重庆医学
重慶醫學
중경의학
CHONGQING MEDICAL JOURNAL
2014年
17期
2172-2174
,共3页
姜升阳%赵朋%杨骏宇%姜东林
薑升暘%趙朋%楊駿宇%薑東林
강승양%조붕%양준우%강동림
硝苯地平%羟丙基-β-环糊精%聚乙二醇%骨架缓释片
硝苯地平%羥丙基-β-環糊精%聚乙二醇%骨架緩釋片
초분지평%간병기-β-배호정%취을이순%골가완석편
nifedipine%hydroxypropyl-beta-cyclodextrin%polyethylene-glycol%skeleton-frame-sustained-release-tablet
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5 h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[(6413±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。
目的:以羥丙基-β-環糊精(HPC)及聚乙二醇(PEG)為基質製備硝苯地平(NP)骨架緩釋片,併研究其對 NP的緩釋效應。方法將 NP和 HPC按1∶1比例配製成包閤物後與 PEG混閤,採用直接壓片法製備 NP骨架緩釋片,與不含包閤物的NP-PEG片、NP-HPC片和 NP 粉末膠囊作對照,測定該緩釋片體外釋藥麯線及體內藥時麯線。結果 NP骨架緩釋片在模擬胃液(pH1.2)試驗中5 h纍積釋放率僅為36.4%,其緩釋效應顯著彊于 NP-HPC片(80%,P<0.01)及 NP-PEG片(100%,P<0.01);體內實驗中,NP骨架緩釋片的 AUC0-12[(6413±436)h/(ng·mL)]、Cmax[(983±192)ng/mL]及 tmax[(5.7±1.1)h]均顯著高于 NP-HPC片組、NP-PEG片組及 NP膠囊組(均P<0.01或<0.05)。結論 NP骨架緩釋片對 NP具有緩釋效應,可延長NP的體外釋放時間及提高 NP的生物利用度,是一種性能良好的新型 NP緩釋片劑。
목적:이간병기-β-배호정(HPC)급취을이순(PEG)위기질제비초분지평(NP)골가완석편,병연구기대 NP적완석효응。방법장 NP화 HPC안1∶1비례배제성포합물후여 PEG혼합,채용직접압편법제비 NP골가완석편,여불함포합물적NP-PEG편、NP-HPC편화 NP 분말효낭작대조,측정해완석편체외석약곡선급체내약시곡선。결과 NP골가완석편재모의위액(pH1.2)시험중5 h루적석방솔부위36.4%,기완석효응현저강우 NP-HPC편(80%,P<0.01)급 NP-PEG편(100%,P<0.01);체내실험중,NP골가완석편적 AUC0-12[(6413±436)h/(ng·mL)]、Cmax[(983±192)ng/mL]급 tmax[(5.7±1.1)h]균현저고우 NP-HPC편조、NP-PEG편조급 NP효낭조(균P<0.01혹<0.05)。결론 NP골가완석편대 NP구유완석효응,가연장NP적체외석방시간급제고 NP적생물이용도,시일충성능량호적신형 NP완석편제。
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.