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海藻提取物与胺碘酮在大鼠体内的药物-药物相互作用:临床实践中胺碘酮生物利用度降低的潜在风险。

Herb-drug interaction of Fucus vesiculosus extract and amiodarone in rats: a potential risk for reduced bioavailability of amiodarone in clinical practice.

机构信息

Laboratory of Pharmacology, Faculty of Pharmacy, University of Coimbra, Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal.

出版信息

Food Chem Toxicol. 2013 Feb;52:121-8. doi: 10.1016/j.fct.2012.11.012. Epub 2012 Nov 20.

Abstract

Fucus vesiculosus is a seaweed claimed to be useful for obesity management. Therefore, considering the relationship between obesity and cardiovascular diseases, this work aimed to assess the potential for an herb-drug interaction among a standardized F. vesiculosus extract (GMP certificate) and amiodarone (a narrow therapeutic index drug) in rats. In a first pharmacokinetic study, rats were simultaneously co-administered with a single-dose of F. vesiculosus (575 mg/kg, p.o.) and amiodarone (50 mg/kg, p.o.); in a second study, rats were pre-treated during 14 days with F. vesiculosus (575 mg/kg/day, p.o.) and received amiodarone (50 mg/kg, p.o.) on the 15th day. Rats of the control groups received the corresponding volume of vehicle. After analysis of the pharmacokinetic data it deserves to be highlighted the significant decrease in the peak plasma concentration of amiodarone (55.4%) as well as the reduction of systemic exposure to the parent drug (~30%) following the simultaneous co-administration of F. vesiculosus extract and amiodarone. This paper reports, for the first time, the herb-drug interaction between F. vesiculosus and amiodarone, which determined a considerable decrease on amiodarone bioavailability in rats. Therefore, the therapeutic efficacy of amiodarone may be compromised by the concurrent administration of herbal slimming medicines/dietary supplements containing F. vesiculosus.

摘要

掌状海带被宣称对肥胖管理有用。因此,考虑到肥胖与心血管疾病之间的关系,这项工作旨在评估一种标准化掌状海带提取物(GMP 证书)和胺碘酮(窄治疗指数药物)在大鼠体内的药物相互作用的潜力。在第一项药代动力学研究中,大鼠同时给予掌状海带(575mg/kg,po)和胺碘酮(50mg/kg,po)单次剂量;在第二项研究中,大鼠在 14 天内用掌状海带(575mg/kg/天,po)预处理,并在第 15 天给予胺碘酮(50mg/kg,po)。对照组大鼠给予相应体积的载体。分析药代动力学数据后值得注意的是,掌状海带提取物和胺碘酮同时给药后,胺碘酮的血浆峰浓度显著降低(55.4%),母体药物的全身暴露量减少(约 30%)。本文首次报道了掌状海带与胺碘酮之间的草药-药物相互作用,这导致大鼠中胺碘酮的生物利用度显著降低。因此,含掌状海带的草药减肥药物/膳食补充剂的同时给药可能会影响胺碘酮的治疗效果。

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