氟喹诺酮类药物的肠道转运机制：环丙沙星（依诺沙星衍生物）对依诺沙星膜电位依赖性摄取的抑制作用。
The intestinal transport mechanism of fluoroquinolones: inhibitory effect of ciprofloxacin, an enoxacin derivative, on the membrane potential-dependent uptake of enoxacin.
作者信息
Hirano T, Iseki K, Sato I, Miyazaki S, Takada M, Kobayashi M, Sugawara M, Miyazaki K
机构信息
Department of Pharmacy, Hokkaido University Hospital, School of Medicine, Sapporo, Japan.
出版信息
Pharm Res. 1995 Sep;12(9):1299-303. doi: 10.1023/a:1016265421919.
PURPOSE
To clarify the absorption-structure relationship for the fluoroquinolones from the point of view of inhibitory behavior.
METHODS
The inhibitory effects of ciprofloxacin on the transport process of enoxacin across the rat intestinal brush-border membrane was examined.
RESULTS
Ciprofloxacin, which has a similar structure to enoxacin, exhibited a pH-dependent interference with enoxacin absorption from rat jejunal loops. The uptake experiments using BBM vesicles showed that ciprofloxacin significantly reduced not only the initial binding of enoxacin to the membrane surface, but also the K(+)- or H(+)-diffusion potential-dependent transport across the membrane. Furthermore, an H(+)-diffusion potential (interior negative) also exhibited a stimulative uptake of ciprofloxacin.
CONCLUSIONS
These results suggest that the inhibition behavior of ciprofloxacin from the jejunal loop was closely related to the ionic diffusion potential-dependent uptake of enoxacin across the brush-border membrane.
目的
从抑制行为的角度阐明氟喹诺酮类药物的吸收-结构关系。
方法
研究了环丙沙星对依诺沙星跨大鼠肠刷状缘膜转运过程的抑制作用。
结果
与依诺沙星结构相似的环丙沙星对依诺沙星从大鼠空肠袢的吸收表现出pH依赖性干扰。使用刷状缘膜囊泡的摄取实验表明，环丙沙星不仅显著降低了依诺沙星与膜表面的初始结合，还显著降低了钾离子或氢离子扩散电位依赖性的跨膜转运。此外，氢离子扩散电位（内膜为负）也表现出对环丙沙星的促进摄取作用。
结论
这些结果表明，环丙沙星在空肠袢的抑制行为与依诺沙星跨刷状缘膜的离子扩散电位依赖性摄取密切相关。
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