以羟丙基-β-环糊精及聚乙二醇为基质的硝苯地平骨架缓释片的制备及特性  

Preparation and characterization of nifedipine skeleton frame sustained release tablets with hydroxypropyl-beta-cyclodextrin and polyethylene glycolas as matrix

作　　者：姜升阳[1] 赵朋[1,2] 杨骏宇[2] 姜东林[1] 

机构地区：[1]南通大学第三附属医院心内科,江苏无锡214041 [2]江南大学药学院,江苏无锡214122

出　　处：《重庆医学》2014年第17期2172-2174,共3页Chongqing medicine

摘　　要：目的以羟丙基-β-环糊精(HPC)及聚乙二醇(PEG)为基质制备硝苯地平(NP)骨架缓释片,并研究其对NP的缓释效应。方法将NP和HPC按1∶1比例配制成包合物后与PEG混合,采用直接压片法制备NP骨架缓释片,与不含包合物的NP-PEG片、NP-HPC片和NP粉末胶囊作对照,测定该缓释片体外释药曲线及体内药时曲线。结果 NP骨架缓释片在模拟胃液(pH1.2)试验中5h累积释放率仅为36.4%,其缓释效应显著强于NP-HPC片(80%,P<0.01)及NP-PEG片(100%,P<0.01);体内实验中,NP骨架缓释片的AUC0-12[(6 413±436)h/(ng·mL)]、Cmax[(983±192)ng/mL]及tmax[(5.7±1.1)h]均显著高于NP-HPC片组、NP-PEG片组及NP胶囊组(均P<0.01或<0.05)。结论 NP骨架缓释片对NP具有缓释效应,可延长NP的体外释放时间及提高NP的生物利用度,是一种性能良好的新型NP缓释片剂。Objective To prepare nifedipine （NP）skeleton frame sustained release tablets by adopting hydroxypropyl-beta-cy-clodextrin （HPC）and polyethylene glycol （PEG）as the matrix and to investigate its sustained release effect on NP.Methods NP skeleton frame sustained release tablets were prepared by the direct compression method after forming the inclusion complex with NP and HPC on a 1∶1 ratio and mixing with PEG.The in vitro drug release curves and the in vivo concentration-time curves of NP skeleton frame sustained release tablets were detected with the NP-PEG tablet without inclusion complex,NP-HPC tablet and NP powder capsule （NP capsule）as the control.Results The 5 h cumulative release rate of NP skeleton frame sustained release tablet in the simulated gastric fluid test（pH 1.2）was 36.4%,its sustained release effect was significantly stronger than that of the NP-HPC tablet group （80%,P〈0.01）and the NP-PEG tablet group （100%,P〈0.01）.The in vivo test showed that AUC0-12 [（6 413±436）h/（ng·mL）],Cmax[（983±192）ng/mL]and tmax[（5.7±1.1）h]in the NP skeleton frame sustained release group were significantly higher than those in the NP-HPC tablet group,the NP-PEG tablet group and the NP Capsule group （all P〈0.01 or 0.05）.Conclusion NP skeleton frame sustained release tablets exhibits the sustained release effect on NP,can extend the NP in vitro release time,and improve the NP′s bioavailability,which is a novel NP sustained release tablet with excellent properties.

关 键 词：硝苯地平 羟丙基-Β-环糊精 聚乙二醇 骨架缓释片 

分 类 号：R943[医药卫生—药剂学]