熔融制粒法制备盐酸二甲双胍缓释片

目的制备盐酸二甲双胍缓释片,并考察其释药行为及影响因素。方法以山嵛酸甘油酯为骨架材料,微晶纤维素为致孔剂,采用熔融制粒技术制备盐酸二甲双胍缓释片,并考察不同释放介质,山嵛酸甘油酯、微晶纤维素的不同用量以及制备工艺参数等对该缓释片体外释放的影响。结果山嵛酸甘油酯和微晶纤维素的用量为药物释放的主要影响因素,制备的缓释片具有明显的缓释特征,体外释药过程符合零级动力学模型。结论采用山嵛酸甘油酯作为蜡质骨架材料,结合其他辅料,采用熔融制粒技术可制备日服1次的盐酸二甲双胍缓释片。

Preparation of Metformin Hydrochloride Sustained-release Tablets By Melt Granulation

OBJECTIVE To prepare metformin hydrochloride sustained-release tablets and to study its release characterization in vitro and the factors affecting drug release. METHODS Metformin hydrochloride sustained-release tablets were prepared with glycery behenate as matrix material, microcrystalline cellulose as pore-forming agent by melt granulation. The impacts of releasing transmitter, contents of glycery behenate and microcrystalline cellulose, and preparation process factors on the drug release in vitro of the tablets were studied. RESULTS The contents of glycery behenate and microcrystalline cellulose were critical factors affecting drug release rate. The tablets had a remarkable sustained-release property, the drug release profile in vitro followed zero order or Higuchi kinetics. CONCLUSION Using glycery behenate as the wax matrix materia1, combining with other filers, a sustained release tablet of once daily administration is prepared by melt granulation.