左氧氟沙星对多索茶碱在健康人体内药动学的影响

目的研究合用左氧氟沙星对健康受试者多索茶碱血药浓度和药动学的影响。方法对10名男性健康受试者采用自身对照交叉试验设计方法给药,用高效液相色谱(HPLC)法测定多索茶碱血药浓度,采用3P97软件进行数据处理,求出药动学参数。结果合用左氧氟沙星组(试验组)多索茶碱平均血药浓度在停药后0～6 h各时间点(除停药后15 min)与单用多索茶碱组(对照组)相比均无显著差异(P>0.05);对照组和试验组多索茶碱的t_(+β)分别为(1.20±s 0.08)、(1.40±0.25)h;AUC分别为(16±4)、(17±3)mg·h·L~(-1);CL分别为(35±6)、(35±10)L·h~(-1);t_(+α)分别为(0.052±0.013)、(0.33±0.27)h;V_d分别为(6.1±2.1)、(34±30)L。合用左氧氟沙星后多索茶碱的V_D和t_(+α)的增加有显著差异(P<0.05),其余药动学参数在2组间均无显著差异(P>0.05)。结论合用左氧氟沙星对多索茶碱的代谢动力学无影响,但可改变其分布动力学,增大t_(+α)和V_d,2药合用不会引起多索茶碱的体内蓄积,提示2药合用相对安全。

Effects of levofloxacin on pharmacokinetics of doxophylline in healthy volunteers

AIM To investigate the influence of levofloxacin on pharmacokinetics and serum concentra- tion of doxophylline in healthy volunteers.METHODS A crossover design was performed in 10 healthy male volunteers.The blood concentration was determined by HPLC.3P97 software was used to figure out the pharmacokinetic parameters.RESULTS There was no significantly difference (P>0.05) in the doxophylline serum concentration between two groups at each time point (0～6 h) except the 15 min.The main parameters of pharmacokinetics of doxophylline in control group and in trial group were as follows:t_(+β) was (1.20±s 0.08) and (1.40±0.25) h;AUC was (16±4) and (17±3) mg·h·L~(-1);CL was (35±6) and (35±10) L·h~(-1);t_(+α) was (0.052±0.013) and (0.33±0.27) h;V_d was (6.1±2.1) and (34±30) L.Compared with control group,t_(+α) and V_d of doxophylline in trial group increased significantly (P<0.05).There was no significant difference in other pharmacokinetic parameters between two groups.CONCLUSION Although the concomitance of levofloxacin could change the distribution of doxophylline by increase t_(+α) and V_d,it has no effects on the elimination process and the accumulation of doxophylline.Doxophylline administrated with levofloxacin is relatively safe.