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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 study the absorption kinetics of tacrolimus in various intestine of rats. Methods: The intestine absorption characteristics of tacrolimus in rats were studied by perfusion experiments in the intestine of rats, mainly from the different parts of the intestine, the different concentrations of tacrolimus and the different pH of the transmitter. Results: The absorption rate constants (Ka) of tacrolimus in the duodenum, jejunum, ileum and colon were 0.1389, 0.1415, 0.1375 and 0.0347 h-1 respectively. At the concentrations of 10, 20 and 30 mg.L- , Ka were 0.2453, 0.2540 and 0.2361 h-1, respectively. At pH 5.4, 6.8 and 7.8, Ka were 0.2620, 0.2541 and 0.2473 h-1, respectively. Conclusion: The absorption of tacrolimus in the intestinal tract of rats shows a first-order kinetic process with passive absorption mechanism. Its absorption in the rat intestine is not affected by the drug concentration and pH. In the duodenum, jejunum and jejunum Ileal absorption is better, while in the colon absorption is poor.