3~H-N-正丁基-苯甲酰-2-磺酰内亚胺在小鼠体内的吸收和分布

The Study on Absorption and Distribution of N-n-Butyl-Benzoyl-2-Sulphimide in Mice

静脉注射正丁基-苯甲酰-2-磺酰内亚胺在小鼠体内的血药过程符合三房室开放模型.表观分布容积 Vd=1.43L/kg,半衰期分别为 T_(2/1)(1)=1.46×10^(-2)h,T_(2/1)(2)=0.433h,T_(2/1)(3)=11.3h,清除速率常数 k_(10)=0.69,口服给药小鼠体内血药浓度过程符合二房室开放模型,口服吸收迅速达峰时间 T_(max)=0.36h。半衰期分别为T_(1/2)(1)=0.235h,T_(1/2)(2)=0.129h,T_(1/2)(3)=11.29h.正丁基-苯甲酰-2-磺酰内亚胺在小鼠体内有广泛的分布但无特异性组织积累.正丁基-苯甲酰-2-磺酰内亚胺口服吸收较少,生物利用度仅为11%.

A study on absorption and distribution of N-n-butyl-benzoyl-2-sulphimide in mice is reported.After intra- venous injection of ~3H-N-n-butyl-benzoyl-2-sulphimide to mice,the blood drug concentration-time curve was shown to fit a three compartment model with the following pharmacokinetic parameters:T1/2(1)=1.48×10^(-2) h.T1/2(2)=0.443h,T1/2(3)=11.3h,Vd=1.4L/kg.~3H-N-n-butyl-benzoyl-2-sulphimide is distributed widely in tissues without specific accumulation.After oral administation of ~3H-N-n-hutyl-benzoyl-2-sulphimide, the blood drug concentration reached its maximum level in 0.37h,the drug concentrattion-time curve was shown to fit a two compartment modal,the distribution of ~3H-N-n-butyl-benzoyl-2-sulphimide in tissues was similar to that of intravenous injection with the bioavailability of 11%.