Department of Pharmaceutics, University of Florida College of Pharmacy, Gainesville, FL, USA.
Translational Drug Development Core, University of Florida Clinical and Translational Science Institute, Gainesville, FL, USA.
Eur J Drug Metab Pharmacokinet. 2023 Jul;48(4):427-435. doi: 10.1007/s13318-023-00839-3. Epub 2023 Jun 19.
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.
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.
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.
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.
市面上有各种各样的含有大麻二酚（CBD）的产品。其中最常见的一种产品是 CBD 油，被用于自行治疗多种疾病。这些油有 CBD 分离物、广谱[除 Δ-9-四氢大麻酚（THC）以外的所有萜烯和少量大麻素]和全谱（含有 THC<0.3%干重的所有萜烯和少量大麻素）产品。进行了一项系统药代动力学研究，以确定以分离物、广谱或全谱产品口服给药后，CBD 的药代动力学参数和全身暴露是否存在差异。
雄性和雌性 Sprague Dawley 大鼠接受了单次、等效的口服 CBD 剂量，以分离物、广谱或全谱产品给药。还进行了一项使用 CBD 分离物加 0.2%THC 的内部制剂的额外研究。还进行了渗透测定，以研究 THC 的存在是否会改变 CBD 的肠道通透性。
与分离物和广谱产品相比，全谱产品给药时 CBD 的口服生物利用度增加（雄性和雌性大鼠分别增加 12%和 21%）。市售全谱制剂（含 0.2%THC 加萜烯和其他少量大麻素的 3.1%CBD）与 CBD 全谱内部制剂（3.2%CBD 分离物加 0.2%THC 分离物）之间，CBD 的生物利用度没有差异。体外渗透测定表明，THC 的存在会增加 CBD 的渗透性，同时减少 CBD 通过肠壁的外排。
0.2%THC 的存在增加了雄性和雌性大鼠 CBD 的口服生物利用度，表明全谱产品可能会因系统内可利用的暴露量增加而提高 CBD 的有效性。
