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目的 分别考察罗格列酮马来酸盐在大鼠各肠段 :空肠、回肠、结肠的吸收动力学特征及不同的药物浓度和pH值的影响。方法 应用大鼠在体肠吸收实验方法。结果 罗格列酮马来酸盐在空肠、回肠、结肠的吸收速率常数分别为 0 .0 46 8,0 .0 76 6 ,0 .10 45h-1;不同的药物浓度 :2 0 ,30 ,45 μg·mL-1在回肠的吸收速率常数分别为 0 .0 76 6 ,0 .0 714,0 .0 782h-1;不同的 pH值 :7.4,7.1,6 .8,6 .5时在回肠的吸收速率常数分别为 0 .0 76 6 ,0 .0 798,0 .0 86 8,0 .0 888h-1。结论 罗格列酮马来酸盐在肠道中下部吸收较好 ;药物浓度对吸收速率常数无影响 ;在 pH6 .5～ 7.4范围内 ,随药物溶液 pH值的减小 ,药物吸收速率常数逐渐增加 ,但不具有统计学意义 ;药物在肠道的吸收呈一级动力学过程 ,吸收机制为被动扩散。
Objective To investigate the effects of rosiglitazone maleate on the absorption kinetics of jejunum, ileum and colon in various intestine of rats and the effect of different drug concentration and pH value. Methods The rat intestinal absorption test method was applied. Results The absorption rates of rosiglitazone maleate in jejunum, ileum and colon were 0.046 8,0. 0 76 6 and 0 0 45 h -1, respectively. Different drug concentrations were 20,30, The absorption rates of 45 μg · mL-1 in the ileum were 0.076 6,0.714 and 0.0782 h-1, respectively. Different pH values were 7.4, 7.1, 6.0, The ileal absorption rate constants were 0.076 6, 0.0798, 0.086 8, 0.0888h-1, respectively. Conclusions The maleate of rosiglitazone is well absorbed in the middle and lower part of the intestine. The drug concentration has no effect on the rate constant of absorption. In the range of pH6.5 ~ 7.4, the drug absorption rate constant increases with the decrease of the pH of the drug solution , But not statistically significant. The absorption of drugs in the intestine showed a first-order kinetic process and the absorption mechanism was passive diffusion.