【摘要】 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。更多还原

【Abstract】 OBJECTIVE To study the relative bioavailability and bioequivalence of Levofloxacin hydrochloride tablets in healthy volunteers.METHODS A single oral dose(200mg 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-1 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.更多还原