Stewart H E, Jackson M J
J Pharmacol Exp Ther. 1981 Aug;218(2):453-8.
A steady-state net absorptive movement of benzylpenicillin across rat small intestine was observed in the absence of transmural gradients of electrochemical potential. The transport process was dependent on tissue metabolism and the presence of sodium, but no evidence of a saturable rate-limiting step was observed. Voltage-clamp studies showed that the transintestinal movement of benzylpenicillin varied with the electric potential across the tissue. It was found that a mathematical model based on a series three-compartment system yielded a good quantitative description of benzylpenicillin transport in the short-circuited condition and of the voltage-dependence of the transport process. A net absorptive movement of benzylpenicillin was also observed in studies on rat stomach in vitro, but on the colon a net secretory movement occurred. It was suggested that the gastric and colonic transport processes may be described in terms similar to those of the small intestine and that the variations of the direction of transport reflect differences in the pattern of acid-base metabolism in tissue.
在不存在电化学势跨膜梯度的情况下,观察到苄青霉素在大鼠小肠中的稳态净吸收运动。该转运过程依赖于组织代谢和钠的存在,但未观察到饱和限速步骤的证据。电压钳研究表明,苄青霉素的跨肠运动随组织两端的电势而变化。结果发现,基于串联三室系统的数学模型对短路条件下苄青霉素的转运以及转运过程的电压依赖性给出了很好的定量描述。在大鼠胃的体外研究中也观察到苄青霉素的净吸收运动,但在结肠中则发生净分泌运动。有人提出,胃和结肠的转运过程可能可用与小肠类似的方式来描述,而转运方向的变化反映了组织中酸碱代谢模式的差异。