克拉霉素颗粒的掩味工艺及效果评价

Taste Masking Technology and Effect Evaluation of Clarithromycin Granules

该研究联合应用湿法制粒及流化床顶喷包衣工艺制备了克拉霉素掩味颗粒。通过扫描电镜、红外光谱、X射线粉末衍射技术对掩味颗粒和共沉淀法制备的克拉霉素-Eudragit EPO固体分散体进行物理表征。结果表明,掩味颗粒外观圆整,其中的克拉霉素晶型未发生变化。此外,考察了不同包衣增重的掩味颗粒和固体分散体在不同pH介质中的溶出行为。结果显示,包衣增重达到18%的颗粒在水中几乎不溶出,但在pH 1.2介质中15 min即完全溶出。最后,通过电子舌试验、动物偏好试验和人体感官试验,对掩味颗粒和固体分散体进行口感测评。结果显示,掩味颗粒较好地掩盖了药物苦味,而固体分散体的掩味效果较差。

Clarithromycin taste-masking granules were prepared by wet granulation and top-spray fluidized bed coating.The taste-masking granules and clarithromycin-Eudragit EPO solid dispersion prepared by co-precipitation were physically characterized by scanning electron microscopy,infrared spectroscopy,and X-ray powder diffraction.The results showed that the taste-masking granules had a rounded appearance,and the crystal form of clarithromycin in tastemasking granules had not changed.Furthermore,the taste-masking granules with different coating weights and solid dispersions in various pH media were investigated.The taste-masking granules with a coating weight gain of 18%were hardly dissolved in water but dissolved completely in a pH 1.2 medium within 15 min.Finally,electronic tongue,animal preference,and human sensory tests were applied to evaluate the taste masking effect.The results showed that the tastemasking granules well masked the bitter taste of clarithromycin,while masking effect of the solid dispersion was poor.