【作者】 恽菲； 徐晓琰； 狄留庆； 康安； 单进军； 赵晓莉； 李俊松； 毕肖林；

【Author】 Yun fei;Xu xiao-yan;Di liu-qing;Kang an;Shan jing-jun;Zhao xiao-li;Li jun-song;Bi xiao-lin;Nanjing university of Chinese medicine;Jiangsu Provincial TCM Efficient Drug Delivery System Engineering Technology Research Center;Nangjing Engineering Research Center for Industrialization of Chinese Medicine pellets;

【机构】 南京中医药大学； 江苏省中药高效给药系统工程技术研究中心； 南京市中药微丸产业化工程技术研究中心；

【摘要】 目的采用三种不同的环糊精(β-环糊精、甲基-β-环糊精、羟丙基-β-环糊精)对蛇床子素进行包合,比较不同环糊精的包合作用对蛇床子素生物利用度的影响。方法采用红外光谱、扫描电镜、差示量热分析法来表征不同环糊精包合物的形成;高效液相色谱法测定包合物中蛇床子素的含量及其溶解度;高效液相色谱-质谱测定法测定不同环糊精包合前后,蛇床子素在大鼠体内的血药浓度。结果经红外光谱、扫描电镜、差示量热分析法表明三种环糊精包合物的形成,经包合后蛇床子素溶解度显著提高,大鼠体内利用度得到显著改善。结论β-环糊精、甲基-β-环糊精、羟丙基-β-环糊精制备的蛇床子素包合物均能显著提高蛇床子素体外溶解度,并能提高其大鼠体内生物利用度。更多还原

【Abstract】 Absract:Objective:To prepare Osthole-β-Cyclodextrin inclusion complex,Osthole-Hydroxypropyl-β- Cyclodextrin inclusion complex,and Methyl-β-Cyclodextrin inclusion complex and investigate their corresponding bioavailability in rats.Method s:The formation of inclusion complex of osthole was confirmed by SEM,IR and DSC to determine the quality of the inclusion complex of osthole.The content and solubility was determined by HPLC.The blood concentration of osthole in rats was assayed by LC-MS/MS.Result s:SEM,IR and DSC study showed the formation of inclusion complex of osthole.Determination of the solubility proved that three cyclodextrin can significantly increase the solubility of osthole in vitro.And bioavailability study in rats exhibited remarkably improved bioavailability by three cyclodextrin inclusion complex compared to pure drug.Conclusion:The results in vitro and in vivo indicate that three cyclodextrin inclusion complex can increase the solubility and enhance bioavailability of osthole in rats.更多还原