Nahler Gerhard, Grotenhermen Franjo, Zuardi Antonio Waldo, Crippa José A S
CIS Clinical Investigation Support GmbH, Wien, Austria.
Nova-Institut GmbH, Chemiepark Knapsack, Hürth, Germany.
Cannabis Cannabinoid Res. 2017 May 1;2(1):81-86. doi: 10.1089/can.2017.0009. eCollection 2017.
Cannabidiol (CBD), a major cannabinoid of hemp, does not bind to CB1 receptors and is therefore devoid of psychotomimetic properties. Under acidic conditions, CBD can be transformed to delta9-tetrahydrocannabinol (THC) and other cannabinoids. It has been argued that this may occur also after oral administration in humans. However, the experimental conversion of CBD to THC and delta8-THC in simulated gastric fluid (SGF) is a highly artificial approach that deviates significantly from physiological conditions in the stomach; therefore, SGF does not allow an extrapolation to conditions. Unsurprisingly, the conversion of oral CBD to THC and its metabolites has not been observed to occur , even after high doses of oral CBD. In addition, the typical spectrum of side effects of THC, or of the very similar synthetic cannabinoid nabilone, as listed in the official Summary of Product Characteristics (e.g., dizziness, euphoria/high, thinking abnormal/concentration difficulties, nausea, tachycardia) has not been observed after treatment with CBD in double-blind, randomized, controlled clinical trials. In conclusion, the conversion of CBD to THC in SGF seems to be an artifact.
大麻二酚(CBD)是大麻的一种主要大麻素,不与CB1受体结合,因此没有拟精神病特性。在酸性条件下,CBD可转化为Δ9-四氢大麻酚(THC)和其他大麻素。有人认为,在人类口服后也可能发生这种情况。然而,在模拟胃液(SGF)中将CBD实验性转化为THC和Δ8-THC是一种高度人为的方法,与胃中的生理状况有很大偏差;因此,SGF不能外推至实际情况。不出所料,即使在高剂量口服CBD后,也未观察到口服CBD转化为THC及其代谢物的情况。此外,在双盲、随机、对照临床试验中,用CBD治疗后,未观察到THC或非常相似的合成大麻素纳布隆的典型副作用谱(如头晕、欣快感/兴奋、思维异常/注意力不集中、恶心、心动过速)。总之,在SGF中CBD向THC的转化似乎是一种假象。