摘要
目的:研究西罗莫司在大鼠各肠段的吸收动力学特征。方法:采用大鼠在体肠段灌流实验,以吸收速率常数(Ka)为指标,主要从大鼠不同肠段吸收部位、西罗莫司不同浓度、介质不同pH值等3方面对西罗莫司的肠吸收特性进行研究。结果:西罗莫司在十二指肠、空肠、回肠、结肠的Ka分别为0.197、0.158、0.122、0.083h-1;在浓度2、5、10、20μg·mL-1时Ka分别为0.246、0.187、0.215、0.232h-1;在介质pH值5.4、6.8、7.4时Ka分别为0.279、0.297、0.285h-1。结论:西罗莫司在大鼠肠道的吸收呈一级动力学过程,吸收机制为被动扩散;其在大鼠肠内的吸收不受药物浓度和pH影响;药物在十二指肠、空肠、回肠和结肠的吸收作用依次降低。
OBJECTIVE： To investigate the in situ absorption kinetics of sirolimus at different intestine segments in rats. METHODS： The intestine in rats was cannulated for in situ perfusion with absorption rate constant （Ka） as index. The effects of absorption site, drug concentration of sirolimus and pH value on sirolimus absorption ability were studied. RESULTS： The Ka of sirolimus at duodenum, jejunum, ileum and colon were 0.197, 0.158, 0.122 and 0.083 h 1, respectively. At the concentration of 2, 5, 10 and 20μg ·mL^-1 from the whole intestine, Ka were 0.246, 0.187, 0.215 and 0.232 h 1, respectively. Ka at pH of 5.4, 6.8, 7.4 from the whole intestine were 0.279, 0.297 and 0.285 h 1, respectively. CONCLUSIONS： The absorption of sirolimus assumed firstorder kinetics with the passive diffusion absorption mechanism. And concentration and pH of the drug solution had no effect on the absorption kinetics. The absorption at duodenum, jejunu, ileum and colon was degraded in order.
出处
《中国药房》
CAS
CSCD
北大核心
2009年第1期27-30,共4页
China Pharmacy
基金
福建省科技计划资助项目(2007Y0063)
关键词
西罗莫司
大鼠
在体肠吸收
吸收动力学
Sirolimus
Rat
In situ intestine absorption
Absorption kinetics
