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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 the preparation of Pulsatilla saponin colon targeting pellets. Methods: The content of total saponins in Pulsatilla was determined by HPLC. The chromatographic conditions were Hypersil ODS-C18 column (4.6 mm × 250 mm, 5 μm), mobile phase acetonitrile-0.1% phosphoric acid solution (39:61), flow rate 1.0 mL · min -1 , Column temperature 30 ℃, detection wavelength 203 nm, injection volume 20μL. Pulsatilla colon-targeted pellets were prepared by the extrusion-spheronization method. The pellets were loaded with pellets by the comprehensive score of pellet yield, roundness, bulk density and friability. The preparation process of pellet heart was studied. The cumulative release rate was used as an index to investigate the effects of plasticizer dosage, anti-sticking agent dosage and weight gain on the coating process. Results: The optimal preparation process of pellets was 60% microcrystalline cellulose, 10% mannitol, 20 Hz extrusion frequency, spheronization frequency 45 Hz and spheronization time 5-8 min. The best coating process was Eudragit S100 is a coating material, 15% triethyl citrate as a plasticizer, 50% talc as an anti-sticking agent, and a coating weight gain of 20%. Conclusion: The optimal process is stable and feasible. The prepared pellets have high formability and good targeting effect.