半夏泻心结肠靶向片的制备及其体外释放行为

目的制备半夏泻心结肠靶向片,并考察其体外释放行为。方法以粉碎度、乙醇体积分数、乙醇用量、渗漉速度为影响因素,黄芩苷、盐酸小檗碱含有量为评价指标,正交试验优化提取工艺。制备包衣片后,小杯法测定黄芩苷、盐酸小檗碱体外释放度,筛选包衣处方。结果最佳提取工艺为粉碎度粗粉,乙醇体积分数70%,乙醇用量10倍,渗漉速度2~3 mL/(min·kg),黄芩苷、盐酸小檗碱含有量分别为14.687 4%、6.993 0%;最佳包衣处方为4.4%Eudragit S100,0.6%邻苯二甲酸二乙酯,1%滑石粉,包衣增重8%。结肠靶向片在0.1 mol/L HCl(2 h)、磷酸盐缓冲液(pH 6.8,4 h)中累积释放度小于5%,而在磷酸盐缓冲液(pH 7.8~8.0,1 h)中达到85%以上。结论半夏泻心结肠靶向片可实现结肠定位释药的目的。

Preparation and in vitro release behaviors of Banxia Xiexin colon-targeted tablets

AIM To prepare Banxia Xiexin colon-targeted tablets and to investigate the in vitro release behaviors. METHODS With comminution degree, ethanol concentration, ethanol consumption and diacolation speed as influencing factors, baicalin and berberine hydrochloride contents as evaluation indices, the extraction process was optimized by orthogonal test. The coated tablets were prepared, after which small glass method was adopted in the in vitro release rate determination of baicalin and berberine hydrochloride, and the coating formulation was screened. RESULTS The optimal extraction process was determined to be coarse powder for comminution degree, 70% for ethanol concentration, 10 times for ethanol consumption, and 2-3 mL/(min·kg) for diacolation speed, the baicalin and berberine hydrochloride contents were 14.687 4% and 6.993 0%, respectively. The optimal coating formulation was determined to be 4.4% Eudragit S100, 0.6% diethyl phthalate, 1% talcum powder, and 8% for coating weight gain. The accumulative release rates of colon-targeted tablets were less than 5% in 0.1 mol/L HCl(2 h) and phosphate buffer(pH 6.8, 4 h), which reached more than 85% in phosphate buffer(pH 7.8-8.0, 1 h).CONCLUSION Banxia Xiexin colon-targeted tablets can achieve the aim of colon-specific drug release.