酒石酸美托洛尔双脉冲片的研制

Preparation of Metoprolol Tartaric Acid Double-pulsatile Tablets

目的:制备酒石酸美托洛尔双脉冲片。方法:采用混合粉末直接压片法制备3层片芯(2层速释层和1层阻滞层),采用干压包衣技术制备杯形片,以时滞时间和累积释药率为指标,评价杯形片的顶层阻滞层辅料、用量以及压片硬度对释放行为的影响,确定片芯速释层和阻滞层处方及用量。结果:顶层阻滞层的辅料、用量以及压片硬度对释药时滞和累积释药率都有影响。确定了片芯速释层和阻滞层的处方和硬度;顶层阻滞层的用量为0.12g,可达到4h的第1个脉冲效果;片芯阻滞层的用量为70mg,可达到8h的第2个脉冲效果。结论:研制的酒石酸美托洛尔双脉冲片体外释放达到双脉冲要求。

OBJECTIVE：To prepare Metoprolol tartaric acid double-pulsatile tablets.METHODS：Mixed powder direct compression method was used to prepare 3 layers of tablet core（2 quick release layers and 1 blocking layer）,and core-in-cup tablets were prepared by dry-compression coated technology.Effects of excipients and amount of top blocking layer of core-in-cup tablets and the hardness on drug release were evaluated using lag time and accumulative drug release rate as index to determine formula and amount of quick release layer and blocking layer.RESULTS：The excipients and amount of top blocking layer and the hardness had effect on lag time and accumulative drug release rate.The formula and hardness of quick release layer and blocking layer quantity were all determined;the amount of top blocking layer was 0.12 g,and the first pulse can be obtained at 4 h;the amount of blocking layer of core was 70 mg,and the second pulse can be obtained at 8 h.CONCLUSION：Metoprolol tartaric acid double-pulsatile tablets can meet the standard of double-pulsatile release.