烟酸缓释微丸的制备及体外释放度考察  

Preparation and release test of nicotinic acid sustained-release pellets

作　　者：陈金脱[1] 尹莉芳[1] 周建平[1] 

机构地区：[1]中国药科大学药剂教研室,南京210009

出　　处：《中国新药杂志》2012年第3期246-250,共5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)

摘　　要：目的:制备24 h烟酸缓释微丸,考察其体外释放度。方法:使用离心造粒机,采用空白丸芯粉末上药法制备烟酸载药素丸;使用国产流化床包衣机,以乙基纤维素为包衣材料进行包衣。考察包衣处方因素、热处理条件和释放介质对释放度的影响。结果:烟酸素丸圆整度良好,光滑;16～20目收率约90%。包衣增重、致孔剂类型以及用量是影响药物释放的关键因素。烟酸缓释微丸在pH 1.2的盐酸溶液中释放较快,在水,pH 4.5的醋酸盐缓冲溶液,pH 6.8和pH 7.9的磷酸盐溶液中释放无明显区别。以乙基纤维素包衣增重9%,以PEG 4000为致孔剂用量37%,得到的缓释微丸具备体外24 h缓释特征。结论:该缓释微丸的体外释放符合缓释制剂要求。Objective：To prepare nicotinic acid （NA） 24 h sustained-release pellets and to study their release behavior in vitro. Methods：NA pellets were prepared by centrifugal granulation and coated by ethylcelulose using domestic fluizing bed. The impacts on the release profiles of different coating gains, pore-forming agents and their amounts,heat-treatment conditions and dissolution media adjusted to different pH values were investigated. Results：NA-free pellets had excellent geometeric roundness and smoothness;and the pellets yield amounted to about 90% in the range of 16 -20 mesh. The key factors influencing drug release were coating gains,pore-forming agent and its amount. It was found that the most effective pore-forming agent was PEG 4000. The drug release was the quickest in pH 1.0 HCl,and had no difference at pH 4.5, pH 6.8,pH 7.0（water） ,and pH 7.9. NA pellets coated by 5% EC and 37% PEG 4000 with 9% gains exhibited significant 24 h sustain-release characteristic invitro. Conclusion：NA pellets exhibited an excellent release profile in vitro.

关 键 词：缓释微丸 烟酸 离心造粒 乙基纤维素 致孔剂 

分 类 号：R943.41[医药卫生—药剂学]