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市售大麻二酚(CBD)分离物、广谱和全谱产品的比较药代动力学。

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

机构信息

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.

出版信息

Eur J Drug Metab Pharmacokinet. 2023 Jul;48(4):427-435. doi: 10.1007/s13318-023-00839-3. Epub 2023 Jun 19.

Abstract

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.

摘要

背景和目的

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。

方法

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。

结果

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。

结论

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。

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