Objective To explore the pharmacokinetics and tissue distribution in rats with a single dose by orally administra‐tion of moxifloxacin .Methods Totally 60 rats were equally divided into 10 groups with orally administration moxifloxacin for 50 mg/kg .The lungs ,uterus ,ovaries (tube) ,kidney ,ureter and bladder tissues were collected at different time points (before give med‐icine and after 0 .25 ,0 .50 ,1 .00 ,2 .00 ,3 .00 ,4 .00 ,6 .00 ,8 .00 ,12 .00 ,24 .00 h) .The concentrations of moxifloxacin in tissues were determined by the established HPLC method and the pharmacokinetic parameters were calculated by 3p97 .Results The established HPLC methods had good specificities ,and the linear range was between 0 .001 6-50 .000 0μg/mL for tissue sample .T1/2βof moxi‐floxacin were (13 .65 ± 3 .56) ,(12 .64 ± 2 .86) ,(13 .27 ± 3 .51) ,(13 .47 ± 3 .29) ,(14 .78 ± 2 .64) ,(11 .56 ± 1 .58)h in lung ,uterus , ureterine adnexa ,kidney ,ureter and bladder ;Cmax of moxifloxac in various tissues were (15 .61 ± 3 .58) ,(12 .48 ± 4 .57) ,(16 .18 ± 4 .21) ,(12 .65 ± 3 .17) ,(26 .68 ± 7 .42) ,(1 .13 ± 0 .58)μg/mL ;Tmax of moxifloxac in above tissues were (3 .15 ± 1 .24) ,(2 .66 ± 1 .74) ,(2 .97 ± 1 .65) ,(2 .58 ± 1 .36) ,(3 .47 ± 1 .84) ,(2 .46 ± 1 .87)h;AUC0 -t of moxifloxac in above tissues were (87 .2 ± 5 .41) , (70 .89 ± 4 .56) ,(92 .41 ± 7 .65) ,(88 .26 ± 6 .94) ,(170 .59 ± 21 .48) ,(14 .57 ± 5 .47)μg · h-1 · mL -1 .Conclusion Moxifloxacin had a higher concentration in ureterine adnexa and ureter by orally administration with single dose ,and it can maintain for a long time .%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50 mg／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、24．00 h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0．0016～50．0000μg／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。
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