TY - JOUR
T1 - Intestinal brush‐border transport of the oral cephalosporin antibiotic, cefdinir, mediated by dipeptide and monocarboxylic acid transport systems in rabbits
AU - TSUJI, AKIRA
AU - TAMAI, IKUMI
AU - NAKANISHI, MASARU
AU - TERASAKI, TETSUYA
AU - HAMANO, SCHOICHIRO
PY - 1993/11
Y1 - 1993/11
N2 - Abstract— Intestinal absorption of the orally active cephalosporin, cefdinir, was investigated using brush‐border membrane vesicles prepared from rabbit small intestine. The initial uptake of cefdinir was pH‐dependent, with increased uptake at acidic pH, and was not influenced by either sodium gradient or membrane potential difference. Cefdinir uptake was saturable with an apparent Michaelis constant of 8·1 Mm. Initial uptake of cefdinir was inhibited by dipeptides (glycyl‐l‐proline and glycylsarcosine), β‐lactam antibiotics (cephradine, cefixime and penicillin V), and monocarboxylic acids (acetic acid and l‐lactic acid), whereas the uptake of cephradine and cefixime was not inhibited by monocarboxylic acids. Cefdinir significantly inhibited the initial uptake of cephradine, cefixime and [3H]acetic acid. From these results, it was suggested that cefdinir was transported across brush‐border membranes by both dipeptide and monocarboxylic acid carriers. 1993 Royal Pharmaceutical Society of Great Britain
AB - Abstract— Intestinal absorption of the orally active cephalosporin, cefdinir, was investigated using brush‐border membrane vesicles prepared from rabbit small intestine. The initial uptake of cefdinir was pH‐dependent, with increased uptake at acidic pH, and was not influenced by either sodium gradient or membrane potential difference. Cefdinir uptake was saturable with an apparent Michaelis constant of 8·1 Mm. Initial uptake of cefdinir was inhibited by dipeptides (glycyl‐l‐proline and glycylsarcosine), β‐lactam antibiotics (cephradine, cefixime and penicillin V), and monocarboxylic acids (acetic acid and l‐lactic acid), whereas the uptake of cephradine and cefixime was not inhibited by monocarboxylic acids. Cefdinir significantly inhibited the initial uptake of cephradine, cefixime and [3H]acetic acid. From these results, it was suggested that cefdinir was transported across brush‐border membranes by both dipeptide and monocarboxylic acid carriers. 1993 Royal Pharmaceutical Society of Great Britain
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U2 - 10.1111/j.2042-7158.1993.tb05645.x
DO - 10.1111/j.2042-7158.1993.tb05645.x
M3 - Article
C2 - 7908046
AN - SCOPUS:0027527749
VL - 45
SP - 996
EP - 998
JO - Journal of Pharmacy and Pharmacology
JF - Journal of Pharmacy and Pharmacology
SN - 0022-3573
IS - 11
ER -