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在一项针对老年马的随机交叉试验中,评估大麻二酚的药代动力学。

Pharmacokinetics of cannabidiol in a randomized crossover trial in senior horses.

机构信息

M. H. Gluck Equine Research Center, Department of Veterinary Science, University of Kentucky, Lexington, KY.

K.L Maddy Equine Analytical Pharmacology Laboratory, School of Veterinary Medicine, University of California-Davis, Davis, CA.

出版信息

Am J Vet Res. 2022 Jul 18;83(9):ajvr.22.02.0028. doi: 10.2460/ajvr.22.02.0028.

DOI:10.2460/ajvr.22.02.0028
PMID:35895770
Abstract

OBJECTIVE

To determine the pharmacokinetics, bioavailability, and pharmacological effects of cannabidiol (CBD) in senior horses.

ANIMALS

8 university-owned senior horses.

PROCEDURES

In this randomized, crossover study, horses were assigned to receive either a single oral dose of 2 mg/kg CBD in oil or a single IV dose of 0.1 mg/kg CBD in DMSO between August 10 and September 4, 2020. Blood samples were collected before and then 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, and 264 hours after CBD administration. Serum biochemical analyses and CBCs were performed. Plasma concentrations of CBD and its metabolites were determined with the use of liquid chromatography-tandem mass spectrometry.

RESULTS

Concentrations of CBD and metabolites (7-COH CBD and 7-COOH CBD) were detected in all plasma samples up to 8 hours after dosing (oral and IV), with 7-COOH CBD being the most predominant metabolite. Pharmacokinetic results for CBD oral dosing at 2 mg/kg were mean ± SD half-life of 7.22 ± 2.86 hours, maximum concentration of 18.54 ± 9.80 ng/mL, and time to maximum concentration of 2.46 ± 1.62 hours. For both oral and IV administrations, 7-COOH CBD did not fall below the limit of quantification for the times reported. Oral bioavailability for CBD was 7.92%. There was no meaningful effect of CBD on results for CBC, serum biochemical analyses, or vital signs for any horse.

CLINICAL RELEVANCE

Pharmacokinetics and bioavailability of CBD in senior horses were determined, and there were no adverse effects of administering either the oral or IV dose of CBD evaluated.

摘要

目的

确定大麻二酚(CBD)在老年马中的药代动力学、生物利用度和药效。

动物

8 匹大学所有的老年马。

程序

在这项随机、交叉研究中,2020 年 8 月 10 日至 9 月 4 日,马匹被分配接受单剂量 2 毫克/千克 CBD 油或单剂量 0.1 毫克/千克 CBD 二甲基亚砜静脉注射。在 CBD 给药前和给药后 0.5、1、4、8、24、48、72、96、120、144、168、192、216、240 和 264 小时采集血样。进行血清生化分析和全血细胞计数。使用液相色谱-串联质谱法测定 CBD 及其代谢物的血浆浓度。

结果

在给药后 8 小时内,所有血浆样本中均检测到 CBD 和代谢物(7-COH CBD 和 7-COOH CBD)的浓度(口服和静脉注射),其中 7-COOH CBD 是最主要的代谢物。2 毫克/千克口服 CBD 的药代动力学结果为平均 ± SD 半衰期为 7.22 ± 2.86 小时,最大浓度为 18.54 ± 9.80ng/mL,达峰时间为 2.46 ± 1.62 小时。对于口服和静脉注射,7-COOH CBD 在报告的时间内均未低于定量下限。CBD 的口服生物利用度为 7.92%。对于任何一匹马,CBD 对全血细胞计数、血清生化分析或生命体征均无明显影响。

临床意义

确定了 CBD 在老年马中的药代动力学和生物利用度,且评估的口服或静脉注射 CBD 剂量均无不良反应。

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