(741f) Micronization of Pharmaceutical Compounds Using the Supercritical Antisolvent Process

Supercritical anti-solvent (SAS) process has been demonstrated as a useful method for the recrystallization and micronization of the active pharmaceutical ingredients (API). The micronized pharmaceutical compounds allow the use of a more appropriate administration route with less required dosage or side effects. After the supercritical fluid technology treatment, the particle size of the pharmaceutical compound can be decreased to the range of 1 to 5 micron. The particle morphology and polymorphism can also be modified with enhanced pharmaceutical effects.

This study presents our experimental results for the micronization of some pharmaceutical compounds including sulfonamide drug and non-steroidal anti-inflammatory drug (NSAID).The experiments were conducted using the continuous SAS process. Organic fluids such as acetone were used as the solvent, and supercritical carbon dioxide was used as the anti-solvent. The experimental temperature and pressure ranges were 308 to 328 K and 100 to 140 bar, respectively. The re-crystallization process was carried out in a stainless steel tube with a volume of 75 mL. The micronized pharmaceutical particles were collected at the bottom of the precipitation cell. The SAS treated particles were analyzed by SEM, DSC and XRD to investigate the micronization effects. Finally, the dissolution rate tests were examined in simulated intestinal fluid. The re-crystallized and micronized API showed significantly enhanced dissolution profiles.