人血清中左氧氟沙星的HPLC测定及其相对生物利用度  

HPLC assay of levofloxacin in human plasma and its relative bioavailability

作　　者：徐维平[1] 姜玲[1] 周薇[1] 殷实[1] 肖峰[2] 胡世莲[1] 魏伟[2] 

机构地区：[1]安徽省立医院,安徽合肥230001 [2]安徽医科大学,安徽合肥230032

出　　处：《安徽医药》2006年第5期339-340,共2页Anhui Medical and Pharmaceutical Journal

摘　　要：目的 用HPLC法测定人血清中左氧氟沙星的含量，评价左氧氟沙星胶囊在健康人体内的药动学及生物等效性。方法 采用改进的反相HPLC法，测定20名健康受试者单剂量交叉口服100mg左氧氟沙星供试片或参比片后不同时间点的血药浓度，计算其药动学参数及相对生物利用度，评价两药的生物等效性。结果 左氧氟沙星供试片（T）与参比片（R）的药动学参数接近，主要药动学参数为：AUC0-t。（R）为6．77±1．74mg·L^-1·h^-1、AUC0-t（T）为7．26±1．34mg·L^-1·h^-1，AUC0-∞，（R）为8．58±1．72mg·L^-1·h^-1,AUC0-∞（T）为8．96±1．27mg·L^-1·h^-1，Cmax（R）为0．99±0．16mg·L^-1、Cmax（T）为0．98±0．18mg·L^-1，Tmax（R）0．93±0．23h，Tmax（T）0．96±0．26h，T1／2α（R）为9．71±3．31h、T1/2α（T）为11．15±3．55h。相对生物利用度：分别为110．66±37．14％（T）和113．05±38．89％（R），两均值均在81％-126％内，符合相对生物利用度的要求。生物等效性评价：log（AUC0-t）和log（Cmax）在制剂间、个体间差异均无显著性。结论两制剂具有生物等效性。Aim To use the HPLC assay for determination of levofloxacin in human plasma and to investigate the pharmacokinetics and bioequivalence of levofloxacin. Methods The improved RP-HPLC assay was performed to determine different timespot in 20 healthy volunteers. In the study periods, a single 500 mg dose of each tablet was administered to each volunteer. The main pharmacokinetics parameter and relative bioavailability were calculated, and the bioequivalence were estimated. Results There were similar pharmacokinetics parameter between the reference and the test tablet, and the main pharmacokinetics parameter were as follows ：AUC0-t （R） （6.77 ± 1.74 ） mg.L^-1.h^-1,AUC0-t（T）（7.26±1.34）mg. L^-1 .h^-1,AUC0-t（R）（8.58±1.72）mg. L^-1. h^-1,AUC0-∞（T）（8.96±1.27） mg.L^-1 .h^-1,Cmax（R）（0.99±0.16）mg. L^-1 Cmax（T）（0.98±0.18）mg. L^-1, Tmax（R）（0.93 ±0.23）h,Tmax（T）（ 0.96±0. 26） h, T1/2α （R）（9.71 ± 3.31 ）h, T1/2α （T）（ 11.15 ± 3.55 ）h. The relative bioavailability of the test tablet was （110.66 ± 37.14）%; （ 113.05 ± 38.89）% for the reference tablet. Either was between the range of 81% - 126%, and in accordance with the requirementment of relative bioavailability. The results of bioequivalence showed that there was no signifieant difference between the reference and test formulations in the AUC and Cmax. Conclusion The reference and test formulations are bioequivalent.

关 键 词：左氧氟沙星 药动学 生物等效性 高效液相色谱 

分 类 号：R96[医药卫生—药理学]