pH-酶触型盐酸小檗碱结肠定位片大鼠体内的释药研究

Study on Release Characteristics of pH-and Enzyme-Controlled Tablets of Berberine Hydrochloride for Colon-Specific Delivery in Rats

目的：对pH-酶触型盐酸小檗碱结肠定位片在大鼠体内的释药特点进行研究。方法：将pH-酶触型盐酸小檗碱结肠定位片（Ф3mm）大鼠灌胃给药,在各时间点将大鼠处死,取出胃肠道,采用HPLC检测,内标法分别测得大鼠各段胃肠道内容物中盐酸小檗碱的含量,研究药物在胃肠道各部位内容物中含量的经时变化,评价其释药特性。结果：盐酸小檗碱在胃肠道内容物中的线性范围为0.1-20.0μg.mL-1,线性关系良好（r〉0.999）,定量限为0.1μg.mL-1;药物于6-14h在盲肠和结肠内具有较高的药物浓度。结论：pH-酶触型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 release characteristics of berberine hydrochloride colon-specific tablets in rats.Methods：The rats were administrated orally with the colon-specific tablets of diameter 3mm and killed at different time points.The gastrointestinal tracts were removed and disposed.The contents of berberine,in different segments of the gastrointestinal tract,were determined by HPLC respectively,using internal standard method.The changes of berberine in gastrointestinal contents were studied to evaluate the release characteristics of the tablet.Results：The linear range of berberine in different contents of the gastrointestinal tract was 0.1~20.0μg·mL-1,the standard curve was in good linearity（r0.999）.The detection limit of berberine was 0.1μg·mL-1.The drug was specifically released in caecum and colon and maintained at a higher concentration between 6~14h.Conclusion：The pH-and enzyme-controlled tablet of berberine hydrochloride is a carrier for targeting the colon.