葛根大豆甙元与poloxamer共沉淀物的研究

应用溶剂-熔融法将葛根大豆甙元与载体poloxamer制成不同比例的共沉淀物以提高药物的溶出速度。采用差热分析和热台显微镜技术,测得其组成中含药物2.1%时共熔点为44℃,偏光显微镜观察及X射线图谱表明,1.7%以下的共沉淀物为固溶体,2.1%的共沉淀物中,甙元以最微细的晶体分散于载体中,在人工肠液中溶出速度和平衡溶解度测定显示,溶出度(T_(60))1%为2min,2.1%为4min,甙元约为60min,相应的平衡溶解度分别为52.47、35.30和4.37μg/ml(37±0.5℃)。

STUDIES ON DAIHZEIN-POLOXAMER COPRECIPITATES

Daihzein is a synthetical chemical compound used for the treatment of cardio-vascular diseases. Its solubilities in water and in fat are very low. Differential thermal analysis and hot stage microscope technique were employed to study the phase transition temperatures of Daihzein-poloxamer coprecipitate, prepared by melting-solvent method. Using X-ray diffraction and hot stage microscope photography, we found that when the solid dispersions were below 1.7% the coprecipitates were solid solution. The mixture of 2.1% was identified as the finest crystals dispersed in the carrier. Experiments on dissolution rate and equilibrium solubility at 37±0.5℃ indicated: the solubilities in the simulated intestinal fluid were 4.37(μg/ml) for Daihzein, 52.47(μg/ml) for the mixture of 1%, 35.3(μg/ml) for the mixture of 2.1%. T_(60) of the above coprecipitates were 2min for 1%, 4min for 2%, about 60 min for Daihzein. The conclusion was: the coprecipitate was responsible for the enhanced dissolution rate and equilibrium solibility of the compound.