甲氨蝶呤在抑郁SD大鼠体内药代动力学  

Pharmacokinetics of Methotrexate in SD rats with Depressive Mood

作　　者：段晶晶[1] 周婷[1] 徐峰[1] 

机构地区：[1]南方医科大学珠江医院,广东广州510280

出　　处：《今日药学》2010年第11期23-25,共3页Pharmacy Today

基　　金：广东省医院药学研究基金(编号:2010A04)

摘　　要：目的研究抑郁大鼠抗肿瘤药物甲氨蝶呤(MTX)的药代动力学。方法对抑郁组大鼠连续8 w给予慢性不可预见性温和应激建立抑郁实验动物模型。采用荧光偏振免疫法(FPIA)测定SD大鼠给药后0.0830、.5、12、、48、、12 h各时间点血浆中MTX浓度,采用DAS药代动力学软件计算相应药代动力学参数。结果甲氨蝶呤在抑郁组大鼠和对照组大鼠体内药代动力学主要参数:Cmax分别为(8.10±0.99)和(7.99±1.04)μmol/L;t1/2分别为(2.11±0.24)和(2.24±0.32)h;AUC0→∞分别为(13.92±3.46)和(13.73±1.55)μmol.h.L-1;MRT0→∞分别为(1.99±0.45)和(2.15±0.44)h;CL分别为(0.13±0.03)和(0.14±0.04)L/h,显示甲氨蝶呤在抑郁组和对照组大鼠体内药代动力学参数基本一致,两组数据没有显著性差异。结论抑郁大鼠甲氨蝶呤体内代谢动力学与正常大鼠药代动力学相近。Objective To investigate the pharmacokinetics of methotrexate in rats with depression.Methods The depression rats model were build through exposure to chronic unpredicted mild stresses（CUMS） for 8 w.The concentration of methotrexate in plasma at 0.083,0.5,1,2,4,8,and 12 h after a single dose of methotrexate intravenous injection in rats were tested by fluorescence polarization immunoassay（FPIA） method.The corresponding pharmacokinetic parameters were processed with DAS software.Results Main pharmacokinetic parameters of methotrexate in rats of depression group and the normal control group were C max（8.10±0.99）and（7.99±1.04）μmol/L;t 1/2（2.11±0.24）and（2.24±0.32）h;AUC 0→∞（13.92±3.46）and（13.73±1.55）μmol·h·L-1;MRT 0→∞（1.99±0.45）and（2.15±0.44）h;CL（0.13±0.03）and（0.14±0.04）L/h,respectively.There was no significant difference between the pharmacokinetic parameters in rats of depression group and the normal control group.Conclusion The metabolism of methotrexate in rats with depression is similar with that in the normal rats.

关 键 词：甲氨蝶呤 抑郁模型 荧光偏振免疫法 药代动力学 

分 类 号：R973.2[医药卫生—药品]