中国临床药学杂志

目的　研究司帕沙星及洛美沙星对老年慢性阻塞性肺病(COPD)患者茶碱缓释片药动学的影响。方法　36例老年COPD患者口服茶碱缓释片10 0mg ,q8h×9d ,d 4起Ⅰ组18例合用司帕沙星片2 0 0mg ,qd ;Ⅱ组18例合用洛美沙星胶囊4 0 0mg ,q12h。于d 4、10采集血样,采用荧光偏振免疫法检测茶碱的血药浓度,用PKBP N1程序求得药动学参数。结果　合用司帕沙星后茶碱血药浓度较合用前明显升高(P <0 .0 1) ,AUC及cmax差异有高度统计学意义(P <0 .0 1) ;而合用洛美沙星后其血药浓度较合用前稍有升高(P >0 .0 5 ) ,药动学参数除tmax有统计学意义(P <0 .0 5 )外,其余的变化均无统计学意义。结论　司帕沙星对茶碱的药动学有显著性影响,而洛美沙星对茶碱的药动学情况基本上无明显的影响。

AIM To study the effects of sparfloxacin and lomefloxacin on the pharmacokinetics of theophylline in chronic obstructive pulmonary disease old patients. METHODS Thirty-six chronic obstructive pulmonary disease old patients were given theophylline orally 100 mg,q8 h for 9 d,then group Ⅰ(n=18)received sparfloxacin 200 mg,qd,while group Ⅱ(n=18)added lomefloxacin 400 mg,q12 h from d 4-9. The theophylline serum concentration before and after being concomitant with sparfloxacin or lomefloxacin were determined by fluorescence polarization immunoassay(FPIA),PKBP-N1 program was used for the calculation of the pharmacokinetic parameters and statistical analysis was finished by computer. RESULTS The theophylline serum concentrations after being concomitant with sparfloxacin increased remarkably(P<0.01).There were highly significant differences between with and without concomitant sparfloxacin in the AUC 0→12 and c max(P<0.01).The theophylline serum concentrations after being concomitant with lomefloxacin increased (P>0.05). There were no significant differences in main pharmacokinetic parameters but t max(P<0.05). CONCLUSION The effect of sparfloxacin on the pharmacokinetics of theophylline is considerable in chronic obstructive pulmonary disease old patients,and it suggests that it is clinically necessary to detect the theophylline serum concentration while administrated concomitantly with sparfloxacin to prevent patients poisoning.There is no effect of lomefloxacin on the distribution and elimination of theophylline.Theophylline administrated with lomefloxacin is relatively safe.