pH-时滞型愈肠宁结肠靶向片的制备及体外释放评价

Preparation and in vivo evaluation of pH and time dependent Yuchangning tablets for colon-specific delivery

目的:以中药复方愈肠宁为研究药物,制备得pH-时滞型愈肠宁结肠靶向片,并对其体外释放性能进行评价。方法:以苦参碱、氧化苦参碱体外释放度及药片吸水率为指标,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:该制剂制备方法为:取药物制备得素片,按7∶3取乙基纤维素(EC)∶丙烯酸树脂Ⅱ(Eudragit)混合,加乙醇溶解,加入包衣量10%的邻苯二甲酸二乙酯(DEP)混匀,调整含量为4%,包衣增重3%,即得;该制剂在人工胃液2 h后中未见苦参碱、氧化苦参碱的溶出,在人工小肠液4h后两指标累积溶出率均<10%,在人工结肠液2 h后分别溶出75.7%,76.8%。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 Yuchangning as a research model, prepared the pH and time dependent Yuehangning tablets for colon-specific delivery （ PT-YT-CSD）, and evaluated the releasing property in vitro. Method： The coating prescription is filtered by the release extent of matrine and oxymatrine in vitro and the wieking rate of the tablet, which including the category and proportion of film forming agent and porogen, the sort and dosage of fluidizing agent, the increment of weight after coating and so on. The releasing property of the preparation is evaluated by the dissolution tests in vitro through measuring the content of matrine and oxymatrine content. Result： The preparation method of the PYTCSD： After prepared plain tablets, the 95% alcoholic solution of EC and Eudragit Ⅱ are mixed in a 7：3 EC： Eudragit Ⅱ ratio and then added in DEP up to 10% of the coating amount, redueed the alcohol concentration to 4% by diluting with ethonal. Tablet was coated by the alcohol solution and the weight of the plain tablet was increased by 3%. The dissolution tests in vitro indicated that matrine and oxymatrine were not dissolved in the simulated gastric juice after 2 h. The accumulative quantities of matrine and oxymatrine were less than 10% in the simulated intestinal juice after 4 h. The quantities of matrine and oxymatrine are 75.7% and 76. 8% in the simulated colon juice after 1 h. Conclusion： The PYTCSD was prepared and the preparation could fulfil the aim of delivering in the specific colon in vitro.