In situ gelling pectin formulations for oral sustained delivery of paracetamol

Drug Dev Ind Pharm. 2004 Jul;30(6):593-9. doi: 10.1081/ddc-120037490.

Abstract

The purpose of this study was to evaluate the potential of a pectin formulation with in situ gelling properties for the oral sustained delivery of paracetamol (acetaminophen). The formulations consisted of dilute aqueous solutions (1% to 2% w/v) of low methoxy pectin containing calcium ions in complexed form, which on release in the acidic environment of the stomach caused gelation of the pectin. In vitro studies demonstrated diffusion-controlled release of paracetamol from the gels over a period of 6 h. A bioavailability of approximately 96% of that of a paracetamol solution could be achieved from gels containing an identical dose of drug formed in situ in the stomachs of rats, with appreciably lower peak plasma levels and a sustained release of drug over a period of at least 6 h.

Publication types

  • Comparative Study

MeSH terms

  • Acetaminophen / administration & dosage
  • Acetaminophen / chemistry*
  • Acetaminophen / pharmacokinetics
  • Administration, Oral
  • Animals
  • Biological Availability
  • Calcium Citrate / chemistry
  • Chemistry, Pharmaceutical
  • Delayed-Action Preparations
  • Excipients / chemistry*
  • Gels
  • In Vitro Techniques
  • Male
  • Pectins / chemistry*
  • Pharmaceutical Solutions
  • Rats
  • Rats, Wistar
  • Water

Substances

  • Delayed-Action Preparations
  • Excipients
  • Gels
  • Pharmaceutical Solutions
  • Water
  • Acetaminophen
  • Pectins
  • Calcium Citrate