氟罗沙星片的人体生物等效性研究  

A Study of the Bioequivalence of Fleroxacin Tablets in Healthy Chinese Volunteers

作　　者：胡卢丰[1] 杨迪 胡国新[1] 邱相君[3] 代宗顺[4] 

机构地区：[1]温州医学院药理学教研室,325027 [2]温州市永嘉县中医院,325102 [3]河南科技大学医学院药理学教研室,洛阳471003 [4]华中科技大学同济医学院临床药理研究所,武汉430030

出　　处：《医药导报》2007年第12期1411-1414,共4页Herald of Medicine

摘　　要：目的研究氟罗沙星片的人体相对生物利用度和生物等效性。方法健康志愿者20例，随机双交叉单荆量口服氟罗沙星片试验和参比制剂，剂量均为0．4g，剂间间隔为2周。分别于服药后48h内多点抽取静脉血；用高效液相色谱（HPLC）法测定血浆中氟罗沙星浓度。用DAS药动学程序计算相对生物利用度并评价两种制剂生物等效性。AUC（0-48）、AUC（0-∞）和Cmax经方差分析和双单侧t检验，tmax进行秩和检验。结果单剂量口服试验和参比制剂后血浆中氟罗沙星的Cmax分别为（5．30±1．20），（5．58±1．01）mg·L^-1；tmax分别为（2．10±0．97），（1．90±0．79）h；AUC（048）分别为（91．05±17．76），（90．39±14．58）mg·h·L^-1。；AUC（0-∞）分别为（97．49±19．33），（97．29±17．90）mg·h·L^-1。AUC（0-48）、AUC（0-∞）、Cmax的90％可信区间分别为94．0％～105．9％，92．9％～106．6％和88．6％～100．0％。结论氟罗沙星试验制剂与参比制剂的人体相对生物利用度为（100．82±14．66）％，试验制剂与参比制剂具有生物学等效性。Objective To study the relative bioavailability and bioequivalence of fleroxacin tablets in the human body. Methods A single oral dose of one of the 2 preparations of fleroxacin（0.4 g of the test and reference preparations） was given successively to each of the 20 healthy volunteers in a randomized crossover study with an inter-preparation interval of 2 weeks. Venous blood samples were collected separately at different time points within the 48 h. after the medication. Concentrations of fleroxacin in the blood plasma were determined with HPLC. The DAS pharmacokinetic program was used to calculate the relative bioavailability and assess the bioequivalence of the two preparations. The AUC（0-48） ,AUC（0-∞ ） and Cmax were subjected to analysis of variance and bilateral/unilateral t test and tmax was submitted to the rank test. Results After a single oral dose of the two preparations , the serum parameters for fleroxacin were as follows： Cmax were （5.30 ± 1.20 ） and （5.58 ± 1.01 ） mg · L^-1 ;tmax were （2.10 ±0.97 ） and （ 1.90 ±0.79） h; AUC（0-48） were （91.05 ± 17.76 ） and （90.39 ± 14.58 ） mg · h^-1 · L^-1 ; AUC（0-∞）. were （97.49 ± 19.33 ） and（ 97.29 ± 17.90 ） mg · h · L^-1 for the test and reference preparations, respectively. The 90% confidential interval of AUC（0-48） and AUC（0-∞ ）, Cmax for the test preparation were 94.0% - 105.9% , 92.9% - 106.6% and 88.6% - 100.0%, respectively. Conclusion The relative bioavailability of the test and reference preparations of fleroxacin in the human body was （ 100. 82 ± 14. 66 ） %. The results of the statistic analysis showed that the two preparations were bioequivalent.

关 键 词：氟罗沙星 药动学 生物利用度 生物等效性 色谱法 高压液相 

分 类 号：R978[医药卫生—药品] R969[医药卫生—药学]