乳酸左氧氟沙星片剂的健康人体药代动力学和相对生物利用度研究

Pharmacokinetics and Relative Bioavailablity of Levofloxacin Lactate Tablet in Chinese Healthy Volunteers

目的：研究乳酸左旋氧氟沙星片剂的健康人体药代动力学和相对生物利用度。方法：18名健康受试者单次，交叉口服乳酸左旋氧氟沙星片200mg后，用HPLC-荧光法测定血浆中左氧氟沙星浓度，用BAPP2．0软件进行数据处理，计算药代动力学参数。结果：供试与参比制剂的药时曲线可用二室模型拟合，两者主要药代动力学参数Cmax分别为（2．92±0．60）μg／mL、（3．22±0．53）μg／mL,Tmax分别为（0．9±0．3）h、（0．9±0．3）h；t1/2分别为（7．27±1．02）h、（6．83±0．80）h；AUC0-24分别为（17．18±2．46）μg／（mL·h）、（17．19±2．55）μg／（mL·h）。乳酸左氧氟沙星片供试制剂的相对生物利用度为（100．3±9．4）％。结论：供试与参比制剂具有生物等效性。

Objective：To investigate the pharmacokinetics and relative bioavailability of levofloxacin lactate tablets and to evaluate its bioequivalence. Methods. A single oral dose 200mg of two levofloxacin lactate tablets was given to 18 healthy volunteers in a randomized cross-over study. The concentration of levofloxacin in plasma was determined by HPLC with fluorimetric detection. The pharmacokinetic parameters were calculated by BAPP 2. 0 software. Results：The concentrationtime curves after medication conformed to a two-compartment open model. The main pharmacokinetic parameters of the test tablets and reference tablets mL.（3.22 ± 0.53）μg/mL; Tmax（0.9 ±0. 3）h.0. 9±0. 3 were as follow： Cmax（2. 92±0. 60）μg/ h;t1/2 （7. 27±1.02）h; （6.83±0. 80）h; AUC0-24 （17. 18±2.46）μg/（mL · h）,（17. 19±2. 55）μg/（mL · h）;The relative bioavailability of the test tablets was （100. 3 ±9.4）%. Conclusion： The results demonstrated that the two levofloxacin lactate tablets were bioeouivalent.