双氯芬酸钠脉冲控释微丸的制备与体外释放影响因素的研究

 目的制备双氯芬酸钠脉冲控释微丸并考察体外释放影响因素。方法采用挤出滚圆法制备载药丸芯，以水溶胀性材料低取代羟丙基纤维素为内包衣溶胀层，乙基纤维素水分散体为外包衣作为控释层制备脉冲控释微丸，并考察溶胀层材料类型、溶胀层和控释层包衣增重、介质pH值和微丸粒径等对药物释放的影响。结果药物通过控释层衣膜破裂释放，溶胀层材料类型、溶胀层和控释层包衣增重和微丸粒径等对脉冲控释微丸的释药时滞和释放速率均具有显著影响，药物释放情况不受介质pH值的影响。结论采用水溶胀性材料低取代羟丙基纤维素为内包衣层，制备的脉冲控释微丸，当内包衣层增重为11%和外包衣层增重胀层为17%时，达到了时滞为4h，时滞后1.5h累积释药80%以上的脉冲释药效果。

Studies on preparation of diclofenac sodium pulsatile controlled-release pellets and various influence factors

OBTECTIVE To prepare the diclofenac sodium(DS) pu ls atile controlled release pellets(PCRP).METHODS DS loaded p ellets were prepared by extrusion spheronization technology.PRP were prepared w ith low substituted hydroxypropylcellulose (L HPC ) as the inner swelling laye r and ethylcellulose aqueous dispersion (Surelease) as the outer controlled laye r.The influences of the coating material of the swelling layer,the coating level of the swelling layer and the controlled layer,the pH values of the media and t he size of final pellets on the release of DS from PCRP were investigated respec tively.RESULTS The drug release was triggered while rupturin g the membrane of the controlled layer.The coating material of the swelling laye r,the coating lever of the swelling layer and the controlled layer and the size of final pellets had significant effect on the lag time and the release rate of DS from PRP.CONCLUSION After the lag time of 4 h,the drug re lease from DS PCRP with 11%(w/w) Surelease coating level as controlled layer wa s more than 80% within the following 1.5 h.