摘要
目的:研究东莨菪素在大鼠胃、小肠的吸收特性。方法:采用大鼠在体胃、小肠吸收实验模型,以高效液相色谱法测定灌注液中药物的浓度,紫外分光光度法测定酚红的浓度。结果:东莨菪素在大鼠胃中2 h的吸收百分率为76.31%;东莨菪素在结肠、十二指肠、回肠、空肠的吸收率分别为46.25%,40.54%,38.21%,32.77%;不同质量浓度东莨菪素(10.014 4,20.028 8,40.057 6 mg.L-1在小肠的吸收速率常数分别为0.643 4,0.613 7,0.597 0h-1;不同pH(6.0,6.8,7.4)在小肠的吸收速率常数分别为0.621 7,0.603 3,0.613 7 h-1。结论:不同质量浓度、pH对东莨菪素在大鼠全肠道的吸收没有显著性影响,药物的吸收呈一级动力学过程,吸收机制主要为被动扩散;东莨菪素在胃肠道均有较好的吸收,结肠为最佳吸收部位,提示适宜制成缓控释制剂。
Objective: To study absorption kinetics of scopoletin in rat stomachs and intestines. Method: Rats was cannulated for in situ recirculation. UV and HPLC methods were used to determine the concentrations of phenolsulfonphthalein and scopoletin, respectively. Result: The absorption rates in rat stomachs at 2 h after administration was 76. 31% ; The absorption rates at colon, duodenum, ileum and jejunum were 46. 25%, 40. 54%, 38.21%, 32.77%, respectively. The absorption rate constant (Ka) at concentrations of 10. 014 4, 20. 028 8-40. 057 6 mg · L^-1 in intestine were 0. 643 4, 0. 613 7, 0. 597 0 h^-1 , respectively. The Ka of seopoletin at pH of 6. 0, 6. 8 and 7.4 in intestine were 0.621 7,0. 603 3,0.613 7 h ^- 1, respectively. Conclusion: The concentrations and pH values of scopoletin solution had no distinctive effect on the absorption kinetics. The absorption of scopoletin was a first-order process with passive diffusion mechanism. Scopoletin was well absorbed at stomachs and intestines in rats. Colon was the best absorption site of scopoletin, which suggest that a sustained-release preparation should be suitable for this compound.
出处
《中国中药杂志》
CAS
CSCD
北大核心
2008年第15期1890-1894,共5页
China Journal of Chinese Materia Medica
基金
分子医学生物技术江苏省重点实验室开放基金项目(164070304301)
江苏省“青蓝工程”学术带头人项目
关键词
东莨菪素
在体胃肠吸收
高效液相色谱法
scopoletin
in situ absorption from stomach and intestine
HPLC