【摘要】 目的:制备含葛根素-羟丙基-β-环糊精(HP-β-CD)包合物的漂浮型胃滞留制剂及其体外药剂学特征评价。方法:冷冻干燥法制备葛根素的HP-β-CD包合物。分别以葛根素和包合物为内容物制备海藻酸钙微丸,考察甲基纤维素、硬脂酸镁和壳聚糖对微丸漂浮百分率及释放度的影响。结果:红外光谱图和X-射线粉末衍射图显示葛根素与HP-β-CD形成了包合物。硬脂酸镁对其微丸的漂浮百分率影响大,当含量为2%时漂浮效果最佳。葛根素被包合后,溶解度增加约65.6倍,微丸中药物的释放速度和累计释放百分率均得到明显改善,但存在突释现象。将葛根素包合物与葛根素按照1∶1的比例混合,经分散机处理后的微丸具有明显的缓释特征。结论:葛根素-HP-β-CD包合物提高了药物的溶解度和释放度,胃滞留微丸具有满意的漂浮性能和缓释性能。更多还原

【Abstract】 Objective: To prepare a novel floating micropellets containing hydroxy propyl-β-oyclodextrin(puerarin-HP-β-CD) for gastroretentive dosage form and evaluate its pharmaceutical characteristics in vitro.Method: The puerarin HP-β-cyclodextrin inclusion complex was prepared by freeze-drying method.Puerarin and its HP-β-CD inclusion complex were incorporated into alginate beads,respectively.The effect of methyl cellulose(MC),Mg-Stearate and chitosan on buoyancy and cumulative release rate of puerarin were investigated in simulated gastric fluid.Result: The spectrums of FTIR and profiles of X-ray powder diffraction of samples proved the formation of inclusion complex between puerarin and HP-β-CD.Magnesium stearate had a significant effect on the buoyancy of micropellets,and satisfied results were gained by the content with 2%.The solubility of puerarin was increased 65.6-fold by the formation of inclusion complex,the dissolution rate and cumulative release percentage also improved significantly although with the burst release phenomena.The micropellets showed sustained release properties by using puerarin-HP-β-CD inclusion complex mixed with puerarin(1∶1) and treated thoroughly under homogenizer.Conclusion: The solubility and release rate of puerarin are increased by the formation of inclusion complex with HP-β-CD and its gastroretentive dosage forms displayed satisfied floating and sustained release characteristics.更多还原