论文部分内容阅读
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。
Objective To study the plasma pharmacokinetics of drugs in rats after the administration of N- (4-bromobenzyl) -N- (4-bromobenzyloxy) urea (BBU) and provide a reference for the development of new drugs. Methods A single dose of 600 mg · kg -1 N- (4-bromobenzyl) -N- (4-bromobenzyloxy) urea was administered orally. The content of N- Yl) -N- (4-bromobenzyloxy) urea. Results After intragastric administration of 600 mg · kg -1 N- (4-bromobenzyl) -N- (4-bromobenzyloxy) urea in rats, N- (4-bromobenzyl) The AUC0-t and AUC0-∞ of (4-bromobenzyloxy) urea were 110.55 and 122.79 mg.hL-1, respectively; the average values of t1 / 2z and tmax were 3.71 and 3.67 h, respectively, and the pmax was 17.49 mg.L- ; CLz / F for N- (4-bromobenzyl) -N- (4-bromobenzyloxy) urea was 4.97 Lh-1.kg-1 and Vz / F was 26.10 L.kg-1 for MRT0-∞ 6.71 h. Conclusion The fitting parameters of N- (4-bromobenzyl) -N- (4-bromobenzyloxy) urea one-compartment model and two-compartment model are very close to each other, and both models can be selected. .