单向灌流法研究阿奇霉素泡囊的大鼠在体肠吸收

Single-pass intestinal perfusion for studying intestinal absorption of azithromycin niosomes in rats

目的研究阿奇霉素泡囊的大鼠在体肠吸收性质。方法选择健康SD雄性大鼠6只,分为2组,运用单向灌流模型考察大鼠的十二指肠、空肠、回肠以及结肠在灌流速度为0.2mL/min以及灌流时间为1h条件下的药物吸收情况。采用HPLC法对药物的质量浓度进行检测,并计算其吸收速率常数(Ka)及有效渗透率(Peff)。结果阿奇霉素泡囊在十二指肠、空肠、回肠以及结肠的Ka和Peff分别是阿奇霉素的2.41、2.35、2.54、2.95倍和2.34、1.47、2.20、1.40倍,差异均有统计学意义(P<0.05)。结论阿奇霉素泡囊能明显改善药物在体肠吸收。

Objective To study the role of azithromycin niosomes （AM-NS） in promoting the intestinal absorption of AM in rats. Methods Six healthy male rates were randomly divided into two groups. Single-pass intestinal perfusion was employed to investigate the intestinal absorption of the duodenum, jejunum, ileum and colon when the perfusion rate was 0.2 mL/min and period was 1 h. The concentrations of the drugs were determined by HPLC; the drug absorption rate constant （Ka） and the intestinal apparent permeation coefficients（Peff） were calculated. Results The absorption Ka of AM-NS in the duodenum, jejunum, ileum and colon were 2.41, 2.35, 2.54 and 2.95 folds that of the free AM, and the Peff were 2.34, 1.47, 2.20, and 1.40 folds that of the free AM, respectively, with significant differences found between the two groups for both Ka and Peff （P〈0. 05）. Conclusion AM-NS can significantly improve the absorption of azithromycin in the intestine of rats.