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单向灌流法研究阿奇霉素泡囊的大鼠在体肠吸收
钟萌1,杨林2,杨梅1,胡雪原1,张景勍1*
0
(1. 重庆医科大学药物高校工程研究中心, 重庆 400016;
2. 重庆市食品药品检验所, 重庆 401121
*通信作者)
摘要:
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(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KaPeff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。
关键词:  肠吸收  阿奇霉素  泡囊  单向灌流法
DOI:10.3724/SP.J.1008.2014.00419
投稿时间:2013-10-20修订日期:2013-11-22
基金项目:教育部博士点基金(20095503120008).
Single-pass intestinal perfusion for studying intestinal absorption of azithromycin niosomes in rats
ZHONG Meng1,YANG Lin2,YANG Mei1,HU Xue-yuan1,ZHANG Jing-qing1*
(1. Medicine Engineering Research Center, Chongqing Medical University, Chongqing 400016, China;
2. Chongqing Institute for Food and Drug Control, Chongqing 401121, China
*Corresponding author.)
Abstract:
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.
Key words:  intestinal absorption  azithromycin  niosomes  single-pass intestinal perfusion