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采用大鼠在体灌流法,以灌流液中剩余药物浓度为指标,考察普拉克索(1)在不同吸收部位的吸收动力学特征以及不同pH、不同药物浓度对1全肠段吸收的影响。结果显示,1在不同肠段的吸收速率常数(h-1)分别为:十二指肠0.295、结肠0.513、回肠0.480 h和空肠0.808 h。药物在大鼠全肠道内的吸收量随药物浓度的增大而升高,药物浓度和pH对吸收速率常数无显著性影响。1在肠道的吸收符合一级动力学特征,吸收机制为被动吸收。采用大鼠在体胃灌注法,以胃灌注液中药物前后浓度变化计算1在胃部吸收情况。结果表明1几乎不吸收。
Rat in vivo perfusion method, the remaining drug concentration in the perfusate as an indicator to investigate the absorption characteristics of pramipexole (1) in different absorption sites and different pH, different concentrations of drugs on the absorption of the whole bowel. The results showed that the absorption rate constant (h-1) of 1 in different intestine segments were 0.295 in the duodenum, 0.513 in the colon, 0.480 h in the ileum and 0.808 h in the jejunum, respectively. The absorption of drugs in the whole intestine of rats increased with the increase of the drug concentration. The drug concentration and pH had no significant effect on the absorption rate constant. 1 absorption in the intestine conforms to the first-order kinetic characteristics, and the absorption mechanism is passive absorption. Rats in vivo gastric perfusion method to gastric perfusion fluid concentration before and after the change in the calculation of a gastric absorption. The results show that 1 hardly absorbs.