We successfully performed the micronization of Glycyrrhizic acid by Supercritical AntiSolvent (SAS) process and evaluated the effect of temperature, pressure, carbon dioxide flow rate, solution flow rate and drug concentration on the precipitation process. In particular, we varied temperature from 60 to 90℃, pressure from 15 to 30 MPa, CO2 flow rate from 10 to 25 mL/min, solution rate from to mL/min and drug concentration from 0.01 to 0.04 mg/mL. The as-prepared ultrafine GA was characterized by scanning electron microscopy (SEM), X-ray diffraction (XRD), fourier transform infrared (FT-IR) spectroscopy, thermal gravimetric analysis (TG), differential scanning calorimetry (DSC), dissolution and bioavailability test. And to investigate the competence of glycyrrhizic acid which was prepared based on the supercritical anti-solvent process as an improved drug formulation system for the clinical application. Then the rats were obtained liver fibrosis and injury, then treated with glycyrrhizic acid micro-nano (GM), glycyrrhizic acid (G) and compound glycyrrhizin tablets (P).As shown in the result, The optimization of SAS process parameters to obtain the ultrafine GA particles are pressure of 20 MPa, temperature of 90℃, CO2 flow rate of 25mL/min, solution flow rate of 6 mL/min and drug concentration of 0.01 mg/mL. The other analyses indicated that the prepared ultrafine GA was amorphous. In the dissolution and bioavailability test, ultrafine GA is exhibited enhanced dissolution property and absorption in rats when compared to the raw material. As to the pharmacological tests, it suggested that GM had therapeutical effect on liver fibrosis and injury. |