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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 dispersions in order to achieve the purpose of colon colonization and rapid drug release. Methods: Baicalin-Eudragit S100 solid dispersion was prepared by solvent method and analyzed by differential scanning calorimetry (DSC), scanning electron microscopy (SEM), X-ray powder diffraction (XRD) and infrared spectroscopy (IR) Methods The microstructure and physicochemical properties were analyzed and their in vitro release properties were investigated. Results: The results of DSC and XRD showed that baicalin was dispersed in the solid dispersion in the form of amorphous. The results of IR indicated that non-covalent bond might exist between baicalin and Eudragit S100. The results of in vitro release showed that when the ratio of baicalin-Eudragit S100 reached 1: 6, the drug did not release in dilute hydrochloric acid solution at pH 1.2 for 2 h. In the pH 6.8 phosphate buffer solution, the cumulative dissolution rate at 4 h was less than 15 %; In the pH 7.6 phosphate buffer, 1 h cumulative dissolution reached more than 90%. Conclusion: The prepared baicalin-Eudragit S100 solid dispersion can achieve the purpose of colonic localization and rapid release, and increase the concentration of baicalin in the colon.