摘要
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EudragitR○L100-55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EudragitR○L100-55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。
OBJECTIVE To develop enteric coated pellets containing mefformin hydrochloride. METHODS Mefformin hydrochlotide loaded pellets were prepared using GPCG 1 fluid bed with the bottom spray processs, and mefformin hydrochloride was layered on sugar pellets containing HPMC （6 ×10^-3Pa·s, 2.0% ） as a binder. And Eudragit L 100-55 or Eudragit L 30D-55 were selected as emetic coated poly- mer 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 mefformin hydmchloride loaded pellets was investigated. RESULTS In order to pass the ClaP 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 motformin hydrochlotide release in 0.1mol·L^-1 HCI, 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 hydroehloride enteric pellets containing 3% weight gain of HPMC as subcoat can meet the ChP enteric claim.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2006年第24期1872-1876,共5页
Chinese Pharmaceutical Journal
