盐酸左氧氟沙星胶囊的生物等效性研究

Study on the Bioequivalence of Levofloxacin Hydrochloride Capsules in Healthy Volunteers

目的研究盐酸左氧氟沙星胶囊的人体生物等效性。方法健康志愿者20例,随机双交叉单剂量口服盐酸左氧氟沙星胶囊受试和参比制剂,分别于服药后24h内多点抽取静脉血,采用反相高效液相色谱(RP-HPLC)法测定血浆左氧氟沙星浓度,计算其药动学参数和相对生物利用度,评价其生物等效性。结果单剂量口服受试和参比制剂后血浆左氧氟沙星峰浓度(Cmax)分别为(3.05±0.64)和(3.25±0.82)μg.mL-1;达峰时间(tmax)分别为(1.00±0.30)和(1.10±0.50)h,半衰期(t1/2)分别为(7.51±1.26)和(7.45±1.30)h,血药浓度-时间曲线下面积(AUC0～t)分别为(17.58±3.25)和(18.21±2.96)μg.h.mL-1;AUC(0-∞)分别为(19.04±3.35)和(18.96±3.12)μg.h.mL-1。受试制剂AUC0～t的90%置信区间为参比制剂相应参数的90.9%～102.5%;Cmax的90%置信区间为参比制剂相应参数的84.7%～105.4%。结论盐酸左氧氟沙星受试制剂与参比制剂的人体相对生物利用度为(98.5±16.3)%,受试制剂与参比制剂具有生物等效性。

Objective To study the bioequivalence of levofloxacin hydrochloride capsules in healthy volunteers.Methods 20 healthy male volunteers were administered orally with single dose of either the tested or referenced formulations by a randomized crossover way.The blood concentrations of levofloxacin hydrochloride were determined by RP-HPLC,and the pharmacokinetics parameters and relative bioavailability were calculated.Results The Cmax were（3.05±0.64）and（3.25±0.82）μg·mL-1,tmax of the tested and referenced formulations were（1.00±0.30）and（1.10±0.50）h,t1/2 were（7.51±1.26）and（7.45±1.30）h,AUC0～t were（17.58±3.25）and（18.21±2.96）μg·h·mL-1,AUC0-∞ were（19.04±3.35）and（18.96±3.12）μg·h·mL-1.AUC0～t at 90% degree of confidence of the tested were 90.9%～102.5% of the referenced;while,Cmax were 84.7%～105.4%.Conclusion The relative bioavailability of the tested to referenced capsules is（98.5±16.3）%,which shows that the two levofloxacin hydrochloride capsules are bioequivalent.