蛇床子素不同环糊精包合物的制备及其生物利用度比较研究  

Preparation of different osthole cyclodextrin inclusion complex and comparison on their bioavailability

作　　者：恽菲[1,2,3] 徐晓琰[1,2,3] 狄留庆[1,2,3] 康安[1] 单进军[1] 赵晓莉[1,2,3] 李俊松[1,2,3] 毕肖林[1,2,3] 

机构地区：[1]南京中医药大学,江苏南京210046 [2]江苏省中药高效给药系统工程技术研究中心,江苏南京210046 [3]南京市中药微丸产业化工程技术研究中心,江苏南京210046

出　　处：《中草药》2014年第3期341-348,共8页Chinese Traditional and Herbal Drugs

基　　金：江苏省科技创新团队支持计划[苏教师(2008)30号];江苏省优势学科建设项目(YSXK-2010)

摘　　要：目的采用3种不同的环糊精[β-环糊精(β-CD)、羟丙基-β-环糊精(HP-β-CD)、甲基-β-环糊精(M-β-CD)]对蛇床子素进行包合,比较不同环糊精的包合物对蛇床子素生物利用度的影响。方法采用红外光谱(IR)、扫描电镜(SEM)、差示量热分析(DSC)法来表征不同环糊精包合物的形成;HPLC法测定包合物中蛇床子素的量及其溶解度;HPLC-MS/MS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IR、SEM、DSC法表明3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,大鼠体内生物利用度得到显著改善。结论β-CD、M-β-CD、HP-β-CD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,并能提高其在大鼠体内生物利用度。Objective To prepare three kinds of inclusion complex of osthole （Ost） using β-cyclodextrin （CD）, hydroxypropyl-β-CD, and methyl-β-CD, and to investigate their corresponding bioavailability in rats. Methods The formation of inclusion complex of Ost was confirmed by scanning electron microscope （SEM）, infrared spectroscopy （IR）, and differential scanning calorimetry （DSC）, and the content and solubility were determined by HPLC. The blood concentration of Ost in rats was assayed by HPLC-MS/MS. Results SEM, IR, and DSC study characterized the formation of inclusion complex of Ost. Determination of the solubility proved that the three kinds of CD could significantly increase the solubility of Ost in vitro. And bioavailability study in rats exhibited remarkably improved bioavailability by three kinds of CD inclusion complex compared to the pure drug. Conclusion The three kinds of CD inclusion complex could increase the solubility and enhance the bioavailability of Ost in rats.

关 键 词：蛇床子素 环糊精 包合物 生物利用度 HPLC-MS MS 

分 类 号：R283.6[医药卫生—中药学]