Intestinal absorption mechanism of amphoteric β‐lactam antibiotics I: Comparative absorption and evidence for saturable transport of amino‐β‐iactam antibiotics by in situ rat small intestine

Akira Tsuji, Emi Nakashima, Izumi Kagami, Tsukinaka Yamana

研究成果: Article査読

82 被引用数 (Scopus)

抄録

The disappearance of various β‐lactam antibiotics from in situ rat small intestinal loops was studied at pH 7.4. For monobasic penicillins, despite the wide variety of apparent partition coefficients in is isobutyl alcohol‐water, the disappearance from the jejunal loops was almost 30% (±5% SD). On the other hand, the disappearance of amphoteric derivatives of penicillins and cephalosporins having very low lipid solubility varied widely between 12 and 80%. The peak blood levels after intraduodenal administration to the rats correlated well with the extent of disappearance of amphoteric penicillins from the intestinal loops. Absorption studies utilizing in situ intestinal loops were performed at variable dose ranges to yield a clear dose‐dependent disappearance. It is suggested that certain carrier‐mediated transport systems underlie the absorption mechanisms of amphoteric β‐lactam antibiotics.

本文言語English
ページ(範囲)768-772
ページ数5
ジャーナルJournal of Pharmaceutical Sciences
70
7
DOI
出版ステータスPublished - 1981 7

ASJC Scopus subject areas

  • 薬科学

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