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大鼠单剂量灌服莫西沙星后泌尿生殖系统的组织分布及其药代动力学研究

发布时间:2018-07-24 17:28
【摘要】:目的探讨单次灌胃给予莫西沙星大鼠的组织分布及药代动力学。方法 60只SD大鼠分为10组,按莫西沙星50mg/kg灌胃给药,给药前及给药后0.25、0.50、1.00、2.00、3.00、4.00、6.00、8.00、12.00、24.00h分别取肺、子宫、卵巢输卵管、肾脏、输尿管及膀胱组织,高效液相色谱法(HPLC)测定各组织中莫西沙星的药物浓度,3p97软件拟合药代动力学参数。结果建立HPLC测定组织中莫西沙星药物浓度的方法,专属性好,药物浓度在0.001 6~50.000 0μg/mL线性关系良好。给药后肺、子宫、卵巢输卵管、肾脏、输尿管及膀胱组织T1/2β分别为(13.65±3.56)h、(12.64±2.86)h、(13.27±3.51)h、(13.47±3.29)h、(14.78±2.64)h及(11.56±1.58)h,Cmax分别为(15.61±3.58)μg/mL、(12.48±4.57)μg/mL、(16.18±4.21)μg/mL、(12.65±3.17)μg/mL、(26.68±7.42)μg/mL和(1.13±0.58)μg/mL,Tmax分别为(3.15±1.24)h、(2.66±1.74)h、(2.97±1.65)h、(2.58±1.36)h、(3.47±1.84)h和(2.46±1.87)h,AUC0~t分别为(87.2±5.41)μg·h-1·mL-1、(70.89±4.56)μg·h-1·mL-1、(92.41±7.65)μg·h-1·mL-1、(88.26±6.94)μg·h-1·mL-1、(170.59±21.48)μg·h-1·mL-1和(14.57±5.47)μg·h-1·mL-1。结论大鼠单剂量灌服莫西沙星后输尿管和卵巢输卵管组织有较高的药物浓度,可维持较长时间。
[Abstract]:Objective to investigate the tissue distribution and pharmacokinetics of moxifloxacin in rats. Methods Sixty Sprague-Dawley rats were divided into 10 groups. The lung, uterus, ovary, kidney, ureter and bladder were collected before and after administration of moxifloxacin 50mg/kg. The pharmacokinetic parameters of moxifloxacin in tissues were determined by (HPLC) with 3p97 software. Results A HPLC method was established for the determination of moxifloxacin in tissues. The specificity of the method was good. The linear relationship between the concentration of moxifloxacin and moxifloxacin was 0.001 ~ 50.000 渭 g/mL. 缁欒嵂鍚庤偤,瀛愬,鍗靛发杈撳嵉绠,

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