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

A. Tsuji, E. Nakashima, I. Kagami, T. Yamana

Research output: Contribution to journalArticle

79 Citations (Scopus)

Abstract

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 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.

Original languageEnglish
Pages (from-to)768-772
Number of pages5
JournalJournal of Pharmaceutical Sciences
Volume70
Issue number7
Publication statusPublished - 1981
Externally publishedYes

Fingerprint

Lactams
Intestinal Absorption
Penicillins
Small Intestine
Rats
Anti-Bacterial Agents
Carrier transport
Cephalosporins
Solubility
Blood
Derivatives
Lipids
Water

ASJC Scopus subject areas

  • Molecular Medicine
  • Chemistry(all)
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science
  • Pharmacology

Cite this

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abstract = "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 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.",
author = "A. Tsuji and E. Nakashima and I. Kagami and T. Yamana",
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T1 - Intestinal absorption mechanism of amphoteric β-lactam antibiotics. I. Comparative absorption and evidence for saturable transport of amino-β-lactam antibiotics by in situ rat small intestine

AU - Tsuji, A.

AU - Nakashima, E.

AU - Kagami, I.

AU - Yamana, T.

PY - 1981

Y1 - 1981

N2 - 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 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.

AB - 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 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.

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