三白草酮固体分散体的制备、体外溶出度及表征

Preparation and Dissolution of Solid Dispersion of Sauchinone Solid Dispersion

目的:采用热熔挤出法制备三白草酮固体分散体,以改善三白草酮的溶出情况。方法:按照不同药辅比,通过热熔挤出技术以聚乙二醇6000为载体材料制备三白草酮固体分散体,采用HPLC测定固体分散体中三白草酮的含量,考察90min累积溶出度和溶出速率,比较不同药辅比所制得的固体分散体其体外溶出效果。采用红外光谱分析、X-射线衍射和扫描电镜对所制得固体分散体的相特征进行研究,鉴别三白草酮在固体分散体中的存在状态。结果:与物理混合物相比,药辅比为1:1、1:4制备所得的固体分散体中三白草酮的体外溶出度与溶出速度均有所提高,其中药辅比为1:4制备的三白草酮-聚乙二醇6000固体分散体的体外溶出度与溶出速度略优,其90min累积溶出度达到98%。红外光谱中,在固体分散体中三白草酮与聚乙二醇系列载体材料之间形成了氢键。X-射线粉末衍射分析,提示没有新的物相形成。结论:选择聚乙二醇6000为载体材料,采用热熔挤出法,按1:4比例制备三白草酮固体分散体,对三白草酮的溶出有改善作用。

Objective:Hot melt extrusion was used to prepare Sauchinone solid dispersion in order to improve the dissolution of Sauchionone.Methods:Polyethylene glycol 6000 was adopted as carrier material.Sauchionone and polyethylene glycol 6000 were mixed with each other in the proportion of 1:1,1:4 to prepare the solid dispersion by the hot melt extrusion.The content of Sauchinone in solid dispersion was determined by HPLC,and the cumulative dissolution rate and dissolution rate in 90 min were investigated.Infrared spectroscopy,X-ray diffraction and scanning electron microscopy were used to study the phase characteristics and identify the existing state of Triadimefon in solid dispersion.Results:Compared with its physical mixture,the in vitro dissolution and dissolution rate of Sauchinone of the solid dispersions which was prepared by PEG6000 increased significantly.Furthermore,the dissolution rate and dissolution rate of Sauchinone-PEG 6000 solid dispersion prepared with 1:4 were slightly better,and the cumulative dissolution rate in 90 min was 98%.In the IR spectrum,hydrogen bonds were formed between Sauchinone and polyethylene glycol in the solid dispersion.X-ray powder diffraction analysis and scanning electron microscopy showed that no new phase was formed.Conclusion:PEG6000 was selected as the carrier material,and the solid dispersion of Sauchinone was prepared by hot melt extrusion at the ratio of 1:4,which can improve the dissolution of Sauchinone.