血液和大脑中的口服小类大麻素的药理动力学
Catherine F Moore1, Elise M Weerts1, Justyna Kulpa2
1Division of Behavioral Biology, Department of Psychiatry and Behavioral Sciences, Johns Hopkins University School of Medicine, Baltimore, Maryland, USA.
Cannabis and cannabinoid research
|September 18, 2023
概括
这项研究跟踪了小大麻素如THCV,CBC,CBN和D8-THC在老鼠中的14天. 结果显示,这些大麻素进入血液和大脑,并以不同的积累和消除模式.
科学领域:
- 药理学 药理学是指药理学的学科.
- 大麻素科学 大麻素科学
- 毒理学 毒理学 毒理学
背景情况:
- 小型大麻素 (THCV,CBC,CBN,D8-THC) 在口服配方中越来越多地使用.
- 了解它们的药理动力学特征对于安全有效的治疗用途至关重要.
- 有限的数据存在于口服输送系统中这些化合物的重复剂量药理动力学.
研究的目的:
- 在口服后研究四化甘 (THCV),大麻基 (CBC),大麻 (CBN) 和delta-8-tetrahydrocannabinol (D8-THC) 的药理动力学 (PKs).
- 为了比较单次 (第1天) 和重复 (第14天) 在14天内服用后的PK参数.
- 为了确定多次口服后大脑组织中大麻素分布的程度.
主要方法:
- 斯普拉格-道利大鼠每天接受THCV,CBC,CBN或D8-THC的口服剂量,持续14天.
- 在第一剂和最后剂后的多个时间点收集血液样本进行PK分析 (Tmax,Cmax,AUC).
- 在第一天和第14天服用后24小时,对大脑组织进行了分析,以评估大麻素度.
主要成果:
- 在一次性和重复剂量后,所有测试的大麻素都在血中被检测到.
- 剂量正常化的Cmax和AUC是D8-THC的最高值,其次是CBC,CBN和THCV.
- D8-THC显示血积累,而THCV水平在第14天下降,表明代谢适应.
结论:
- THCV,CBC,CBN和D8-THC达到可检测的血度,并在重复口服后分布在脑组织中.
- 在这些较小的大麻素中,PK概况各不相同,观察到积累和消除的差异.
- 这些发现对于建立适当的剂量范围和未来临床研究的时间表来评估这些化合物的治疗潜力至关重要.
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