盐酸左氧氟沙星片生物等效性研究

Study on Bioequivalence of Levofloxacin Hydrochloride Tablet

目的评价两个不同厂家的盐酸左氧氟沙星片剂的人体生物等效性。方法对20名男性健康自愿受试者采用两制剂、两周期自身双交叉设计方法,口服单剂量试验药物(重庆市庆余堂制药有限公司)或对照药物(浙江京新药业股份有限公司)300mg,采用高效液相色谱-荧光检测法测定血清中药物浓度,用DAS软件计算药代动力学参数和相对生物利用度。结果试验药物与对照药物的半衰期(t1/2)分别为(6.380±0.592)h和(6.412±0.511)h,达峰时间(Tmax)分别为(0.925±0.294)h和(1.175±0.452)h,峰浓度(Cmax)分别为(3.753±0.609)μg/mL及(3.606±0.605)μg/mL,0～36h药时曲线下面积(AUC0-36)分别为(31.773±3.742)μg·h/mL及(31.640±3.141)μg·h/mL,0～∞药时曲线下面积(AUC0-∞)分别为(32.597±3.786)μg·h/mL及(32.426±3.163)μg·h/mL。试验药物的相对生物利用度为(100.7±8.4)%。结论两种盐酸左氧氟沙星片剂生物等效。

Objective To study the bioequivalence of Levofloxacin Hydrochloride Tablets produced by two different factories in healthy volunteers. Methods A single oral dose of 300 mg test or the reference preparation was given to 20 healthy male volunteers in a randomized crossover study. The serum concentration of levofloxacin was determined by HPLC with the fluorescence detector. The pharmacokinetic parameters and the relative bioavailability were calculated by DAS to evaluate the bioequivalence. Results The main pharmacokinetic parameters of levofloxacin hydrochloride and the reference preparations were as follow： t1/2 were （6. 380 ± 0. 592）h and （6.412± 0. 511 ）h, Tmax were （0. 925 ±0. 294） h and （1. 175 ±0.452） h, Cmax were （3. 753 ±0. 609） μg/mL and （3. 606±0. 605）μg/mL, AUCo-36 were （31. 773 ± 3. 742） μg·h/mL and （31. 640 ± 3. 141） μg · h/mL, AUC0～∞ were （32. 597 ± 3. 786）μg · h/mL and （32. 426 ± 3. 163） μg · h/mL, respectively. The relative bioavailability of the test tablet to the reference one was （100. 7 ±8.4）%. Conclusion The results of statistic analysis show that the test and reference Levofloxacin Hydrochloride Tablets are bioequivalent.