环丙沙星肛栓的尿药动力学研究

Studies on Pharmacokinetics of Ciprofloxacin Suppository in Healthy Volunteers

目的 :研究环丙沙星肛栓和环丙沙星片剂的药代动力学 ,为环丙沙星肛栓治疗慢性细菌性前列腺炎提供依据。方法 :健康成人分别口服250mg 环丙沙星片剂和使用剂量为250mg 的肛塞栓剂 ,留量尿液 ,用双波长分光光度法测定其中环丙沙星的含量 ,计算药代动力学参数。结果 :主要药代动力学参数 :口服组尿中环丙沙星24h回收率 (70 3±11 2) % ,k= (0 161±0 059)h ,Tp=(1 71±0 556)h ;栓剂组24h尿中环丙沙星回收率 (17 2±3 6) % ,栓剂类似于缓释制剂 ,在体内近似于零级速率过程。结论 :环丙沙星肛栓用于治疗慢性细菌性前列腺炎 ,每天1枚即可。

AIM: To provide reference for the treatment of chronic bacterial prostatitis by comparing the pharmacokinetics of ciprofloxacin rectal suppository,with the tablet METHODS:Ciprofloxacin tablet 250mg orally,and one suppository 250mg, were given to healthy volunteers separately The concentrations of ciprofloxacin in urine were determined by dual wavelength UV-spectrophotometry and the pharmacokinetics parameters were obtained RESULTS:The main pharmacokinetics parameters were as follows:The tablet group excreted (70 3±11 2)% in 24 hours; Considering that ciprofloxacin is distributed as one compartment model and eliminated in a first order procedure, we obtained the straight line equation LnΔxu/Δt=—0 161t+3 114,and K=(0 161±0 059)h,γ=0 9 978,Tp=(1 71±0 556)h;The suppository group excreted (17 2±3 6)% in 24 hours,and the average concentration of ciprofloxacin in urine was 30μg/ml The absorption and elimination in suppository group was near to the zero order process The urine drug concentration of supportory was somewhat alike to that of slow release agents CONCLUSION:Ciprofloxacin suppository is suitable for the treatment of chronic bacterial prostatitis with one suppository daily