摘要
目的研究艾拉莫德在正常与佐剂性关节炎大鼠体内的药动学行为。方法用高效液相色谱法测定血清中艾拉莫德的浓度,并计算其药动学参数。结果连续给药后正常组(6mg/kg)的主要药动学参数为:t1/2Ke:6.30h;tpcak:4.00h;Cmax:8.87μg/ml;AUC0-24:98.52μg·ml^-1·h^-1。连续给药后,关节炎大鼠低、中、高三个剂量组(3、6、12mg/kg)的主要药动学参数分别为:t1/2Ke:6.03、6.24、6.89h;tpeak:3.83、3.83、4.67h;Cmax:3.84、8.31、12.69μg/ml;AUC0-24:48.67、91.02、145.10μg·ml^-1·h^-1。经检验,除Cmax和AUC外,关节炎大鼠三个剂量组的药动学参数之间差异无统计学意义,Cmax和AUC值与剂量成正比。正常与关节炎大鼠的药动学参数比较,差异无统计学意义。结论艾拉莫德在正常和佐剂性关节炎大鼠体内的药动学行为符合开放型—室模型—级速率过程。
Objective To study the pharmacokinetics of iguratimod in rats. Methods The concentration of iguratimod in the samples was determined by HPLC method. The pharmacokinetics parameters were calculated with DAS softwrare. Results The main pharmacokinetics parameters of normal group(6mg/kg) were as follows:t1/2Ke: 3.56h, tpeak : 4.00h, Cmax : 8.87μg/ml, AUC0-24 : 74.76μg·ml^-1·h^-1 The main pharmacokinetics parameters of three model groups(3,6,12mg/kg) were as follows : t1/2 Ke : 4.54,3.20,3.17h, tpeak : 3.83,3.83,4.67h, Cmax : 3. 84, 8.31,12.69μg/ml, AUC0-24:40.21,76. 72,117.06μg·ml^-1·h^-1. Except Cmax and AUC, no significant differences were found between the three model groups. And the differences between normal group and model group were not significant. Conclusion The pharmacokinetics of rats is fit to one-compartment model.
出处
《中国基层医药》
CAS
2008年第6期881-882,1057,共3页
Chinese Journal of Primary Medicine and Pharmacy
关键词
艾拉莫德
药代动力学
关节炎
实验性
鼠
Iguratimod
Pharmacokinetics
Arthritis, experimental
Mus