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目的:研究复方盐酸小檗碱结肠定位片在大鼠体内的释药行为,评价其结肠定位释药特性。方法:分别将复方盐酸小檗碱结肠定位片(Ф=3 mm)和盐酸小檗碱混悬液大鼠灌胃给药,以巴马汀为内标,采用HPLC分别测定大鼠血浆和各段胃肠道组织中盐酸小檗碱的含量,分析22 h内各时间点药物在胃肠道组织中的分布和血浆药物浓度,计算药物的相对靶向释药指数(DDI)。结果:盐酸小檗碱在血浆和胃肠道组织中的线性范围分别为0.02～0.40 mg.L-1(r>0.998)和0.05～10.0mg.L-1(r>0.999);复方结肠定位片组药物释放行为具有明显的时滞,药物主要分布于大鼠盲肠和结肠组织,结肠组织的Cmax和AUC0-22 h分别为混悬液组的3.1,3.6倍,大鼠胃、近端小肠、远端小肠、盲肠和结肠组织的DDI值依次为0.00,0.23,1.17,2.36,8.55。结论:复方盐酸小檗碱结肠定位片具有较好的结肠定位释药特性。
OBJECTIVE: To study the drug release of compound Berberine colon-specific tablet in rats and to evaluate its colon-specific drug release. Methods: Berberine hydrochloride colon tablet (Ф = 3 mm) and berberine hydrochloride suspension were intragastrically administered to rats. Palmatine was used as an internal standard. The contents of The content of berberine hydrochloride in the gastrointestinal tract was analyzed. The distribution of drug in the gastrointestinal tract and plasma drug concentration at each time point were analyzed within 22 h, and the relative target release index (DDI) of the drug was calculated. Results: The linear ranges of berberine hydrochloride in plasma and gastrointestinal tract were 0.02-0.40 mg.L-1 (r> 0.998) and 0.05-10.0 mg.L-1 (r> 0.999) The drug release behavior of the tablet group had obvious time lag. The drugs mainly distributed in the cecal and colon tissues of rats. The Cmax and AUC0-22 h of the colon tissue were 3.1 and 3.6 times of those in the suspension group respectively. The gastric and proximal small intestine The DDI values of distal small intestine, cecum and colon were 0.00,0.23,1.17,2.36,8.55. Conclusion: The compound berberine hydrochloride colon positioning tablet has good colonic release characteristics.