喷雾干燥法制备丹参酮ⅡA磺酸钠微球  

Preparation of sulfotanshinone sodium microspheres using spray-drying method

作　　者：游本刚[1] 陆晓文[1] 许苗松[1] 费香东[1] 朱云峰[1] 唐丽华[1] 

机构地区：[1]苏州大学医学部药学院,苏州215123

出　　处：《中国新药杂志》2011年第20期1966-1971,2002,共7页Chinese Journal of New Drugs

基　　金：国家"重大新药创制"科技重大专项(2009ZX09502);2008年江苏省大学生实践创新训练计划项目(SG315820)

摘　　要：目的:采用喷雾干燥法制备丹参酮ⅡA磺酸钠微球,为其口服固体制剂的研究提供基础。方法:采用喷雾干燥法制备丹参酮ⅡA磺酸钠微球,以微球收率、载药量、含水量,吸湿性和体外溶出度等为指标,对微球的处方及工艺条件进行考察。通过扫描电镜、X-射线粉末衍射法、红外光谱等对微球和药物的形态进行鉴别。结果:微球的处方为:丹参酮ⅡA磺酸钠0.5 g,聚丙烯酸树脂Ⅳ号2.5 g,PEG 6000为0.3 g。制备工艺为:将处方量的药物与辅料共溶于60%乙醇125 mL中进行喷雾干燥,条件如下:进样速度为9 mL.min-1,进口温度为80℃,空气流速为838 L.h-1。所制得微球外观圆整,药物主要以无定型或分子状态存在。结论:采用喷雾干燥法可将丹参酮ⅡA磺酸钠制成微球,药物吸湿性降低、溶出较快。Objective： To prepare sulfotanshinone sodium microspheres using a spray-drying method,and to provide evidence for designing its oral administration dose forms.Methods： Spray-drying was used to prepare sulfotanshinone sodium microspheres.The yield,drug-loding,moisture capacity,hydroscopicity and dissolution rate were applied as the indexes to investigate the formulations and process conditions of the microspheres.Methods such as scanning electron micrograph,X-ray powder diffraction and fourier transform infrared spectroscopy were employed to observe the appearance of microspheres and the forms of drug in microspheres.Results： The formulations of microspheres were as follows： sulfotanshinone sodium 0.5g,Eudragit Ⅳ 2.5g,and PEG 6000 0.3g.The formulated drug and adjuvants were dissolved in 125mL alcohol solution（60%）;then the solution was spray-dried at an introduction rate of 9mL·min-1,an entrance temperature of 80℃,and an air flow rate of 838L·h-1.The appearance of microspheres was round,and drug in microspheres was amorphous or molecules.Conclusion： Sulfotanshinone sodium microspheres have been successfully prepared using spray-drying method,which can reduce the hygroscopicity of drug with a desired dissolution rate.

关 键 词：丹参酮ⅡA磺酸钠 喷雾干燥 微球 溶出度 

分 类 号：R943.4[医药卫生—药剂学]