地尔硫■双脉冲控释微丸的制备及体外释放度考察  

Study on preparation and in vitro release of diltiazem dual-pulsatile controlled-release pellets

作　　者：张晓晖[1] 贾晓英[1] ZHANG Xiaohui;JIA Xiaoying(Department of Pharmacy,Affiliated Hospital of Inner Mongolia Medical University,Hohhot 010050,China)

机构地区：[1]内蒙古医科大学附属医院药剂部

出　　处：《山西医科大学学报》2019年第10期1461-1466,共6页Journal of Shanxi Medical University

基　　金：内蒙古自治区自然科学基金资助项目(2017MS0898)

摘　　要：目的制备地尔硫?双脉冲控释微丸,并考察其体外释药性能。方法采用挤出滚圆法制备地尔硫?载药丸芯,正交试验设计法优化丸芯处方;以羧甲基淀粉钠作为溶胀层,尤特奇L30D-55作为控释层,流化床包衣法制备地尔硫脉?冲微丸,考察溶胀层及控释层包衣增重对微丸释药行为的影响。结果优化后的丸芯处方为地尔硫?40%,微晶纤维素40%,乳糖和低取代羟丙甲纤维素各10%,0.4%羟丙甲纤维素溶液作为黏合剂;当溶胀层包衣增重10%,控释层包衣增重20%时,制得微丸释药时滞为4 h,且6 h和9 h药物释放分别超过50%和80%。结论本方法制备的地尔硫?包衣微丸体外脉冲释药性能良好,应用前景广阔。Objective To prepare the diltiazem dual-pulsatile controlled-release pellet and investigate its drug release in vitro.Methods The diltiazem drug-loaded pellet cores were prepared by extrusion-spheronization method,and the prescription of pellet cores was optimized by orthogonal test design.Then the pellets were coated by carboxymethyl starch sodium as swelling layer and Eudragit L30D-55 as controlled release layer via fluidized bed coating method.The effects of coating weight of swelling layer and controlled release membrane on the drug release in vitro were investigated.Results The optimized pellet cores prescription contained 40%of diltiazem,40%of microcrystalline cellulose,10%of lactose,10%of low-substituted hypromellose,and 0.4%of hypromellose solution as a binder.The lag time of drug release was about 4 h when swelling layer coating weight was 10%,and controlled release membrane coating weight was 20%.The drug release at 6 h and 9 h exceeded 50%and 80%,respectively.Conclusion The diltiazem coated pellets prepared by this method have good pulse release properties in vitro,which have a broad potential for application.

关 键 词：地尔硫■ 脉冲控释微丸 正交试验 时滞 

分 类 号：R927[医药卫生—药学]