三七总皂苷缓释微丸的制备及体外释放行为

目的 优选三七总皂苷缓释微丸制备工艺, 完成相关体外评价研究.方法 使用单因素筛选和L9 (34) 正交试验, 确立最佳的成丸条件;单因素试验考察包衣条件;体外释放度考察包衣增重对释放的影响.结果丸心制备方法为:三七总皂苷 (PNG) :微晶纤维素 (MCC) =1:3混匀, 以45%乙醇为润湿剂, 使用挤出-滚圆法制备, 挤出速度为45 r/min, 滚圆速度35 HZ (1 505 r/min) , 滚圆6 min, 60℃减压干燥4 h.正交试验结果为影响因素顺序为滚圆速度>滚圆时间>挤出速度, 其中滚圆速度有显著性差异.包衣条件为:以15%苏丽丝E-7-19050水分散体于40℃包衣, 喷雾压力0.4 MPa, 喷液速度为1.0 m L/min, 包衣1.5 h.体外释放度表明包衣增重17%有较好的缓释效果.药物释放动力学模型拟合表明符合Higuchi模型.结论 三七总皂苷缓释微丸的制备方法稳定、可行, 可用于进一步研发, 并为其释放进行深入探讨奠定基础.

Preparation and in Vitro Release Study of Panax Notoginseng Sustained-release Pellets

Objective To prepare Panax notoginseng (PNG) sustained-release pellets and accomplish in vitro release study.Methods Single-factor test and orthogonal test was used to establish the preparation of pellets.Coating conditions were investigated by single-factor test.In vitro release study was used to research the effects of different coating thickness.Results The preparation of pellets was (PNG) :Cellulose Microcrystalline (MCC) =1:3, 45% ethanol was Wetting Agent, method was extrusion-spheronization, rate of extrusion was 45 r/min, rolling rate was 35 HZ (1 505 r/min) , rolling time was 6 minutes, vacuum drying continued for 4 hours at 60℃.Orthogonal test indicated effect order was rolling rate>rolling time>extrusion tare.15% Surelease E-7-19050 was coated pellet at 40℃, the pressure of spray was 0.4 MPa, the rate of spray was 1.0 m L/min.The in vitro release study confirmed that pellets had released sustainedly with added 17% weight.The in vitro release data were well fitted to Higuchi drug release models.Conclusions The preparation process is simple and reliable and could be used to dig deeper to develop.It could lay the foundation for study of release mechanism further.