黄芩苷结肠定位固体分散体的制备及其体外释放度评价  

Preparation of baicalin colon-specific solid dispersion and evaluation on its in vitro release

作　　者：严红梅[1,2] 张振海[1] 蒋艳荣[1,2] 丁冬梅[1] 孙娥[1] 贾晓斌[1,2] 

机构地区：[1]江苏省中医药研究院国家中医药管理局中药释药系统重点研究室,江苏南京210028 [2]南京中医药大学,江苏南京210046

出　　处：《中国中药杂志》2014年第1期71-74,共4页China Journal of Chinese Materia Medica

基　　金：国家"十一五"科技支撑计划项目(2008BAI51B03);江苏省社会发展科技支撑计划项目(BE2010756);江苏省中医药科技项目(LZ11065)

摘　　要：目的:拟制备pH依赖型黄芩苷结肠定位固体分散体,以期达到结肠定位和快速释药的目的。方法:采用溶剂法制备黄芩苷-Eudragit S100固体分散体,运用差示扫描量热法(DSC)、扫描电镜法(SEM)、X-射线粉末衍射法(XRD)、红外光谱(IR)等分析方法对其微观结构和理化性质进行了分析,并对其体外释放性能进行考察。结果:DSC和XRD分析结果显示黄芩苷以非晶体形式分散在固体分散体中,IR结果表明黄芩苷与Eudragit S100之间可能存在非共价键作用。体外释放度测定结果表明,黄芩苷-Eudragit S100比例达到1∶6时,药物在pH 1.2的稀盐酸溶液2 h中基本不释放;在pH 6.8的磷酸缓冲液中,4 h累积溶出率小于15%;在pH 7.6的磷酸缓冲液中,1 h累积溶出度达到90%以上。结论:所制备的黄芩苷-Eudragit S100固体分散体能够达到结肠定位和快速释药的目的,并提高结肠部位黄芩苷的浓度。Objective： To prepare pH-dependent baicalin colon-specific solid dispersion, with the aim of colon-specific deliv- ery and rapid drug release. Method： Baicalin-eudragit S100 solid dispersion was prepared by using the solvent method. The micro- scopic structure and physicochemical properties were analyzed by using differential scanning calorimetry （DSC）, scanning electron microscopy （SEM）, X-ray powder diffraction （XRD） and infrared spectroscopy （IR）. And its in vitro release was also investigated. Result： The results of DSC and XRD analysis suggested that baicalin may be dispersed in solid dispersion in the amorphous state. IR resuits indicated a non-covalent bond effect may exist between baicalin and eudragit S100. The results of in vitro release determination showed that very few baicalins in pH 1.2 diluted hydrochloric acid solution for 2 h at the baicalin-eudragit S100 ratio of 1 ： 6. The accumulated dissolution rate was less than 15% in pH 6. 8 phosphate buffer solution for 4 h, but exceeding 90% in pH 7. 6 phosphate buffer solution for 1 h. Conclusion： The prepared baicalin-eudragit S100 solid dispersion could achieve the objective of colon-specific delivery and rapid drug release, and helps increase the concentration of baicalin in colons.

关 键 词：PH依赖型 黄芩苷-Eudragit S100固体分散体 体外释放度 

分 类 号：R283[医药卫生—中药学]