坦索罗辛对大鼠细菌性前列腺炎组织中左氧氟沙星药动学的影响

Influence of tamsulosin on the pharmacokinetics of levofloxacin in prostate of rats with bacterial prostatitis

目的探讨坦索罗辛对急性细菌性前列腺炎模型大鼠前列腺组织中左氧氟沙星药动学的影响。方法将96只急性细菌性前列腺炎模型大鼠随机分为实验组（左氧氟沙星和坦索罗辛联合用药组）和对照组（单用左氧氟沙星组），每组48只，分别在给药后0．125、0．25、0．5、1、2、4、8和12h每个时间点处死6只大鼠，采集两组动物的前列腺制作组织匀浆，用HPLC法测定前列腺组织中左氧氟沙星浓度，3p97软件计算药动学参数。结果实验组和对照组药．时曲线均符合一室模型。主要药动学参数如下：t1／2分别为（4．78±0．75）h和（3．64±0．88）h,tpeak分别为（1．18±0．10）h和（O．81±0．29）h，Cmax分别为（6．16±0．57）μg／g和（3．91±0．62）gg／g，AUC0-12分别为（41．91±1．01）μg·h／g和（22．70±3．08）μg·h／g。结论坦索罗辛可以明显提高左氧氟沙星在急性细菌性前列腺炎模型大鼠前列腺组织中的药物浓度。

Objective To study the influence of tamsulosin on the pharmacokinetics of levofloxacin in prostate of model rats with acute bacterial prostatitis. Methods Ninty-six model rats with acute bacterial prostatitis were randomly divided into two groups： experimental group （both tamsulosin and levofloxacin were used, n=48） and control group （only levofloxacin was used, n=48）. Six rats were sacrificed for collecting their prostatic samples to make tissue homogenate at each time point： 0.125, 0.25, 0.5, 1, 2, 4, 8 and 12h after drug administration. The levofloxacin concentrations were detected by HPLC and then pharmacokinetic parameters were calculated with 3p97 software program. Results The levofloxacin concentration-time curves of experimental group and control group were both fit the one-compartment model. The main pharmacokinetic parameters of the two groups as follows： t1/2 were （4.78±0.75）h and （3.64±0.88）h, tpeak were （1.18±0.10）h and （0.81±0.29）h, Cax were （6.16±0.57）μg/g and （3.91±0.62）μg/g, AUC0-12 were （41.91±1.01）μgh/g and （22.70±3.08）μgh/g, respectively. Conclusion Tamsulosin can obviously increase the concentration of levofloxacin in the prostate of model rats with acute bacterial prostatitis.