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饮食脂肪和口服给药系统对成年人中大麻二酚药代动力学的影响。

Impact of Dietary Fat and Oral Delivery System on Cannabigerol Pharmacokinetics in Adults.

作者信息

Story Galaxie, Lee Junghak, Cohen Gil, Rani Asha, Doherty Jeffery, Sela David A

机构信息

Department of Food Science, University of Massachusetts, Amherst, Massachusetts, USA.

Massachusetts Hemp Analysis Facility, and University of Massachusetts, Amherst, Massachusetts, USA.

出版信息

Cannabis Cannabinoid Res. 2024 Dec;9(6):1543-1555. doi: 10.1089/can.2023.0174. Epub 2024 Apr 4.

Abstract

Cannabigerol (CBG) is a nonintoxicating cannabinoid synthesized in the plant that is incorporated into dietary supplements. This study investigated the influence of dietary fat and an emulsified delivery vehicle on CBG pharmacokinetics (PKs) after oral ingestion by adults. Consented participants were enrolled in a double-crossover pilot study and were blinded to the delivery vehicle type (isolate or emulsification) and isocaloric meal condition (low-fat=<5 g fat/meal or high-fat [HF]=>30 g fat/meal). The concentration of CBG in human plasma was measured after a single 25 mg dose of CBG using liquid chromatography-tandem mass spectrometry (LC-MS/MS). PK parameters were calculated using noncompartmental analysis. The PKs of the two delivery systems (emulsified vs. non-emulsified) were significantly impacted by the HF meal condition. Participants in the HF meal group exhibited significantly higher area under the plasma concentration time curve from time 0 to last quantifiable value, maximum concentration, and terminal half-life. Participants in the HF meal group also had a significantly lower terminal elimination rate constant and time to maximum concentration (), in addition to decreased variation. The threshold for bioequivalence between conditions was not met. An exploratory aim correlated anthropometric measures and previous day's dietary intake on PK parameters which yielded inconsistent results across dietary fat conditions. In aggregate, dietary fat had a greater effect on CBG PKs than the emulsified delivery vehicle. This supports accounting for dietary intake in development of therapeutics and administration guidelines for orally delivered CBG.

摘要

大麻二酚(CBG)是一种在植物中合成的无致幻作用的大麻素,已被纳入膳食补充剂中。本研究调查了膳食脂肪和乳化递送载体对成年人口服后CBG药代动力学(PKs)的影响。获得同意的参与者被纳入一项双交叉试点研究,并对递送载体类型(分离物或乳化剂)和等热量膳食条件(低脂=每餐<5克脂肪或高脂[HF]=每餐>30克脂肪)不知情。使用液相色谱-串联质谱法(LC-MS/MS)在单次服用25毫克CBG后测量人血浆中CBG的浓度。使用非房室分析计算PK参数。两种递送系统(乳化与未乳化)的PKs受到高脂膳食条件的显著影响。高脂膳食组的参与者在血浆浓度-时间曲线下从时间0到最后可量化值的面积、最大浓度和末端半衰期显著更高。高脂膳食组的参与者除了变异减少外,末端消除速率常数和达到最大浓度的时间()也显著更低。未达到不同条件之间生物等效性的阈值。一个探索性目标是将人体测量指标和前一天的膳食摄入量与PK参数相关联,结果在不同膳食脂肪条件下不一致。总体而言,膳食脂肪对CBG PKs的影响大于乳化递送载体。这支持在开发口服CBG的治疗方法和给药指南时考虑膳食摄入量。

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The Pharmacological Case for Cannabigerol.大麻素二醇的药理学案例。
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