阿昔替尼胃漂浮丸剂的制备及药效学研究  

Preparation and pharmacodynamics of Axitinib gastric floating pellets

作　　者：洪益平 裘方剑 HONG Yi-ping;QIU Fang-jian(Jin Hua Hospital of TCM,Jinhua 321000,China)

机构地区：[1]金华市中医医院,321000

出　　处：《中国实用医药》2024年第4期177-180,共4页China Practical Medicine

基　　金：浙江省金华市科技计划项目(项目编号:2019-4-055)。

摘　　要：目的制备阿昔替尼胃漂浮丸剂,延长其在胃肠道滞留时间,提高其口服生物利用度。方法采用挤出滚圆法,分别以羟丙基甲基纤维素(HPMC)、羟丙基纤维素(HPC)为粘附阻滞材料,以碳酸氢钠(NaHCO3)为起泡剂,制备阿昔替尼胃漂浮丸剂。结果以主药∶HPMC K100M∶HPC(2.5∶1∶5),主药∶起泡剂(1∶2)设计的处方,2 h释放达37%,4 h释放达67%,6 h释放达80%。大鼠药代动力学研究结果表明,胃漂浮丸剂生物利用度提高2.39倍,Cmax提高80%。结论阿昔替尼生物粘附漂浮丸剂具有显著的缓释效果,可延长药物在体内的滞留时间,提高阿昔替尼在大鼠体内的口服生物利用度。Objective To prepare Axitinib gastric floating pellets,prolong its retention time in gastrointestinal tract and improve its oral bioavailability.Methods Axitinib gastric floating pellets were prepared by extrusion spheronization method with hydroxypropyl methylcellulose(HPMC)and hydroxypropyl cellulose(HPC)as adhesion blocking materials and sodium bicarbonate(NaHCO3)as foaming agent respectively.Results With the formulation of main drug∶HPMC K100M∶HPC(2.5∶1∶5)and main drug∶foaming agent(1∶2),the release rate was 37%at 2 h,67%at 4 h and 80%at 6 h.The pharmacokinetic study in rats showed that the bioavailability of gastric floating pellets was increased by 2.39 times,and Cmax was increased by 80%.Conclusion The bioadhesive floating pellets of Axitinib have significant sustained-release effect,can prolong the drug retention time in vivo,and improve the oral bioavailability of Axitinib in rats.

关 键 词：阿昔替尼 生物粘附漂浮 体外释放 药代动力学 

分 类 号：R943[医药卫生—药剂学] R965[医药卫生—药学]