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乙醇和pH值对药物吸附于活性炭的影响:体外及人体研究

Effect of ethanol and pH on the adsorption of drugs to activated charcoal: studies in vitro and in man.

作者信息

Neuvonen P J, Olkkola K T, Alanen T

出版信息

Acta Pharmacol Toxicol (Copenh). 1984 Jan;54(1):1-7. doi: 10.1111/j.1600-0773.1984.tb01888.x.

Abstract

The effect of ethanol on the adsorption of aspirin, quinidine and amitriptyline to activated charcoal was studied in vitro at pH 1.2 and 7.0. The adsorption of these drugs was greatly dependent on the charcoal-drug ratio and on the pH. Ethanol (10%) significantly (P less than 0.001) increased the percentage of their unadsorbed fraction at both pHs in vitro. In six healthy volunteers activated charcoal (50 g), ingested 5 min. after aspirin (1000 mg) and quinidine sulfate (200 mg), reduced their bioavailability by about 70% (aspirin) and 99% (quinidine). A significant desorption of aspirin but not that of quinidine from charcoal was obvious on the second and third days and seemed to be related to the effect of pH. The absorption of ethanol was not significantly prevented by charcoal. The concomitant ingestion of alcohol (50 g) with drugs antagonized only slightly the ability of charcoal to reduce the absorption of aspirin and quinidine.

摘要

在体外pH值为1.2和7.0的条件下,研究了乙醇对阿司匹林、奎尼丁和阿米替林在活性炭上吸附作用的影响。这些药物的吸附很大程度上取决于活性炭与药物的比例以及pH值。乙醇(10%)在体外两种pH值条件下均显著(P<0.001)增加了它们未被吸附部分的百分比。在6名健康志愿者中,在服用阿司匹林(1000mg)和硫酸奎尼丁(200mg)5分钟后摄入50g活性炭,使阿司匹林的生物利用度降低约70%,奎尼丁降低99%。在第二天和第三天,阿司匹林从活性炭上有明显的解吸现象,而奎尼丁没有,这似乎与pH值的影响有关。活性炭对乙醇的吸收没有显著的抑制作用。同时摄入酒精(50g)与药物仅轻微拮抗了活性炭降低阿司匹林和奎尼丁吸收的能力。

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