酒石酸美托洛尔双层漂浮型脉冲释药片制备及其体外释药行为研究  

Preparation of Metoprolol Tartaric Acid Bilayer Floating Tablets for Pulsatile Release and Study on Its in Vitro Release Mechanism

作　　者：张丹霞[1] 

机构地区：[1]广东省深圳市宝安区人民医院,广东深圳518101

出　　处：《中国药业》2016年第9期53-55,共3页China Pharmaceuticals

摘　　要：目的制备用于时辰治疗心绞痛的酒石酸美托洛尔漂浮型脉冲释药片,并探讨其体外释药机制。方法采用混合粉末直接压片法制备双层片,以崩解时间和溶出度为指标,筛选酒石酸美托洛尔速释片芯的崩解剂,优选最佳漂浮层处方。以体外释药试验考察对时滞的影响。结果优选的处方和工艺条件:交联聚维酮作为片芯崩解剂,用量为8%;包衣层处方中羟丙甲基纤维素作为凝胶材料,乳糖作为致孔剂,用量比为4∶1,漂浮层以聚羧乙烯30%,羟丙甲基纤维素36.3%,碳酸氢钠33.7%组合最优。体外释放试验表明,酒石酸美托洛尔双层漂浮型脉冲释药片经6 h滞后期药物脉冲释放。结论酒石酸美托洛尔双层漂浮型脉冲释药片可达到瞬时起漂并持续到预定时滞期后脉冲释药,能满足时辰治疗学、治疗心绞痛的需求。Objective To prepare metoprolol tartaric Acid Bilayer Floating Tablets for the treatment of angina pectoris and to investigate the in vitro release mechanism. Methods The direct compression of mixed powder method was used to prepare the bilayer tablets, the disintegration time and dissolution rate were used as the indicators to screen out the core disintegrating agent of metoprolol taetaric release tablets, and to obtain the preferred formulation. The in vitro release test was used to study the influence on delay. Results The preferred formulation and process conditions： crosslinked povidone as the tablet core disintegrating agent in an amount of 8%; hydroxypropyl methylcellulose as the gel material in the coating layer formulation, lactose as porogen, amount ratio 4 ∶ 1; the optimal combination of floating layer was carbopol of 30%, hydroxypropyl methylcellulose 36. 3%, sodium bicarbonate 33. 7%. In vitro release tests showed that Metoprolol Tartaric Acid Bilayer Floating Tablets released the drug by 6 h of delay. Conclusion The metoprolol tartaric Acid Bi-layer Floating Tablets achieves instantaneous drift and continues to play after a predetermined time demurrage pulse release to meet the demand of hour therapy and angina treatment.

关 键 词：酒石酸美托洛尔 双层漂浮 脉冲释药 时滞 

分 类 号：TQ460.6[化学工程—制药化工] R972.3[医药卫生—药品]