(9e) Particle Design for Improved Tabletting Characteristic Via Hot Granulation of Drug (Ibuprofen) Particles with Sublimation Tendency

Ibuprofen is widely used as analgesic and antifebrile drugs. However, ibuprofen is a poor water-soluble material with a low melting point that causes sticking in the tablet compression process. In this study a powder mixture of jet-milled ibuprofen and lactose was granulated and coated with jet-milled lactose particles by heating below the melting point of ibuprofen in Pressure Swing Granulation (PSG) method. The poor solubility was improved by reducing ibuprofen particle size. Sticking in the tablet compression process was made possible to avoid by coating with lactose particles. Tablets from coated granules showed a higher initial dissolution rate than those from uncoated granules. Ibuprofen sublimation in coated granules and its condensation on the boundary of coat layer were analyzed by laser Raman spectrum. Coated granules had higher strength than uncoated granules by this effect.