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目的:研究华蟾酥毒基在大鼠胃、肠以及各肠段吸收动力学特征及吸收机制。为华蟾酥毒基的开发提供依据。方法:应用大鼠在体灌流技术,取低、中、高不同质量浓度(11,22,33 mg·L-1)华蟾酥毒基在大鼠胃、小肠中灌流3 h,以高效液相色谱法测定华蟾酥毒基的浓度,研究华蟾酥毒基大鼠胃肠道的吸收特征。结果:华蟾酥毒基低、中、高质量浓度在胃、小肠中灌流3 h均能较好的吸收,累积吸收量均为75%左右,且与药物的浓度无关,在小肠中的吸收表现出明显的一级动力学特征,3种浓度吸收速率常数分别为0.548,0.547,0.590 h-1;华蟾酥毒基在各肠段均能吸收,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 6,0.015 2,0.016 4,0.013 5 cm-1·h-1。结论:华蟾酥毒基在大鼠胃、全肠道均能吸收;吸收呈一级动力学过程,吸收机制为被动扩散。
OBJECTIVE: To study the absorption kinetics and mechanism of cinobufagin in rat stomach, intestine and intestine. To provide basis for the development of Chinese toad venom. Methods: Rat ventricular myocytes were perfused in rat stomach and small intestine for 3 h by using in vivo perfusion technique. The rat was treated with 11, 22, and 33 mg · L -1 of cinobufacini at different concentrations (11, 22 and 33 mg · L -1) The concentration of cinobufagin was determined by chromatography and the gastrointestinal absorption characteristics of cinobufagin-induced rats were studied. Results: The concentration of cinobufagin in the stomach and small intestine was better than that of the control group at low, middle and high concentrations for 3 h, and the cumulative absorption was about 75%. The absorption of cinobufagin in the small intestine was not related to the drug concentration A significant first-order kinetic characteristic was observed. The absorption constants of the three concentrations were 0.548, 0.547 and 0.590 h-1, respectively. The Chinese cinobufagin was absorbed in all intestine segments and showed a first-order kinetic model. The duodenum The absorption rate constants of jejunum, ileum and colon were 0.024 6,0.015 2,0.016 4,0.013 5 cm-1 · h-1. CONCLUSION: Cinobufagin can be absorbed in the stomach and intestine of rats. The absorption is in first-order kinetics and the absorption mechanism is passive diffusion.