高乌总碱缓释片处方优化研究

Study on Optimization of Formula of Total Alkaloids of Aconitum Sinomontanum Nakai Sustained-release Tablets

目的:优选高乌总碱缓释片处方,并对其体外释药机制进行研究。方法:采用正交试验法,以高乌总碱缓释片中高乌甲素的累积释放量为指标,综合评分法确定最优处方,并进行释药方程拟合,研究其释药机制。结果:所制备的缓释片在10 h内呈现良好的缓释特征,符合《中国药典》2005年版对缓释片的要求,释药机制符合Higuchi方程(Q=0.349 t1/2-0.150 5,r=0.997 2)和Peppas方程(lnQ=0.688 9 lnt-1.595 7,r=0.995 5),表明药物以Fick扩散和溶蚀协同作用的方式释放。结论:该缓释片处方设计合理,制备方法简单,缓释效果理想,药物释放机制符合释放动力学模型,值得进一步研究开发。

Objective： To optimize the formula of total alkaloids of Aconitum sinomontanum Nakai sustained-release tablets and evaluate its drug release property.Method：Orthogonal design was used to obtain the best formula.The best formula was determined by dissolution of lappaconitine in total alkaloids of Aconitum sinomontanum Nakai sustained-release tablets and comprehensive scoring method.The release formula was made to investigate the release mechanism.Result：The dissolution curves in-vitro showed that the drug release could be best described by the Higuchi equation（Q = 0.349 t1/2-0.150 5,r = 0.997 2） and Peppas equation（lnQ = 0.688 9 lnt-1.595 7,r = 0.995 5）.It showed that the release mechanism were Fick diffusion and backbone corrosion.The release rate matched the requirement of quality control on sustained-release tablets in Chinese Pharmacopoeia（2005）.Conclusion：The method of content determination was simple and sustained-releasing rate was significant.The release mechanism followed the kinetic model of sustained-release tablets.It is worth doing further research for clinical use.