pH依赖型黄连总生物碱结肠靶向微丸的制备及其体内外释放性能评价

目的:制备用于治疗溃疡性结肠炎的pH依赖型黄连总生物碱靶向微丸并对其体内外释放性能进行评价。方法:采用丙烯酸树脂(eudragit)S100和eudragit L100-55双层包衣制备pH依赖型黄连总生物碱结肠靶向微丸。以盐酸小檗碱为指标进行了体外释放度和大鼠体内释放的初步评价。结果:体外释放度试验表明盐酸小檗碱在人工胃液中2 h累计释放度<0.1%,在人工小肠液中4 h累计释放度<10%,在人工结肠液中3 h累计释放度>90%;体内试验表明在大鼠体内包衣微丸大部分能完整到达盲肠或结肠部,并在上述部位开始崩解释放。结论:pH依赖型黄连总生物碱靶向微丸能够实现结肠的定向释放。

Preparation of Total Alkaloids from Coptidis Rhizoma Colon Targeted Pellets and Evaluation of Its in vivo and in vitro Release Characteristics

Objective: To prepare pH-dependent total alkaloids from Coptidis Rhizoma colon targeted pellets for treatment of ulcerative colitis and finish its in vitro and in vivo release performance evaluation. Method: Acrylic resin S100(eudragit S100) and eudragit L100-55 double-coated was adopted to prepare colon targeted pellets of total alkaloids from Coptidis Rhizoma.In vitro release and in vivo site-specific drug release of this preparation were evaluated with berberine hydrochloride as index. Result: In vitro release test showed that cumulative release rate of berberine hydrochloride was less than 0.1% in artificial gastric juice after 2 h and less than 10% in artificial intestinal fluid after 4 h,but cumulative release rate in artificial colon juice after 3 h was more than 90%.In vivo test showed that coated pellets could complete arrive to the cecum or colon in rats,and began to disintegrate and release. Conclusion: Colon targeted pellets of total alkaloids from Coptidis Rhizoma can achieve targeted release in the colon.