Pharmacokinetic properties of Δ9-tetrahydrocannabinol in serum and oral fluid

Pharmacokinetic properties of Δ9-tetrahydrocannabinol in serum and oral fluid
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DOI:
10.1093/jat/31.5.288
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发表时间:
2007-06-01
影响因子:
2.5
通讯作者:
Toennes, Stefan W.
Toennes, Stefan W.
中科院分区:
医学3区
文献类型:
--
作者:
Kauert, Gerold F.;Ramaekers, Johannes G.;Toennes, Stefan W.

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在一项关于吸食大麻的影响的研究中从10名研究参与者收集配对的血液和口腔液样品(低剂量为18.2 ± 2.8 mg,高剂量为36.5 ± 5.6 mg),直至吸烟后6小时,并分析大麻素Δ 9-四氢大麻酚(THC),11-羟基-THC(THC-OH)和11-去甲-9-羧基-THC(THCA)。吸烟结束时血清中的最高浓度分别为47.8 ± 35.0和79.1 ± 42.5 µ g/L(分别为低剂量和高剂量),并在6小时内降至低于1 µ g/L,消除半衰期为1.4 ± 0.1小时(从1到6小时计算),比之前报道的要短。THC-OH(2.0 ± 0.3 h)和THCA(3.4 ± 0.9 h)的消除半衰期显著更长。在0.25 h采集的第一份样本中,口腔液中的THC浓度最高,分别为900 ± 589和1041 ± 652 µ g/L(分别为低剂量和高剂量),6 h后降至18 ± 12 µ g/L,消除半衰期为1.5 ± 0.6 h。THC在血清和口服液中的消除半衰期以及两种剂量之间的消除半衰期没有显著差异。口服液/血清比为46 ± 27和36 ± 20(分别为低剂量和高剂量),高于先前报告的值,可能是基于样本采集和/或分析问题。总之,尽管血清和口腔液中THC的消除率相似(这似乎是偶然的),但口腔液/血清比率的高度差异不是将口腔液和血清中THC浓度相关联的可靠基础。药物,特别是THC的口腔隔室及其动力学尚未得到令人满意的理解。
In a study on the effects of smoked cannabis (18.2 ± 2.8 mg as low and 36.5 ± 5.6 mg as high dose) paired blood and oral fluid samples were collected from 10 study participants up to 6 h after smoking and analyzed for the cannabinoids Δ9-tetrahydrocannabinol (THC), 11-hydroxy-THC (THC-OH) and 11-nor-9-carboxy-THC (THCA) using gas chromatography-mass spectrometry. Highest concentrations in serum were 47.8 ± 35.0 and 79.1 ± 42.5 µg/L at the end of smoking (low and high dose, respectively) and decreased to less than 1 µg/L during 6 h with elimination half-lives of 1.4 ± 0.1 h calculated from 1 to 6 h, which is shorter than reported previously. The elimination half-lives of THC-OH (2.0 ± 0.3 h) and THCA (3.4 ± 0.9 h) were significantly higher. The THC concentrations in oral fluid were highest with 900 ± 589 and 1041 ± 652 µg/L (low and high dose, respectively) in the first sample collected at 0.25 h and decreased to 18 ± 12 µg/L over 6 h with elimination half-lives of 1.5 ± 0.6 h. The elimination half-life of THC in serum and oral fluid and between the two doses did not significantly differ. Oral fluid/serum ratios were 46 ± 27 and 36 ± 20 (low and high dose, respectively), which are higher than previously reported and might be based on sample collection and/or analytical issues. In conclusion, despite similar elimination rates of THC in serum and oral fluid, which appear incidental, the high differences in oral fluid/serum ratios are not a reliable basis for correlating THC concentrations in oral fluid and serum. The oral compartment and its kinetics for drugs, particularly THC, are not yet satisfactorily understood.