甲磺酸加替沙星胶囊人体药代动力学及生物等效性评价  

Assessment on pharmacokinetics and bioavailability of gatifloxacin mesylate capsules in healthy volunteers

作　　者：李宏力[1] 樊代明[1] 李哲[1] 文爱东[1] 赵磊[1] 吴寅[1] 郭征[1] 石茹[1] 

机构地区：[1]第四军医大学西京医院临床药理基地,陕西西安710033

出　　处：《第四军医大学学报》2003年第20期1915-1918,共4页Journal of the Fourth Military Medical University

摘　　要：目的 :研究甲磺酸加替沙星胶囊在健康人体内的药代动力学及相对生物等效性 .方法 :采用双周期随机交叉、自身对照试验设计法 ,将 1 8例男性健康志愿者随机分为两组 ,分别单剂量口服甲磺酸加替沙星胶囊 4 0 0mg(试验品 )和甲磺酸加替沙星片 4 0 0mg(参照品 ) ,经 1w清洗期后交叉换药 ,以高效液相色谱法测定受试者服药后血浆中加替沙星的经时浓度 ,计算加替沙星药动学参数 ,以双单侧t检验统计法比较两种甲磺酸加替沙星制剂是否具有生物等效性 .结果 :甲磺酸加替沙星在人体内的处置为一级吸收单室模型 ,试验品和参照品的主要药动学参数Tmax(实测值 )、Cmax(实测值 )、AUC(0 -2 4h) 分别为 :为 (1 .5 1± 0 .39)和 (1 .5 4± 0 .4 0 )h ,(3.4 8± 0 .84 )和 (3.4 3± 0 .96 )mg·L-1 ,(34.5 1± 8.4 9)和(33.0 4± 1 0 .2 5 )mg·h·L-1 ;试验品的相对生物利用度为1 0 7.4 % .结论 :甲磺酸加替沙星具有口服后吸收快、血药浓度较高、体内平均滞留时间 (MRT)较长的特点 ;两种甲磺酸加替沙星制剂在人体内具有生物等效性 (P >0 .0 5 ) .AIM: To study the pharmacokinetic parameters and bioavailability of gatifloxacin mesylate capsules. METHODS: An open, randomized, two period crossover study was conducted in 18 healthy volunteers. Concentrations of gatifloxacin in plasma were assayed by HPLC after a single oral dose of 400 mg of the tested capsules or the referenced tablets. The main pharmacokinetic parameters [ AUC (0-24h) , C max and T max ] were analyzed by two one sided t test. RESULTS: The concentration time curve after medication conformed to one compartment open model with a first order absorption. T max , C max and AUC (0-24h) of the tested capsules and the referenced tablet were(1.51± 0.39) and (1.54±0.40) h, (3.48±0.84) and (3.43± 0.96) mg·L -1 ,(34.51±8.49) and (33.04±10.25)mg· h· L -1 respectively. The relative bioavailability of the tested capsules tothe referenced tablets was 107.4%. CONCLUSION: The gatifloxacin mesylate has characteristic of quick absorption, high peak concentration in plasma and longer mean retention time; The result of statistical analysis showed that two formulations were bioequivalent ( P > 0.05).

关 键 词：甲磺酸加替沙星 药代动力学 生物利用度 色谱法 高压液相 

分 类 号：R944[医药卫生—药剂学]