N-(4-溴苄基)-N-(4-溴苄氧基)脲在大鼠体内的药动学研究  

Pharmacokinetics of N-(4-bromobenzyl)-N-(4-bromobenzyloxy)urea in Rats

作　　者：童伟[1,2] 麦曦[1] 冯丽华[1] 向婧[1] 孙文[1] 

机构地区：[1]南昌大学药学系,南昌330006 [2]南昌市第一医院,南昌330008

出　　处：《中国药学杂志》2012年第21期1746-1749,共4页Chinese Pharmaceutical Journal

基　　金：国家"重大新药创制"科技重大专项课题(2009ZX09103-087)

摘　　要：目的研究N-(4-溴苄基)-N-(4-溴苄氧基)脲(BBU)给药后药物在大鼠体内的血浆药动学特征,为新药开发提供参考依据。方法单剂量600 mg.kg-1N-(4-溴苄基)-N-(4-溴苄氧基)脲口服给药,应用高效液相色谱法测定大鼠体内N-(4-溴苄基)-N-(4-溴苄氧基)脲的浓度。结果大鼠灌胃给予600 mg.kg-1N-(4-溴苄基)-N-(4-溴苄氧基)脲后,大鼠血浆中N-(4-溴苄基)-N-(4-溴苄氧基)脲的AUC0-t和AUC0-∞分别为110.55和122.79 mg.h.L-1;t1/2z和tmax平均值分别为3.71和3.67h,ρmax为17.49 mg.L-1;N-(4-溴苄基)-N-(4-溴苄氧基)脲的CLz/F为4.97 L.h-1.kg-1,Vz/F为26.10 L.kg-1,MRT0-∞为6.71 h。结论 N-(4-溴苄基)-N-(4-溴苄氧基)脲一室模型和二室模型拟合效果参数非常接近,两种模型都可选择,但以二室模型为好。ABSTRACT ： OBJECTIVE To characterize the pharmacokinetics of N- （ 4-bromobenzyl ） -N- （ 4-bromobenzyloxy ） urea （ BBU ） in rats after oral administration, thus to provide reference for its development. METHODS A single dose of 600 mg · kg - 1 of BBU was orally administered to rats. The concentration of free BBU in rat plasma was determined by HPLC. RESULTS The AUC0_, and AUC0-∞ were 110. 55 and 122.79 mg· L · h-1 , t1/2z and tmax were 3.71 and 3.67 h, Pmax was 17. 49 mg ·L-1 , CLz/F and Vz/F were 4.97 L · h-1 · kg-1 and 26. 10 L · kg-1 , and MRT0-∞ was 6. 71 h for free BBU. CONCLUSION The fitting goodness is between one-compartment model and two-compartment model. Both models can be chosen, but two-compartment model is better. KEY WORDS ： N- （4-bromobenzyl） -N- （4-bromobenzyloxy） urea ; HPLC ; rat ; pharmaeokinetics

关 键 词：N-(4-溴苄基)-N-(4-溴苄氧基)脲 高效液相色谱法 大鼠 药动学 

分 类 号：I1969.1[文学—世界文学]