Iseki K, Iemura A, Sato H, Sunada K, Miyazaki K, Arita T
J Pharmacobiodyn. 1984 Oct;7(10):768-75. doi: 10.1248/bpb1978.7.768.
The absorption mechanism of amino beta-lactam antibiotics was investigated by using the whole small intestine of a rat. Mutual inhibition among amino beta-lactam analogues and the effects of dipeptides were studied. The influences of glycylglycine on the absorption of cephradine at the four different parts of intestine were also studied. Similarly to the case of cephalexin and cephradine, the absorption of amoxicillin was significantly inhibited by cyclacillin, cephradine, and cephalexin, but the absorption of ampicillin was not reduced by all tested antibiotics. In the experiments using dipeptides (6.0 mM), the absorption of cyclacillin was reduced significantly by glycylglycine, not by L-carnosine. And cephalexin absorption was influenced by L-carnosine (6.0, 10 mM), not by glycylglycine (6 mM). On the contrary, the absorption of cephradine was not reduced at all by these dipeptides. And from the experiment using the four different parts of intestine, it was shown that the transport interaction of glycylglycine with cephradine was observed in only one segment (the upper part of jejunum). These result suggest that the carrier-mediated transport system correlated to dipeptides participates only to a small degree in the common absorption mechanisms of these amino beta-lactam antibiotics.
通过使用大鼠的整个小肠研究了氨基β-内酰胺抗生素的吸收机制。研究了氨基β-内酰胺类似物之间的相互抑制作用以及二肽的影响。还研究了甘氨酰甘氨酸对头孢拉定在小肠四个不同部位吸收的影响。与头孢氨苄和头孢拉定的情况类似，阿莫西林的吸收受到环青霉素、头孢拉定和头孢氨苄的显著抑制，但氨苄西林的吸收未被所有测试抗生素降低。在使用二肽（6.0 mM）的实验中，甘氨酰甘氨酸显著降低了环青霉素的吸收，而L-肌肽则没有。头孢氨苄的吸收受L-肌肽（6.0、10 mM）影响，不受甘氨酰甘氨酸（6 mM）影响。相反，这些二肽对头孢拉定的吸收完全没有降低。并且从使用小肠四个不同部位的实验表明，仅在一个节段（空肠上部）观察到甘氨酰甘氨酸与头孢拉定的转运相互作用。这些结果表明，与二肽相关的载体介导转运系统在这些氨基β-内酰胺抗生素的共同吸收机制中仅起很小的作用。
