摘要
目的:制备水飞蓟素缓释片,并研究其体外释药机制。方法:选取不同载体、不同载药比、不同制备方法分别制备不同固体分散体,比较其体外溶出度,并以优化的固体分散体制备水飞蓟素缓释片。根据水飞蓟素缓释片体外溶出曲线和释药过程的数学模型拟合结果,考察其体外释药机制。结果:采用热熔挤出法,以聚乙烯吡咯烷酮VA64为载体,载药比为1∶4(m/m)制备水飞蓟素缓释片,其可体外持续释药12h以上,12h累积溶出度可达96.87%,体外释药行为符合零级动力学方程。结论:所选方法合理、可行,制备的水飞蓟素缓释片可提高水飞蓟素的体外溶出度,达到长效的目的。
OBJECTIVE： To prepare Silymarin sustained-release tablets, and to study the in vitro release mechanism. METH- ODS： Different solid dispersions were prepared with different preparation methods using different carrier and drug-loading amount. The in vitro dissolution rates of them were compared, and the optimized solid dispersion was used to prepare Silymarin sustained-re- lease tablets. The release mechanism of the tablets was studied according to in vitro dissolution curves and fitted mathematical mod- el of drug release process. RESULTS： Silymarin sustained-release tablets were prepared with hot melt extrusion method using PVP- VA64 as carrier （1：4）. The drug can be sustainably released over 12 h in vitro. The accumulative dissolution rate reached 96.87% within 12 h, and its release behavior imitated as the zero-grade kinetics equation. CONCLUSIONS： The method is reasonable and feasible. Prepared Silymarin sustained-release tablets can improve dissolution rate of silymarin in vitro to achieve long-term effect.
出处
《中国药房》
CAS
CSCD
2013年第19期1770-1772,共3页
China Pharmacy
关键词
水飞蓟素
热熔挤出法
固体分散体
缓释片
Silymarin
Hot melt extrusion method
Solid dispersible tablets
Sustained-release tablets
