非甾体抗炎药对安妥沙星在大鼠体内药动学的影响  

Pharmacokinetics of antofloxacin in rats co-administered with non-steroidal anti-inflammatory drugs

作　　者：庞晓雁[1] 谢林[1] 许潇[1] 刘海燕[1] 刘李[1] 刘晓东[1] 

机构地区：[1]中国药科大学药代研究中心,南京210009

出　　处：《中国新药杂志》2007年第8期600-603,共4页Chinese Journal of New Drugs

摘　　要：目的:研究非甾体抗炎药双氯芬酸和吲哚美辛对安妥沙星在大鼠体内的药动学行为的影响。方法:大鼠单用安妥沙星(7.5 mg.kg-1,iv)以及与双氯芬酸(20 mg.kg-1,iv)或吲哚美辛(3 mg.kg-1,iv)合用后,测定血浆中安妥沙星浓度和尿中累积排泄量,计算相应的药动学参数。结果:与单用安妥沙星比较,合用双氯芬酸使大鼠血浆中安妥沙星药物浓度显著增加,安妥沙星的AUC也显著增加[(531.57±87.94)vs.(405.61±14.01)μg.min.mL-1,P<0.05],其血浆清除率和肾清除率分别减少了30%[(14.43±2.33)vs.(18.51±0.62)mL.kg-1.min-1,P<0.05]和50%[(3.16±0.79)vs.(6.07±0.81)mL.kg-1.min-1,P<0.01]。而吲哚美辛不影响安妥沙星在大鼠体内的药动学行为。结论:双氯芬酸能显著影响安妥沙星在大鼠体内的药动学行为。Objective： To investigate whether diclofenac and indomethacin affected the pharma- cokinetics of antofloxacin in rats. Methods： Rats were randomly injected with antofloxacin （7. 5mg.kg^-1, iv） alone ox combination of antofloxacin with diclofenac （ 20mg.kg^-1, iv） or indomethacin （ 3mg.kg^-1,iv）. The plasma samples of the rats were collected to measure blood concentration and accumulative urinary levels of antofloxacin. Results： Compared with the antofloxacin alone, co-administration of diclofenac with antofloxacin resulted in significant increases of the area of antofloxacin plasma concen- tration-time curve （AUC） values [（531.57±87.94） vs. （405.61±14.01）μg.min.mL-1^,P 〈 0.05 ] , and reductions of the plasma clearance （CL） and renal clearance （ CLR ） of antofloxacin by about 30% [（14.43±2.33） vs. （18.51±0.62）mL.kg^-1.min^-1,P〈0.05] and 50 % [（3.16±0.79） vs. （6.07±0.81 ）mL.kg^-1.min^-1,P 〈 0.01 ]. Co-administration of indomethacin showed no impacts on pharmacokinetic profile of antofloxacin in rats. Conclusion： Diclofenac significantly impacted pharma- cokinetic profile of antofloxacin in rats.

关 键 词：药动学 安妥沙星 吲哚美辛 双氯芬酸 相互作用 

分 类 号：R988.1[医药卫生—药品] R944.9[医药卫生—药学]