【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200 mg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;Tm ax分别为(0.90±0.46)h和(1.3±0.62)h;Cm ax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。更多还原

【Abstract】 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 pharmacokinetic 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;Cmax 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 Cmax,In AUC0-T and In AUC0-∞ showed that two formulations were bioequivalent.The 90% confidence interval of AUC0-T and AUC0-∞ were 100.3%～113.0% and 100.1%～112.2%,in the range of 80～125%;Cmax 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.更多还原