盐酸左氢氟沙星口服液的人体生物等效性研究

Bioequivalence of levofloxacin hydrochloride oral liquid in healthy volunteers

目的评价盐酸左氧氟沙星口服液与盐酸左氧氟沙星片的生物等效性。方法 24名男性健康志愿者,采用双周期随机交叉设计,空腹口服盐酸左氧氟沙星口服液(受试制剂)与盐酸左氧氟沙星片(参比制剂)200mg,分别于服药前及服药后各时间点采集血样,采用高效液相色谱法(HPLC)测定血中左氧氟沙星的浓度,并计算C_(max)、T_(max)、T_(1/2)、AUC_((0-t))、AUC_((0-∞)等相关参数,利用方差分析及双单侧t检验判断2种制剂是否具有生物等效性。结果口服含左氧氟沙星200mg的受试制剂和参比制剂后,测得血浆中左氧氟沙星的T_(max)分别为(0.66±0.18)h和(0.82±0.34)h,C_(max)分别为(2.80±0.59)μg/ml和(2.64±0.56)μg/m1,T_(1/2)分别为(6.60±1.37)h和(7.26±1.20)h,AUC_((0-t))分别为(14.97±2.32)μg.h/ml和(15.04±2.32)μg·h/ml,AUC_(0～∞)分别为(15.66±2.38)μg·h/ml和(15.92±2.35)μg·h/ml。左氧氟沙星口服液对左氧氟沙星片的相对生物利用度为(100.1±10.6)%。结论两种制剂具有生物等效性。

Objective To study the relative bioavailability of levofloxacin hydrochloride oral liquid and tablets in healthy volunteers. Methods In a randomized two - way crossover design, a single oral dose of 200mg levofloxacin hydrochloride oral liquid and tablets were given to 24 male healthy volunteers. The plasma levofloxacin concentration within 36 h after administration was determined by HPLC and parameters C T T1/2 , AUC（0-1）, AUC（0-∞ ） were obtained and analyzed by two - one side test. Results The C were（2. 80 ±0. 59） and （2.64 ±0.56） μg /ml, respectively; T were （0. 66 ± 0. 18 ） and （0. 82 ±0. 34 ） h, respectively; T1/2 were （ 6. 60 ± 1.37 ） and （ 7.26 ＋ 1.20 ） h, respectively ; AUC（0-1）were （ 14. 97 ± 2.32 ） μg. h/ml 和 （ 15.04 ± 2. 32 ） μg· h/ml, AUC（0-∞）, were（ 15.66 ± 2.38 ） and （ 15.92 ± 2.35 ） μg. main pharmacokinetie parameters of levofloxaein hydroehloride oral liquid and tablets were as follows： Cmax was （2.80 ±0.59） and （2.64 ＋0.56） p,g/ml, respectively; Tmax was （0.66 ±0.18） and （0.82 ±0.34） h,re- speetively ;T1/2 was （ 6.60 ±1.37 ） and （7.26 ± 1.20） h, respectively ; AUC（0-1） was （ 14.97 ± 2.32） μg · h/ml and （ 15.04± 2.32 ） μg · h/ml, respectively. AUC（0-∞）was （ 15.66 ±2.38） and （ 15.92 ± 2.35 ）μg · h/ml, respectively. There was no statistically significant difference between these two test groups. The relative bioavailability of the test oral liquid was （ 100.1± 10.6 ） %. Conclusions The levofloxaein hydrochloride oral liquid and tablets are bioequivalent.