摘要
目的:制备盐酸二甲双胍(metformin hydrochloride,MH)缓释微丸,并考察其体外释药行为。方法:通过离心造粒法制得MH微丸,以乙基纤维素水分散体(Surelease),丙烯酸树脂水分散体(EudragitNE30D,RS30D)作为膜控释包衣材料,通过流化床包衣制备MH缓释微丸,并考察不同包衣材料、包衣增重、固化时间、释放介质对释放度的影响。结果:离心造粒制得微丸圆整度好,有一定强度,适合包衣,Surelease包衣增重11%时所得的缓释微丸在12 h具有明显的缓释效果,不受释放介质的影响,为零级释放,且12 h释放可以达到85%以上。释放机制主要是通过无孔膜扩散作用。结论:通过离心造粒并用Surelease包衣的MH缓释微丸缓释效果明显,且为零级释放。
Objective： To prepare metformin hydrochloride （MH） sustained-release pellets, and to investigate their in-vitro release behavior and the release mechanism. Methods： MH pellets were prepared by a centrifugal granulation method. Ethyl cellulose aqueous dispersion （Surelease） and acrylic polymers aqueous dispersion （ Eudragit NE30D, RS30D） were used as sustained-release coating materials with fluid bed. The effects of different coating materials, coating weight, curing time and release medium on the in-vitro release were determined. Results： MH pellets prepared by the centrifugal granulation method had good roundness, and were suitable for coating. Coating weight of 11% Surelease had satisfactory sustained-release behavior within 12 h, and the drug release amount could reach over 85%. The pellets showed similar release behaviors in different release media including water, 0.1 mol. L-1 HC1 and PBS 6.8, and their release model was zero-order due to the release mechanism of diffusion through the non-porous membrane. Conclusion： MH sustained-release pellets prepared by the centrifugal granulation method and coated by Surelease possesses an obvious sustained-release property in 12 h and their release model is zero-order.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2011年第21期2069-2072,共4页
Chinese Journal of New Drugs
基金
国家"重大新药创制"科技重大专项--新制剂与新释药系统技术平台(2009ZX09310-004)
2008年度教育部新世纪优秀人才支持计划(NCET-08-0846)
关键词
盐酸二甲双胍
离心造粒
缓释微丸
释放度
零级释放
metformin hydrochloride
centrifugal granulation
sustained-release pellets
release rate
zero-order release
