淫羊藿苷/β-环糊精包合物的表征及体外溶出研究  

Characterization and Dissolution Studies of Icariin-β-cyclodextrin(β-CD) Inclusion Complex

作　　者：张叶[1,2] 崔元璐[1,2] 田俊生[1,2] 蓝晓东 

机构地区：[1]天津中医药大学中医药研究院,天津300193 [2]现代中药发现与制剂技术教育部工程研究中心,天津300193 [3]美国分子仪器公司(Molecular Devices)中国代表处,上海200120

出　　处：《辽宁中医杂志》2009年第3期428-431,共4页Liaoning Journal of Traditional Chinese Medicine

基　　金：国家自然科学基金资助项目(30570495);天津市应用基础研究重点项目(06YFJZJC01900);中医药行业科研专项项目(200807043)

摘　　要：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.

关 键 词：淫羊藿苷 环糊精 包合物 相溶出 溶出 

分 类 号：R285.5[医药卫生—中药学]