摘要
目的:以中药复方肠康宁为研究药物,通过对其包衣工艺的研究,制备得pH-酶依赖型肠康宁结肠靶向片。方法:采用多层包衣法,以盐酸小檗碱体外释放度等为考察指标,对包衣处方中成膜剂及致孔剂种类、成膜剂与致孔剂比例、增塑剂种类及用量、包衣增重进行筛选。结果:该制剂包衣工艺为:取药物制备得素片,取3%果胶溶液,包衣增重4%,得多糖衣;取Eudragit E100、加入12%TEC、1.5%PVPK-30、30%滑石粉配置成聚合物浓度为10%的包衣液,包衣增重5%,得酸溶衣;取HPMC,加1%PEG400为增塑剂,加50%乙醇溶解,包衣增重1.5%,得隔离衣;按1∶2比例取Eudragit L100和Eudragit S100混合,加入10%TEC和60%滑石粉,加乙醇溶解,包衣增重5%,得肠溶衣。该制剂在人工胃液2h后未见盐酸小檗碱溶出,在人工小肠液4h后累积溶出率均<10%,在含酶肠液2 h后溶出90%左右。结论:该制剂在体外能达到结肠定位释药的目的。
Objective： Taking Chinese compound medicine Changkangning as a research model, prepared the pH and enzymes dependent Changkangning tablets for eolon-specific dehvery （PE-CT-CSD）, through the research on trtmdale coating conditions. Methods： Taking multi-layer coating method, the coating prescription is filtered by the release extent of berberine hydrochloride in vitro, which including the category and proportion of film forming agentand porogen, the sortand dosage of fluidizing agent, the increment of weight aftereoating and so on. Result： The preparationmethod of the PECTCSD： After prepared plain tablets, tabletwas coated by the 3 % pectin solution and the weight of the plain tablet was increased by 4 %, the polysaccharides coating was made ; . the EudragitE 100, added in the coating solution mixed by 12 % TEC, 1.5 % PVPK-30, 30 % talc to polymer concentration of 10 %, and the coating weight increased by 5 %, acid-soluble coating was made; HPMC, added 1% PEG400 as plasticizer, 50 % ethanol dissolved, coating weight increased by 1.5 %, isolated clothing made ; the alcoholic solution of Eudragit L100and Eudragit SI00 are mixed in a 1 ： 2 Eudragit LI00： Eudragit S100 ratio and then added in 10 %TEC and 60 % , eoating weight increased by 5 %, the enteric coating was made. The dissolution tests in vitro indicated berberine hydrochloride were not dissolved in the simulated gastric juice after 2h. The accumulative quantities was less than 10 % in the simulated intestinal juice after 4 h. The quantities is about 90 % in the enzyme after 2 h. Conclusion： The PECTCSD was prepared and the preparation could fulfil the aim of delivering in the specific colonin vitro.
出处
《成都中医药大学学报》
2009年第4期69-73,共5页
Journal of Chengdu University of Traditional Chinese Medicine
基金
四川省科技支撑项目(2008SZ0044)
关键词
pH-酶依赖型
肠康宁结肠靶向片
包衣工艺
pH and enzymes dependent
Changkangning tablets for colon-specific delivery
coating prescription
