布洛芬肠溶微囊的研制  

Preparation and Evaluation of Enteric Microcapsules of Ibuprofen

作　　者：杜丽娜 张文明[2] 金义光 

机构地区：[1]中国人民解放军军事医学科学院放射与辐射医学研究所药物化学研究室,北京100850 [2]河南大学药学院,开封475004

出　　处：《医学研究杂志》2011年第9期58-61,共4页Journal of Medical Research

摘　　要：目的以肠溶性高分子材料羟丙基甲基纤维素酞酸酯(HPMCP)为囊材将非甾体抗炎药布洛芬制备成肠溶微囊,对该微囊进行体外释药评价。方法采用HPMCP为囊材,硫酸钠溶液为凝聚剂,布洛芬粉末为囊心物,以单凝聚法制成微囊。布洛芬微囊含量测定以无水乙醇为溶媒,超声破碎微囊并提取,用一阶导数分光光度法在274.2nm处测定。结果布洛芬微囊无布洛芬刺激性气味,在显微镜下,呈不规则晶体状粒子,粒径3～25μm。微囊含量测定方法简单方便,灵敏度可靠。微囊的载药量为38.50%。微囊在人工胃液中2h内几乎不溶解,而在人工肠液中2h释药量达96.5%。结论将非甾体抗炎药布洛芬制备成肠溶微囊,掩盖了药物的刺激性,可达到胃中不溶而肠中溶解的目的。Objective To prepare enteric mierocapsules of anti - inflammatory drug - ibuprofen with hydroxypropyl methylcellulose phthalate （HPMCP）. Methods Ibuprofen microencapsulation with HPMCP through coacervation by the addition of sodium sulphate solu- tion was investigated on the basis of the temperature - dependent coacervating formation of the polymer. The first - order derivative spectro-photometry was used to determine the content of drug at 274.2nm,and it was proved to be a simple and accurate method. Results The enteric microcapsules were anomalistic particles under the microscope. Its diameter was 3 -25μm. Drug load was 38.50%. The drug en- capsulated in the mierocapsules was not released in the artificial gastric juice,whereas in artificial enteric juice the release of microcapsules was 96.5% within 2h. Conclusion The unfavorable stimuli of drug was covered up when its enteric microcapsules were prepared,and the enteric microeapsules would not be soluble in the stomach but soluble when they arrived at the small intestine.

关 键 词：单凝聚法 羟丙基甲基纤维素酞酸酯 肠溶微囊 布洛芬 一阶导数分光光度法 

分 类 号：R994.4[医药卫生—毒理学]