环丙沙星在老年肾损害患者单次给药后的药代动力学研究

 目的:比较5名老年肾功能正常患者(Clcr>70ml·min^-1)与5名老年肾功能受损患者(Clcr<50ml·min^-1)单次静滴400mg乳酸环丙沙星注射液后的药代动力学。方法:应用微生物法测定不同时间的血药浓度,数据用PKBP-N₁软件拟合处理。结果:药-时曲线符合二室开放模型,单次给药后,肾功能正常组与受损组的t_1/2β分别为(3.23±1.17)h,(5.98±1.80)h;Cl分别为(35.2±9.16)L·h^-1,(12.5±4.83)L·h^-1;AUC分别为(11.2±4.89)h·μg·ml^-1,(36.3±17.1)h·μg·ml^-1;其中,两组间的t_1/2β与Cl经t检验有显著性差异。结论:老年肾损害患者的清除率显著下降,半衰期显著延长。因此,在临床用药时需慎重,并注意减少剂量。

Pharmacokinetics of ciprofloxacin following administration of single dose in elderly patients with impairedre nal function

OBJECTIVE:To study the pharmacokinetics of ciprofloxacin(CPFX)in 5 elderly patients with normal renal function(creatinine clearance 70 ml·min^-1 ormore)and 5 elderly one with impaired renal function(creatinine clearance 50 ml·min^-1orless)after a single-dose of 400mg.METHODS:The serum concentrations in different time were determined bybioassay.The data werean alyzed by using PKBP-N₁ imitate program.RESULTS:The pharmacokinetics of CPFX was described by open two-compart mentmodel.The data obtained from the elderly with normal renal function and with impaired renal function showed t_1/2β=(3.23±1.17)h vs(5.98±1.80)h;Cl=(35.2±9.16)L·h^-1vs(12.5±4.83)L·h^-1;AUC=(11.2±4.89)h·μg·m^-1vs(36.3±17.1)h·μg·ml^-1respectively.Among them,t_1/2βand Cl obtained from single dose test showed that there was singnificant difference between the two groups.CONCLUSION:The creatinine clearance of the elderly with impaired renal function markedly reduced,and then the half life extended markedly.Hence,adopting a prudent policy and reducing dose is necessary in clinical practice.