Preparation and Properties of Resveratrol-poloxamer 188-solid Dispersion / 中国药房

ABSTRACT

OBJECTIVE:To prepare Resveratrol-poloxamer 188-solid dispersion(RES-P188-SD)and study its dissolving char-acteristic in vitro and antibacterial activity. METHODS:With P188 as the carrier, solvent method was used to prepare RES-P188-SD. With the mass ratio of drug to carrier,melting temperature and mesh number as the observed factors,and solubility and yield of RES as the observed indexes,L9(34)orthogonal test was designed to optimize the preparation technology,and compre-hensive score of observed indexes were analyzed. The verification test was carried out. After RES-P188-SD was prepared by the op-timal technology,basket method was used to determine its dissolution rate and then its accumulative dissolution rate was calculat-ed,scanning electron microscopy to analyze phase characterization and cylinder-plate method to determine antibacterial activity. RE-SULTSThe optimal technology was as follows as the mass ratio of drug to carrier of 1∶10,melting temperature of 70 ℃ and mesh number of 80. For the sample prepared by the optimal technology,average solubility was 0.51 mg/ml (RSD=1.96%,n=3),average yield was 91%(RSD=0.64%,n=3),average 15 min accumulative dissolution rate was up to 83%(RSD=0.69%, n=3);the drug in amorphous form was homogenously distributed in the carrier;RES-P188-SD could inhibit Staphylococcus aure-us and Escherichia coli. CONCLUSIONS:The optimal technology is stable and feasible,by which RES-P188-SD has been pre-pared successfully,providing reference for increasing the solubility,dissolution rate and antibacterial activity of RES.