传输机制负责loracarbef的吸收、头孢克肟、头孢呋辛axetil人类肠道Caco-2细胞。

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Dantzig啊,Duckworth,塔巴磅

传输机制负责loracarbef的吸收、头孢克肟、头孢呋辛axetil人类肠道Caco-2细胞。

Biochim Biophys学报。1994年4月20日,1191 (1):7 - 13。

PubMed ID

8155686 (在PubMed

]

文摘

Loracarbef,头孢克肟和头孢呋辛axetil beta-lactam口服抗生素。口服吸收loracarbef几乎是完整的,而头孢克肟和头孢呋辛axetil 30 - 50%。调查这我们用人类肠细胞系Caco-2拥有proton-dependent肽转运体,头孢氨苄,头孢克洛。药物吸收测量pH值6通过高效液相色谱法或放射性同位素对药物。头孢克肟1毫米的初始吸附率低于1毫米loracarbef。通过2 h药物集中对梯度的细胞上;然而,头孢克肟的积累loracarbef的仅为40%。这两种药物的吸收速率sodium-independent,温度依赖资源,被二肽,头孢氨苄,头孢克洛,但不是氨基酸。吸收速率的动力学分析的浓度依赖性loracarbef头孢克肟和表明,扩散和一个传输系统负责吸收。头孢克肟loracarbef动力学参数,分别是:8公里的价值观和17毫米和Vmax值6.5和2 nmol /分钟/毫克的蛋白质。 Loracarbef and cefixime were competitive inhibitors of each other's uptake. By contrast, cefuroxime axetil was taken up and rapidly hydrolyzed to cefuroxime by Caco-2 cells. Cefuroxime axetil uptake was not dependent on energy and was not affected by dipeptides. Thus, cefuroxime axetil apparently enters Caco-2 cells by simple diffusion. By contrast, loracarbef and cefixime share a common transport mechanism, the proton-dependent dipeptide transporter. Cefixime was taken up less well than loracarbef due to a substantial reduction in the turnover rate and decreased affinity of the transporter for cefixime.

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药物

Loracarbef