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目的:考察夏枯草有效部位结肠靶向片剂与普通片剂体内药物组织分布的不同,评价该制剂的结肠定位性。方法:选择大鼠为实验对象,分别给予夏枯草有效部位结肠定位片剂及普通片剂,不同时间点分批处死大鼠,HPLC法测定大鼠胃、小肠上段、小肠中段、小肠下段、盲肠及结肠内容物中迷迭香酸的浓度,即采用测定药物组织分布浓度的方法比较结肠定位片剂与普通片剂在大鼠胃肠道各段分布。结果:夏枯草有效部位结肠定位片组大鼠口服给药后在大鼠胃和近端小肠不释放,进入小肠后,肠溶衣膜逐渐溶解,4 h左右于大鼠远端小肠开始释放药物,4~6 h在盲肠和结肠内大量释药,结肠组织中迷迭香酸的Cmax是普通组的3.6倍。结论:夏枯草有效部位结肠定位片组迷迭香酸在大鼠结肠组织中具有较高的分布量,具有结肠定位给药系统的释药特点。
OBJECTIVE: To investigate the difference of the distribution of drug in colon-targeted tablets and ordinary tablets of Prunella vulgaris, and to evaluate the colon localization of the preparations. Methods: The rats were selected as the experimental subjects. Prickly-heat-place colon-specific tablets and common tablets were given respectively. The rats were sacrificed at different time points. The gastric, small intestine, middle small intestine, And the content of rosmarinic acid in the colon contents, that is, the method of determining the distribution density of the drug tissue was used to compare the distribution of the colonic locating tablet and the common tablet in the gastrointestinal tract of rats. Results: After the oral administration of Prunella colonic tablet group, the gastric and proximal small intestine of rats were not released. After entering the small intestine, the enteric coating gradually dissolved, and the drug began to release in the distal small intestine of rats about 4 h , 4 ~ 6 h in the cecum and colon a large number of drug release, colon tissue rosmarinic acid Cmax 3.6 times the normal group. CONCLUSION: Rosmarinic acid is effective component of colonic colonies of rosmarinic acid in rat colon tissue with a higher distribution, with colon-specific drug delivery system release characteristics.