兰婷,郝红,刘荣杰,毕曼,李涛

• 1:西北大学化工学院
• 2:第四军医大学药学系

摘要(Abstract)：

采用溶剂挥发法制备盐酸乌拉地尔PLLA微球并通过SEM对其结构进行了表征,同时对微球的包封率和药物释放进行了测试。通过有机相加入乙醇或外水相加入盐的方法可以提高微球对药物的包封率。结果表明,当无水乙醇与三氯甲烷的比为1:2时,制得的微球包封率最高,达到30.52%。外水相中加入盐类电解质的方法也能提高药物的包封率。盐的加入使得盐酸乌拉地尔在外水相的溶解度降低,减少了药物向外水相的泄漏,从而提高了药物的包封率。其中KCl的加入对药物包封率的影响最大。当KCl浓度达到0.4%(mol)时,微球的包封率最高,达到35.52%。体外药物释放结果表明,PLLA微球具有明显的缓释作用,其释药动力学满足Higuchi方程。

关键词(KeyWords)： 盐酸乌拉地尔;聚(L-乳酸);微球;包封率

Abstract:

Keywords:

基金项目(Foundation): 陕西省13115科技创新工程重大科技专项项目计划(2007ZDKG-50)

作者(Author): 兰婷,郝红,刘荣杰,毕曼,李涛

参考文献(References)：

• [1]WU Hui-zhen(吴惠珍),ZHANG Shu-hui(张淑慧),CAO De-ying(曹德英).Preparation of urapidil HCl sustained-release capsule and its dissolution rate(盐酸乌拉地尔缓释胶囊的制备及体外释放度研究)[J].Chinese Journal of New Drugs(中国新药杂志),2004,13(6):518-520.
• [2]Qi H X,Hu P,Xu J et al.Encapsulation of drug reservoirs in fibers by emulsion electrospinning:Morphology characterization and preliminary release assessment[J].Biomacromoleules,2006,7(8):2327-2330.
• [3]ZHANG Lei(张磊),YANG Song(杨松),GE Zhi-qiang(葛志强).Study on the preparation of recombinant humanα-2b interferon slowly realeasing microcapsules and its in-vitro release properties(重组α-2b干扰素缓释微囊制备工艺及体外释药过程研究)[J].J Chem Eng of Chinese Univ(高校化学工程学报),2004,18(5):628-632.
• [4]Lee S,Kim M S,Kim J S et al.Controlled delivery of a hydrophilic drug from a biodegradable microsphere system by supercritical anti-solvent precipitation technique[J].Journal of Microencapsulation,2006,23(7):741-749.
• [5]Lai M K,Tsang R C C.Microencapsulation of acetaminophen into poly(L-lactide)by three different emulsion solvent-evaporation methods[J].Journal of Microencapsulation,2005,22(3):261-274.
• [6]QUE Li(阙俐),WU Wei(吴伟).Formation and characterization of poly(d,l-lactide)micropheres for water-soluble drugs(水溶性药物聚丙交酯微球的研究)[J].Central South Pharmacy(中南药学),2003,1(1):22-26.
• [7]Al-Maaieh A,Flanagan D R.Salt and cosolvent effects on ionic drug loading into microspheres using an O/W method[J].Journal of Controlled Release,2001,70(1):169-181.