三种左奥硝唑制剂在健康人体的生物利用度与生物等效性分析

The Bioavailability and Bioequivalence Analysis of Three Levornidazole Preparations in Healthy Volunteers

目的比较3种国产左奥硝唑制剂在健康人体内的药代动力学,并评价3种制剂的生物等效性。方法 24名健康男性志愿者三交叉单剂量口服受试制剂左奥硝唑分散片、胶囊和参比制剂左奥硝唑片500mg后,用HPLC-UV法测定血药浓度,用DAS Ver 2.1计算其药代动力学参数并评价三者的生物等效性。结果受试制剂左奥硝唑分散片、胶囊和参比制剂左奥硝唑片的主要药代动力学参数:Cmax分别为(10.6±3.5)、(10.4±3.7)和(11.1±3.3)mg.L-1t;max分别为(0.76±0.70)、(1.35±0.80)和(0.92±0.84)ht;1/2分别为(13.2±1.4)、(12.9±1.7)和(12.3±1.9)h;AUC0→48分别为(140.7 31.3)、(149.5±28.5)和(143.2±37.2)mg.L-1.h;AUC0→∞分别为(152.6±33.4)、(162.0±31.8)和(153.7±30.1)mg.L-1.h。以AUC0→48、AUC0→∞作为评价依据,受试制剂对参比制剂的相对生物利用度F分别为(98.3±12.0)%、(99.512.1)%和(104.9±9.5)%、(106.0±10.5)%。结论左奥硝唑分散片、胶囊和参比制剂左奥硝唑片三种制剂生物等效。

Objective To study the pharmacokinetics and bioequivalence of three Levornidazole preparations in healthy volunteers.Methods The study was conducted in twenty-four healthy male volunteers.After receiving a single dose of 500 mg Levornidazole dispersible tablet,Levornidazole capsule and Levornidazole tablet（Reference） in three crossed way,the drug concentrations in plasma were determined by HPLC-UV method,the pharmacokinetic parameters and the statistical analysis of bioequivalence were obtained by DAS Ver 2.1.Results The pharmacokinetic parameters for Levornidazole dispersible tablet,Levornidazole capsule and the reference Levornidazole tablet were as follows： Cmax were（10.6±3.5）,（10.4±3.7） and（11.1±3.3）mg·L-1,tmax were（0.76±0.70）,（1.35±0.80） and（0.92±0.84）h,t1/2 were（13.2±1.4）,（12.9±1.7） and（12.3±1.9）h,AUC0→48 were（140.7±31.3）,（149.5±28.5） and（143.2±37.2）mg·L-1·h,AUC0→∞ were（152.6±33.4）,（162.0±31.8） and（153.7±30.1）mg·L-1·h.By evaluating AUC0→48 and AUC0→∞,the relative bioavailability of Levornidazole dispersible tablet and capsule to the reference were（98.3±12.0）%,（99.5±12.1）% and（104.9±9.5）%,（106.0±10.5）% respectively.Conclusion Levornidazole dispersible tablet,capsule and the reference tablets were bioequivalent.