基于质量源于设计（QbD）理念的穿心莲内酯结肠靶向微丸研究  

Development of andrographolide colon-targeting release pellets based on quality by design(QbD) approach

作　　者：肖传学 高展 苏娟 王征[1] XIAO Chuan-xue;GAO Zhan;SU Juan;WANG Zheng(College of Pharmacology Science and Technology,Tianjin University,Tianjin 300072,China;Tasly Pharmaceutical Co.,Ltd.,Tianjin 300402,China)

机构地区：[1]天津大学药物科学与技术学院,天津300072 [2]天士力医药集团股份有限公司,天津300402

出　　处：《中草药》2019年第22期5462-5469,共8页Chinese Traditional and Herbal Drugs

摘　　要：目的基于质量源于设计(QbD)理念优化穿心莲内酯结肠靶向微丸。方法采用累积体外释放度为评价指标,利用单因素考察与危害分析对穿心莲内酯结肠靶向微丸丸芯及包衣工艺进行研究,并采用星点设计-响应面法对增塑剂用量、老化时长及包衣增重3个关键因素进行优化与预测。结果最佳包衣工艺参数:增塑剂用量为3 g,包衣增重为20%,老化时长为1 h。经工艺验证,最佳制剂工艺在酸阶段(0.1 mol/L HCl)-缓冲盐阶段(pH 6.0)累积体外释放率6.9%,在pH 7.2缓冲盐阶段累积体外释放率超过90%。结论在穿心莲内酯结肠靶向微丸的研究过程中应用QbD理念优化是可行的。Objective To optimize andrographolide pellet by using a quality by design(QbD)approach.Methods Usingthe cumulative in vitro release as evaluation index,the single-factor investigation and hazard analysis were used to study the core and coating process of andrographolide colon-targeting pellets,and the central composite design-response surface method was used to optimize and predict the three key factors of plasticizer dosage,aging time,and coating weight gain.Results The optimum coating process parameters were as following:plasticizer dosage of 3 g,coating weight gain of 20%,and aging time of 1 h.The process had been verified that the optimal formulation process had a cumulative in vitro release of 6.9%in the acid phase(0.1 mol/L HCl)-buffered salt phase(pH 6.0)and a cumulative in vitro release of more than 90%in the pH 7.2 buffered salt phase.Conclusion It is feasible to apply the QbD concept optimization in the study of andrographolide colon-targeting pellets.

关 键 词：质量源于设计 穿心莲内酯 结肠靶向微丸 危害分析法 星点设计-响应面法 

分 类 号：R283.6[医药卫生—中药学]