摘要
目的:研究他克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,主要从大鼠不同肠段吸收部位、他克莫司不同浓度、递质不同pH等3方面对他克莫司的肠段吸收特性进行研究。结果:他克莫司在十二指肠、空肠、回肠、结肠的吸收速率常数(Ka)分别为0.1389,0.1415,0.1375,0.0347h-1;在质量浓度为10,20,30mg.L-1时,Ka分别为0.2453,0.2540,0.2361h-1;在递质pH5.4,6.8,7.8时,Ka分别为0.2620,0.2541,0.2473h-1。结论:他克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;在十二指肠、空肠和回肠的吸收较好,而在结肠部位的吸收较差。
OBJECTIVE To investigate the absorption kinetics of tacrolimus in rats＇ different intestines segments. METHODS The intestine in rats was cannulated for in situ perfusion. The effects of absorption site, drug concentration and pH value on taerolimus absorption ability were studied. RESULTS The absorption rate constants （Ka） of tacrolimus at duodenum, jejunum, ileum and colon were 0. 138 9, 0. 14l 5, 0. 137 5 and 0. 034 7 h^-1 , respectively. The concentration of 10, 20 and 30μg·mL^-1 from the whole intestine, Ka were 0. 245 3, 0. 254 0 and 0. 236 1 h^-1, respectively. Ka at pH of 5.4, 6. 8, 7. 8 from the whole intestine were 0. 262 0, 0. 254 1 and 0. 247 3 h^-1, respectively. CONCLUSION The absorption of tacrolimus assumed a first-order kinetics with the passive diffusion absorption mechanism. Concentration and pH of the drug solution had no effect on the absorption kinetics. The absorption of tacrolimus was better in duodenum, jejunum and ileum than in colon.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2010年第8期639-642,共4页
Chinese Journal of Hospital Pharmacy
基金
福建省科技计划项目(编号:2008Y0058)
关键词
他克莫司
大鼠
吸收动力学
在体肠吸收
tacrolimus
rat
absorption kinetics
in situ intestine absorption
