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Related Experiment Videos

pH and P.E.G.-400 effects on flucloxacillin absorption.

L J Nuñez-Vergara1, I R Lemus, J A Squella

  • 1Laboratory of Pharmacology, Facultad de Ciencias Quimicas y Farmaceuticas, Universidad de Chile, Santiago.

General Pharmacology
|January 1, 1988
PubMed
Summary

Intestinal absorption of flucloxacillin decreases as pH rises, but polyethylene glycol 400 enhances its clearance. This study details flucloxacillin

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Area of Science:

  • Pharmacokinetics and Drug Absorption
  • Gastrointestinal Physiology

Background:

  • Flucloxacillin is an antibiotic with variable oral absorption.
  • The impact of intestinal pH and excipients on flucloxacillin absorption requires further elucidation.

Purpose of the Study:

  • To investigate the effect of pH on flucloxacillin intestinal clearance and absorption.
  • To evaluate the influence of polyethylene glycol 400 (PEG-400) on flucloxacillin intestinal clearance and water flux.

Main Methods:

  • Measurement of flucloxacillin intestinal clearance across a range of pH values.
  • Determination of apparent rate constants for ionized and unionized flucloxacillin.
  • Assessment of PEG-400's effect on flucloxacillin clearance and net water flux in the small intestine.

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Main Results:

  • Intestinal clearance and 60-minute absorption of flucloxacillin significantly decreased with increasing pH.
  • Apparent rate constants for unionized and ionized flucloxacillin were 0.173 min-1 and 0.017 min-1, respectively.
  • PEG-400 addition enhanced flucloxacillin intestinal clearance and increased net water flux.

Conclusions:

  • Intestinal pH is a critical factor influencing flucloxacillin absorption, with higher pH reducing clearance.
  • PEG-400 demonstrates potential as an absorption enhancer for flucloxacillin by increasing intestinal clearance and water flux.