Properties of Hot-Melt Extruded Theophylline Tablets Containing Poly(Vinyl Acetate)

作者：Feng Zhang, James W. McGinity · 发表于：Drug Development and Industrial Pharmacy · 年份：2000 · DOI：10.1081/ddc-100101320 · 被引用次数：75 · 研究领域：Drug Solubulity and Delivery Systems、Advanced Polymer Synthesis and Characterization、Analytical Methods in Pharmaceuticals

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.