…Additionally, the body composition of the edible marijuana consumer may have an influence on pharmacokinetics. Case in point, cannabidiol (CBD) is a non-psychoactive component of Cannabis sativa L.; the time to maximal circulating CBD concentration (T max ) following ingestion of a commercial oral CBD preparation is related to fat free mass (R 2 = 0.365) [ 11 ]. Further, adiposity may also influence the pharmacokinetics of THC absorption on account of the lipophilic properties of THC [ 12 ].…”

Pharmacokinetic Investigation of Commercially Available Edible Marijuana Products in Humans: Potential Influence of Body Composition and Influence on Glucose Control

“…Previously, it has been reported that parameters of oral CBD pharmacokinetics, including Tmax, were associated with anthropometric variables, including fat free mass and body mass index [11]. A number of explanations were proposed, such as the positive relationship between fat free mass and blood volume [32,33], representing a greater reservoir in which to dilute circulating metabolites; greater perfusion of metabolically active tissues, thereby leading to enhanced clearance of circulating metabolites; and, the lipophilic nature of CBD.…”

Cannabinoid Formulations and Delivery Systems: Current and Future Options to Treat Pain

“…An interesting recent analysis of five oral CBD formulations has been described by Williams [ 128 ]. A dose of 30 mg CBD was tested as a solid in suspension in water (code 203), with oil and starch (code 472), in an oil solution (code 178), as a liquid formulation with Quillaja extract (20% CBD, code 340) and with gum Arabic (5% CBD code 707).…”