重庆医学Issue(17)：2172-2174,3.DOI:10.3969/j.issn.1671-8348.2014.17.022
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
姜升阳 1赵朋 1杨骏宇 2姜东林3
作者信息
- 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
- 3. 江南大学药学院，江苏无锡 214122
- 折叠
摘要
Abstract
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Key words
nifedipine/hydroxypropyl-beta-cyclodextrin/polyethylene-glycol/skeleton-frame-sustained-release-tablet引用本文复制引用
姜升阳,赵朋,杨骏宇,姜东林..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[J].重庆医学,2014,(17):2172-2174,3.
