复方阿司匹林/硫酸氢氯吡格雷双层缓释片的制备

Preparation of compound aspirin-clopidogrel bisulphate double-layed sustained-release tablets

目的以阿司匹林为缓释,硫酸氢氯吡格雷为速释部分,制备复方阿司匹林/硫酸氢氯吡格雷双层缓释片。方法用HPLC法作为分析方法,考察其体外释放特性。通过单因素考察,优化片剂处方。结果优化的片剂处方为,阿司匹林缓释层:阿司匹林150.0mg、羟丙基甲基纤维素(hydroxypropylmethylcellulose,HPMC)K15M100.0mg、枸橼酸7.5mg、滑石粉5.0mg,硫酸氢氯吡格雷速释层:硫酸氢氯吡格雷97.9mg、预胶化淀粉60.0mg、微晶纤维素20.0mg、交联聚维酮8.0mg、滑石粉5.0mg。体外释放研究表明,该复方片1～24h内阿司匹林缓释效果良好,45min内硫酸氢氯吡格雷溶出质量分数达到90%以上。结论研制的复方阿司匹林/硫酸氢氯吡格雷双层缓释片达到了设计要求,具有开发价值。

Objective To prepare the compound aspirin-clopidogrel bisulfate tablets by using aspirin as the sustained-release part and clopidogrel bisulfate as the quick-release part. Method The content of the two drugs was determined by HPLC method, and the optimal formulation was selected via the single-factor experimental design. Result The optimized formulations were: sustained-release part: aspirin 150.0 mg, HPMC K15M 100.0 mg, citric acid 7.5 mg, Talc 5.0 mg; quick-release part: clopidogrel bisulfate 97.9 mg, α-starch 60.0 mg, MCC 20.0 mg, PVPP 8.0 mg, Talc 5.0 mg. In dissolution test indicated that aspirin was released according to zero order kinetics, and the accumulative release of clopidogrel bisulfate after 45 min was over 90%.Conclution The prepared tablets meet the designed requirements, and have the value to be exploited.