盐酸二甲双胍肠溶微丸的成型工艺研究

 目的通过工艺参数优化,制备释放度符合肠溶制剂要求的盐酸二甲双胍肠溶微丸。方法使用流化床底喷包衣设备,首先制备并优化盐酸二甲双胍的载药微丸(黏合剂是HPMC,6×10^-3Pa·s,用量为质量分数2.0%),然后考察肠溶包衣溶媒、HPMC隔离层和Eudragit?L 100-55用量对肠溶衣膜抗酸能力的影响。结果水分散体包衣法比乙醇溶液包衣法需要更多的包衣增重。隔离层可以显著降低水分散体包衣法所需的肠溶材料用量,但对于乙醇溶液包衣法制备的样品几乎没有影响结论当Eudragit?L 100-55包衣增重在25%以上时,以水分散体为包衣溶媒并增加隔离层的工艺方法,能使盐酸二甲双胍载药微丸具备较理想的肠溶特征。

Development of Enteric Coated Metformin Hydrochloride Pellets

OBJECTIVE To develop enteric coated pellets containing metformin hydrochloride. METHODS Metformin hydrochloride loaded pellets were prepared using GPCG 1 fluid bed with the bottom spray processs, and metformin hydrochloride was layered on sugar pellets containing HPMC (6×10^-3 Pa·s, 2.0%) as a binder. And Eudragit?L 100-55 or Eudragit?L 30D-55 were selected as enteric coated polymer of drug loaded pellets in the study. The influence of weight gain of polymers, coating medium and subcoat application on the dissolution properties of enteric coated metformin hydrochloride loaded pellets was investigated. RESULTS In order to pass the ChP enteric test, the aqueous and organic enteric coated pellets required 35% weight gain of Eudragit?L 30D-55 and 25% weight gain of Eudragit?L 100-55, respectively. The application of a subcoat of 3% weight gain of HPMC to the aqueous enteric coated pellets resulted in an evidently delay in metformin hydrochloride release in 0.1 mol·L^-1 HCl, but it did not work in the organic enteric coated pellets. CONCLUSION When weight gain of Eudragit?L 30D-55 aqueous dispersions is above 25%, the metformin hydrochloride enteric pellets containing 3% weight gain of HPMC as subcoat can meet the ChP enteric claim.