鸢尾苷元胃内漂浮型缓释片制备及体外释放研究.docVIP

鸢尾苷元胃内漂浮型缓释片制备及体外释放研究 　　[摘要]研究鸢尾苷元胃内漂浮型缓释片的制备工艺及释放机制。采用羟丙基甲基纤维素（HPMCK15M）、交联聚乙烯吡咯烷酮（PVPP）、十八醇、碳酸氢钠为辅料，湿法制粒压片，以体外漂浮性能和体外释放性能为考察指标，采用正交实验设计对处方进行筛选与优化。优化的处方为鸢尾苷元333%、HPMCK15M 167%、PVPP 200%、十八醇133%、碳酸氢钠5%、预胶化淀粉107%。制得的片剂在人工胃液中10 s内起漂，体外持续漂浮时间12 h；10 h累积释放度在70%以上。RitgerPeppas方程拟合分析表明，该缓释片有药物扩散和骨架溶蚀双重作用。鸢尾苷元胃内漂浮型缓释片外观与可压性良好，且具有良好的漂浮性能和释药特征。 　　[关键词]鸢尾苷元； 胃漂浮片； 体外释放度； 体外漂浮性 　　Preparation and release mechanism of tectorigenin intragastric 　　floating sustainedrelease tablets 　　WANG Jinfeng*， WANG Fang， ZHAO Nan， YANG Cuiyan， WANG Guoyu， WEI Ying， ZHANG Wenya 　　（208th Hospital of People′s Liberation Army， Changchun 130062， China） 　　[Abstract]To investigate the preparation technology and release mechanism of tectorigenin intragastric floating sustainedrelease tablets The tablet was produced by wet granulation compression method， with hydroxypropyl methyl cellulose （HPMCK15M）， crosslinked polyvinyl pyrrolidone （PVPP）， octadecanol and sodium bicarbonate as excipient The prescriptions were screened and optimized by orthogonal experimental design with in vitro floating capacity and drug release characteristics as the evaluation indexes The optimization results were as follows： tectorigenin 333%， HPMCK15M 167%， PVPP 200%， octadecanol 133%， sodium bicarbonate 5%， and starch gel 107% The prepared tablet can be floated within 10 s in the artificial gastric juice， lasting for 12 h in vitro， with a cumulative release rate of 70% in 10 h The analysis of RritgerPeppas equation showed that the sustainedrelease tablet had two advantages of both drug diffusion and skeleton dissolution The tablet had good appearance and compressibility， as well as favorable floating capacity and drug release characteristics 　　[Key words]tectorigenin； gastric floating tablets； in vitro release； in vitro floating performance 　　葛花Puerariae Flos?槎箍浦参镆案?Pueraria lobata（Willd） Ohwi或甘葛藤P thomsonii Benth的花。主要用于治伤酒发热烦渴、解酒醒脾，是传统的解酒保肝药物[12]。鸢尾苷元是葛花异黄酮的主要生物活性成分[34]，为多酚羟基化合物，拥有抗氧化损伤、降血脂、保肝、抗病毒、预防和治疗心血管疾病等多种功效，具有