Senius K E, Fendrich Z, Hradil J
Arzneimittelforschung. 1981;31(12):2092-5.
Absorption kinetics of 14C-labelled N-(3-chloro-o-tolyl)-anthranilic acid (tolfenamic acid, 14C-TA, Clotam) from the small intestine was studied in intact rats and in rats with malabsorption states provoked by methotrexate, starvation, and triparanol. 14C-TA was administered intravenously and intraduodenally, and the drug concentrations in the blood were followed up radiometrically. A multi-compartmental model was applied for mathematical analysis. Theoretical model parameters were computed, and absorption parameters were then derived from the theoretical ones. The absorption half-life of 14C-TA was 5.3 min in the controls, 10.8 min in the methotrexate-intoxicated, 7.5 min in the fasted, and 5.3 min in the triparanol-intoxicated rats. The absorbed fraction of the intraduodenal 14C-TA dose was 100% in each experimental group as well as in the controls. It is suggested that the slower transfer of 14C-TA through the intestinal barrier in the methotrexate-intoxicated and fasted rats may be caused by the reduction of the absorptive surface.
在完整大鼠以及由甲氨蝶呤、饥饿和三苯乙醇胺引发吸收不良状态的大鼠中，研究了14C标记的N-(3-氯-邻甲苯基)-邻氨基苯甲酸（托芬那酸，14C-TA，氯胺）从小肠的吸收动力学。静脉内和十二指肠内给予14C-TA，并通过放射性测定法跟踪血液中的药物浓度。应用多室模型进行数学分析。计算理论模型参数，然后从理论参数推导出吸收参数。14C-TA的吸收半衰期在对照组中为5.3分钟，在甲氨蝶呤中毒组中为10.8分钟，在禁食组中为7.5分钟，在三苯乙醇胺中毒组中为5.3分钟。在每个实验组以及对照组中，十二指肠内给予的14C-TA剂量的吸收分数均为100%。提示在甲氨蝶呤中毒和禁食的大鼠中，14C-TA通过肠屏障的转运较慢可能是由于吸收表面减少所致。
