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目的制备盐酸地尔硫牙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,以流化床包衣法分别包覆内层低取代羟丙基纤维素(low substituted hydroxypropylcellulose,L-HPC)溶胀层和外层乙基纤维素水分散体控释层来制备脉冲控释微丸,并考察溶胀层材料类型、溶胀层包衣增重、溶胀层包衣液中十二烷基硫酸钠(sodium alkyl sulfate,SDS)浓度及控释层包衣增重对释药的影响。结果药物通过控释层衣膜破裂而释放,溶胀层材料类型、溶胀层包衣增重、溶胀层包衣液中SDS浓度及控释层包衣增重等对脉冲控释微丸的释药时滞和释放速度均有显著影响。结论该方法制备的脉冲控释微丸,在模拟人体内胃肠道pH值变化条件下达到了时滞为4h,滞后1.5h,累积释药80%以上的脉冲释药效果。
Objective To prepare diltiazem pulsatile controlled-release pellets and investigate the influencing factors in vitro. Methods Pellets were prepared by extrusion-spheronization method. The inner layer of low-substituted hydroxypropylcellulose (L-HPC) swollen layer and the outer layer of ethylcellulose The controlled release tablets were used to prepare controlled release pellets. The types of the swelling layer, the weight gain of the swelling layer, the concentration of sodium alkyl sulfate (SDS) and the controlled release layer Effect of coating weight gain on drug release. Results The drug was released through the rupture of the controlled release coating. The release of the controlled release pellets by the type of swelling layer, the weight gain of the swelling layer, the SDS concentration in the coating layer of the swelling layer and the weight gain of the controlled release layer coating Delay and release rate have a significant impact. Conclusion The pulse controlled release pellets prepared by this method achieve the effect of pulse release with a delay of 4 h, a lag of 1.5 h and a cumulative release of over 80% under the condition of simulating the change of gastrointestinal pH in the human body.