【作者】 郑玲利； 张志荣； 袁芳； 黄园；

【Author】 Zheng Ling-li, Zhang Zhi-rong, Yuan Fang, Huang Yuan* (West China School of pharmacy, Sichuan University, Chengdu 610041, P.R. China )

【机构】 四川大学华西药学院；

【摘要】 目的研制具有良好粘附性能和pH依赖性的盐酸黄连素生物粘附包衣小片。方法采用正交设计方法,确定生物粘附材料羟丙甲纤维素、卡波姆的用量及配比与制剂体外释放度及粘附力的关系。并对释放度进行释药动力学模拟,根据各模型拟合的AIC值、计算值与实测值的相对误差来研究其释药规律。根据Peppas方程特征参数判断其释药机制。结果羟丙甲纤维素与卡波姆对阻滞药物的释放及粘附力影响较大,且卡波姆的效果强于羟丙甲纤维素。生物粘附小片以Hixson-Crowell方程拟合最佳,药物释放机制为非Fick扩散。结论盐酸黄连素生物粘附小片具有良好的粘附性能和pH依赖性。更多还原

【Abstract】 Objective To prepare Berberine chloride coated bioadhesive micro-tablet with good bioadhesive and pH-sensitive. Method Orthogonal design is used to determine the relation of the amount as well as proportion of hydroxypropyl methylcellulose and Carbopol with in vitro release and adhesive force of the tablets. AIC and the biggest relative error between calculated results and experiment data were used as comprehesive indices to select the best imitating model. And the release mechanism is determined according to the parameters of Peppas equation. Results Hydroxypropyl methylcellulose and Carbopol have great influence on the retardarce of drug release and the adhesive force, and Carbopol has relatively greater effect. The release rate in vitro imitated in Hixson-Crowell equation was the best. The release mechanism is proved to be non-Fickian diffusion. Conclusion Berberine chloride bioadhesive tablet has sound adhesive and pH dependent ability.更多还原