穿心莲内酯结肠靶向片的制备及体外释放性能评价  

Preparation and in vitro evaluation of andrographolide tablets for colon-specific delivery

作　　者：单春燕[1] 陈文[2] 王园姬[2] 徐建国 

机构地区：[1]新疆医科大学药学院,新疆乌鲁木齐830011 [2]新疆石河子大学药学院,新疆石河子832002 [3]新疆药物研究所,新疆乌鲁木齐830004

出　　处：《新疆医科大学学报》2011年第1期36-40,共5页Journal of Xinjiang Medical University

基　　金："新疆维吾尔自治区特种植物药资源教育部重点实验室"开放课题基金(200702)

摘　　要：目的评价以穿心莲内酯制备的pH依赖型结肠靶向片的体外释放性能。方法以穿心莲内酯为评价指标,对制剂的包衣处方进行筛选,在单因素试验基础上,应用正交试验设计优化包衣液处方。通过溶出曲线的相似性f2因子法评价不同释放曲线的相似性,采用体外释放度测定方法考察制剂的体外释药性能。结果以Eudragit S100为包衣材料、邻苯二甲酸二乙酯为增塑剂,增塑剂用量占聚合物30%的包衣液,使片芯包衣增重达6%。体外释放度测定结果表明,在人工胃液2 h、人工小肠液3 h未检测到穿心莲内酯,而在人工结肠液2 h指标累积溶出率达80%以上。结论制备的穿心莲内酯结肠靶向片能达到结肠定位释药目的 。Objrctive To prepare the pH-dependent Andrographolide tablets for colon-specific delivery and evaluate the releasing property in vitro.Methods Using Andrographolide as the evaluation index,the prescription of the coating solution was screened.Based on the single factor tests,the orthogonal design was used to optimize the coating solution.The similarity f2 factor was used to evaluate the resemblance of different release curves.The release characteristic was inspected in vitro.Results Using Eudragit S100 as the coating material and diethyl phthalate as the elasticizer,when the amount of elasticizer occupied reached to 30% in the polymer,the weight gain of the core reached to 6%.The release in vitro showed that Andrographolide could not be detected when the tablets were put into the gastric juice of 2 hours and the artificial small intestinal juice for 4 hours,but when it was put into the artificial colon just for 2 hours,the cumulative release rate reached to 80%.Conclusion The prepared Andrographolide tablets for colon-specific delivery could fulfill the aim of colon-release.

关 键 词：穿心莲内酯 结肠靶向片 体外释放度 

分 类 号：R94[医药卫生—药剂学]