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目的用流化床包衣技术制备苦参碱时控型结肠定位给药微丸。方法使用流化床包衣设备,首先在空白丸芯上采用溶液上药法制备苦参碱载药微丸,然后以羟丙甲纤维素(HPMC)和乙基纤维素水分散体(Surelease)的混合物包衣作为溶胀控释层,以Surelease包衣作为时控包衣层,制备时控型结肠定位给药微丸。分别用扫描电镜、溶出度测定和光学显微镜考察微丸的包衣质量、体外释药率和释放过程中微丸的变化。结果药物通过时控层破裂开始大量释放,调节该层增重和溶胀控释层的增重及此层中HPMC与Surelease比例,均可以调节释药时滞,控制药物的释放速度。优化后的包衣微丸在模拟胃肠道pH情况下延迟5h释药,之后药物近恒速释放,16h内药物释放完全。结论可通过调节时控层的增重,溶胀控释层的增重及此层中HPMC与Surelease比例来制备不同时滞的苦参碱时控型结肠定位给药微丸,为小分子水溶性药物制成时控型延迟释药微丸提供参考。
Objective To prepare matrine-controlled colon-targeted pellets by fluid-bed coating technique. Methods The fluidized bed coating equipment was used. First, matrine-loaded drug-loaded pellets were prepared by solution on blank pellets, and then treated with hypromellose (HPMC) and Surelease Of the mixture coating as a swellable controlled release layer, Surelease coating as a time-controlled coating, when the preparation of colon-controlled colon-targeted drug pellets. The microspheres’ coating quality, drug release rate in vitro and changes of pellets during the release process were investigated by scanning electron microscopy, dissolution assay and optical microscope respectively. Results The drug started to release largely through the rupture of the control layer. Adjusting the weight gain of the layer and swelling control release layer and the ratio of HPMC and Surelease in this layer could adjust the release delay and control the drug release rate. Optimized coated pellets in the simulated gastrointestinal pH 5h delayed release of drugs, after nearly constant release of drug, drug release completely within 16h. CONCLUSIONS: Matrine-controlled colon-targeted pellets with different time-lags can be prepared by adjusting the weight gain of time-controlled layer, the weight gain of swollen controlled release layer and the ratio of HPMC to Surelease in this layer. Drug-controlled delayed release drug-controlled pellets provide a reference.