甲磺酸加替沙星片健康人连续给药药代动力学  

Pharmacokinetics of gatifloxacin mesylate tablet in healthy volunteers after multiple dosage administrations

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,400016 [2]北京大学临床药理研究所

出　　处：《中国抗感染化疗杂志》2004年第2期79-81,共3页Chinese Journal of Infection and Chemotherapy

摘　　要：目的 :研究健康人口服甲磺酸加替沙星片连续给药后药代动力学 ,为该药Ⅱ期临床试验提供依据。方法 :8名受试者服用甲磺酸加替沙星片 2 0 0mg ,每日 1次 ,连续 7d。以高效液相色谱法 (HPLC)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。第 1天和第 7天的血药浓度达峰时间 (Tmax)分别为 1.2 2h和 1.35h ,高峰血药浓度 (Cmax)分别为 1.94mg/L和 2 .0 2mg/L ,血消除半衰期 (t1/ 2 β)分别为 6 .4 8h和 7.89h ,药时曲线下面积 (AUC0 ∞)分别为 2 0 .5 4mg·h/L和 19.81mg·h/L ,给药后 2 4h内尿药累积回收率为 5 9.86 %。 结论 :甲磺酸加替沙星片具有良好的药代动力学特征 ,每日 2 0 0mg 1～ 2次口服可用于治疗敏感菌感染。Objective: To study the pharmacokinetics of gatifloxacin mesylate tablet in healthy volunteers after multiple dosage administrations. Methods:Multiple doses of 200 mg gatifloxacin once daily were administered orally for 7 days to 8 healthy volunteers, serum and urine concentrations of gatifloxacin were detected by high performance liquid chromatography. Results:Gati-floxacin was well tolerated in every subject. The concentration-time data were fitted to a two-compartment open model. On days 1 and 7, T max were 1.22 h and 1.35 h respectively, C max were 1.94 mg/L and 2.02 mg/L respectively, t 1/2β were 6.48 h and 7.89 h respectively, AUC 0-∞ were 20.54 mg·h/L and 19.81 mg·h/L respectively, 59.86 % of the given doses were recovered in the urine within 24 h after dosage. Conclusions:Gatifloxacin has favorable pharmacokinetic properties. Gatifloxacin 200 mg once or twice daily dosage may be applied in the treatment of bacterial infections caused by susceptible organisms.

关 键 词：甲磺酸加替沙星 药代动力学 健康志愿者 连续给药 

分 类 号：R96[医药卫生—药理学]