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胡椒碱对急性和慢性给药后大麻二酚经口腔吸收的影响。

The effect of piperine on oral absorption of cannabidiol following acute vs. chronic administration.

机构信息

Institute for Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, P.O. Box 12065, Jerusalem 91120, Israel.

Institute for Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, P.O. Box 12065, Jerusalem 91120, Israel.

出版信息

Eur J Pharm Sci. 2020 May 30;148:105313. doi: 10.1016/j.ejps.2020.105313. Epub 2020 Mar 19.

Abstract

Piperine is an alkaloid naturally found in black pepper with a myriad of pharmacological attributes. Piperine's most far reaching indication is drug absorption enhancment, with supportive data regarding its ability to inhibit first pass effect mechanisms. However, alongside these findings, the role of piperine as an absorption enhancer is undermined with publications stating an apparent effect of a metabolic inducer. The aim of this work is to investigate the effect of repeated administration of piperine in a lipid-based formulation ,on oral absorption of cannabidiol (CBD), compared to acute piperine dosing. The effect of piperine on CBD absorption was determined pre-clinically in the freely moving rat model. Results of this work demonstrated that there was no significant difference in piperine's effect, when given chronically or in a single dose regimen. Both groups resulted in approximate 2.5-fold increase in oral bioavailability of CBD compared to control group without piperine.

摘要

胡椒碱是黑胡椒中天然存在的一种生物碱,具有多种药理学特性。胡椒碱最广泛的用途是增强药物吸收,有数据支持其抑制首过效应机制的能力。然而,除了这些发现,胡椒碱作为吸收增强剂的作用受到质疑,有出版物指出其作为代谢诱导剂的明显作用。这项工作的目的是研究在脂质制剂中重复给予胡椒碱对大麻二酚(CBD)口服吸收的影响,与急性胡椒碱给药相比。在自由活动的大鼠模型中,预先研究了胡椒碱对 CBD 吸收的影响。这项工作的结果表明,无论是长期给予还是单次剂量方案,胡椒碱的作用都没有显著差异。与没有胡椒碱的对照组相比,两组都使 CBD 的口服生物利用度增加了约 2.5 倍。

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