盐酸左氧氟沙星片在健康人体内的药代动力学和生物等效性研究  

Pharmacokinetics and Bioequivalence Assessment of Levofloxacin Hydrochloride Tablets in Chinese Healthy Volunteers

作　　者：刘灵晔 李娟[1] 曹蓓[1] 杨元勋[1] 钱薇[1] LIU Lingye;LI Juan;CAO Bei;YANG Yuanxun;QIAN Wei(Nanjing Drum Tower Hospital,the Affiliated Hospital of Nanjing University Medical School,Nanjing 210008,China)

机构地区：[1]南京大学医学院附属鼓楼医院Ⅰ期临床试验研究室,南京210008

出　　处：《药学与临床研究》2020年第2期89-92,共4页Pharmaceutical and Clinical Research

摘　　要：目的:研究已上市盐酸左氧氟沙星片在健康中国人体内的生物等效性。方法:48例健康志愿者随机分组,分别在空腹及进食高脂餐后,两周期双交叉单剂量口服盐酸左氧氟沙星片及其参比制剂左氧氟沙星片各500 mg,采用高效液相色谱-串联质谱法测定给药前与给药后48 h内不同时间点的血药浓度,计算主要药代动力学参数,评价生物等效性。结果:在空腹试验中,盐酸左氧氟沙星片及其参比制剂的AUC0~48 h分别为(50.0±8.4)、(48.8±8.6)μg·h·mL^-1,Cmax分别为(6.15±1.42)、(5.98±1.55)μg·mL^-1,tmax分别为(1.19±0.62)、(1.30±0.73)h,t1/2分别为(6.56±1.13)、(6.51±1.14)h^-1,相对生物利用度为(103.0±8.7)%;在餐后试验中,盐酸左氧氟沙星片及其参比制剂的AUC0~48 h分别为(45.4±8.4)、(44.5±8.2)μg·h·mL^-1,Cmax分别为(5.85±1.08)、(6.58±1.89)μg·mL^-1,tmax分别为(1.93±0.72)、(1.82±0.81)h,t1/2分别为(6.69±0.81)、(6.63±0.76)h^-1,相对生物利用度为(102.3±5.3)%。结论:盐酸左氧氟沙星片与其参比制剂具有生物等效性。Objective:To reevaluate the bioequivalence of post-marketing levofloxacin hydrochloride tablets.Methods:In a randomized,two cross-over,single-dose administration,48 healthy volunteers were given 500 mg dose of levofloxacin hydrochloride tablets or reference preparations after fasting or high fat meals.Plasma concentrations at different time points before and after the administration were determined by high performance liquid chromatography-tandem mass spectrometry,to calculate the main pharmacokinetic parameters and evaluate the bioequivalence.Results:In the fasting test,the main pharmacokinetic parameters of the test and the reference tablets were as follows:AUC0-48 h(50.0±8.4)and(48.8±8.6)μg·h·mL^-1,Cmax(6.15±1.42)and(5.98±1.55)μg·mL^-1,tmax(1.19±0.62)and(1.30±0.73)h,t1/2(6.56±1.13)and(6.51±1.14)h^-1,respectively.The relative bioavailability was(103.0±8.7)%.In the high fat test,the main pharmacokinetic parameters of the test and the reference tablets were as follows:AUC0-48 h(45.4±8.4)and(44.5±8.2)μg·h·mL^-1,Cmax(5.85±1.08)and(6.58±1.89)μg·mL^-1,tmax(1.93±0.72)and(1.82±0.81)h,t1/2(6.69±0.81)and(6.63±0.76)h^-1,respectively.The relative bioavailability was(102.3±5.3)%.Conclusion:Levofloxacin hydrochloride tablets are bioequivalent to the reference preparations.

关 键 词：盐酸左氧氟沙星 药代动力学 生物等效性 

分 类 号：R969.1[医药卫生—药理学]