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
Key words
Axitinib/Biological adhesion and floating/In vitro release/Pharmacokinetics
维普
万方数据