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头孢氨苄和氨苄西林经大鼠空肠转运机制的进一步研究。

Further investigations on the transport mechanism of cephalexin and ampicillin across rat jejunum.

作者信息

Yamashita S, Yamazaki Y, Mizuno M, Masada M, Nadai T, Kimura T, Sezaki H

出版信息

J Pharmacobiodyn. 1984 Apr;7(4):227-33. doi: 10.1248/bpb1978.7.227.

Abstract

The transport mechanisms of cephalexin (CEX) and ampicillin (AB-PC) across rat jejunum were examined using the electrophysiological technique in vitro. From the experiments under the short-circuit condition, it became evident that the specific transport system participates in the mucosal-to-serosal transport of CEX, while AB-PC is transport only by the simple diffusion. In addition, the transport routes of these drugs were examined using the voltage-clamp technique. Salicylate, a model drug of the weak electrolyte, was transported mainly via a paracellular route, while CEX, in the absence of Na, penetrated the membrane via two routes, i.e. the transcellular route and the paracellular route. Similar result was obtained as to AB-PC. So it seems to be likely that these two drugs diffuse through the intestinal epithelium via the similar pathways in the Na-free condition.

摘要

采用体外电生理技术研究了头孢氨苄(CEX)和氨苄青霉素(AB-PC)在大鼠空肠中的转运机制。在短路条件下进行的实验表明,特异性转运系统参与了CEX从黏膜到浆膜的转运,而AB-PC仅通过简单扩散进行转运。此外,使用电压钳技术研究了这些药物的转运途径。弱电解质模型药物水杨酸盐主要通过细胞旁途径转运,而在无钠条件下,CEX通过两条途径穿透细胞膜,即跨细胞途径和细胞旁途径。AB-PC也得到了类似的结果。因此,在无钠条件下,这两种药物似乎可能通过相似的途径扩散穿过肠上皮。

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