Arout Caroline A, Harris Hannah M, Wilson Noah M, Mastropietro Kyle F, Bozorgi Amanda M, Fazilov Gabriela, Tempero José, Walker Mariah, Haney Margaret
Department of Psychiatry, New York State Psychiatric Institute, Columbia University Irving Medical Center, New York, New York, USA.
Center for Medicinal Cannabis Research, San Diego State University/University of California, San Diego, California, USA.
Cannabis Cannabinoid Res. 2025 Jun;10(3):457-466. doi: 10.1089/can.2023.0249. Epub 2024 Dec 9.
Few studies have directly compared the bioavailability of different cannabinoid formulations. Our goal was to assess the pharmacokinetic parameters and relative bioavailability of two Δ9-tetrahydrocannabinol:cannabidiol (THC:CBD) formulations: orally administered THC:CBD extract and oromucosally administered nabiximols. This pilot crossover study counterbalanced (1) 1 mL of orally administered THC:CBD extract (10 mg/mL each of THC and CBD in grapeseed oil) and (2) oromucosally administered nabiximols (four sprays of 2.7 mg THC and 2.5 mg CBD per spray, for a total dose of 10.8 mg THC and 10 mg CBD). Blood samples were obtained pre-dose and at 16 post-dose timepoints over 24 h. Pharmacokinetic parameters were calculated for THC, 11-hydroxy-tetrahydrocannabinol (11-OH-THC), and CBD. Twelve occasional cannabis users (6 male, 6 female) were tested under fasting conditions. for THC and CBD was significantly higher with significantly shorter half-lives for THC:CBD extract versus nabiximols. for nabiximols was significantly higher in males compared with females. Under both treatment conditions, THC and CBD were undetectable by 24 h post-dose, and 11-OH-THC was markedly reduced from its peak. No serious adverse events were reported. Little is known about the comparative pharmacokinetics of commercially available cannabis products. This pilot study shows that the extract formulation achieved higher THC and CBD concentrations within a shorter time frame than nabiximols. These findings may have implications for clinical populations using these formulations therapeutically. Future studies should examine multiple doses in the context of therapeutic outcomes to characterize the relative clinical utility of these formulations.
很少有研究直接比较不同大麻素制剂的生物利用度。我们的目标是评估两种Δ9-四氢大麻酚:大麻二酚(THC:CBD)制剂的药代动力学参数和相对生物利用度:口服THC:CBD提取物和口腔黏膜给药的纳比西林。这项初步交叉研究采用了平衡设计,(1)口服1 mL THC:CBD提取物(葡萄籽油中THC和CBD各10 mg/mL),(2)口腔黏膜给药纳比西林(每次喷雾含2.7 mg THC和2.5 mg CBD,共四次喷雾,THC总剂量为10.8 mg,CBD总剂量为10 mg)。在给药前以及给药后24小时内的16个时间点采集血样。计算了THC、11-羟基-四氢大麻酚(11-OH-THC)和CBD的药代动力学参数。12名偶尔使用大麻的使用者(6名男性,6名女性)在禁食条件下接受测试。THC和CBD的[此处原文缺失部分内容]显著更高,THC:CBD提取物的半衰期明显短于纳比西林。纳比西林在男性中的[此处原文缺失部分内容]显著高于女性。在两种治疗条件下,给药后24小时时均未检测到THC和CBD,且11-OH-THC从峰值显著下降。未报告严重不良事件。关于市售大麻产品的比较药代动力学知之甚少。这项初步研究表明,提取物制剂在比纳比西林更短的时间内达到了更高的THC和CBD浓度。这些发现可能对治疗性使用这些制剂的临床人群有影响。未来的研究应在治疗结果的背景下检查多剂量情况,以确定这些制剂的相对临床效用。