白头翁总皂苷结肠靶向微丸的制备  

Preparation of Pulsatilla Total Saponins Colon-Targeted Pellets

作　　者：王勇[1] 岳国超[2] 朱婉婷[2] 严霞[1] 王红军[1] 

机构地区：[1]湖北中医药大学附属襄阳市中医医院,湖北襄阳441000 [2]江西中医学院现代中药制剂教育部重点实验室,南昌330004

出　　处：《中国实验方剂学杂志》2013年第19期53-57,共5页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：江西省教育厅科技落地计划项目(赣财教[2011]243号)

摘　　要：目的:优选白头翁总皂苷结肠靶向微丸的制备工艺。方法:采用HPLC测定白头翁总皂苷含量,色谱条件为Hypersil ODS-C18色谱柱(4.6 mm×250 mm,5μm),流动相乙腈-0.1%磷酸水溶液(39∶61),流速1.0 mL·min-1,柱温30℃,检测波长203 nm,进样量20μL。利用挤出滚圆法制备白头翁结肠靶向微丸载药丸心,以微丸得率、圆整度、堆密度、脆碎度的综合评分为指标,通过正交试验优选白头翁结肠靶向微丸载药丸心的制备工艺;以累积释放率为指标,通过单因素试验考察增塑剂用量、抗黏剂用量、包衣增重对包衣工艺的影响。结果:载药丸心的最佳制备工艺为微晶纤维素用量60%,甘露醇用量10%,挤出频率20 Hz,滚圆频率45 Hz,滚圆时间5～8 min;最佳包衣工艺为以Eudragit S100为包衣材料,15%柠檬酸三乙酯为增塑剂,50%滑石粉为抗黏剂,包衣增重20%。结论:优选的工艺稳定可行,制备的微丸成型性高、靶向效果好。Objective： To optimize preparation technology of pulsatilla total saponins colon-targeted pellets. Method： HPLC was adopted to determined the content of total saponins from Pulsatillae Radix, chromatographic conditions were as follows： Hypersil ODS-C18 column （4.6 mm x 250 mm, 5 μm） , mobile phase of acetonitrile-0. 1% phosphoric acid solution （39：61 ）, flow rate 1.0 mL .min^-1, column temperature 30 ℃ , detection wavelength 203 nm, injection volume 20 μL. Pellets core was prepared by extrusion spheronization method, with pellets yield, roundness, bulk density, friability as comprehensive evaluation index, orthogonal test was adopted to optimize preparation technology of pulsatilla total saponins colon-targeted pellets; With cumulative release rate as index, effects of plasticizer amount, anti-adhesion agent dosage and coating weight on coating process were investigated by single factor tests. Result： The best preparation technology of pellets core was as following： dosage of MCC 60% , mannitol amount 10% , extrusion frequency 20 Hz, rolling frequency 45 Hz, roiling time 5-8 min; Optimum coating process was： with Eudragit S100 as coating material, 15% triethyl citrate as plasiticizer, 50% talcum powder as anti-adhesion agent, coating weight of 20%. Conclusion： Optimized process was stable and feasible, prepared pellets had good molding and colon-targeted effect.

关 键 词：白头翁 结肠靶向微丸 正交试验 流化床包衣 单因素试验 

分 类 号：R283.6[医药卫生—中药学]