Properties of hot-melt extruded theophylline tablets containing poly(vinyl acetate)

Drug Dev Ind Pharm. 2000 Sep;26(9):931-42. doi: 10.1081/ddc-100101320.

Abstract

The objectives of this study were to investigate the properties of poly(vinyl acetate) (PVAc) as a retardant polymer and to study the drug release mechanism of theophylline from matrix tablets prepared by hot-melt extrusion. A physical mixture of drug, polymer, and drug release modifiers was fed into the equipment and heated inside the barrel of the extruder. The cylindrical extrudates were either cut into tablets or ground into granules and compressed with other excipients into tablets. Due to the low glass transition temperature of the PVAc, the melt extrusion process was conducted at approximately 70 degrees C. Theophylline was used as the model drug in this study. Theophylline was present in the extrudate in its crystalline form and was released from the tablets by diffusion. The Higuchi diffusion model and percolation theories were applied to the dissolution data to explain the drug release properties of the matrix systems. The release rate was shown to be dependent on the granule size, drug particle size, and drug loading in the tablets. Water-soluble polymers were demonstrated to be efficient release rate modifiers for this system.

MeSH terms

  • Bronchodilator Agents / administration & dosage
  • Bronchodilator Agents / chemistry
  • Calorimetry, Differential Scanning
  • Chemical Phenomena
  • Chemistry, Physical
  • Delayed-Action Preparations
  • Drug Carriers
  • Drug Stability
  • Hot Temperature
  • Microscopy, Electron, Scanning
  • Particle Size
  • Polyvinyls / administration & dosage
  • Polyvinyls / chemistry*
  • Surface Properties
  • Tablets
  • Technology, Pharmaceutical / methods
  • Theophylline / administration & dosage
  • Theophylline / chemistry*
  • X-Ray Diffraction

Substances

  • Bronchodilator Agents
  • Delayed-Action Preparations
  • Drug Carriers
  • Polyvinyls
  • Tablets
  • polyvinyl acetate
  • Theophylline