Preparation process of apigenin particles by supercritical CO2 anti-solvent method / 中草药

ABSTRACT

Objective: To prepare the apigenin particles by supercritical CO2 anti-solvent technology, to optimize the preparation process of apigenin particles on the basis of single factor experiments using the average particle size as evaluation index through orthogonal test design, and to investigate the in vitro dissolution rate. Methods: The particle size distribution, scanning electro- microscope (SEM) analysis, infrared spectrum (IR), and differential scanning calorimetry (DSC) were used to validate the selected process. The external dissolution rates of apigenin ingredient and apigenin particles of the optimal process were tested to speculate the bioavailability of apigenin. Results: The optimal process conditions by orthogonal test were set as follows: The proportion of acetone and dimethyl sulfoxide (DMSO) was 24:1, temperature was 40°C, pressure was 10 MPa, solution volumetric flow rate was 2.0 mL/min, and mass concentration of apigenin was 8 mg/mL. Under the optimal conditions, the volume average particle size was obviously smaller than that of ingredient. And the shapes of apigenin were irregular. FTIR and DSC analyses showed that the chemical structure did not change. The results showed that the in vitro dissolution rate of apigenin particles of the optimal process was significantly larger than that of apigenin ingredient. Conclusion: The supercritical CO2 anti-solvent technology is feasible to prepare apigenin particles and promote its bioavailability, and it provides a reference basis for preparing ultrafine particles.