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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。
OBJECTIVE: To develop a detoxification and antidiarrheal tablet into a new formulation of a dosage form (pellets), two-step release (stomach and colon), investigate its preparation process and in vitro release. Methods: The gastric ulcer and colon-targeted sustained-release pellets were prepared by the pan-system method and the coating pan coating technique. The excipients and the coating process were optimized by the single factor test. The content of quercetin was determined by HPLC. The mobile phase consisted of methanol-0.4% phosphoric acid solution (53:47) and the detection wavelength was 370 nm. RESULTS: The pellets were pan-formed from powdered-sodium carboxymethylcellulose (8: 1) and 95% ethanol as wetting agents. The gastric juice pellets were prepared with 3% iron red as coating solution and 4% coating weight gain. The coating weight was 6% with 6% Eudragit L100-Eudragit S100 (1: 2) Release pellets. Gastrointestinal micro-pellets were completely released within 45 min in artificial gastric juice. Colon-targeted pellets did not release drugs in artificial gastric juice for 2 h, release rate was less than 20% at 3 h in artificial gastric juice and 5 h in artificial colon fluid. Conclusion: The preparation process is simple, reproducible, and suitable for industrial production of detoxification anti-diarrhea pellets.