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Formulation and evaluation of floating, pulsatile, multiparticulates using pH-dependent swellable polymers.

Madhuri Gaikwad1, Veena S Belgamwar, Avinash Tekade

  • 1Department of Pharmaceutics, R.C. Patel College of Pharmacy, Karvand Naka, Shirpur-425405, Maharashtra, India.

Pharmaceutical Development and Technology
|July 23, 2009
PubMed
Summary

Researchers developed floating, pulsatile beads for arthritis chronotherapy. These beads, using pectin and alginate, successfully delivered aceclofenac after a lag time, showing high drug entrapment and controlled release.

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Materials Science

Background:

  • Chronotherapy requires drug release timed to physiological rhythms.
  • Pulsatile drug delivery systems offer controlled drug release after a specific lag time.
  • Floating drug delivery systems enhance gastric residence time for improved drug absorption.

Purpose of the Study:

  • To develop a floating, pulsatile, multiparticulate drug delivery system for arthritis chronotherapy.
  • To utilize pectin and sodium alginate for creating cross-linked beads via ionotropic gelation.
  • To encapsulate aceclofenac as a model drug for evaluating the system's performance.

Main Methods:

  • Preparation of cross-linked beads using low methoxylated pectin (LM104AS) and sodium alginate.
  • Ionotropic gelation employing an acid-base reaction for bead formation.
  • Characterization included entrapment efficiency, surface topography, size analysis, in vitro release, buoyancy, DSC, and radio imaging.

Main Results:

  • Calcium pectinate beads demonstrated maximum drug entrapment efficiency.
  • Floating properties were confirmed for pectin-containing formulations.
  • In vitro release studies showed 5-10% drug release in acidic media (pH 1.2) and 90-94% in basic media (pH 7.4) after specific time intervals.

Conclusions:

  • The developed floating, pulsatile multiparticulate system effectively encapsulates aceclofenac.
  • The system exhibits potential for chronopharmacotherapy of arthritis by providing a delayed drug release profile.
  • Pectin-based formulations are suitable for creating floating, pulsatile drug delivery systems with controlled release characteristics.