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

IF 1.9 4区 医学 Q3 PHARMACOLOGY & PHARMACY European Journal of Drug Metabolism and Pharmacokinetics Pub Date : 2023-07-01 DOI:10.1007/s13318-023-00839-3
Erin C Berthold, Shyam H Kamble, Siva Rama Raju Kanumuri, Michelle A Kuntz, Alexandria S Senetra, Yi-Hua Chiang, Lance R McMahon, Christopher R McCurdy, Abhisheak Sharma
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引用次数: 1

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.

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市售大麻二酚分离物、广谱和全谱产品的比较药代动力学。
背景和目的:商业市场上有多种含有大麻二酚(CBD)的产品。CBD油是最常见的产品之一,用于自我治疗各种疾病。这些油可作为CBD分离物,广谱[除Δ-9-tetrahydrocannabinol (THC)外的所有萜烯和少量大麻素]或全谱(所有萜烯和少量大麻素,THC干重< 0.3%)产品。进行了一项系统药代动力学研究,以确定口服分离、广谱或全谱产品给药后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大鼠分别以分离物、广谱或全谱产品的形式口服单一、等量剂量的CBD。使用CBD分离物加0.2%四氢大麻酚的内部制备进行了另一项研究。通过渗透性测定,研究四氢大麻酚的存在是否会改变CBD的肠道渗透性。结果:与分离物和广谱产品相比,作为全谱产品给药时,CBD的口服生物利用度增加(雄性和雌性大鼠分别为12%和21%)。市售全谱制剂(CBD 3.1%;含有0.2% THC +萜烯和其他少量大麻素)与内部制备的CBD全谱(CBD分离物3.2% + 0.2% THC分离物)。体外渗透性试验表明,THC的存在增加了CBD的渗透性,同时也减少了通过肠壁的外排。结论:0.2% THC的存在增加了雄性和雌性大鼠对CBD的口服生物利用度,表明全谱产品可能由于更多的系统可用暴露而提高CBD的有效性。
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来源期刊
CiteScore
3.70
自引率
0.00%
发文量
64
审稿时长
>12 weeks
期刊介绍: Hepatology International is a peer-reviewed journal featuring articles written by clinicians, clinical researchers and basic scientists is dedicated to research and patient care issues in hepatology. This journal focuses mainly on new and emerging diagnostic and treatment options, protocols and molecular and cellular basis of disease pathogenesis, new technologies, in liver and biliary sciences. Hepatology International publishes original research articles related to clinical care and basic research; review articles; consensus guidelines for diagnosis and treatment; invited editorials, and controversies in contemporary issues. The journal does not publish case reports.
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