硫酸沙丁胺醇脉冲控释微丸的制备

目的制备硫酸沙丁胺醇脉冲控释微丸。方法采用挤出滚圆法制备载药丸芯 ,使用水溶胀性材料为内包衣溶胀层 ,乙基纤维素水分散体为外包衣控释层制备脉冲控释微丸 ,并考察溶胀层材料类型、十二烷基硫酸钠 (SDS)含量、溶胀层和控释层包衣增重量对药物释放的影响。结果药物通过控释层衣膜破裂而释放 ,溶胀层材料类型、内包衣层中SDS的加入与否、溶胀层和控释层厚度对脉冲控释微丸的释药时滞和释药速率均具有显著性影响。结论采用低取代羟丙基纤维素为溶胀性材料 ,并加入 0 0 5 2mol LSDS ,共同作为内包衣层 ,制备的脉冲控释微丸 ,当内包衣层和外包衣层增重均为 1 8%时 ,在模拟人体内胃肠道pH值变化条件下达到了时滞为 4 5h ,时滞后 1 5h累积释药 80 %以上的脉冲释药效果

Preparation of salbutamol sulfate pulsatile controlled-release pellets

Objective To prepare salbutamol sulfate pulsatile controlled-release pellets (SS-PCRP).Methods The salbutamol sulfate-loaded pellets prepared by extrusion-spheronization technology were coated in a mini-fluided bed spray coater with swelling material as the inner coating swelling layer and ethylcellulose aqueous dispersion as the outer coating controlled layer.The effects of the coating materials of the swelling layer,the concentration of sodium dodecyl sulfate (SDS),the coating level of the swelling layer and the controlled layer on the release of salbutamol sulfate from SS-PCRP were evaluated.Results The drug release is triggered while rupturing the membrane of the controlled layer.The lag time and released rate of salbutamol sulfate from SS-PCRP are influenced obviously by the species of the swelling material,the concentration of SDS,the coating level of the inner swelling layer and the outer controlled layer.Conclusions The SS-PCRP,with a lag time of 4.5 h and more than 80% released within following 1.5 h under the simulated gastrointestinal pH conditions,are prepared by using low-substituted hydroxypropylcellulose and 0.052 mol/L SDS as the inner swelling layer with the 18% (w) coating level and ethylcellulose aqueous dispersion as the outer controlled layer with the 18% (w) coating level.