盐酸普罗帕酮β-CD包合物缓释片的制备及体外释放度的研究  

Preparation and optimization of sustained-release tablets of propafenone hydrochloride β-CD inclusion complex

作　　者：尹莉芳[1] 耿文君[1] 周建平[1] 朱春莉[1] 张陆勇[2] 

机构地区：[1]中国药科大学药剂教研室,南京210009 [2]中国药科大学新药筛选中心,南京210009

出　　处：《中国新药杂志》2010年第18期1657-1660,1668,共5页Chinese Journal of New Drugs

基　　金：重大新药创制科技重大专项(2009ZX09310-004);2008年度教育部新世纪优秀人才支持计划(NCET-08-0846)

摘　　要：目的:制备盐酸普罗帕酮β-环糊精(β-CD)包合物缓释片并研究其体外释放度。方法:以β-CD为包合材料,用研磨法制备盐酸普罗帕酮β-CD包合物,采用羟丙甲纤维素(HPMC)为缓释材料,乳糖为填充剂制备盐酸普罗帕酮β-CD包合物缓释片,并通过单因素考察法筛选出最优的处方。结果:体外释放度试验表明,制得的盐酸普罗帕酮β-CD包合物缓释片累积释放百分率1 h为28.4%,2 h为46.1%,8 h为94.4%,体外缓释效果明显,释药行为符合一级动力学方程。结论:盐酸普罗帕酮β-CD包合物缓释片处方简单,易于工业化大生产,体外缓释效果明显。Objective： To prepare sustained-release tablets of propafenone hydrochloride β-cyclodextrin（β-CD） inclusion complex,and to investigate its release behavior in vitro.Methods： β-CD was used as the wall material.The inclusion complex was prepared by grinding PPF and β-CD.We selected HPMC as matrix material and lactose as loading agent to prepare β-CD inclusion complex sustained-release tablets.Single factor method was applied to optimize formulas.Results： The in vitro release results showed that its accumulated release rates at 1,2 and 8 h were 28.4%,46.1% and 94.4%,respectively,which was conformed to first order equation.Conclusion： The preparation technique is simple and easy to implement commercial process.The release behavior is well described in vitro and meets the design criteria.

关 键 词：盐酸普罗帕酮 包合物 缓释片 释放度 

分 类 号：R944.9[医药卫生—药剂学] R972.2[医药卫生—药学]