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目的:研究不同剂量氯苯氧异丁酸甲氧基苯丙烯酸酯{(E)-3-[4-[2-(4-chlorophenoxy)-2-methylpropanoyloxy]-3-me-thoxyphenyl]acrylic acid,AZ}灌胃给药后活性代谢产物氯苯氧异丁酸在大鼠体内药动学。方法:3组大鼠按体质量分别灌胃给予125,250,500 mg.kg-1的AZ后,以布洛芬为内标物,采用高效液相色谱法测定代谢产物氯苯氧异丁酸的血药浓度,各组结果分别用DAS 2.0软件进行药动学分析,组间药动学参数用SPSS11.5软件进行统计分析。结果:低、中剂量组氯苯氧异丁酸的t1/2,CL/F,MRT均无显著性差异,AUC随给药剂量增加线性增大。高剂量组与中剂量相比,t1/2变大,CL/F显著减小,MRT显著延长。结论:口服AZ在125～250 mg.kg-1剂量时,其代谢产物氯苯氧异丁酸在大鼠体内符合线性动力学过程,剂量在500 mg.kg-1以上时则表现为非线性动力学特征。
OBJECTIVE: To study the effects of different doses of chlorphenoxyisobutyric acid methoxyphenyl acrylate (E) -3- [4- [2- (4-chlorophenoxy) -2-methylpropanoyloxy] AZ} After intragastric administration of active metabolite chlorophenoxyisobutyric acid in rats pharmacokinetics. METHODS: Three groups of rats were given 125, 250, and 500 mg.kg-1 of AZ by gavage, respectively. Ibuprofen was used as internal standard, and the metabolites chlorophenoxyisobutyric acid Concentration, the results of each group were analyzed by DAS 2.0 software pharmacokinetics, pharmacokinetic parameters between groups using SPSS11.5 software for statistical analysis. Results: There was no significant difference in the values of t1 / 2, CL / F and MRT between low and medium doses of chlorphenyloxyisobutyric acid. AUC increased linearly with the dose of chlorphenyloxy isobutyric acid. The high dose group compared with the middle dose, t1 / 2 becomes larger, CL / F significantly reduced, MRT significantly prolonged. CONCLUSION: Chlorphenoxyisobutyric acid, a metabolite of oral AZ at 125 ~ 250 mg.kg-1, conforms to the linear kinetic process in rats. When the dose is above 500 mg.kg-1, AZ is non-linear Kinetic characteristics.