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目的研究尼美舒利的大鼠肠吸收动力学特征。方法运用大鼠在体单向灌流法进行肠吸收实验,收集灌流流出液,测定其质量,采用HPLC法测定灌流液中尼美舒利的含量,利用重量法计算动力学参数。结果灌流速度对药物吸收速率常数(K_a)和表观吸收系数(P_(app))影响显著(P<0.05);一定范围内的药物浓度和pH值对K_a和P_(app)无显著影响(P>0.05);药物在全肠道吸收较好,十二指肠、空肠、回肠和结肠的K_a值分别为(0.070±s 0.003)、(0.067±0.008)、(0.074±0.006)和(0.058 0±0.002 0)·min~(-1)。结论尼美舒利在大鼠肠道的吸收呈现一级动力学特征,且吸收机制为被动扩散。尼美舒利在整个肠道均有吸收。
Objective To study the intestinal absorption kinetics of nimesulide in rats. Methods The intestine absorption test was performed in rats by the one-way perfusion method. The perfusate effluent was collected and its quality was determined. The content of nimesulide in the perfusate was determined by HPLC, and the kinetic parameters were calculated by gravimetric method. Results The perfusion rate had significant effects on the rate of absorption (K_a) and apparent absorption coefficient (P_ (app)) (P <0.05). The drug concentration and pH value within a certain range had no significant effect on K_a and P_ (app) (0.070 ± 0.008), (0.074 ± 0.006), (0.058 ± 0.006) and (0.058 ± 0.006), respectively. The K_a values in the duodenum, jejunum, ileum and colon were (0.070 ± 0.003) 0 ± 0.002 0) · min ~ (-1). Conclusion The absorption of nimesulide in rat intestine shows first-order kinetic characteristics and the absorption mechanism is passive diffusion. Nimesulide is absorbed throughout the gut.