共研磨法改善尼群地平体外溶出度的研究

目的:采用共研磨法改善尼群地平的体外溶出度。方法:设计单因素试验考察药物与辅料的共研相数(单相、两相和三相)、共研辅料种类(微晶纤维素(MCC)、聚乙烯吡咯烷酮k30(PVPk30)、羟丙基纤维素(HPC)、羟丙基甲基纤维素(HPMC))、共研时间(0、10、20、30、40、50、60min)及主药与共研辅料MCC比例(1∶1、1∶2、1∶3、1∶4、1∶5、1∶6、1∶7、1∶8、1∶9)对尼群地平粉末及片剂体外溶出度的影响。结果:确定共研磨法条件为共研相数为两相,辅料为HPC或MCC,共研时间40min,主药与MCC比例1∶4。在此条件时,共研粉末的药物10min累积溶出百分率可达80%以上,共研粉末片剂40min可达80%以上。结论:难溶性药物尼群地平在适当条件下采用共研磨法可以显著改善其体外溶出度。

Study on Co-grinding Method Improving the Dissolution Rate of Nitrendipine in Vitro

OBJECTIVE： To improve the dissolution rate of nitrendipine in vitro using co-grinding method.METHODS： Single-factor test was adopted to detect effect of phases of co-grinding,category of excipients （MCC,PVPk30,HPC,HPMC）,time （0,10,20,30,40,50,60 min） of co-grinding and ratio of principal component to excipients （1 ∶ 1,1 ∶ 2,1 ∶ 3,1 ∶ 4,1 ∶ 5,1 ∶ 6,1 ∶ 7,1 ∶ 8,1 ∶ 9） on in vitro dissolution of nitrendipine power and tablet.RESULTS： The condition of co-grinding method was as follows： dual co-grinding phase,HPC or MCC as excipients,co-grinding time of 40 min,ratio of principal component to excipients was 1 ∶ 4.Accumulative dissolution rate of nitrendipine powder was more than 80% within 10 min and that of nitrendipine tablet was more than 80% within 40 min.CONCLUSION： Co-grinding method can improve the dissolution rate of poorly water-soluble nitrendipine in vitro under suitable condition.