单向灌流法研究阿奇霉素泡囊的大鼠在体肠吸收

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0.2 mL/min以及灌流时间为1 h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（K_a）及有效渗透率（P_eff）。结果 阿奇霉素泡囊在十二指肠、空肠、回肠以及结肠的K_a和P_eff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。

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

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 (K_a) and the intestinal apparent permeation coefficients(P_eff) were calculated. Results The absorption K_a 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 P_eff 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 K_a and P_eff (P<0.05). Conclusion AM-NS can significantly improve the absorption of azithromycin in the intestine of rats.