高乌总碱缓释片处方优化研究

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。

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

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 t_1/2-0.150 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.