三苯双脒代谢物氨脒和乙酰氨脒人体药代动力学研究  

Pharmacokinetic study of dADT and acetylizad dADT,metabolites of tribendimidine in human

作　　者：窦学杰 袁桂艳[2] 张蕊[2] 魏春敏[2] 王本杰[2] 郭瑞臣[2] 

机构地区：[1]山东新华制药有限公司,山东淄博255005 [2]山东大学齐鲁医院临床药理研究所,山东济南250012

出　　处：《药学研究》2013年第9期543-545,共3页Journal of Pharmaceutical Research

摘　　要：目的 评价三苯双脒代谢物氨脒和乙酰氨脒人体药代动力学研究.方法 8名健康志愿者单次口服400 mg三苯双脒肠溶片后,采用LC-MS法测定不同时间点三苯双脒代谢物氨脒和乙酰氨脒浓度,DAS 2.0程序计算药代动力学参数.结果 氨脒和乙酰氨脒的药代动力学参数分别为：半衰期t1/2 （5.38±2.15）h和（7.09±2.06）h,达峰时Tmax （5.25±1.25）h和（7.13±2.42）h,峰浓度Cmax （449.38 ±136.41）ng·mL-1和（148.30±117.13）ng·mL-1,血浓度-时间曲线下面积AUC0～36 （4 655.04± 1 113.24）ng·mL-1·h和（1 904.93 ± 976.81）ng·mL-1·h,AUC0～∞分别为（4 768.90±1 158.38）ng·mL-1·h和（1 989.49± 1 014.42）ng·mL-1·h.结论 健康志愿者单次口服400 mg三苯双脒肠溶片后,氨脒和乙酰氨脒体内药代动力学过程均符合w=1/cc的一室模型,吸收、分布迅速.Objective To study the pharmacokinetic characteristics of dADT and acetylizad dADT, metabolites of tri- bendimidine, in human. Methods Eight healthy subjects were given 400 mg tribendimidine enteric - coated tablets. The concentration of dADT and acetylizad dADT in plasma were determined by LC - MS. The pharmacokinetic parameters were calculated with DAS 2. 0 software. Results The main pharmacokinetic parameters of dADT and acetylizad dADT were as follows ：tl/2 were （ 5.38 ± 2. 15 ） h and （ 7.09 ± 2. 06 } h ;Tmax were （ 5.25 ± 1.25 ） h and （ 7.13 ± 2.42 ） h ; Cmax were （ 449. 38 ± 136.41 ng·mL-l and（148.30±117. 13）ng· mL-1 ;AUC0-36 were{4 655.04±1113. 24）ng· mL-1 ·h and（1 904.93 ± 976. 81）ng· mL-1·h;AUC0-∞ were（4768.90 ±1 158. 38）ng· mL-1· h and（1 989.49±1 014.42）ng· mL-1·h,re- spectively. Conclusion The pharmacokinetic process of p - （ 1- dimethylamino ethylimino ） aniline and acetylizad p - （ 1 - dimethylamino ethylimino } aniline in healthy volunteers after orally administrated 400 mg tribendimidine enteric - coated tab- lets both fitted to one - compartment model with weight coefficient of 1/cc. They could be absorbed and distributed rapidly.

关 键 词：三苯双脒 高效液相色谱串联质谱法 药代动力学 代谢 

分 类 号：R969.1[医药卫生—药理学]