Saturable absorption of amino‐cephalosporins by the rat intestine

Saturable absorption of amino‐cephalosporins by the rat intestine
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大鼠肠道对氨基头孢菌素的饱和吸收

DOI:
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发表时间:
1979
期刊:
The Journal of pharmacy and pharmacology
影响因子:
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通讯作者:
T. Yamana
T. Yamana
中科院分区:
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文献类型:
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作者:
A. Tsuji;E. Nakashima;T. Asano;Ryoko Nakashima;T. Yamana

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我们之前已经提供了动力学证据,表明阿莫西林和环拉西林的浓度与大鼠肠道原位吸收之间存在相互关系(Tsuji et al 1977,1978),并提出某些类型的载体介导动力学是吸收机制的基础。在本通讯中,我们报告的新发现表明,在体内吸收氨基头孢菌素类药物的大鼠肠道是由饱和动力学的方式类似的氨基青霉素。头孢氨苄一水合物和头孢拉定一水合物由Shionogi & Co.日本大坂和三共株式会社,日本东京,分别。先前描述了实验条件和原位环路和再循环灌注方法(Tsuji et al 1977)。根据高压液相色谱法(h.p.1.c.)测定的残留氨基头孢菌素的量计算抗生素从肠中的消失。如下所示:将装有UVIDEC 100型紫外检测器的FLCA-700型紫外检测器设置在254 nm(日本光谱公司,Tokyo,Japan)和反相柱(SC-02,Japan Spectroscopic Co.)用了载体为7%乙腈-93%001M乙酸铵。将50 μ l适当稀释的溶液通过可变环管进样器流动进样,
We have previously presented kinetic evidence indicating the existence of an interrelationship between concentration and in situ absorption of amoxicillin and cyclacillin by rat intestine (Tsuji et al 1977, 1978) and proposed that some types of carrier-mediated kinetics underlie the absorption mechanisms. In the present communication we report new findings indicating that in vivo absorption of amino-cephalosporins by rat intestine is governed by saturable kinetics in a manner similar to that of amino-penicillins. Cephalexin monohydrate and cephradine monohydrate were kindly supplied by Shionogi & Co., Osaka, Japan and Sankyo Co., Tokyo, Japan, respectively. Experimental conditions and in situ loop and recirculating perfusion methods were described previously (Tsuji et al 1977). Disappearance of antibiotics from the intestine was calculated from the amount of residual amino-cephalosporin assayed by high-pressure liquid chromatography (h.p.1.c.) as follows: A Model FLC A-700 equipped with a Model UVIDEC 100 ultraviolet detector set at 254 nm (Japan Spectroscopic Co., Tokyo, Japan) and a reversed phase column (SC-02, Japan Spectroscopic Co.) were used. The carrier was 7% acetonitrile-93% 001 M ammonium acetate. 50 pl of an appropriately diluted solution was injected through a variable loop-injector on flow, and peak