盐酸加替沙星胶囊人体药代动力学及生物等效性评价.docVIP

盐酸加替沙星胶囊人体药代动力学及生物等效性评价【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400 mg（试验品）或盐酸加替沙星片400 mg（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Tmax、Cmax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Tmax（实测值）、Cmax（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/（hL）；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(P0.05)。 【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 文章编号：1009-5519（2007）22-3326-02 中图分类号：R9 文献标识码：A Assessment on pharmacokinetics and bioavailability of gatifloxacin HCL capsules in healthy volunteers LI Hong-Li1，ZHAO Lei2 (1.Department of Medical Technique,Shaanxi Energy Vocational College,Xi’an 710033,China;2.Clinical Pharmacology Base，Xijing Hospital，Fourth Military Medical University，Xi’an710613，China) 【Abstract】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 gatifloxacin in plasma was assayed by HPLC after a single oral dose of 400 mg test or reference preparation. The main pharmacokinetic 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 first 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/（hL） respectively. The relative bioavailability of test was 105.2%.Conclusion：The gatifloxacin 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(P0.05). 【Key words】Gatifloxacin HCL；Pharmacokinetics；Bioequival