Microparticle Production of Active Pharmaceutical Ingredient Using Supercritical Antisolvent Process: A Case Study of Allopurinol

Allopurinol is a relatively water-insoluble drug and, consequently, its efficacy was frequently limited by the dissolution or solubility phenomena. The purpose of this study was to improve the solid-state properties and dissolution behavior of allopurinol via a supercritical antisolvent (SAS) process using CO2 as an antisolvent. The effects of operating parameters: temperature (35-55 degrees C), pressure (80-100 bar), solution concentration (8-15 mg/mL), CO2 flow rate (2-4 L/min), and solution flow rate (0.25-0.50 mL/min) were studied. Moreover, the physical properties of unprocessed and SAS-processed allopurinol were analyzed by SEM, FTIR, DSC, TGA, and PXRD. The dissolution rate of unprocessed and SAS-processed allopurinol was also investigated and compared. In this case study, allopurinol was effectively micronized from 15.3 mu m to 1.35 mu m at the optimal operating condition. The results verify that the solid-state properties and dissolution rate of allopurinol can be controlled and improved via the micronization process by using SAS technology.

Automated summary

This study aimed to improve the solid-state properties and dissolution behavior of allopurinol using a supercritical antisolvent (SAS) process with CO2 as an antisolvent. The results showed that the micronization process effectively controlled and improved the solid-state properties and dissolution rate of allopurinol.