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口服褐藻糖胶后在大鼠体内的药代动力学和组织分布。

Pharmacokinetic and Tissue Distribution of Fucoidan from after Oral Administration to Rats.

机构信息

Saint-Petersburg Institute of Pharmacy, Leningrad Region, Vsevolozhsky District, Kuzmolovo P 245, 188663 Saint-Petersburg, Russia.

RMC "House of Pharmacy", Leningrad Region, Vsevolozhsky District, Zavodskaya str., 3, Kuzmolovo P 245, 188663 Saint-Petersburg, Russia.

出版信息

Mar Drugs. 2018 Apr 18;16(4):132. doi: 10.3390/md16040132.

Abstract

L., known as bladderwrack, belongs to the brown seaweeds, which are widely distributed throughout northern Russia, Atlantic shores of Europe, the Baltic Sea, Greenland, the Azores, the Canary Islands, and shores of the Pacific Ocean. Fucoidan is a major fucose-rich sulfated polysaccharide found in () . The pharmacokinetic profiling of active compounds is essential for drug development and approval. The aim of the study was to evaluate the pharmacokinetics and tissue distribution of fucoidan in rats after a single-dose oral administration. Fucoidan was isolated from . The method of measuring anti-activated factor X (anti-Xa) activity by amidolytic assay was used to analyze the plasma and tissue concentrations of fucoidan. The tissue distribution of fucoidan after intragastric administration to the rats was characterized, and it exhibited considerable heterogeneity. Fucoidan preferentially accumulates in the kidneys (AUC = 10.74 µg·h/g; C = 1.23 µg/g after 5 h), spleen (AUC = 6.89 µg·h/g; C = 0.78 µg/g after 3 h), and liver (AUC = 3.26 µg·h/g; C = 0.53 µg/g after 2 h) and shows a relatively long absorption time and extended circulation in the blood, with a mean residence time (MRT) = 6.79 h. The outcome of this study provides additional scientific data for traditional use of fucoidan-containing plants and offers tangible support for the continued development of new effective pharmaceuticals using fucoidan.

摘要

裙带菜属于褐藻,广泛分布于俄罗斯北部、欧洲大西洋沿岸、波罗的海、格陵兰、亚速尔群岛、加那利群岛和太平洋海岸。褐藻糖胶是一种主要的富含岩藻糖的硫酸多糖,存在于 () 中。活性化合物的药代动力学特征分析对于药物开发和审批至关重要。本研究旨在评估单次口服给药后褐藻糖胶在大鼠体内的药代动力学和组织分布。褐藻糖胶从 中分离得到。采用 amidolytic assay 法测定抗活化因子 X (anti-Xa) 活性来分析褐藻糖胶在血浆和组织中的浓度。研究了褐藻糖胶经灌胃给予大鼠后的组织分布特征,结果显示其具有明显的异质性。褐藻糖胶优先在肾脏(AUC = 10.74 µg·h/g;C = 1.23 µg/g 于 5 h)、脾脏(AUC = 6.89 µg·h/g;C = 0.78 µg/g 于 3 h)和肝脏(AUC = 3.26 µg·h/g;C = 0.53 µg/g 于 2 h)中积聚,且在血液中具有较长的吸收时间和延长的循环,平均驻留时间(MRT)= 6.79 h。本研究的结果为含褐藻糖胶植物的传统应用提供了额外的科学数据,并为利用褐藻糖胶开发新的有效药物提供了切实支持。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1dba/5923419/de0daca2b635/marinedrugs-16-00132-g001a.jpg

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