解毒止泻微丸制备工艺考察

目的:将解毒止泻片开发成一种剂型(微丸)、二步释放(胃与结肠)的新制剂,考察其制备工艺和体外释放情况。方法:采用泛制法及包衣锅包衣技术分别制备胃溶微丸和结肠定位缓释微丸,通过单因素试验优选辅料和包衣工艺。运用HPLC测定槲皮素含量,流动相甲醇-0.4%磷酸溶液(53∶47),检测波长370 nm。结果:丸芯由药粉-羧甲基纤维素钠(8∶1)和95%乙醇为润湿剂泛制成丸。以3%铁红为包衣液,包衣增重4%制备胃溶微丸;以6%Eudragit L100-Eudragit S100(1∶2)混合物为包衣材料,包衣增重6%制备结肠缓释微丸。胃溶微丸在人工胃液内45 min内释放完全;结肠定位微丸在人工胃液中2 h不释放药物,在人工肠液3 h释放度20%,在人工结肠液5 h释放完全。结论:该制备工艺简单易行、重复性好,适用于解毒止泻微丸的工业化生产。

Investigation of Preparation Process of Jiedu Zhixie Pellets

Objective: To develop Jiedu Zhixie tablets into a new dosage form, which was stomach-colon two step and colon-targeted sustained release pellets.To investigate its preparation process and in vitro release. Method: Stomach-released and colon-targeted pellets were produced through roiling into ball method and pan coating technology, adjuvant materials and coating process were optimized by single factor tests.HPLC was adopted to determine the content of quercetin with mobile phase of methanol-0.4% phosphoric acid (53:47) and detection wavelength at 260 nm. Result: Mixed power of extract powder-carboxymethylcellulose sodium (8:1) was rolled into pellets with 95% alcohol as a wetting agent.Stomach-released pellets were prepared with increasing weight about 4% and 3% red iron as coating solution.Colon-targeted sustained release pellets were prepared with increasing weight about 6% and 6% combination solution of Eudragit L100-Eudragit S100 (1:2) as coating material.Stomach-released pellets released completely in artificial gastric fluid within 45 minutes.Colon-targeted sustained release pellets weren't released in artificial gastric fluid within 2 h, less than 20% were released in artificial intestinal fluid within 3 h, but pellets were slowly released in artificial colon fluid and released completely at 5 h. Conclusion: This preparation process is simple, reproducible and available for industrial production of Jiedu Zhixie pellets.