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

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

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。

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.