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西咪替丁胃漂浮片的研制与体外释放
Preparation and in vitro release of cimetidine intra-gastric floating sustained release tablets
【摘要】 目的研制西咪替丁胃漂浮片,以便减慢释药、延长药效、减少服药次数。方法以漂浮性、释药性能为指标,对处方和工艺进行单因素考察。结果羟丙甲基纤维素(HPMC K15M)含量在12.5%左右时,对西咪替丁有缓释作用,卡波姆974p可以阻滞释放,碳酸氢钠对释放速率有影响。HPMC K15M、卡波姆974p及碳酸氢钠均对漂浮性能有影响,而硬度对漂浮性能影响较小。结论制备的西咪替丁胃漂浮片漂浮迟滞时间小于1 min,持续漂浮时间大于12 h,10 h累积释放量达90%,体外释药行为符合Higuchi方程,释药机理为非Fick扩散。
【Abstract】 Objective To develop the cimetidine gastric floating controlled drug delivery systems,which can prolong gastric residence time,extend release,and reduce administration times.Methods The floating behavior and the in vitro release characteristics of cimetidine was used as the screening indexes.A single-factor study was also employed to optimize formulation.Results When the content of HPMC K15M was about 12.5 %,the release rate of cimetidine was obviously sustained,Carbopol 974p could slower the release,and sodium bicarbonate also had an effect on the release profile.HPMC K 15M,Carbopol 974 p and sodium bicarbonate could affect the floating properties of tablets while hardness had little effect on them.Conclusion Floating lag time of cimetidine intra-gastric floating sustained release tablets is less than1 min,duration of floating is more than 12 h,and the tables has total drug release in10 h is more 90 percent,and the in vitro release of cimetidine fits Higuchi equation well.
【Key words】 pharmaceutics; floating tablets; formulation; in vitro dissolution; cimetidine;
- 【文献出处】 中国药剂学杂志(网络版) ,Chinese Journal of Pharmaceutics(Online Edition) , 编辑部邮箱 ,2006年02期
- 【分类号】R94
- 【被引频次】1
- 【下载频次】114