Nagwekar J B, Kundu S
J Pharm Sci. 1982 Apr;71(4):422-6. doi: 10.1002/jps.2600710412.
The pharmacokinetics of sulfisoxazole and sulfanilamide were studied in control rats and in rats treated for 5 days with a daily 100 mg/kg ip dose of phenobarbital. These drugs represent the organic anionic and nonionized drugs, respectively, whose nonmicrosomal enzymatic metabolisms were unstimulated by phenobarbital. Sulfisoxazole showed the characteristics of a two-compartment open model. However, its biological half-life and the apparent distribution volume of the central compartment were significantly lower and the intercompartmental transport rate constants and the urinary excretion rate constant were significantly greater, in phenobarbital treated rats than in control rats. The apparent steady-state distribution volume of sulfisoxazole was smaller in the phenobarbital treated rats at the 90% confidence level. Sulfanilamide showed characteristics of a one-compartment model in both the control and phenobarbital treated rats, but none of the pharmacokinetic parameters of the compound in the phenobarbital treated rats were significantly different from those in the control rats.
在对照大鼠以及用苯巴比妥以每日100mg/kg腹腔注射剂量处理5天的大鼠中研究了磺胺异恶唑和磺胺的药代动力学。这些药物分别代表有机阴离子药物和非离子化药物，其非微粒体酶代谢不受苯巴比妥刺激。磺胺异恶唑呈现双室开放模型的特征。然而，在苯巴比妥处理的大鼠中，其生物半衰期和中央室的表观分布容积显著更低，而室间转运速率常数和尿排泄速率常数显著更高，与对照大鼠相比。在90%置信水平下，苯巴比妥处理的大鼠中磺胺异恶唑的表观稳态分布容积更小。磺胺在对照大鼠和苯巴比妥处理的大鼠中均呈现一室模型的特征，但苯巴比妥处理的大鼠中该化合物的药代动力学参数与对照大鼠相比均无显著差异。
