易溶性药物酒石酸美托洛尔速释联合缓释片的制备

Preparation of immediate and sustained release tablets of water soluble metoprolol tartrate

目的采用熔融法制备水中易溶药物酒石酸美托洛尔缓释片,并联合速释片,以期抑制第一个血压高峰,减缓第二血压高峰。方法采用熔融制粒法,将药物、羟丙基甲基纤维素(hydroxypropyl methyl cellulose,HPMC)和羧甲基纤维素钠(carboxymethyl cellulose sodium,CMC-Na)混合粉末加入到熔融状态下的硬脂酸中,制备缓释片。考察缓释骨架的用量、不同型号HPMC对药物释放的影响,并采用正交设计对实验进行优化。结果当处方中含有质量分数为25%的酒石酸美托洛尔、质量分数为10%的HPMC K100M、质量分数为30%的硬脂酸和质量分数为35%的CMC-Na时,基本达到缓释效果。结论水中易溶药物采用熔融制粒法制备缓释片,缓释效果较好。结合速释,可实现速释和缓释双释效果。

Objective To prepare and evaluate the immediate sustained-release tablets of ater soluble drug metoprolol tartrate（ MT）. The tablets match the circadian rhythms of hypertension ith pharmacotherapy.Methods MT sustained-release tablets ere prepared by melt granulation method by adding MT,HPMC and CMC-Na to the melted stearic acid. The effect of the level of HPMC and stearic acid,the types of HPMC and the preparation method as studied ith the accumulative release percentages as indexes. Results The optimized sustained-formulation as 25%（w） MT,10%（w） HPMC K100 M,30%（w） stearic acid,35%（w）CMC-Na. Conclusions The sustained-release tablets of ater soluble drug can be successfully prepared by the melt granulation method. It reached the immediate and sustained biphasic-release.