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目的研究西尼地平在大鼠各肠段的药物动力学吸收特点。方法采用大鼠在体肠灌流实验装置,利用紫外-可见分光光度法和HPLC法分别测定酚红和西尼地平的含量。结果西尼地平在十二指肠、空肠、回肠、结肠的吸收速率分别为(2.05±0.013)、(1.95±0.010)、(1.96±0.005)、(1.82±0.005)h-1;药物质量浓度为5、10、15 mg·L-1时,在肠的吸收速率常数分别为(2.25±0.006 9)、(2.24±0.005 3)、(2.24±0.005 7)h-1;当pH值为6.4、7.2、7.9时,肠的吸收速率常数分别为(2.23±0.012 3)、(2.24±0.005 3)、(2.21±0.213 1)h-1。结论不同质量浓度的西尼地平在大鼠全肠道的吸收无显著差异,吸收机制为被动扩散;西尼地平在各肠段吸收较好。
Objective To study the pharmacodynamic characteristics of cilnidipine in various intestine of rats. Methods Rat intestine perfusion experiment apparatus was used to determine the content of phenol red and cilnidipine by UV-Vis spectrophotometry and HPLC respectively. Results The absorption rates of cilnidipine in the duodenum, jejunum, ileum and colon were (2.05 ± 0.013), (1.95 ± 0.010), (1.96 ± 0.005) and (1.82 ± 0.005) h- (2.25 ± 0.006 9), (2.24 ± 0.005 3) and (2.24 ± 0.005 7) h-1, respectively, for the intestinal mucosa of 5, 10 and 15 mg · L-1. The intestinal absorption rate constants were (2.23 ± 0.012 3), (2.24 ± 0.005 3) and (2.21 ± 0.213 1) h-1, respectively. Conclusion There is no significant difference in the total intestinal absorption of cilnidipine with different concentrations, and the absorption mechanism is passive diffusion. Sinidipine is better absorbed in the whole intestine.