磷酸川芎嗪缓释片的研制

Preparation of tetramethylpyrazine phosphate sustained-release tablets

目的 :制备磷酸川芎嗪缓释片。方法 :用正交设计优选处方 ,以羟丙甲基纤维素 (HPMC ,K10 0M)为骨架材料 ,用适量疏水性阻滞剂乙基纤维素 (EC ,10 0cps)调节药物释放速度 ,采用湿法制粒压片制备磷酸川芎嗪骨架片。用紫外分光光度法在 2 95nm测定吸收度A来测主药含量 ,根据中国药典 2 0 0 0年版释放度测定法测定其体外释放度 ,并对其稳定性作了初步考察。结果 :所制备的缓释片在 12h内呈现良好的缓释特征 ,符合Higuchi方程 ,累积释放百分率Q =3 0 .2 915t1/ 2 -6.7776(r =0 .993 7) ,释放速度符合中国药典 2 0 0 0年版对缓释片的质控要求 ,且对湿、光、热稳定性良好。结论 :该磷酸川芎嗪缓释片处方设计合理 ,制备方法简单 ,质控容易 ,缓释效果明显 ,稳定性理想 ,值得进一步研究开发。

Objective: To prepare tetramethylpyrazine phosphate sustained release tablets and to investigate its quality in vitro . Methods: Orthogonal design was utilized to obtain the best formula. The hydrophilic matrix material hydroxypropylmethyl cellulose(HPMC K 100M )was used to prepare tetramethylpyrazine phosphate sustained release tablets by the wet granule compression technique. Ethylcellulose(EC,100cps)was used to adjust the releasing rate. The content of the major drug was determined by UV spectrophotometry at 295 nm. The drug release in vitro was determined according to the method of Chinese Pharmacopoeia(2000)and a survey of its stability was conducted. Results: The dissolution curves in vitro showed that the drug release could be best described by the Higuchi equation ( Q=30.2915 t 1/2 -6.7776,r =0.9937)and other indices matched the requirement of quality control on sustained release tablets in Chinese Pharmacopoeia(2000). Conclusions: The method of content determination was simple and sustained releasing rate was significant. It is worth doing further research in order to provide tetramethylpyrazine phosphate sustained release tablets for clinical use.