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安替比林、酚红和头孢美唑结肠吸收促进机制的差异。

Differences in the promotion mechanism of the colonic absorption of antipyrine, phenol red and cefmetazole.

作者信息

Shiga M, Hayashi M, Horie T, Awazu S

出版信息

J Pharm Pharmacol. 1987 Feb;39(2):118-23. doi: 10.1111/j.2042-7158.1987.tb06956.x.

Abstract

The promotion of antipyrine, phenol red and cefmetazole absorption by sodium ethylenediaminetetraacetate (EDTA-Na) as a paracellular promoter, diethyl maleate (DEM) as a transcellular promoter, and sodium taurocholate (TC-Na), whose promotion mechanism is still unclear, has been investigated by the rat in-situ colonic loop technique. All these promoters increased AP absorption and water influx from the lumen to the blood. Ouabain treatment suppressed the increase in antipyrine absorption and water influx induced by TC-Na and EDTA-Na, but did not modify the enhancing effect of DEM. Thus, the promotion mechanism of TC-Na may be similar to that of EDTA-Na. Phenol red and cefmetazole absorption were increased by TC-Na and EDTA-Na but not by DEM. Accordingly, phenol red and cefmetazole absorption appears to be promoted via paracellular but not transcellular routes. The collection of blood for plasma samples reduced the influx of water which had been increased by TC-Na or EDTA-Na. Consequently, the enhancement in antipyrine plasma concentration by these promoters was reduced to the control level. The inhibitory mechanism for this is discussed on the basis of the blood-flow limitation of antipyrine and water absorption.

摘要

通过大鼠原位结肠袢技术,研究了作为细胞旁促进剂的乙二胺四乙酸钠(EDTA-Na)、作为跨细胞促进剂的马来酸二乙酯(DEM)以及促进机制尚不清楚的牛磺胆酸钠(TC-Na)对安替比林、酚红和头孢美唑吸收的促进作用。所有这些促进剂均增加了安替比林的吸收以及从肠腔到血液的水流入量。哇巴因处理抑制了TC-Na和EDTA-Na诱导的安替比林吸收增加和水流入,但并未改变DEM的增强作用。因此,TC-Na的促进机制可能与EDTA-Na相似。TC-Na和EDTA-Na增加了酚红和头孢美唑的吸收,但DEM没有。因此,酚红和头孢美唑的吸收似乎是通过细胞旁途径而非跨细胞途径促进的。采集血液用于血浆样本减少了由TC-Na或EDTA-Na增加的水流入。因此,这些促进剂对安替比林血浆浓度的增强作用降低到了对照水平。基于安替比林和水吸收的血流限制,讨论了其抑制机制。

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