Passage-delaying microbeads for controlled delivery of loratadine

PDA J Pharm Sci Technol. 2008 Nov-Dec;62(6):421-8.

Abstract

A passage-delaying, multiple unit, controlled release system of loratadine was designed to increase residence time in the stomach involving minimum contact with the gastric mucosa. Oil-entrapped floating microbeads prepared using the emulsion gelation method were optimized by a 2(3) factorial design and a polymer ratio of 1.5:0.5 (casein:sodium alginate) by weight, and 15% w/v of oil (mineral oil/castor oil) and 1 M calcium chloride solution were selected as the optimized processing conditions for the desired buoyancy and physical stability. In vitro drug release in acid phthalate buffer, pH 3.12, demonstrated a sustained release for 8 h that best fitted the peppas model with n < 0.45. The ethylcellulose coating of the passage-delaying microbeads optimized by a 2(2) factorial design resulted in a controlled release formulation of loratadine that provided zero-order release for 8 h.

MeSH terms

  • Calorimetry, Differential Scanning
  • Delayed-Action Preparations
  • Hydrogen-Ion Concentration
  • Loratadine / administration & dosage*
  • Loratadine / chemistry
  • Microspheres*
  • Solubility

Substances

  • Delayed-Action Preparations
  • Loratadine