复方盐酸小檗碱结肠定位片在大鼠体内的释药行为研究

Study on Release Characteristics of Compound Berberine Hydrochloride Colon Specific Tablets in Rats

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 evaluate the release characteristics of compound berberine hydrochloride colon specific tablets in rats.Method：The rats were administrated orally with the colon-specific tablets of diameter 3 mm and berberine hydrochloride（BH） suspension respectively.After administration,the rat＇s plasma and gastrointestinal tissues were collected at different time points within 22 h.The berberine in biosamples was determined by HPLC,using palmatine as internal standard.Drug delivery index（DDI） was calculated.Result：BH in plasma and gastrointestinal tissues showed good linear relationship in the range of 0.02-0.40 mg · L-1（r0.998） and 0.05-10.0 mg · L-1（r0.999） respectively.The release of BH in tablets mainly distributed in rat＇s caecum and colon and showed an obvious lag time.The value of Cmaxand AUC0-22 h in rat＇s colon were 3.1 times and 3.6 times of BH suspension group respectively.The DDI of the tablets was 0.00,0.23,1.17,2.36,8.55 in the rats＇ gastric,proximal and distal small intestinal,caecal,colonic tissue,respectively.Conclusion：The compound berberine hydrochloride tablet is a carrier for targeting the drug to the colon.