甲磺酸加替沙星片健康人单剂口服药代动力学  

Pharmacokinetics of gatifloxacin mesylate tablet in healthy volunteers after a single oral administration

作　　者：蔡素芳[1] 杨鸿[1] 肖永红[2] 余泽波[1] 

机构地区：[1]重庆医科大学附属第一医院感染科,重庆400016 [2]北京大学临床药理研究所,北京100083

出　　处：《中国抗生素杂志》2004年第1期44-47,共4页Chinese Journal of Antibiotics

摘　　要：目的研究健康人口服单剂甲磺酸加替沙星片后药代动力学特征,为该药II期临床试验提供依据。方法采用3剂量3周期拉丁方实验设计。9名健康受试者单剂口服甲磺酸加替沙星片100、200、300mg,HPLC法测其血清、尿药物浓度。结果受试者口服甲磺酸加替沙星片后,人体耐受良好,体内过程符合二室开放模型。主要药代动力学参数与给药剂量呈线性关系,tmax为0.5～0.7h,Cmax分别为1.42、2.42、3.25μg/ml,AUC0-∞分别为11.33、21.85、32.32μg·h/ml,V/Fc值为50～80L,t1/2β为8～9h,72h尿药累积回收率约为63.5%。结论甲磺酸加替沙星片口服吸收良好,血峰浓度高,组织分布广,消除半衰期长。200mg每日一次口服用于治疗敏感菌感染。Objective To study the pharmacokinetics of gatifloxacin mesylate tablet in healthy volunteers after single oral administration.Method A single-dose of 100,200,or 300 mg gatifloxacin mesylate were administered orally to nine healthy volunteers in 3×3 latin square;the concentrations of gatifloxacin in serum and urine were detected by HPLC.Results Gatifloxacin was well tolerated in everyone.The concentration-time data after single oral dose of 100,200,or 300 mg gatifloxacin conformed to a two-compartment open model and there were linear relationship between dosages and major parameters,tmax were 0.5～0.7h,Cmax were 1.42,2.42,3.25μg/ml respectively.AUC0-∞were 11.33,21.85,32.32μg·h/ml;V/Fc were 50～80L,t1/2βwere 8～9h respectively.63.5%of the administered doses were recovered in the urine within 72h.Conclusion These results indicate that gatifloxacin has a favorable pharmacokinetic properties with high blood concentration and good tissue distribution.200mg once or twice daily dose may be used for the treatment of bacterial infections caused by susceptible organisms.

关 键 词：甲磺酸加替沙星片 药代动力学 健康人 

分 类 号：R978.19[医药卫生—药品] R969.1[医药卫生—药学]