黄芩苷固体分散体及其微丸的制备和表征研究

Preparation and characterization of baicalin solid dispersions and pellets

目的:制备黄芩苷固体分散体及其微丸,改善黄芩苷的溶解性,对其进行制剂学和体外释放行为考察。方法:采用溶剂法制备黄芩苷固体分散体,通过红外光谱和核磁共振光谱对黄芩苷固体分散体进行表征,采用挤出-滚圆法制备黄芩苷固体分散体微丸,桨法测定黄芩苷原料药、黄芩苷固体分散体和黄芩苷固体分散体微丸在模拟胃液环境和肠液环境中的释放行为。结果:黄芩苷能够较好地分散在固体分散体载体中,水溶性增加;黄芩苷固体分散体微丸的圆整度和休止角分别为24.3°和26.3°,微丸的收率为32.13%,黄芩苷固体分散体微丸在两种释放介质中的累计释放速度较快。结论:黄芩苷固体分散体在模拟胃液环境和肠液环境的体外释放度都符合速释要求,制备的黄芩苷固体分散体微丸的圆整度、流动性较好,有利于增加在胃肠道的溶解及吸收。

Objective:To investigate the solid dispersions and pellets of Baicalin and their release behavior in vitro,so as to improve the solubility of baicalin.Methods:Using solvent of baicalin solid dispersions prepared,through infrared spectrum and nuclear magnetic resonance spectra of baicalin solid dispersions were characterized,and the extrusion-rolling of baicalin solid dispersions prepared by micro pill,paddle method for determination of baicalin apis,baicalin solid dispersion and baicalin solid dispersion micro pill in simulated gastric juice and intestinal juice environment release behavior.Results:Baicalin could disperse well in the solid dispersive carrier and its water solubility increased.The fineness and resting Angle of baicalin solid dispersive pellets were 24.3°and 26.3°,respectively,and the yield of pellets was 32.13%.The cumulative release rate of baicalin solid dispersive pellets in the two release media was faster.Conclusion:The in vitro release rate of baicalin solid dispersion conforms to the requirement of rapid release in simulated gastric fluid environment and intestinal fluid environment,and the prepared baicalin solid dispersion pellets have better round degree and fluidity,which is beneficial to increase the dissolution and absorption in the gastrointestinal tract.