盐酸左氧氟沙星片的人体生物等效性研究

目的研究盐酸左氧氟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名,随机双交叉单剂量口服盐酸左氧氟沙星片试验和参比制剂,剂量分别为200mg,剂间间隔为1周。分别于服药后24h内多点抽取静脉血;用高效液相色谱（HPLC）法测定血浆中左氧氟沙星的浓度。用DAS药代动力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（0-24）,AUC（0-inf）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制剂和参比制剂后血浆中的左氧氟沙星的Cmax分别为（2.88±0.61）mg·L^-1和（2.90±0.58）mg·L^-1;Tmax分别为（1.17±0.62）h和（1.09±0.79）h;AUC（0-24）分别为（20.23±3.41）mg/（h·L）和（20.11±3.61）mg/（h·L）;AUC（0-inf）分别为（21.97±3.84）mg/（h·L）和（21.72±4.22）mg/（h·L）。AUC（0-24）、AUC（0-inf）和Cmax的90%可信区间分别为97.5%～104.2%、98.2%～104.9%和92.5%～106.5%。结论试验制剂与参比制剂的人体相对生物利用度为（97．53±18．49）％，2制剂具有生物学等效性。

Bioequivalence of levofloxacin hydrochloride tablets in Chinese healthy volunteers

OBJECTIVE To study the relative bioavailability and bioequivalence of Levofloxacin hydrochloride tablets in healthy volunteers.METHODS A single oral dose （200rag of tested and reference formulation） were given to 20 healthy volunteers in a randomised crossover study. The concentrations of Levofloxacin in plasma were determined by HPLC. The pharmacokinetics parameters were calculated and the bioavailability and bioequivalence of two formulations were evaluated by DAS program. RESULTS After a single dose, the pharmacokinetics parameters for Levofloxacin were as follows： Cmax were （2.88 ± 0.61 ） mg·L^-1 and （2.90 ± 0.58） mg·L^-1; Tmax were （1.17±0.62）h and （1.09 ± 0.79）h; AUC（0.24） were （20.23 ± 3.41） mg＂ h＂ L-l and （20.11 ± 3.61 ） mg·h·L^- 1 ; AUC（0-inf） were （21.97 ± 3.84） mg·h·L^- 1 and （21.72 ± 4.22）mg·h·L^- 1 for tested and reference formulations respectively. The 90 % confidential interval of AUC（0-24）, AUC（0-inf） and Cmax, of tested formulation were 97.5% --104.2%,98.2% --104.9% and 92.5% --106.5% .CONCLUSION The relative bioavailability was （97.53 ± 18.49） % ; The results of the statistic analysis showed that the two formulations were bioequivalence.