目的 研究不同剂量与溶解度模型药的小丸上药处方和工艺。方法 以盐酸二甲双胍作为高剂量高水溶性模型药,以对乙酰氨基酚作为低剂量低水溶性模型药,蔗糖丸芯作为上药载体,根据药物剂量与溶解度选择不同型号欧巴代^作为上药黏合剂,以流化床底喷方式上药,评价上药工艺过程与上药小丸的质量。结果 以欧巴代^作为上药黏合剂,上药工艺稳健、小丸粘连率低、上药率高、含量均匀、上药小丸溶出完全、粒径均匀、分布范围窄、表面光滑圆整。结论 高配液固含量及高药物与黏合剂比例可缩短高剂量高水溶性模型药上药时间;对低剂量低水溶性药物来说,低配液固含量及低药物与黏合剂比例可实现均匀的上药,使用欧巴代^03A系列产品作为上药黏合剂,获得质量优良的载药小丸,为功能包衣打下良好基础。

OBJECTIVE To study drug layering process of model drugs with different dose and solubility. METHODS Metformin hydrochloride was selected as high dose high soluble model drug while acetaminophen was selected as low dose low soluble model drug, the two model drugs were loaded onto sugar spheres (Suglet^ ) in a bottom spray fluid bed separately using different types of Opadry^ as binder, then the coating process and quality of drug loaded beads were evaluated. RESULTS A robust coating process is achieved with low agglomeration rate and high drug yield, the loaded beads are uniform in content and particle size distribution, smooth in appearance and round in shape, drug release from the beads is complete.CONCLUSION Process time of high dose high soluble drug can be minimized by using high suspension solids and high drug to binder ratio, for low dose low soluble drug, content uniformity can be achieved by utilizing low suspension solids and low drug to binder ratio; drug loaded beads with good quality are prepared using Opadry 03A series products as drug layering binder, so a solid foundation is laid for functional coating.