【作者】 张媛； 谭晓黎； 郭瑞臣； 王本杰；

【Author】 Zhang Yuan, Tan Xiaoli, Guo Ruichen and Wang Benjie (Weihai Municipal Hospital, 264200),Institute of clinical Pharmacology, Qilu Hospital of Shandong University, Jinan,250013)

【机构】 威海市立医院； 山东大学齐鲁医院临床药理研究所；

【摘要】 目的以市售盐酸环丙沙星普通片为参比制剂进行盐酸环丙沙星胃漂浮片的人体药代动力学及相对生物利用度研究。方法采用二周期交叉试验方法,以RP-HPLC法测定环丙沙星血浓度,采用DAS程序计算环丙沙星约动学参数并进行生物等效性评价。结果单剂口服给药试验制剂和参比制剂环丙沙星时间-浓度曲线下面积(AUC0-t)分别为10.889±1.385 μg ·h·ml-1和12.406±1.384 μg ·h ·ml-1;AUC0-∞分别10.889±1.385 μg ·h·ml-1和12.406±1.384 μg·h·ml-1; Cmax分别为1.026±0.247 μg·ml-1和3.093±0.452 μg·ml-1,Tmax分别为5.4±1.1h,1.5±0.46h;试验制剂相对于普通制剂单剂给药的生物利用度(F)为87.79%±5.61%。结论盐酸环丙沙星胃漂浮片与盐酸环丙沙星普通片AUC无显著性差异,但Cmax 和Tmax有显著性差异,提示盐酸环丙沙星缓释片具有明显的缓释特征。更多还原

【Abstract】 OBJECTIVE : To study the pharmacokinetics and bioavailability of extended-release tablet of ciprofloxacin in 20 healthy volunteers. METHODS: A single dose of extended-release tablet of ciprofloxacin (500mg) or ciprofloxacin conventional tablet (2SOmgx2) was given to 20 healthy male volunteers in a randomized crosserover study. The concentrations of ciprofloxacin in serum samples were determined by RP-HPLC, and the bioequivalence were evaluated. RESULTS: The main pharmacokinetic parameters of the test and reference in volunteers were as follows, AUC0-t were 10.889±1.385 μ g ·h ·ml-1 and 12.406±1.384 μ g ·h ·ml-1; AUC0-∞10.889±1.385μg·h ·ml-1 and 12.406±1.384lμ g ·h ·ml-1; Cmax 1.026±0.247μg·ml-1 和3.093±0.452 μ g · ml-1 ,Tmax 5.4±1.1h and 1.5±0.46h, respectively. The relative bioavailability of test compared to reference was 87.79%±5.61%. CONCLUSIONS: The Cmax and Tmax of test showed slowly release behavior, with no significant differerces for AUC between the two preparations.更多还原