左氧氟沙星分散片人体相对生物利用度及生物等效性研究  

Bioavailability and Bioequivalence Study of Levofloxacin Tablets in Chinese Healthy Volunteers

作　　者：周志凌[1] 余细勇[1] 杨敏[1] 林秋雄[1] 陈树桢[1] 陈铁峰[1] 单志新[1] 邓春玉[1] 郑猛[1] 刘晓颖[1] 江桂芬[1] 林曙光[1] 

机构地区：[1]广东省人民医院医学研究中心,广州510080

出　　处：《中国现代应用药学》2008年第3期220-223,共4页Chinese Journal of Modern Applied Pharmacy

摘　　要：目的研究国产左氧氟沙星片剂的相对生物利用度，并且评价该制剂的生物等效性。方法20名男性健康受试者随机交叉双周期给药，分别口服单剂量左氧氟沙星试验制剂及参比制剂，采用反相高效液相色谱法测定血药浓度，计算两者的药动学参数及相对生物利用度，并评价试验制剂的生物等效性。结果口服左氧氟沙星200mg试验和参比制剂的主要药代力学参数，t1／2分别为（11．0±3．2）h和（9．5±2．6）h；Tmax分别为（0．90±0．46）h和（1．3±0．62）h；Cmax分别为（2．7±0．75）μg·mL^-1和（2．65±0．70）μg·mL^-1；AUC0-T分别为（16．6±3．0）μg·h·mL^-1和（16．5±2．6）μg·h·mL^-1；AUC0-∞分别为（18．2±3、9）μg·h·mL^-1和（19．2±3．5）μg·h·mL^-1。按实测值AUC0-T计算，试验制剂对于参比制剂的平均相对生物利用度为（100．6±10．2）％。Cmax、AUC0-T和AUC0-∞三个药动学参数制剂间均无显著性差异（P〉0．05），服药周期对Cmax，AUC0-T和AUC0-∞三个参数亦无明显影响（P〉0．05），Cmax、AUC0-T和AUC0-∞三个药动学参数均存在明显的个体间差异（P〈0．05）。统计结果显示，AUC0-T的置信区间为100．7％～113．0％，AUC0-∞的置信区间为100．1％～112．2％，Cmax的置信区间为95.0％～115．4％，均符合等效标准；Cmax，AUC0-T和AUC0-∞三个参数的双向t检验结果同样符合等效标准；Tmax经非参检验结果合格。结论左氧氟沙星分散片试验制剂相对参比制剂生物等效。OBJECTIVE The aim is to study the relative bioavailability of levofloxacin tablet in Chinese healthy volunteers and to evaluate the bioequivalence. METHODS A single oral dose 200mg of test and reference formulations was given to 20 healthy volunteers in a randomized cross-over study. The concentrations of levofloxacin in plasma were determined by HPLC. RESULTS The main pharrnacokinetic parameters of two formulations, test and reference, were as follows ： t1/2 were （ 11.0 ± 3.2） h and （ 9.5 ± 2.6） h Tmax were （0.90±0.46）h and （1.3±0.62）h;C were （2.7±0.75）μg · mL^-1 and （2.65±0.70）μg· mL^-1; AUC0-T were （16.6±3.0）μg· h · mL^-1 and （16.5 ±2.6）μg · h · mL^-1;AUC0-∞ were （18.2±3.9）μg · h · mL^-1 and （18.9±3.2） μg · h · mL^-1 ,respectively. The relative bioavailability of AUC0-T was （ 100.6 ± 10.2） %. The results of ANOVA and two one-sided t test statistical analysis for In C In AUC0-Tand In AUC0-∞ showed that two formulations were bioequivalent. The 90% confidence interval ofAUC0-Tand AUC0-∞ were 100.3% -113.0% and 100.1% -112.2%,in the range of 80-125%; C was 95.0% 115.4% , also in the range of 70% - 143% , so the two tablets were bioequivalent. CONCLUSION The test and reference levofloxacin tablets were bioequivalent

关 键 词：左氧氟沙星 生物利用度 高效液相色谱 

分 类 号：R978.27[医药卫生—药品] R944.4[医药卫生—药学]