甲硝唑大鼠肠吸收实验研究  

Intestinal absorption of metronidazole in rats: an in-vitro study

作　　者：郝正华[1] 张丽锋[2] 王锐利[2] 张淑秋[2] 

机构地区：[1]山西医科大学第二医院药剂科,太原030001 [2]山西医科大学药学院

出　　处：《中国药物与临床》2007年第11期822-824,共3页Chinese Remedies & Clinics

基　　金：山西省归国人员基金资助项目(2005029);山西医科大学第二医院青年基金资助项目(20070101)

摘　　要：目的考察甲硝唑在大鼠不同肠段的吸收动力学特征、吸收部位及吸收机制,为其结肠定位缓控释制剂的设计提供理论依据。方法采用大鼠在体灌流肠吸收实验,考察了甲硝唑的吸收部位和吸收动力学特征。结果甲硝唑在大鼠肠道内无特定吸收部位,各肠段吸收速率常数按十二指肠、空肠、结肠、回肠顺序依次上升,吸收速率常数分别为0.078、0.136、0.155、0.168/h。在2～20μg/ml的浓度范围内,甲硝唑的吸收量与浓度有良好的线性关系。结论甲硝唑在大鼠全肠段均有吸收,吸收符合一级动力学特征,吸收机制为被动扩散,适于制备结肠定位缓控释制剂。Objective To identify the characteristics, sites and mechanisms for metronidazole absorption by various intestinal segments in rats, in order to devise the colon-specific sustained/controlled release preparations. Methotis In-situ recirculation perfusion was used to study the absorption mechanism and sites of metronidazole in rats. Results Absorption of Metronidazole was not site-specific in rat intestines. The absorption rate constants were 0.078, 0.136, 0.155, 0.168 h^-1 at duodenum, jejunum, ileum and colon, respectively. Within the range of 2-20 μg/mL, there was a good linear correlation between absorption amount and concentration. Conclusion Metronidazole appeared absorbable in all segments of rat intestine. The absorption showed characteristics of first-order kinetics and was consistent with passive transportation. These findings indicated that Metronidazole can be formulated and prepared as colonspecific sustained/controlled release preparations.

关 键 词：甲硝唑 肠吸收 高效液相色谱 

分 类 号：R96[医药卫生—药理学]