盐酸加替沙星胶囊的人体药代动力学及生物等效性评价  

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

作　　者：李宏力[1] 赵磊[2] 

机构地区：[1]陕西能源职业技术学院医学校区医学技术系,陕西西安710613 [2]第四军医大学西京医院临床药理基地,陕西西安710033

出　　处：《现代医药卫生》2007年第22期3326-3327,共2页Journal of Modern Medicine & Health

摘　　要：目的:研究盐酸加替沙星胶囊在健康人体内的药代动力学特征及相对生物等效性。方法:采用标准二阶段交叉设计自身对照试验法,将18例男性健康志愿受试者随机分为两组,单剂量口服盐酸加替沙星胶囊400mg(试验品)或盐酸加替沙星片400mg(参照品),,以高效液相色谱法测定受试者服药24小时内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盐酸加替沙星制剂T_(max)、C_(max)和AUC(0￣24h)间的差异。结果:盐酸加替沙星在健康志愿者体内的处置为一级吸收单室模型,试验品和参比品的主要药动学参数T_(max)(实测值)、C_(max)(实测值)、AUC(0￣24h)分别为:(1.51±0.35)小时和(1.53±0.38)小时,(3.46±0.79)和(3.43±0.92)mg/L,(34.51±8.43)和(33.04±10.20)mg/(h·L);试验品的相对生物利用度为105.2%。结论:盐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;两种盐酸加替沙星制剂在人体内具有生物等效性(P>0.05)。Objective：To compare the pharmacokinetic parameters and bioavailability of gatifloxacin HCL capsules.Methods：An open, randomized, two-period crossover study was conducted in 18 healthy volunteers. The concentration of gatifloxaein in plasma was assayed by HPLC after a single oral dose of 400 mg test or reference preparation. The main pharmaeokinetie parameters （AUC 〈0-24h）,Cmax and Tmax） were analyzed by two one-sided t test.Results：The concentration -time curve ：after medication conformed to one--compartment open model with a In＇st order absorption.Tmax,Cmax, and AUC （0-24h） of test and reference preparation were （1.51±0.35） and （1.53±0.38）h, （3.46±0.79） and （3.43±0.92）mg/L, （34.51±8.43） and （33.04±10.20）mg/（h .L） respectively. The relative bioavailability of test was 105.2%.Conclusion：The gatifloxaein HCL had the characteristics of absorbing quickly, high peak concentration in plasma and longer mean retention time in vivo.The result of statistical analysis showed that two formulations were bioequivalent（P〉0.05）.

关 键 词：盐酸加替沙星胶囊 药动学 生物等效性 高效液相色谱 

分 类 号：R9[医药卫生—药学]