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目的制备pH依赖-时滞型大黄素结肠定位微丸并对影响其体外释药的包衣处方因素进行研究。方法采用离心造粒包衣机以粉末层积法制备载药微丸,并通过依次包衣时滞内层(Eudragit RL 30D)和pH依赖外层(Eudragit FS 30D)制备pH依赖-时滞型大黄素结肠定位微丸;以体外释放度为评价指标,采用相似因子(f2)法统计分析释药曲线,考察影响大黄素微丸体外释药的处方因素。结果最佳时滞层包衣液处方为:Eudragit RL 30D增重5%,HPMC用量60%,滑石粉用量50%,柠檬酸三乙酯用量15%;最佳pH依赖层包衣液处方为:Eudragit FS 30D增重4.6%,滑石粉用量50%,柠檬酸三乙酯用量5%。体外释放度实验表明,pH依赖-时滞型大黄素结肠定位微丸在人工胃液中2 h和人工肠液中3 h的累积释药率小于10%,人工结肠液7 h内基本释放完全,具有明显的结肠定位释药特性。结论通过调整时滞层及pH依赖层包衣厚度可以制备pH依赖-时滞型大黄素结肠定位微丸。
OBJECTIVE To prepare pH-dependent and time-lapsed emodin colon-targeting pellets and study the prescription factors that affect their in vitro drug release. Methods The drug-loaded pellets were prepared by powder layering method using a centrifugal granulation and coating machine and the pH-dependent-time-lag type was prepared by sequential coating of Eudragit RL 30D and Eudragit FS 30D Emodin colon-targeting pellets; in vitro release as the evaluation index, the similar factor (f2) method of statistical analysis of drug release curves to investigate the prescription factors affecting release of emodin pellets in vitro. Results The optimal lavaged coating solution was: Eudragit RL 30D 5% weight gain, HPMC dosage 60%, talc 50% and triethyl citrate 15%. The optimal pH-dependent coating solution was : Eudragit FS 30D gain 4.6%, talc 50%, triethyl citrate 5%. In vitro release experiments showed that the cumulative release rate of pH dependent-time-dependent emodin colon-targeting pellets in artificial gastric juice for 2 h and artificial intestinal fluid for 3 h was less than 10%, and that for artificial colon fluid was completely released in 7 h with Significant colonic release characteristics. Conclusion pH-dependent time-lapsed emodin colon-targeted pellets can be prepared by adjusting the thickness of the lag layer and pH-dependent coating.