Intestinal absorption of several .BETA.-lactam antibiotics, V. Effect of amino .BETA.-lactam analogues and dipeptides on the absorption of amino .BETA.-lactam antibiotics.

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Abstract
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 analogs and the effects of dipeptides were studied. The influences of glycylglycine on the absorption of cephradine at 4 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. Cephalexin absorption was influenced by L-carnosine (6.0, 10 mM), not by glycylglycine (6 mM). The absorption of cephradine was not reduced at all by these dipeptides. From the experiment using the 4 different parts of intestine, it was shown that the transport interaction of glycylglycine with cephradine was observed in only 1 segment (the upper part of jejunum). 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.