木香内酯胃漂浮片的处方优化及体外释放研究  

Research on formulation optimization and in vitro drug release of Costunolide and Dehydrocostus lactone gastric floating tablets

作　　者：黄泽铖 徐纯艺 杨苛 喻子薇 胡慧玲[1] 王战国[2] HUANG Ze-cheng;XU Chun-yi;YANG Ke;YUZi-wei;HUHui-ling;WANG Zhan-guo(School of Pharmacy,Chengdu University of Traditional Chinese Medicine,State Key Laboratory of Southwestern Chinese Medicine Resources,Chengdu 611137,Sichuan;Chengdu University,Chengdu 610106,Sichuan)

机构地区：[1]成都中医药大学药学院西南特色中药资源国家重点实验室,四川成都611137 [2]成都大学,四川成都610106

出　　处：《中药与临床》2022年第1期6-10,共5页Pharmacy and Clinics of Chinese Materia Medica

基　　金：成都中医药大学“杏林学者”学科人才提升计划(No.ZRYY1916);阿坝州羌药制剂创新研发与应用示范(No.2019ZYD052)。

摘　　要：目的:研究木香内酯(木香烃内酯和去氢木香内酯)胃漂浮片的处方优化及体外释放。方法:以木香烃内酯(COS)和去氢木香内酯(DEH)为模型药物,采用全粉末直接压片法制备胃漂浮片,以浮动滞后时间、总漂浮时间和药物累积释放度为指标,通过单因素实验确定骨架材料、低密度辅料、起泡剂的种类及比例;以2 h、6 h、12 h时间点的累计释放度为评价指标,采用Box-Behnken设计对木香内酯胃漂浮片的处方比例进行优化,得到最佳处方。结果:本实验通过单因素实验确定了骨架材料为HPMC K4M、低密度辅料硬脂酸和起泡剂碳酸钠,通过Box-Benhnken设计实验进一步得到了制剂的最佳处方为HPMC K4M 26.44%、硬脂酸6.29%、碳酸钠5.22%;木香内酯胃漂浮片在0.1 mol·L^(-1)的盐酸介质中能立即起漂,总漂浮时间大于12 h,具有良好的缓释效果,在12 h药物累积释放度达到60%。结论:优化后的木香内酯胃漂浮片浮动滞后时间短,总漂浮时间长,且具有良好的缓释效果。Objective:To study the formulation optimization and in vitro drug release of gastric floating tablets of Costunolide(COS)and Dehydrocostus lactone(DEH).Method:Costunolide and Dehydrocostus lactone were viewed as model drugs,gastric floating tablets were prepared by full direct compression method.Taking the floating lag time,total floating time and drug cumulative release as indexes,the types and concentration of skeleton materials,low-density excipients and effervescent agents were determined by single factor experiments.Furthermore,the cumulative release at 2 h,6 h and 12 h were regarded the evaluation index,and the Box-Behnken design was used to optimize the formulation of Costunolide and Dehydrocostus lactone gastric floating tablets.Result:The optimized formulation was HPMC K4M 26.44%,stearic acid 6.29%,sodium carbonate 5.22%.Showed by single factor experiments and Box-Behnken design.The results showed that the gastric floating tablets could start floating immediately in 0.1 mol·L^(-1)hydrochloric acid medium,and the sustained-release time was more than 12 h.The cumulative drug release was more than 60%at 12 h,which had a good sustained-release characteristics.Conclusion:The results showed that the Costunolide and Dehydrocostus lactone gastric floating tablets had short floating lag time,long floating time and good sustained-release effect.

关 键 词：木香烃内酯 去氢木香内酯 胃漂浮片 浮动滞后时间 总漂浮时间 药物累积释放度 

分 类 号：R283[医药卫生—中药学]