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绿茶儿茶素摄入对健康志愿者中赖诺普利药代动力学的影响。

Impact of Green Tea Catechin Ingestion on the Pharmacokinetics of Lisinopril in Healthy Volunteers.

机构信息

Department of Bioregulation and Pharmacological Medicine, School of Medicine, Fukushima Medical University School of Medicine, Fukushima, Japan.

Department of Pharmacy, University of Yamanashi Hospital, Chuo-city, Japan.

出版信息

Clin Transl Sci. 2021 Mar;14(2):476-480. doi: 10.1111/cts.12905. Epub 2020 Oct 22.

DOI:10.1111/cts.12905
PMID:33048477
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7993260/
Abstract

Lisinopril, a highly hydrophilic long-acting angiotensin-converting enzyme inhibitor, is frequently prescribed for the treatment of hypertension and congestive heart failure. Green tea consumption may reduce the risk of cardiovascular outcomes and total mortality, whereas green tea or its catechin components has been reported to decrease plasma concentrations of a hydrophilic β blocker, nadolol, in humans. The aim of this study was to evaluate possible effects of green tea extract (GTE) on the lisinopril pharmacokinetics. In an open-label, randomized, single-center, 2-phase crossover study, 10 healthy subjects ingested 200 mL of an aqueous solution of GTE containing ~ 300 mg of (-)-epigallocatechin gallate, a major catechin component in green tea, or water (control) when receiving 10 mg of lisinopril after overnight fasting. The geometric mean ratio (GTE/control) for maximum plasma concentration and the area under the plasma concentration-time curve of lisinopril were 0.289 (90% confidence interval (CI) 0.226-0.352) and 0.337 (90% CI 0.269-0.405), respectively. In contrast, there were no significant differences in time to reach maximum lisinopril concentration (6 hours in both phases) and renal clearance of lisinopril (57.7 mL/minute in control vs. 56.9 mL/minute in GTE). These results suggest that the extent of intestinal absorption of lisinopril was significantly impaired in the presence of GTE, whereas it had no major effect on the absorption rate and renal excretion of lisinopril. Concomitant use of lisinopril and green tea may decrease oral exposure to lisinopril, and therefore result in reduced therapeutic efficacy.

摘要

赖诺普利是一种高度亲水的长效血管紧张素转换酶抑制剂,常用于治疗高血压和充血性心力衰竭。绿茶的摄入可能降低心血管事件和全因死亡率的风险,而绿茶或其儿茶素成分已被报道可降低人体中亲水性β受体阻滞剂纳多洛尔的血浆浓度。本研究旨在评估绿茶提取物(GTE)对赖诺普利药代动力学的可能影响。在一项开放标签、随机、单中心、2 期交叉研究中,10 名健康受试者在禁食过夜后服用 10 毫克赖诺普利时,分别饮用 200 毫升含有约 300 毫克(-)-表没食子儿茶素没食子酸酯(绿茶中的主要儿茶素成分)的绿茶提取物水溶液或水(对照)。赖诺普利的最大血浆浓度和血浆浓度-时间曲线下面积的几何均数比值(GTE/对照)分别为 0.289(90%置信区间 0.226-0.352)和 0.337(90%置信区间 0.269-0.405)。相比之下,达到赖诺普利最大浓度的时间(两个阶段均为 6 小时)和赖诺普利的肾清除率(对照 57.7 毫升/分钟与 GTE 56.9 毫升/分钟)没有显著差异。这些结果表明,在 GTE 存在的情况下,赖诺普利的肠道吸收程度显著受损,而对赖诺普利的吸收速率和肾排泄没有主要影响。赖诺普利和绿茶的同时使用可能会降低赖诺普利的口服暴露量,从而降低治疗效果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0c0d/7993260/f25fda2c353b/CTS-14-476-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0c0d/7993260/f25fda2c353b/CTS-14-476-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0c0d/7993260/f25fda2c353b/CTS-14-476-g001.jpg

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