复方氢氯噻嗪双层片中酒石酸美托洛尔缓释片的处方筛选

Optimization of the Formulation of Metoprolol Tartrate Sustained-release Tablets in Compound Hydrochlorothiazide Double Layer Tablets

目的:筛选复方氢氯噻嗪双层片中酒石酸美托洛尔缓释片处方。方法:以体外释放度为主要考察指标,并以羟丙基甲基纤维素(HPMC)与卡波姆的总用量(A)及二者的质量比(B)、微晶纤维素用量比例(C)、聚丙烯吡咯烷酮(PVP)无水乙醇溶液浓度(D)为因素进行正交试验优选处方。结果:优化处方确定A为30%,B为1∶2,C为20%,D为5%。优化后所制3批酒石酸美托洛尔缓释片1h内的累积释放度均在25%～45%,4h内的累积释放度均在40%～75%,8h内的累积释放度均>75%,24h累积释放度均>90%。结论:所选酒石酸美托洛尔缓释片的处方合理、工艺简单。

OBJECTIVE： To optimize the formulation of metoprolol tartrate sustained-release tablets in compound hydrochlorothiazide double layer tablet.METHODS： The formulation of metoprolol tartrate sustained-release tablets was optimized using orthogonal experiment with release rate in vitro as index,total amount of HPMC and carbomer （A） and its ratio （B）,amount of MCC （C） and the concentration of PVP ethanol solution （D） as factors.RESULTS： The optimal formulation was as follows： A=30%,B=1 ∶ 2,C=20% and D=5%.Accumulative release rate of 3 batches of metoprolol tartrate sustained-release tablet prepared by optimized formulation were 25%～45% within 1 h,40%～75% within 4 h,more than 75% within 8 h and more than 90% within 24 h.CONCLUSION： Optimized formulation of metoprolol tartrate sustained-release tablets is reasonable and simple.