蟾毒灵胃肠道吸收动力学研究  

Study on Kinetics of Gastrointestinal Absorption of Bufalin

作　　者：赵杰[1] 胡乃合[1] 战兵 林桂涛[1] 

机构地区：[1]山东中医药大学 [2]迪沙药业集团有限公司,山东威海264205

出　　处：《山东中医药大学学报》2015年第5期472-475,共4页Journal of Shandong University of Traditional Chinese Medicine

基　　金：济南市科技局高校自主创新项目(编号:JN100586)

摘　　要：目的 :研究蟾毒灵在大鼠胃、肠以及各肠段吸收动力学特征及吸收机制,为蟾毒灵的进一步开发提供依据。方法 :应用大鼠在体灌流技术,研究蟾毒灵大鼠胃肠道的吸收特征,以高效液相色谱法测定蟾毒灵的浓度。结果:蟾毒灵不同质量浓度(10.0,20.0,30.0μg·m L-1)在胃灌流3 h均能较好地吸收,累积吸收率均为90%左右,且与药物的浓度无关;在小肠全肠段的吸收表现为一级动力学特征,三种浓度吸收速率常数分别0.017,0.017,0.019/cm·h-1;蟾毒灵在各肠段均能吸收均呈一级动力学模式,十二指肠、空肠、回肠和结肠的吸收速率常数依次为0.024,0.027,0.022,0.021/cm·h-1。结论 :蟾毒灵在胃、全肠道及全肠各段均能吸收;吸收呈一级动力学模式,吸收机制为被动扩散。Objective：To explore the absorption kinetics and absorption mechanisms of bufalin in stomach , intestine and gastrointestine in rats,so as to provide a basis for the development of bufalin. Methods：The absorption kinetics of gastrointestine in rats were obtained by in situ perfusion method and the concentration was determined by HPLC method. Results：3 hours after perfusion,bufalin in different concentrations （10.0, 20.0,30.0μg·mL^-1）can be absorbed in the stomach and the cumulative uptake rate was around 90%. The absorption was not rated to the concentration of the drug. The absorption in the small intestine showed the first-order kinetics characteristics and the absorption rate constant of the three concentrations were 0.017 , 0.017 and 0.019/cm·h. Bufalin was absorbed at all segments of the intestine and it was a first-order pro-cess. The absorption rate constant in the duodenum,jejunum,ileum and colon were 0.024,0.027,0.022 and 0.021/cm·h^-1. Conclusion：Bufalin can be absorbed at stomach and all segments of intestine of rats. It was a first-order process with passive diffusion mechanism.

关 键 词：蟾毒灵 吸收动力学 高效液相色谱法 大鼠 

分 类 号：R283.6[医药卫生—中药学]