目的:制备和鉴定淫羊藿苷/β-环糊精包合物,考察了淫羊藿苷与β-环糊精之间的构成摩尔质量比,并进行体外释放研究。方法:采用冷冻干燥法制备淫羊藿苷/β-环糊精包合物,采用荧光光谱、红外光谱、差示扫描量热分析、X—Ray衍射分析、扫描电镜分析等方法对包合物进行了鉴定。用HPLC法测定包合物的含药量及其体外释放。结果:证实淫羊藿苷/β-环糊精包合物已经形成,主、客分子的摩尔比为1:1,包合常数为39.62M^-1,溶解度和溶出速率均有所增大。结论:淫羊藿苷/β-环糊精包合物能显著增大药物的溶解度、稳定性和溶出速率。
Objective :To study the preparation and characterization of icariin - β - cyclodextrin ( β - CD) inclusion complex, to determine the stoichiometry of host and guest and to investigate the dissolubility. Methods:The inclusion complex was prepared by freeze-drying method, and evaluated comprehensively by Fluorescence spectroscopy (FS) , Fourier-transform infrared spectroscopy ( FT - IR ) , differential scanning calorimetry ( DSC ) , scarming electron microscopy ( SEM ) and X-ray diffractometry (XRD). Drug content and release in vitro was determined by HPLC. Results :The formation of icariin-β-CD inclusion complex was defined by Fs,FS-IR,DSC ,SEM ,and XRD. The phase solubility diagram of icariin with β - CD was classified as AL-type,indicating the formation of 1 : 1 stoichimetric inclusion complex The complexation constant calculated from phase diagram was 39. 62M^-1 Fluorescence study also proof the above results. Solubility and dissolution studies indicated improvement in inclusion complex,comparing to the drug alone. Conclusion : Inclusion complex of icariin - β - CD could increase solubility ,stability and dissolution rates.